Note: Descriptions are shown in the official language in which they were submitted.
CA 02352526 2001-05-23
1
USE OF N-SUBSTITUTED AZABICYCLOALKANE DERIVATIVES FOR
TREATING DISEASES OF THE CENTRAL NERVOUS SYSTEM
N-substituted azabicycloalkane derivatives are already known as
neuroleptics (WO 95/13279, WO 95/15327, WO 96/04272, US
5.475.105, US 5.521.209, US 5.616.705, US 5.753.690). It has now
been found that these substances are also suitable for
controlling addictive disorders and other disorders of the
central nervous system.
The present invention provides the use of N-substituted
3-azabicycloalkane derivatives of the formula I
R1
N-( GHy ) n-R2
in which
B is a 4-, 5- or 6-membered ring, which may contain a double
bond,
R1 is a phenyl, naphthyl, phenanthryl or thienyl group, in. each
case unsubstituted or mono- or disubstituted by halogen
atoms, C1-4-alkyl, trifluoromethyl, hydroxyl, C1_4-alkoxy,
ariino, monomethylamino, dimethylamino, cyano or nitro groups,
n is the number 0, 1, 2, 3 or 4 and
RZ is a naphthyl group which is unsubstituted or substituted by
one or two halogen atoms, or is one of the following
radicals:
'' 0050/49558 CA 02352526 2001-05-23
2
1 3 R8
R5 ~ NR6 C R~ ~ NR6 SOp O
.
R4
6- ~~ R8 ~ Rs Rs
-NR C O~ ~ -O-C O ' -O O
_ Rs -N /O Rs
-.0 O . ~ --N
O
O
Rs
N ~ O R9 O
- N~
~- R1~ -N 0 ,
~R8 . -N
~~ Rs .
Rs
~ O
-_t3 ~N ~ ~~CH3 R11
~N R9 ~N~~ .
. ..
H3C N~N/ . X .Y
2
Rs
O R8
02S
-N~ or -N O
in which
R3 is a hydrogen atom, a hydroxyl group or a phenyl radical
which is unsubstituted or substituted by a fluorine, chlorine
or bromine atom,
R4 is a hydrogen atom or
R3 and R4 together are an oxygen atom,
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' 0050/49558
3
R5 is a phenyl, naphthyl or thienyl group, each of which is
unsubstituted or mono- or disubstituted by fluorine, chlorine
or bromine atoms or by hydroxyl, vitro, amino,
C1_q-alkanoylamino, C1_q-alkylamino, C1_q-alkyl or methoxy
groups,
R6 is a hydrogen atom or a methyl group,
R~ is a phenyl, naphthyl, benzofuryl, benzothienyl, thienyl,
indolyl, N-methylindolyl or indenyl group, in each case
unsubstituted or mono- or disubstituted by fluorine, chlorine
or bromine atoms or by C1_q-alkyl, hydroxyl, methoxy, vitro,
cyano, trifluoromethyl, amino or di-C1_q-alkylamino groups, or
is a C3_~-cycloalkyl group,
R8 is a hydrogen atom or a fluorine or chlorine atom or a
Ci-q-alkyl, methoxy or amino group,
R9 is a hydrogen atom or a methyl group and
R1~ is a hydrogen atom or a methyl group or
R9 and Rlo together with the ring carbon atom are a
spirocyclopropane ring,
R11 is a hydrogen atom, a hydroxyl, C1-Cq-alkyl or C~-C4-alkoxy
group, or together with the adjacent carbon atom is a C=O- or
C=S group,
X and Y are carbon atoms, CH, CH2, NH or C1-Cq-alkyl-N groups or
nitrogen atoms,
Z is a direct bond, a CO group, CS group or a CH or CH2 group in
which a hydrogen atom may be replaced by a hydroxyl, amino or
C1-Cq-alkoxy group or by a halogen atom, and
A is a hydrogen atom, a hydroxyl, amino, mercapto,
C1-Cq-alkylamino, di-C1-Cq-alkylamino, C1-Cq-alkylthio or
CZ-Cq-alkoxy group or together with the adjacent carbon atom
is a C=0 group or
A is a Y-bonded C3-Cq-alkylene group which may contain one or
two non-cumulated double bonds and in which one CH or CH2
group may be replaced by a nitrogen or sulfur atom or an NH
or N-CH3 group and where the ring is either monosubstituted
by a fluorine or chlorine atom or a methyl, methoxy, vitro or
amino group or, in the case of a benzene ring, this may be
0050/49558 ~ 02352526 2001-05-23
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mono-, di- or trisubstituted by fluorine or chlorine atoms or
methyl, trifluoromethyl, nitro, hydroxyl, methoxy, amino,
monomethyl or dimethylamino groups,
and in which the X-, Y- and Z-containing ring at the nitrogen
atom No. 1 may carry a C1-C4-alkyl, allyl or benzyl group and may
contain 1 to 3 non-cumulated double bonds,
and their salts with physiologically acceptable acids for
preparing medicaments for controlling addiction, for treating
concentration disorders (attention deficit disorders),
hyperactivity in children (attention deficit hyperactivity
disorders), learning and memory weaknesses (impaired cognitive
function).
The use according to the invention relates to all addictive
disorders, whether they are caused by abuse of substances or
other addictive disorders such as, for example, addiction to
gambling. Habit-forming substances can be:
opioids such as, for example, morphine or heroin,
nicotine,
alcohol,
substances which interact with the benzodiazepine receptor
complex, sedatives or tranquilizers, such as, for example, the
benzodiazepines.
Possible habit-forming substances according to the invention are,
in particular, cocaine or amphetamine and amphetamine-like
substances.
The compounds of the formula I can be employed both in the form
of their racemates and their optical isomers.
For the novel indication, the compounds can be administered in a
customary manner orally or parenterally, intravenously or
intramuscularly.
The dosage depends on the age, condition and weight of the
patient and on the type of administration. In general, the daily
dose of active compound is between about 1 and 100 mg/kg of
bodyweight in the case of oral administration and between 0.1 and
10 mg/kg of bodyweight in the case of parenteral administration.
