CN1328455A - N-取代的氮杂二环烷衍生物在治疗中枢神经系统疾病中的应用 - Google Patents
N-取代的氮杂二环烷衍生物在治疗中枢神经系统疾病中的应用 Download PDFInfo
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- CN1328455A CN1328455A CN99813559A CN99813559A CN1328455A CN 1328455 A CN1328455 A CN 1328455A CN 99813559 A CN99813559 A CN 99813559A CN 99813559 A CN99813559 A CN 99813559A CN 1328455 A CN1328455 A CN 1328455A
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- CN
- China
- Prior art keywords
- azabicyclic
- ethyl
- heptane
- fluorophenyl
- cis
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 6
- 201000010099 disease Diseases 0.000 title abstract description 4
- 210000003169 central nervous system Anatomy 0.000 title abstract description 3
- -1 amino, monomethyl amino, dimethylamino Chemical group 0.000 claims description 79
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 19
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 16
- 229910052801 chlorine Inorganic materials 0.000 claims description 13
- 229910052731 fluorine Inorganic materials 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
- 125000001624 naphthyl group Chemical group 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 125000005843 halogen group Chemical group 0.000 claims description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000001544 thienyl group Chemical group 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
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- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 4
- 150000001335 aliphatic alkanes Chemical class 0.000 claims description 4
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- 125000001246 bromo group Chemical group Br* 0.000 claims description 4
- 230000001955 cumulated effect Effects 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 3
- 208000015114 central nervous system disease Diseases 0.000 claims description 3
- 239000000460 chlorine Substances 0.000 claims description 3
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 2
- BLRHMMGNCXNXJL-UHFFFAOYSA-N 1-methylindole Chemical compound C1=CC=C2N(C)C=CC2=C1 BLRHMMGNCXNXJL-UHFFFAOYSA-N 0.000 claims description 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims description 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 2
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
- 125000001118 alkylidene group Chemical group 0.000 claims description 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000005561 phenanthryl group Chemical group 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
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- 208000022497 Cocaine-Related disease Diseases 0.000 claims 1
- 201000006145 cocaine dependence Diseases 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 206010012335 Dependence Diseases 0.000 abstract description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 167
- CVIBKISSHDMEKJ-UHFFFAOYSA-N 1-ethylquinazoline-2,4-dione Chemical class C1=CC=C2C(=O)NC(=O)N(CC)C2=C1 CVIBKISSHDMEKJ-UHFFFAOYSA-N 0.000 description 53