The compounds can be employed in customary pharmaceutical
administration forms, in solid or liquid form, for example as
tablets, film-coated tablets, capsules, powders, granules,
0050/49558 ~ 02352526 2001-05-23
sugar-coated tablets, suppositories, solutions, ointments, creams
or sprays. These are prepared in a customary manner. For this
purpose, the active compounds can be processed with the customary
pharmaceutical auxiliaries such as tablet binders, fillers,
5 preservatives, tablet disintegrants, flow regulators,
plasticizers, wetting agents, dispersants, emulsifiers, solvents,
release-delaying agents, antioxidants and/or propellants (cf. H.
Sucker et al.: Pharmazeutische Technologie [Pharmaceutical
Technology], Thieme-Verlag, Stuttgart, 1978). The resulting
administration forms usually comprise the active compound in an
amount of from 1 to 99% by weight.
The following substances may be mentioned as examples of
compounds of the formula I:
1. 1-(4-fluorophenyl)-4-[exo-6-phenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]butan-1-one
2. 1-phenyl-4-[exo-6-phenyl-3-azabicyclo[3.2.Ojheptan-3-yl]-
butan-1-one
3. 1-(4-fluorophenyl)-4-[exo-6,7-diphenyl-3-azabicyclo-
[3.2.0]heptan-3-yljbutan-1-one
4. 1-(4-fluorophenyl)-4-[exo-6-phenyl-3-azabicyclo[3.2.0j-
heptan-3-yljbutane
5. 1-phenyl-2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethan-1-one
6. 1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butane
7. 1-(4-fluorophenyl)-4-[exo-6-m-fluorophenyl-3-azabicyclo-
[3.2.0)heptan-3-yl]butan-1-one
8. 1-(4-fluorophenyl)-4-[exo-6-o-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
9. 1-(4-fluorophenyl)-4-[exo-6-p-chlorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
10. 1-(4-fluorophenyl)-4-[exo-6-m-chlorophenyl-3-azabicyclo-
[3.2.Ojheptan-3-yl]butan-1-one
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11. 1-(4-fluorophenyl)-4-[exo-6-p-methoxyphenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
12. 1-(4-fluorophenyl)-4-[exo-6-m,p-dichlorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
13. 1-(4-fluorophenyl)-4-[exo-6-m,p-dimethoxyphenyl-3-aza-
bicyclo[3.2.0]heptan-3-yl]butan-1-one
14. 1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
15. 1-phenyl-4-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]butan-1-one
16. 1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butane
17. 1-(4-fluorophenyl)-4-[exo-6-p-nitrophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
18. 1-(4-fluorophenyl)-4-[exo-6-m-nitrophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
19. 1-(4-fluorophenyl)-4-[exo-6-p-trifluoromethylphenyl-3-
azabicyclo[3.2.0]heptan-3-yl]butan-1-one
20. I-(4-fluorophenyl)-4-[exo-6-p-cyanophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
21. 1-(4-fluorophenyl)-4-[exo-6-thien-3-yl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
22. 1-(4-fluorophenyl)-4-[exo-6-pyrid-3-yl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
23. 1-(4-fluorophenyl)-3-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]propan-1-one
24. 1-(bis-4-fluorophenyl)-4-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butane
25. 1-(bis-4-fluorophenyl)-4-[exo-6-phenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butane
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0050/49558
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26. 1-(4-fluorophenyl)-4-[exo-6-phenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]butan-1-of
27. 1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-of
28. 1-(4-fluorophenyl)-4-[exo-6,7-Biphenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]butan-I-of
29. 1-phenyl-4-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
butan-1-of
30. 1-phenyl-4-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]butan-1-of
31. 1-(4-fluorophenyl)-4-[exo-6-o-fluorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-of
32. 1-(4-fluorophenyl)-4-[exo-6-m-chlorophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-of
33. 1-(4-fluorophenyl)-4-[exo-6-p-trifluoromethylphenyl-3-
azabicyclo[3.2.0]heptan-3-yl]butan-1-of
34. 1-(4-fluorophenyl)-4-[exo-6-p-aminophenyl-3-azabicyclo-
[3.2.0]heptan-3-yl]butan-1-one
35. N-(3-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]propyl)-4-
fluorobenzamide
36. N-(3-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
propyl)benzamide
37. N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-4-fluorobenzamide
38. N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)benzamide
39. N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-N-methyl-4-fluorobenzamide
40. N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-N-methylbenzamide
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41. N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-N-methyl-4-isopropylbenzamide
42. N-(3-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
propyl)-4-chlorobenzamide
43. N-(2-[exo-6-p-trifluoromethylphenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)-4-chlorobenzamide
44. N-(3-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
propyl)-3-methoxybenzamide
45. N-(3-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
propyl)-3-nitrobenzamide
46. N-(3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]propyl)-4-fluorobenzamide
47. N-(3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]propyl)benzamide
48. N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-4-fluorobenzamide~
49. N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)benzamide
50. N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-N-methyl-4-fluorobenzamide
51. N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-N-methylbenzamide
52. N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-N-methyl-4-isopropylbenzamide
53. N-(3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]propyl)-4-chlorobenzamide
54. N-(3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]propyl)-3-methoxybenzamide
55. N-(3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]propyl)-3-nitrobenzamide
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56. N-(2-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-4-chlorobenzamide
57. N-(2-[exo-6-o-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl)-4-chlorobenzamide
58. N-(2-(exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-2-hydroxybenzamide
59. N-(2-[exo-6-m-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-4-chlorobenzamide
60. exo-3-n-butyl-6-phenyl-3-azabicyclo[3.2.0)heptane
61. exo-3-methyl-6-phenyl-3-azabicyclo[3.2.0]heptane
62, exo-3-methyl-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptane
63. exo-3-n-propyl-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptane
64. exo-3-methyl-6,7-diphenyl-3-azabicyclo[3.2.0]heptane
65. exo-3-n-propyl-6-m-hydroxyphenyl-3-azabicyclo[3.2.0]-
heptane
66, exo-3-allyl-6-m-methoxyphenyl-3-azabicyclo[3.2.0]-
heptane
67. exo-3-(3,4-dimethoxy)phenethyl-6-phenyl-3-azabicyclo-
[3.2.0]heptane
68. exo-3-(3,4-dimethoxy)phenethyl-6-p-fluorophenyl-3-
azabicyclo(3.2.0)heptane
69. exo-3-(3,4-dihydroxy)phenethyl-3-azabicyclo[3.2.0]-
heptane
70. exo-3-phenethyl-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptane
71. 6-~-[exo-6-p-fluorophenyl-3-azabicyclo(3.2.0]heptan-3-yl)-
ethyl-7-methyl-SH-thiazolo[3,2-a]pyrimidin-5-one
72. (+)-6-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
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73. (-)-6-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan
3-yljethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
74. 6-~-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-7-
5 methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
75. 6-~-[exo-6,7-diphenyl-3-azabicyclo[3.2.0]heptan-3-yljethyl-
7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
10 76. 6-~-[exo-6,7-bis-(p-fluorophenyl)-3-azabicyclo[3.2.0]heptan
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