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 40
- YJJOJBNUDCBRTM-UHFFFAOYSA-N 5-ethyl-3,6-dimethyl-2-(methylamino)pyrimidin-4-one Chemical compound CCC1=C(C)N=C(NC)N(C)C1=O YJJOJBNUDCBRTM-UHFFFAOYSA-N 0.000 description 35
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 29
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 28
- QQVIHTHCMHWDBS-UHFFFAOYSA-N perisophthalic acid Natural products OC(=O)C1=CC=CC(C(O)=O)=C1 QQVIHTHCMHWDBS-UHFFFAOYSA-N 0.000 description 26
- RMHJJUOPOWPRBP-UHFFFAOYSA-N naphthalene-1-carboxamide Chemical compound C1=CC=C2C(C(=O)N)=CC=CC2=C1 RMHJJUOPOWPRBP-UHFFFAOYSA-N 0.000 description 16
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 description 13
- VNDHYTGVCGVETQ-UHFFFAOYSA-N 4-fluorobenzamide Chemical compound NC(=O)C1=CC=C(F)C=C1 VNDHYTGVCGVETQ-UHFFFAOYSA-N 0.000 description 12
- VSMXLKGFTKFOSB-UHFFFAOYSA-N 1-ethyl-3h-indol-2-one Chemical compound C1=CC=C2N(CC)C(=O)CC2=C1 VSMXLKGFTKFOSB-UHFFFAOYSA-N 0.000 description 11
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 11
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical compound C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 description 10
- JRXCUTAHLPYHAY-UHFFFAOYSA-N 1-ethylquinolin-2-one Chemical class C1=CC=C2C=CC(=O)N(CC)C2=C1 JRXCUTAHLPYHAY-UHFFFAOYSA-N 0.000 description 9
- BLNVISNJTIRAHF-UHFFFAOYSA-N 4-chlorobenzamide Chemical compound NC(=O)C1=CC=C(Cl)C=C1 BLNVISNJTIRAHF-UHFFFAOYSA-N 0.000 description 8
- CXUCKELNYMZTRT-UHFFFAOYSA-N 1-Ethyl-2-benzimidazolinone Chemical compound C1=CC=C2NC(=O)N(CC)C2=C1 CXUCKELNYMZTRT-UHFFFAOYSA-N 0.000 description 7
- 229940053202 antiepileptics carboxamide derivative Drugs 0.000 description 7
- 150000001875 compounds Chemical class 0.000 description 7
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 description 6
- DKKRVLCXVRLMMU-UHFFFAOYSA-N 3-ethyl-2-methylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC=CN2C(=O)C(CC)=C(C)N=C21 DKKRVLCXVRLMMU-UHFFFAOYSA-N 0.000 description 6
- 125000001207 fluorophenyl group Chemical group 0.000 description 6
- 239000000463 material Substances 0.000 description 6
- PXBFMLJZNCDSMP-UHFFFAOYSA-N 2-Aminobenzamide Chemical compound NC(=O)C1=CC=CC=C1N PXBFMLJZNCDSMP-UHFFFAOYSA-N 0.000 description 5
- 239000001273 butane Substances 0.000 description 5
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 5
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 5
- BWNBLGQCCSCCHF-UHFFFAOYSA-N 2-ethyl-1h-indole Chemical compound C1=CC=C2NC(CC)=CC2=C1 BWNBLGQCCSCCHF-UHFFFAOYSA-N 0.000 description 4
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- DENPQNAWGQXKCU-UHFFFAOYSA-N thiophene-2-carboxamide Chemical class NC(=O)C1=CC=CS1 DENPQNAWGQXKCU-UHFFFAOYSA-N 0.000 description 4
- OCJBOOLMMGQPQU-UHFFFAOYSA-N 1,4-dichlorobenzene Chemical compound ClC1=CC=C(Cl)C=C1 OCJBOOLMMGQPQU-UHFFFAOYSA-N 0.000 description 3