77. 6-~-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-ylj-
ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
78. 6-~-[exo-6-m-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
79. 6-~-[exo-6-m-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
80. 6-~-(2-[exo-6-p-aminophenyl-3-azabicyclo[3.2.Ojheptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
81. 6-~-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
82..6-~-[exo-6-p-methoxyphenyl-3-azabicyclo[3.2.0]heptan
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
83. 6-~-[exo-6-p-nitrophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
84. 6-B-[exo-6-m-fluorophenyl-3-azabicyclo[3.2.0jheptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
85. 6-~-[exo-6-p-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
86. 6-~-[exo-6-p-trifluoromethylphenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-
5-one
87. 6-~-[exo-6-(p-t-butylphenyl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
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88. 6-B-[endo-6-(p-t-butylphenyl)-3-azabicyclo[3.2.0)heptan
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
89. 6-~-[exo-6-(3,4-dichlorophenyl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
90. 6-~-[exo-6-(3,4-dimethoxyphenyl)-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-
5-one
91. 6-~-[exo-6-p-cyanophenyl-3-azabicyclo[3.2.0)heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
92. 6-~-[exo-6-(3,4-dihydroxyphenyl)-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-
5-one
93. 6-~-[exo-6-(o-fluorophenyl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
94. 6-~-[exo-6-thien-3-yl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
95. 6-B-[exo-6-(5-chlorothien-2-yl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
96. 6-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-
5-one
97. 6-~-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidin-
5-one
98. 6-B-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,3,7-trimethyl-5H-thiazolo[3,2-a)pyrimidin-5-one
99. 6-B-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl-5H-thiazolo[3,2-a]pyrimidin-5-one
100.6-~-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-5H-
thiazolo[3,2-a]pyrimidin-5-one
101.7-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methyl-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one
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102.7-~-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-
8-methyl-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one
103.7-H-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methyl-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one
104.7-~-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
ethyl-8-methyl-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one
105.7-~-[exo-6-p-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methyl-2H,6H-pyrimido[2,1-b][1.3]thiazin-6-one
106.7-~-[exo-6-m-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methyl-2H,6H-pyrimido[2,1-b][1,3]thiazin-6-one
107.3-H-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
108.(+)-3-H-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
109.(-)-3-H-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
110.3-~-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-2,4-
(1H,3H)quinazolinedione
111.3-H-[exo-6-m-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
112.3-H-[exo-6-p-cyanophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
113.3-H-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
114.3-~-[exo-6-p-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
115.3-~-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
116.3-~-[exo-6-m-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
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117.3-f3-[exo-6-p-nitrophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
ethyl-2,4-(iH,3H)quinazolinedione
118.3-J3-[endo-6-p-nitrophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
119.3-!3-[exo-6-m-hydroxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
120.3-!3-[exo-6-p-aminophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl-2,4-(1H,3H)quinazolinedione
121.3-fi-[exo-6-p-iodophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl-2,4-(1H,3H)quinazolinedione
122.3-I3-[exo-6-p-trifluoromethylphenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
123.3-fi-[exo-6-(3,4-dichlorophenyl)-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
124.3-!3-[exo-6-(3,4-dihydroxyphenyl)-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
?5 125.3-!3-[exo-6-(3,5-dichlorophenyl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
126.3-!3-[exo-6-o-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
127.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methyl-2,4-(1H,3H)quinazolinedione
128.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-chloro-2,4-(1H,3H)quinazolinedione
129.3-J3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-fluoro-2,4-(1H,3H)quinazolinedione
130.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-5-chloro-2,4-(1H,3H)quinazolinedione
131.3-!i-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-fluoro-2,4-(1H,3H)quinazolinedione
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132.3-J3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-methyl-2,4-(1H,3H)quinazolinedione
133.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-8-methoxy-2,4-(1H,3H)quinazolinedione
134.3-f3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-trifluoromethyl-2,4-(1H,3H)quinazolinedione
135.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-vitro-2,4-(1H,3H)quinazolinedione
136.3-l3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-vitro-2,4-(1H,3H)quinazolinedione
137.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0)heptan-3-yl]-
ethyl-7-amino-2,4-(1H,3H)quinazolinedione
138.3-J3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-amino-2,4-(1H,3H)quinazolinedione
139.3-l3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6-hydroxy-2,4-(1H,3H)quinazolinedione
140.3-!i-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-5-chloro-2,4-(1H,3H)quinazolinedione
141.3-l3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,7-dimethoxy-2,4-(1H,3H)quinazolinedione
142.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,8-dichloro-2,4-(1H,3H)quinazolinedione
143.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,7,8-trimethoxy-2,4-(1H,3H)quinazolinedione
144.3-B-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1-methyl-2,4-(1H,3H)quinazolinedione
145.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1-ethyl-2,4-(1H,3H)quinazolinedione
146.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1-allyl-2,4-(1H,3H)quin~zolinedione
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147.3-H-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1-benzyl-2,4-(1H,3H)quinazolinedione
148.3-y-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
5 propyl-2,4-(1H,3H)quinazolinedione
149.3-b-(exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
butyl-2,4-(1H,3H)quinazolinedione
10 150.3-~-[exo-6-(2-thienyl)-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
151.3-~-(exo-6-(5-chloro-2-thienyl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
152.3-~-[exo-6-(3-thienyl)-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
153.3-H-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1H-thieno[3,2-d]pyrimidine-2,4-dione
154.3 -~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1H-thieno[2,3-d]pyrimidine-2,4-dione
155.3-~-[exo-6-p-fluorophenyl-3-azabicyclo(3.2.0]heptan-3-yl]-
ethyl-1H-thieno(3,4-d]pyrimidine-2,4-dione
156.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
ethyl-1-methyl-1H,3H-pyrido[2,3-d]pyrimidine-2,4-dione
157.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methyl-3H-quinazolin-4-one
158.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methoxy-3H-quinazolin-4-one
159.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methyl-4H-pyrido(1,2-a]pyrimidin-4-one
dihydrochloride
160.3-B-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-
2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
161.3-~-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
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162.3-f3-[exo-6-m-methoxyphenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
163.3-13-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan
3-yl)ethyl-2,6-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
164.3-t3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,7-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
165.3-J3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,8-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
166.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
167.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,6,8-trimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
168.3-!3-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan
3-yl]ethyl-2,7-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
169.3-13-[exo-6-o-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,7-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
170.3-fi-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl-
2,8-dimethyl-4H-pyrido[1,2-a)pyrimidin-4-one
171.3-!3-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
172.3-13-[exo-6-(5-chlorothien-2-yl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
173.3-!3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-
4-one
174.3-!3-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-
4-one
175.3-J3-[exo-6-p-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-
4-one
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176.3-5-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methyl-4H-pyrimido[1,2-a]pyrimidin-4-one
177.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-ylj-
ethyl-2-methyl-7-chloro-4H-pyrimido[1,2-a]pyrimidin-4-one
178.6-8-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-7-methyl-1H,5H-imidazo[1,2-a]pyrimidin-5-one
179.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.Ojheptan-3-yl]-
ethyl-2-methyl-7,8-dihydro-4H,6H-pyrrolo[1,2-a]pyrimidin-
4-one
180.2-(exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
methylbenzimidazole
181.1-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-ylj-
ethylbenzimidazale
182.1-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2,3-dihydrobenzimidazol-2-one
183.2-[exo-6-m-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-ylj-
methylbenzimidazole
184.3-~-(exo-6-p-fluorophenyl-3-azabicyclo[3.2.Ojheptan-3-yl]-
ethylindole, m.p. 193-195~C (hydrochloride)
185.3-~-(2-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-
yl]ethylindole
186.3-~-[exo-6-phenyl-3-azabicyclo[3.2.0]he tan-3- 1 eth 1-
P Y j Y
indole, m.p. 104-105~C (hydrochloride)
187.3-~-[exo-6-m-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethylindole
I88.2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
methyl-3,4-dihydroquinazolin-4-one
189.2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
methyl-3,4-dihydroquinazoline-4-thione
190.2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yI]methyl-
3,4-dihydroquinazolin-4-one
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191.2-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
methyl-3,4-dihydroquinazolin-4-one
192.2-[exo-6-o-methoxyphenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
methyl-3,4-dihydroquinazolin-4-one
193.2-[exo-6-p-fluorophenyl-3-azabicyclo(3.2.0]heptan-3-yl]-
methyl-4-hydroxy-6-methylpyrimidine
194.6-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-
methyl-2-methyl-4-hydroxypyrimidine
195.6-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
methyluracil
196.6-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]methyl-
uracil
197.6-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
1,2,3,4-tetrahydro-1,3-dimethyl-2,4-dioxopyrimidine
198.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0)heptan-
3-yl]ethyl-1,2,3,4-tetrahydro-6-methyl-2,4-dioxopyrimidine
199.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0)heptan-3-yl]-
ethyl-1,2,3,4-tetrahydro-1,6-dimethyl-2,4-dioxopyrimidine
200.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1,2,3,4-tetrahydro-3,6-dimethyl-2,4-dioxopyrimidine
201.5-~-[exo-6-p-fluorophenyl-3-azabicyclo(3.2.0]heptan-3-yl)-
ethyl-1,2,3,4-tetrahydro-3,6-dimethyl-2,4-dithiopyrimidine
202.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0)heptan-3-yl]
ethyl-1,2,3,4-tetrahydro-1,3,6-trimethyl-2,4-dioxopyrimidine
203.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-1,2,3,4-tetrahydro-6-amino-1-methyl-2,4-dioxo-
pyrimidine
204.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-amino-6-methyl-4(3H)pyrimidinone
205.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-amino-3,6-dimethyl-4(3H)pyrimidinone
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206.5-13-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
207.5-J3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methylamino-3-ethyl-6-methyl-4(3H)pyrimidinone
208.5-!3-[exo-6-p-fluorophenyl-3-azabicyclo(3.2.0]heptan-3-yl]-
ethyl-2-amino-3-ethyl-6-methyl-4(3H)pyrimidinone
209.5-J3-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
210.5-13-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
211.5-!3-[exo-6-o-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
212.5-13-[exo-6-p-trifluoromethylphenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
213.5-J3-[exo-6-p-cyanophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
214.5-f3-[exo-6-m-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
215.5-B-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl-2-methylamino-4-methoxy-6-methylpyrimidine
216.3-~-[exo-6-phenyl-7-methyl-1,5-cis-3,7-diazabic clo 3.3.0 -
Y I 1
octan-3-yl]ethyl-2,4-(iH,3H)quinazolinedione
217.~3-~-[endo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
218.3-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan- 3-yl]ethyl-2,4-(1H,3H)quinazolinedione
219.3-~3-[exo-6-p-trifluoromethylphenyl-7-methyl-1,5-cis-3,7-
diazabicyclo[3.3.0]octan-3-yl]ethyl-6-fluoro-2,4-(1H,3H)-
quinazolinedione
220.3-~-[exo-6-m-chlorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
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221.3-~-[exo-6-p-methoxyphenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-6-methyl-2,4-(1H,3H)quinazolinedione
222.5-~-[exo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
5 octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
223.5-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-
10 4(3H)pyrimidinone
224.1-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2(3H)benzimidazolone
15 225.5-~-[exo-6-p-nitrophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-
4(3H)pyrimidinone
226.5-~-[exo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
20 octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
227.5-~-[endo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
228.3-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2-methyl-4H-pyrido[1.2-a]-
pyrimidin-4-one
229.1-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethylindolin-2-one
230.6-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-7-methyl-5H-thiazolo[3.2-a]-
pyrimidin-5-one
231.I-~-[exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yl]ethyl-2(1H)quinolone
232.3-~-[7-phenyl-1,5-cis-3,7-diazabicyclo[3.3.0]octan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
233.3-~-[7-p-fluorophenyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
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234.5-~-[7-p-fluorophenyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