- GYSCBCSGKXNZRH-UHFFFAOYSA-N 1-benzothiophene-2-carboxamide Chemical class C1=CC=C2SC(C(=O)N)=CC2=C1 GYSCBCSGKXNZRH-UHFFFAOYSA-N 0.000 description 3
- XFYIIXTWGSQBFN-UHFFFAOYSA-N 3-ethyl-2,7-dimethylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC(C)=CN2C(=O)C(CC)=C(C)N=C21 XFYIIXTWGSQBFN-UHFFFAOYSA-N 0.000 description 3
- HNYOPLTXPVRDBG-UHFFFAOYSA-N barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 150000008515 quinazolinediones Chemical class 0.000 description 3
- OHBQPCCCRFSCAX-UHFFFAOYSA-N 1,4-Dimethoxybenzene Chemical compound COC1=CC=C(OC)C=C1 OHBQPCCCRFSCAX-UHFFFAOYSA-N 0.000 description 2
- QNPCLOIFWORBJP-UHFFFAOYSA-N 1-ethyl-6-fluoroquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=CC=C12)F)=O)=O QNPCLOIFWORBJP-UHFFFAOYSA-N 0.000 description 2
- HKDKELZTBPEWSU-UHFFFAOYSA-N 1-ethyl-6-methylquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=CC=C12)C)=O)=O HKDKELZTBPEWSU-UHFFFAOYSA-N 0.000 description 2
- RETWPUNUUVAWIM-UHFFFAOYSA-N 2-ethyl-2,5-dihydro-1,3-thiazole Chemical compound CCC1SCC=N1 RETWPUNUUVAWIM-UHFFFAOYSA-N 0.000 description 2
- AAIZLBJGGDQXFD-UHFFFAOYSA-N 3-ethyl-2,8-dimethylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1=C(C)C=CN2C(=O)C(CC)=C(C)N=C21 AAIZLBJGGDQXFD-UHFFFAOYSA-N 0.000 description 2
- KIYKJTIONPRZJR-UHFFFAOYSA-N 3-ethyl-2,9-dimethylpyrido[1,2-a]pyrimidin-4-one Chemical compound CC1=CC=CN2C(=O)C(CC)=C(C)N=C21 KIYKJTIONPRZJR-UHFFFAOYSA-N 0.000 description 2
- VKPLPDIMEREJJF-UHFFFAOYSA-N 3-methoxybenzamide Chemical compound COC1=CC=CC(C(N)=O)=C1 VKPLPDIMEREJJF-UHFFFAOYSA-N 0.000 description 2
- KWAYEPXDGHYGRW-UHFFFAOYSA-N 3-nitrobenzamide Chemical compound NC(=O)C1=CC=CC([N+]([O-])=O)=C1 KWAYEPXDGHYGRW-UHFFFAOYSA-N 0.000 description 2
- QXSAKPUBHTZHKW-UHFFFAOYSA-N 4-hydroxybenzamide Chemical compound NC(=O)C1=CC=C(O)C=C1 QXSAKPUBHTZHKW-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- PNZXMIKHJXIPEK-UHFFFAOYSA-N cyclohexanecarboxamide Chemical compound NC(=O)C1CCCCC1 PNZXMIKHJXIPEK-UHFFFAOYSA-N 0.000 description 2
- PYRYOLOOOPVOHJ-UHFFFAOYSA-N cyclopentane formamide Chemical compound C(=O)N.C1CCCC1 PYRYOLOOOPVOHJ-UHFFFAOYSA-N 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- XBCXJKGHPABGSD-UHFFFAOYSA-N methyluracil Natural products CN1C=CC(=O)NC1=O XBCXJKGHPABGSD-UHFFFAOYSA-N 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 239000001294 propane Substances 0.000 description 2
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- 239000000126 substance Substances 0.000 description 2
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 description 2
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- WCKVTLHFRUMPJD-UHFFFAOYSA-N 1-benzyl-3-ethylquinazoline-2,4-dione Chemical class C12=CC=CC=C2C(=O)N(CC)C(=O)N1CC1=CC=CC=C1 WCKVTLHFRUMPJD-UHFFFAOYSA-N 0.000 description 1
- LDQMACURBNQQID-UHFFFAOYSA-N 1-butylquinazoline-2,4-dione Chemical class C1=CC=C2C(=O)NC(=O)N(CCCC)C2=C1 LDQMACURBNQQID-UHFFFAOYSA-N 0.000 description 1