235.3-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.1.0]hexan-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
236.3-~-[exo-6-phenyl-3-azabicyclo[3.1.0]hexan-3-yl)ethyl-2,4-
(1H,3H)quinazolinedione
237.3-~-[6,6-diphenyl-3-azabicyclo[3.1.0]hexan-3-yl]ethyl-2,4-
(1H,3H)quinazolinedione
238.5-~-[exo-6-p-fluorophenyl-3-azabicyclo[3.1.0]hexan-3-yl)-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
239.6-~-[exo-6-m-chlorophenyl-3-azabicyclo[3.1.0]hexan-3-yl]-
ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
240.3-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-
en-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
241.5-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0)oct-6-
en-3-yl)ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
242.6-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-
en-3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a)pyrimidin-5-one
243.1-~-[6-phenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-en-3-yl]-
ethyl-2(3H)benzimidazolone
244.1-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-
en-3-yl]ethylindolin-2-one
245.1-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-
en-3-yl)ethyl-2(1H)quinolone
246.3-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl)ethyl-2,4-(1H,3H)quinazolinedione
247.5-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
248.6-~-[exo-6-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
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249.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethylindolin-2-one
250.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2(1H)quinolone
251.3-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
252.5-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
253.6-~-[endophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl-7-methyl-5H-thiazolo[3.2-a]pyrimidin-5-one
254.1-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethylindolin-2-one
255.1-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2(1H)quinolone
256.3-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
257.5-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
258.6-~-[exo-7-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yI]-
ethyl-7-methyl-SH-thiazolo[3.2-a]pyrimidin-5-one
259.1-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethylindolin-2-one
260.1-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl-2(iH)quinolone
261.3-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
262.5-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
263.3-~-[endo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]-
ethyl-2,4-(1H,3H)quinazolined~one
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264.5-~-[endo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
265.3-~-[endo-6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo-
[4.3.0]non-3-yl]ethyl-2,4-(1H,3H)quinazolinedione,
266.5-/3-(endo-6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo-
[4.3.0]non-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
267.3-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
268.5-~-(endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
269.1-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl-2(3H)benzimidazolone
270.1-~-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethylindolin-2-one
271.3-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
272.5-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
273.3-~-[6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
274.5-~-[6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
275.3-~-[6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo-
[4.3.0]non-6-en-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
276.5-~-[6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo[4.3.0]-
non-6-en-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
277.1-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl-2(3H)benzimidazolone
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278.1-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethylindolin-2-one
279.1-~-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl-2(1H)quinolone
280.3-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethyl-2,4-(1H,3H)quinazolidone
281.5-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
282.3-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethyl-2-methyl-4H-pyrido[1.2-a]pyrimidin-4-one
283.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethyl-2(1H)quinolone
284.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethyl-2(3H)benzimidazolone
285.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-
en-3-yl]ethylindolin-2-one
286.3-~-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-en-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
287.5-~-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-en-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
288.3-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
289.5-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
290.3-~-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0)non-3-yl]ethyl-
2,4-(1H,3H)quinazolinedione
291.5-~-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]ethyl-
2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
292.6-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non
3-yl]ethyl-7-methyl-5H-thiazQlo[3.2-a]pyrimidin-5-one
0050/49558 ~ 02352526 2001-05-23
293.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0)non-
3-yl)ethyl-2(3H)benzimidazolone
294.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0)non-
5 3-yl]ethylindolin-2-one
295.1-~-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2(1H)quinolone
10 296.3-~-[exo-7-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-8-en-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
297.5-~-[exo-7-phenyl-1,5-cis-3-azabicyclo[4.3.0)non-8-en-3-yl]-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
298.3-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
8-en-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
299.5-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0)non-
8-en-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
300.3-~-[7-p-fluorophenyl-3-azabicyclo[4.3.0]non-1-en-3-yl]-
ethyl-2,4-(1H,3H)quinazolinedione
301.5-~-[7-phenyl-3-azabicyclo[4.3.0]non-1-en-3-yl]ethyl-
2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
302.5-~-[7-p-fluorophenyl-3-azabicyclo[4.3.0)non-1-en-3-yl)-
ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
303.3-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2,4-(1H,3H)quinazolinedione
304.5-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)pyrimidinone
305.1-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2(3H)benzimidazolone
306.1-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethylindolin-2-one
307.1-~-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl-2(1H)quinolone
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308.3-~-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl-2,4-(1H,3H)quinazolinedione
309.5-~-[6-p-fluorophenyl-1,5-cis-8-oxa-3,?-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl-2-methylamino-3,6-dimethyl-4(3H)-
pyrimidinone
310.3-~-[exo/endo-6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diaza-
bicyclo[3.3.0j-octan-3-yljethyl-2,4-(1H,3H)quinazolinedione
311.5-~-[exo/endo-6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diaza-
bicyclo[3.3.0]octan-3-yl]ethyl-2-methylamino-3,6-dimethyl-
4(3H)pyrimidinone
312.1-~-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethylindolin-2-one
313.6-~-[6-phenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.Oj-
oct-6-en-3-yl]ethyl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-
5-one
314.N-(2-[exo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl)-4-fluorobenzamide
315.N-(2-[endo-6-phenyl-7-methyl-1,5-cis-3,?-diazabicyclo[3.3.0]-
octan-3-yl]ethyl)-4-fluorobenzamide
316.N-(2-(exo-6-p-fluorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yljethyl)-4-fluorobenzamide
317.N-(2-[exo-6-p-trifluoromethylphenyl-7-methyl-1,5-cis-3,7-
diazabicyclo[3.3.0]octan-3-yl]ethyl)benzamide
318.N-(2-[exo-6-m-chlorophenyl-7-methyl-1,5-cis-3,7-diazabicyclo-
[3.3.0]octan-3-yljethyl)benzamide
319.N-(2-[exo-6-p-methoxyphenyl-7-methyl-1,5-cis-3,7-diaza-
bicyclo[3.3.0]octan-3-yl]ethyl)-4-chlorobenzamide
320.N-(2-[exo-6-phenyl-7-methyl-1,5-cis-3,7-diazabicyclo[3.3.0]-
octan-3-yl]ethyl)naphthalene-1-carboxamide
321.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-7-methyl-1,5-
cis-3,7-diazabicyclo[3.3.Ojoc.tan-3-yljbutan-1-one
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322.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-7-methyl-1,5-
cis-3,7-diazabicyclo[3.3.0]octan-3-yl]butan-1-of
323.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]-
non-3-yl]ethyl)benzamide
324.1-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]-
non-3-yl]ethyl)naphthalene
325.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-one
326.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-of
327.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)-2-(N-methyl)aminobenzamide
328.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)-5-chlorothien-2-ylcarboxamide
329.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)indene-3-carboxamide
330.N-(2-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]-
ethyl)-4-fluorobenzamide
331.N-(2-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]-
ethyl)naphthalene-1-carboxamide
332.1-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl)naphthalene
333.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-1,5-cis-3-aza-
bicyclo[4.3.0]non-7-en-3-yl]butan-1-one
334.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl)benzamide
335.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl)indene-3-carboxamide
336.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl)naphthalene-1-carboxamide
0050/49558 ~ 02352526 2001-05-23
28
337.N-(2-(exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-en-3-yl]-
ethyl)-4-fluorobenzamide
338.N-(2-[exo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-7-en-3-yl]-
ethyl)-3-chloro-1-benzothien-2-ylcarboxamide
339.1-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)naphthalene
340.1-(4-fluorophenyl)-4-[6-p-fluorophenyl-1,5-cis-3-azabicyclo-
[4.3.0]non-6-en-3-yl]butan-1-one
341.1-(4-fluorophenyl)-4-[6-p-fluorophenyl-I,5-cis-3-azabicyclo-
[4.3.0]non-6-en-3-yl]butan-1-of
342.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)-2-(N-methyl)aminobenzamide
343.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)-5-chlorothien-2-ylcarboxamide
344.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)benzamide
345.N-(2-[6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-3-yl]-
ethyl)-3-chloro-1-benzothien-2-ylcarboxamide
346.N-(2-[6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo[4.3.0]-
non-6-en-3-yl]ethyl)naphthalene-1-carboxamide
347.N-(2-(6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)indene-3-carbonimide
348.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-6-en-
3-yl]ethyl)napthalene-1-carboxamide
349.1-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)naphthalene
350.1-(4-fluorophenyl)-4-[endo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-one
351.1-(4-fluorophenyl)-4-(endo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-of
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0050/49558
29
352.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-ylj-2-(N-methyl)aminobenzamide
353.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)benzamide
354.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yljethyl)-5-chlorothien-2-ylcarboxamide
355.N-(2-[endo-6-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-3-yl]-
ethyl)-4-fluorobenzamide
356.N-(2-[endo-6-p-trifluoromethylphenyl-1,5-cis-3-azabicyclo-
[4.3.0]non-3-yl]ethyl)indene-3-carboxamide
357.2-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.Ojnon-
7-en-3-yl]ethyl)naphthalene
358.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yl]ethyl)benzamide
359.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
7-en-3-yljethyl)-2-(N-methyl)aminobenzamide
360.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.Ojnon-
7-en-3-yl]ethyl)naphthalene-1-carboxamide
361.1-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.Ojnon-
8-en-3-yl]ethyl)naphthalene
362.1-(4-fluorophenyl)-4-[exo-7-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-8-en-3-yl]butan-1-one
363.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
8-en-3-yl]ethyl)benzamide
364.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
8-en-3-yl]ethyl)-5-chlorothien-2-ylcarboxamide
365.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
8-en-3-yl]ethyl)-3-chloro-1-benzothien-2-ylcarboxamide
366.N-(2-[exo-7-phenyl-1,5-cis-3-azabicyclo[4.3.0]non-8-en-
3-yl]ethyl)indene-3-carboxamide
CA 02352526 2001-05-23
0050/49558
367.N-(2-[exo-7-phenyl-1,5-cis-3-azabicyclo(4.3.0]non-8-en-
3-yl]ethyl)naphthalene-1-carboxamide
368.1-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
5 3-yl]ethyl)naphthalene
369.1-(4-fluorophenyl)-4-[exo-7-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-one
10 370.1-(4-fluorophenyl)-4-[exo-7-p-fluorophenyl-1,5-cis-3-
azabicyclo[4.3.0]non-3-yl]butan-1-of
371.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)-2-(N-methyl)aminobenzamide
372.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)benzamide
373.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)-5-chlorothien-2-ylcarboxamide
374.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)naphthalene-1-carboxamide
375.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[4.3.0]non-
3-yl]ethyl)indene-3-carboxamide
376.1-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-en-
3-yl]ethyl)naphthalene
377.1-(4-fluorophenyl)-4-[6-p-fluorophenyl-1,5-cis-3-azabicyclo-
[3.3.0]oct-6-en-3-yl]butan-1-one
378.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-en-
3-yl]ethyl)benzamide,
379.N-(2-[6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]oct-6-en-
3-yl]ethyl)naphthalene-1-carboxamide
380.1-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)naphthalene
381.1-(4-fluorophenyl)-4-[exo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo-(3.3.0]octan-3-yl]butan-1-of
0050/49558 ~ 02352526 2001-05-23
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382.N-(2-[exo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)benzamide
383.N-(2-[exo-6-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl)naphthalene-1-carboxamide
384.N-(2-[exo-6-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl)indene-3-carboxamide
385.1-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)naphthalene
386.1-(4-fluorophenyl)-4-[endo-6-p-fluorophenyl-1,5-cis-3-
azabicyclo[3.3.0]octan-3-yl]butan-1-one
387.N-(2-[endo-6-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)benzamide
388.N-(2-[endo-6-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl)naphthalene-1-carboxamide
389.1-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)naphthalene
390.1-(4-fluorophenyl)-4-[exo-7-p-fluorophenyl-1,5-cis-3-
azabicyclo[3.3.0]octan-3-yl]butan-1-one
391.N-(2-[exo-7-p-fluorophenyl-1,5-cis-3-azabicyclo[3.3.0]octan-
3-yl]ethyl)benzamide
392.N-(2-[exo-7-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl)naphthalene-1-carboxamide
393.N-(2-[exo-7-phenyl-1,5-cis-3-azabicyclo[3.3.0]octan-3-yl]-
ethyl)indene-3-carboxamide
394.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.1.0]hexan-3-yl]-
ethyl)-4-fluorobenzamide
395.N-(2-[exo-6-phenyl-3-azabicyclo[3.1.0]hexan-3-yl]ethyl)-
5-chlorothien-2-ylcarboxamide
396.N-(2-[6,6-diphenyl-3-azabicyclo[3.1.0]hexan-3-yl]ethyl)-
naphth-1-ylcarboxamide .