- HFJMCDYTVQDJJS-UHFFFAOYSA-N 1-chloroquinazoline-2,4-dione Chemical class C1=CC=C2C(=O)NC(=O)N(Cl)C2=C1 HFJMCDYTVQDJJS-UHFFFAOYSA-N 0.000 description 1
- WDALVHHIHIZUQY-UHFFFAOYSA-N 1-ethyl-6,7,8-trimethoxyquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=C(C(=C12)OC)OC)OC)=O)=O WDALVHHIHIZUQY-UHFFFAOYSA-N 0.000 description 1
- UWEZBQZUYGDKIY-UHFFFAOYSA-N 1-ethyl-6,7-dimethoxyquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=C(C=C12)OC)OC)=O)=O UWEZBQZUYGDKIY-UHFFFAOYSA-N 0.000 description 1
- PIVOTOHAEKDRTL-UHFFFAOYSA-N 1-ethyl-6-(trifluoromethyl)quinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=CC=C12)C(F)(F)F)=O)=O PIVOTOHAEKDRTL-UHFFFAOYSA-N 0.000 description 1
- YPLDIIDRJIFICP-UHFFFAOYSA-N 1-ethyl-6-hydroxyquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=CC=C12)O)=O)=O YPLDIIDRJIFICP-UHFFFAOYSA-N 0.000 description 1
- RQSQBVYHLGJWOC-UHFFFAOYSA-N 1-ethyl-6-nitroquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC(=CC=C12)[N+](=O)[O-])=O)=O RQSQBVYHLGJWOC-UHFFFAOYSA-N 0.000 description 1
- BBZFPVPLNWGTKT-UHFFFAOYSA-N 1-ethyl-7-fluoroquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC=C(C=C12)F)=O)=O BBZFPVPLNWGTKT-UHFFFAOYSA-N 0.000 description 1
- XDCYJSWKKNULSF-UHFFFAOYSA-N 1-ethyl-7-nitroquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC=C(C=C12)[N+](=O)[O-])=O)=O XDCYJSWKKNULSF-UHFFFAOYSA-N 0.000 description 1
- TWFRPKKXZVEXEA-UHFFFAOYSA-N 1-ethyl-8-methylquinazoline-2,4-dione Chemical class C(C)N1C(NC(C2=CC=CC(=C12)C)=O)=O TWFRPKKXZVEXEA-UHFFFAOYSA-N 0.000 description 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 description 1
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- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
- VFHUJFBEFDVZPJ-UHFFFAOYSA-N 1h-indole-2-carboxamide Chemical compound C1=CC=C2NC(C(=O)N)=CC2=C1 VFHUJFBEFDVZPJ-UHFFFAOYSA-N 0.000 description 1
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- 125000003163 2-(2-naphthyl)ethyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(C([H])=C([H])C2=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
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- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 description 1
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- QZFJPVDLQICTAW-UHFFFAOYSA-N 3-ethyl-2-methylpyrimido[1,2-a]pyrimidin-4-one Chemical compound C(C)C1=C(N=C2N(C1=O)C=CC=N2)C QZFJPVDLQICTAW-UHFFFAOYSA-N 0.000 description 1
- UMQKDYHNDQNEBD-UHFFFAOYSA-N 3-ethyl-2-methylquinazolin-4-one Chemical compound C1=CC=C2C(=O)N(CC)C(C)=NC2=C1 UMQKDYHNDQNEBD-UHFFFAOYSA-N 0.000 description 1
- VQFOHZWOKJQOGO-UHFFFAOYSA-N 4-fluorobenzenecarbothioamide Chemical compound NC(=S)C1=CC=C(F)C=C1 VQFOHZWOKJQOGO-UHFFFAOYSA-N 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract
本发明涉及式(Ⅰ)所示N-取代的3-氮杂二环烷衍生物在制备用于治疗成瘾性疾病和其它中枢神经系统疾病的药物中的应用,其中B、R1、R2和n的定义同说明书中所述。
Description
N-取代的氮杂二环烷衍生物在治疗中枢神经系统疾病中的应用