0050/49558 ~ 02352526 2001-05-23
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397.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.1.0]hexan-3-yl]-
ethyl)-3-chloro-1-benzothien-2-ylcarboxamide
398.N-(2-[exo-6-m-chlorophenyl-3-azabicyclo[3.1.0]hexan-3-yl]-
ethyl)-4-chlorobenzamide
399.1-(2-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl)naphthalene
400.N-(2-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl)benzamide
401.N-(2-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl)naphthalene-1-carboxamide
402.N-(2-[6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diazabicyclo[3.3.0]-
oct-6-en-3-yl]ethyl)indene-3-carboxamide
403.1-(2-[exo/endo-6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diaza-
bicyclo[3.3.0]octan-3-yl]ethyl)naphthalene
404.N-(2-[exo/endo-6-p-fluorophenyl-1,5-cis-8-oxa-3,7-diaza-
bicyclo[3.3.0]octan-3-yl]ethyl)benzamide
405.1-(2-[6-phenyl-1-5-cis-8-oxa-3,7-diazabicyclo[3.3.0]oct-
6-en-3-yl]ethyl)naphthalene
406.N-(2-[6-phenyl-1-5-cis-8-oxa-3,7-diazabicyclo[3.3.0]oct-
6-en-3-yl]ethyl)benzamide
407.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)benzosulfonamide
408.N-(2-[exo-6-phenyl-3-azabicyclo[3.2.0]heptan-3-yl]ethyl)-
benzosulfonamide
409.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-N-methylbenzosulfonamide
410.N-(2-[exo-6-(5-chlorothien-2-yl)-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)-4-fluorobenzosulfonamide
411.3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-1-
phenoxypropane .
0050/49558 ~ 02352526 2001-05-23
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412.2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-1-p-
fluorophenoxyethane
413.3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-1-
(1-naphthyloxy)propane
414.3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-1-p-
t-butylphenoxypropane
415.3-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]-1-p-fluorophenoxypropane
416.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl)thiobenzamide
417.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-4-fluorothiobenzamide
418.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-4-chlorothiobenzamide
419.0-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)benzoate
420.0-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl-4-fluorobenzoate
421.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]
ethyl)-1H-benzo[cd]indol-2-one
422.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-1H-benzo[cd]indol-2-one
423.N-(2-[exo-6-m-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-1H-benzo[cd]indol-2-one
424.N-(2-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0)heptan-3-yl]-
ethyl)-1H-benzo[cd]indol-2-one
425.3,3-dimethyl-1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)indolin-2-one
426.3,3-dimethyl-1-(2-(exo-6-p-chlorophenyl-3-azabicyclo[3.2.0)-
heptan-3-yl]ethyl)indolin-2-Qne
005049558 ~ 02352526 2001-05-23
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427.3,3-dimethyl-1-(2-[exo-6-m-chlorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)indolin-2-one
428.1-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.Ojheptan-3-yl]-
ethyl)-3,3,5-trimethylindolin-2-one
429.3,4-dichloro-N-(2-[exo-6-p-nitrophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzamide
430.2,5-difluoro-N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzamide
431.2-amino-N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzamide
432.2-amino-N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzamide
433.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0jheptan-3-yl]-
ethyl)-2-methylaminobenzamide
434.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-2-methylaminobenzamide
435.3-amino-N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)benzamide
436.4-amino-N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-
3-yl]ethyl)benzamide
437.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.Ojheptan-3-yl]-
ethyl)thiophene-2-carboxamide
438.5-chloro-N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)thiophene-2-carboxamide
439.5-chloro-N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)thiophene-2-carboxamide
440.5-chloro-N-(2-[exo-6-(5-chloro-2-thienyl)-3-azabicyclo
[3.2.Ojheptan-3-yl]ethyl)thiophene-2-carboxamide
441.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)benzo[b]furan-2-carboxamide
005/49558 ~ 02352526 2001-05-23
442.3-chloro-N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzo[b]thiophene-2-carboxamide
443.3-chloro-N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]-
5 heptan-3-yl]ethyl)benzo[b]thiophene-2-carboxamide
444.3-chloro-N-(2-[exo-6-p-nitrophenyl-3 -azabicyclo[3.2.0]-
heptan-3-yl]ethyl)benzo[b]thiophene-2-carboxamide
10 445.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indene-3-carboxamide
446.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indene-3-carboxamide
447.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)cyclopropanecarboxamide
448.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)cyclopentanecarboxamide
449.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)cyclopentanecarboxamide
450.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)cyclohexanecarboxamide
451.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)cyclohexanecarboxamide
_ 30
452.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)naphthalene-1-carboxamide
453.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indole-2-carboxamide
454.N-(2-[exo-6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indole-3-carboxamide
455.exo-6-p-fluorophenyl-3-[2-(1-naphthyl)ethyl]-3-azabicyclo-
[3.2.0]heptane
456.exo-6-p-chlorophenyl-3-[2-(1-naphthyl)ethyl]-3-azabicyclo-
[3.2.0]heptane .
0050/49558 CA 02352526 2001-05-23
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457.exo-6-m-chlorophenyl-3-[2-(1-naphthyl)ethyl]-3-azabicyclo-
[3.2.0]heptane
458.exo-6-(5-chloro-2-thienyl)-3-[2-(1-naphthyl)ethyl]-3-
azabicyclo[3.2.0]heptane
459.exo-6-p-fluorophenyl-3-[2-(2-naphthyl)ethyl]-3-azabicyclo-
[3.2.0]heptane
460.exo-6-p-fluorophenyl-3-[1-naphthylmethyl]-3-azabicyclo-
[3.2.0]heptane
461.exo-6-p-fluorophenyl-3-[2-naphthylmethyl]-3-azabicyclo-
[3.2.0]heptane
462.4-(6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-1-(thio-
phen-2-yl)butan-1-one
463.4-(6-p-chlorophenyl-3-azabicyclo[3.2.0]heptan-3-yl)-1-(thio-
phen-2-yl)butan-1-one
464.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-4-phenylpyrrolidin-2-one
465.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)benzoxazolin-2-one
466.N-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)isoindolinone
467.1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indazole
468.1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-1,8-naphthalenesultam
469.4-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)-1,4-benzoxazin-3-one
470.1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)quinoxalin-2(1H)-one
471.1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)indolin-2-one
0050/49558 ~ 02352526 2001-05-23
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472.1-(2-[exo-6-p-fluorophenyl-3-azabicyclo[3.2.0]heptan-3-yl]-
ethyl)spiro[cyclopropane-1',3-indolin-2-one]
473.3,6-dimethyl-2-methylamino-5-[2-(exo-6-(2-naphthyl)-3-aza-
bicyclo[3.2.0]heptan-3-yl)ethyl]-3H-pyrimidin-4-one
474.3,6-dimethyl-2-methylamino-5-[2-(exo-6-(1-naphthyl)-3-aza-
bicyclo[3.2.0]heptan-3-yl)ethyl]-3H-pyrimidin-4-one
475.3,6-dimethyl-2-methylamino-5-[2-(exo-6-(5-chloro-
1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)ethyl]-3H-
pyrimidin-4-one
476.3,6-dimethyl-2-methylamino-5-[2-(exo-6-(6-chloro-2-naphthyl)-
3-azabicyclo[3.2.0]heptan-3-yl)ethyl]-3H-pyrimidin-4-one
477.3,6-dimethyl-2-methylamino-5-[2-(exo-6-(9-phenanthryl)-3
azabicyclo[3.2.0]heptan-3-yl)ethyl]-3H-pyrimidin-4-one
478.7-methyl-6-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl)-5H-thiazolo[3,2-a]pyrimidin-5-one
479.3-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-1H,3H-quinazoline-2,4-dione
480.3-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-1H,3H-quinazoline-2,4-dione
481.6-fluoro-3-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl]-1H,3H-quinazoline-2,4-dione
482.3-[2-(exo-6-(5-chloro-2-naphthyl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl]-1H,3H-quinazoline-2,4-dione
483.3-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-2-methyl-4H-pyrido[1.2-a]pyrimidin-4-one
484.1-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-2(1H)quinolone
485.1-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]indolin-2-one
486.1-[2-(exo-6-(1-naphthyl)-3-a2abicyclo[3.2.0]heptan-3-yl)-
ethyl]-2(3H)benzimidazolone
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487.1-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-3-methyl-2(3H)benzimidazolone
488.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]benzamide
489.N-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]benzamide
490.N-[2-(exo-6-(5-chloro-1-naphthyl)-3-azabicyclo[3.2.0]-
heptan-3-yl)ethyl]benzamide
491.3-[2-(1-naphthyl)ethyl]-exo-6-(1-naphthyl)-3-azabicyclo-
[3.2.0]heptane
492.3-[2-(1-naphthyl)ethyl]-exo-6-(2-naphthyl)-3-azabicyclo-
[3.2.0]heptane
493.1-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-1H-benzo[cd]indol-2-one
494.1-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-1H-benzo[cd]indol-2-one
495.3,3-dimethyl-1-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]-
heptan-3-yl)ethyl]-1,3-dihydroindol-2-one
496.3,3-dimethyl-1-[2-(exo-6-(2-naphthyl)-3-azabicyclo-
[3.2.0]heptan-3-yl)ethyl]-1,3-dihydroindol-2-one
,~ 497.3,3-dimethyl-1-[2-(exo-6-(6-chloro-2-naphthyl)-3-azabicyclo-
[3.2.0]heptan-3-yl)ethyl]-1,3-dihydroindol-2-one
498.5-chloro-N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]-
heptan-3-yl)ethyl]-2-thiophenecarboxamide
499.5-chloro-N-[2-(exo- 6-(2-naphthyl)-3-azabicyclo[3.2.0]-
heptan-3-yl)ethyl]-2-thiophenecarboxamide
500.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-4-fluorobenzamide
501.N-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-4-nitrobenzamide
0050/49558 ~ 02352526 2001-05-23
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502.N-[2-(exo-6-(6-chloro-2-naphthyl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl]benzamide
503.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-4-methoxybenzamide
504.N-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-4-hydroxybenzamide
505.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]-3,4-dichlorobenzamide
506.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]naphthalene-1-carboxamide
507.N-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]naphthalene-1-carboxamide
508.N-[2-(exo-6-(9-phenanthryl)-3-azabicyclo[3.2.0]heptan-
3-yl)ethyl]benzamide
509.1-[2-(exo-6-(6-chloro-2-naphthyl)-3-azabicyclo[3.2.0]-
heptan-3-yl)ethyl]-1H-benzo[cd]indol-2-one
510.1-[2-(exo-6-(9-phenanthryl)-3-azabicyclo[3.2.0]
heptan-3-yl)ethyl]-1H-benzo[cd]indol-2-one
511.N-[2-(exo-6-(1-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]isoindolinone
512.N-[2-(exo-6-(2-naphthyl)-3-azabicyclo[3.2.0]heptan-3-yl)-
ethyl]isoindolinone
513.(+)-(iS,5R,6S)exo-1-[2-[6-(4-chlorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-3-methyl-2H-1,3-dihydro-
benzimidazol-2-one
514.(+)-(1S,5R,6S)exo-1-[2-[6-(4-chlorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-3-ethyl-2H-1,3-dihydro-
benzimidazol-2-one
515.(+)-(iS,5R,6S)exo-1-[2-[6-(4-chlorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-3-n-propyl-2H-1,3-dihydro-
benzimidazol-2-one _
0050/49558 ~ 02352526 2001-05-23
516.(+)-(1S,5R,6S)exo-2-[2-[6-(4-chlorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-3,3-dimethyl-2,3-dihydro-1,2-
benzisothiazole 1,1-dioxide
5 517.(+)-(1S,5R,6S)exo-2-[2-[6-(4-chlorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-2,3-dihydro-1,2-benzisothiazole
1,1-dioxide
518.(+)-(1S,5R,6S)exo-2-[2-[6-(4-fluorophenyl)-3-azabicyclo-
10 [3.2.0]heptan-3-yl]ethyl]-3,3-dimethyl-2,3-dihydro-1,2-
benzisothiazole 1,1-dioxide
519.(+)-(1S,5R,6S)exo-2-[2-[6-(4-fluorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-3,3-diethyl-2,3-dihydro-1,2-
15 benzisothiazole 1,1-dioxide
520.(+)-(1S,5R,6S)exo-2-[2-[6-(4-fluorophenyl)-3-azabicyclo-
[3.2.0]heptan-3-yl]ethyl]-2,3-dihydro-1,2-benzisothiazole
1,1-dioxide
25
35
45