N-取代的氮杂二环烷衍生物已作为精神抑制药为人们所知(WO95/13279、WO95/15327、WO96/04272、US5475105、US5521209、US5616705、US5753690)。现在已发现这些物质还适于控制成瘾性疾病以及其它中枢神经系统疾病。
本发明提供了式I所示N-取代的3-氮杂二环烷衍生物及其与生理可接受酸的盐在制备用于治疗成瘾、用于治疗精神集中障碍(注意力不足障碍)、儿童活动过强(注意力不足活动过强障碍)、学习和记忆薄弱(认知功能受损)的药物中的应用:
其中
B是可以含有双键的4元、5元或6元环,
R1是苯基、萘基、菲基或噻吩基,所述基团分别可未取代或者被卤素原子、C1-4-烷基、三氟甲基、羟基、C1-4-烷氧基、氨基、一甲基氨基、二甲基氨基、氰基或硝基单取代或二取代,
n是数字0、1、2、3或4,且
其中
R3是氢原子、羟基或苯基,所述苯基未取代或者被氟、氯或溴原子取代,
R4是氢原子,或者
R3与R4一起为氧原子,
R5是苯基、萘基或噻吩基,所述基团分别可未取代或者被氟原子、氯原子、溴原子、羟基、硝基、氨基、C1-4-链烷酰基氨基、C1-4-烷基氨基、C1-4-烷基或甲氧基单取代或二取代,
R6是氢原子或甲基,
R7是苯基、萘基、苯并呋喃基、苯并噻吩基、噻吩基、吲哚基、N-甲基吲哚基或茚基,所述基团分别可未取代或者被氟原子、氯原子、溴原子、C1-4-烷基、羟基、甲氧基、硝基、氰基、三氟甲基、氨基或二-C1-4-烷基氨基单取代或二取代,或者R7是C3-7-环烷基,
R8是氢原子或氟或氯原子或C1-4-烷基、甲氧基或氨基,
R9是氢原子或甲基,且
R10是氢原子或甲基,或者
R9和R10与环碳原子一起形成螺环丙烷环,
R11是氢原子、羟基、C1-4-烷基或C1-4-烷氧基,或者与相邻碳原子一起为C=O-或C=S基,
X和Y是碳原子、CH、CH2、NH或C1-4-烷基-N或氮原子,
Z为直接键,或者Z是CO、CS、或CH或CH2,其中所述CH或CH2上的氢原子可被羟基、氨基或C1-4-烷氧基或卤素原子代替,且
A是氢原子、羟基、氨基、巯基、C1-4-烷基氨基、二-C1-4-烷基氨基、C1-4-烷硫基或C1-4-烷氧基,或者与相邻碳原子一起为C=O,或者
A是与Y结合的C3-C4-亚烷基,所述亚烷基可包含一个或两个非累积双键,并且其中的一个CH或CH2可被氮原子或硫原子或NH或N-CH3代替,并且该环可被氟原子、氯原子、甲基、甲氧基、硝基或氨基单取代,或者当该环是苯环时,其可以被氟原子、氯原子、甲基、三氟甲基、硝基、羟基、甲氧基、氨基、一甲基氨基或二甲基氨基单取代、二取代或三取代,
并且其中含有X、Y和Z的环可在1-位氮原子上携带C1-4-烷基、烯丙基或苄基,并且可含有1-3个非累积双键。
本发明的应用涉及所有成瘾性障碍,不论它们是由于物质滥用引起的还是其它成瘾性障碍例如对赌博成瘾。成瘾物质可以是:
鸦片类物质,例如吗啡或海洛因,
尼古丁,
酒精,
与苯并二氮杂受体复合物相互作用的物质、镇静剂或安定药,例如苯并二氮杂。
依据本发明,可能的成瘾物质特别是可卡因、安非他明、或类似于安非他明的物质。
式I化合物既可以以其外消旋物形式、也可以以其旋光异构体形式使用。
对于该新的适应征,本发明化合物可以通过常规方式口服或经非胃肠道、静脉内或肌内给药。
剂量取决于患者的年龄、身体状况和体重以及给药的类型。对于口服给药,活性化合物的日剂量一般为约1-100mg/kg体重,对于非胃肠道给药,一般为0.1-10mg/kg体重。
本发明化合物可在常规给药剂型、固体或液体剂型中使用,例如片剂、膜包衣片剂、胶囊、粉剂、粒剂、糖包衣片剂、栓剂、溶液剂、软膏剂、霜剂或喷雾剂。这些剂型是以常规方法制得的。为了制备剂型,可用常规药物辅料加工活性化合物,所述药物辅料有例如片剂粘合剂、填充剂、防腐剂、片剂崩解剂、流动调节剂、增塑剂、润湿剂、分散剂、乳化剂、溶剂、缓释剂、抗氧化剂和/或推进气体(参见H.Sucker等人:Pharmazeutische Technologie[制药技术],Thieme-Verlag,Stuttgart,1978)。所制得的给药剂型一般包含1-99%重量的活性化合物。
可提及下述物质作为式I化合物的实例:
1. 1-(4-氟苯基)-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
2. 1-苯基-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
3. 1-(4-氟苯基)-4-[外-6,7-二苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
4. 1-(4-氟苯基)-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁烷
5. 1-苯基-2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙-1-酮
6. 1-(4-氟苯基)-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁烷
7. 1-(4-氟苯基)-4-[外-6-间氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
8. 1-(4-氟苯基)-4-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
9. 1-(4-氟苯基)-4-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
10. 1-(4-氟苯基)-4-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
11. 1-(4-氟苯基)-4-[外-6-对甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
12. 1-(4-氟苯基)-4-[外-6-间,对二氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
13. 1-(4-氟苯基)-4-[外-6-间,对二甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
14. 1-(4-氟苯基)-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
15. 1-苯基-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
16. 1-(4-氟苯基)-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁烷
17. 1-(4-氟苯基)-4-[外-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
18. 1-(4-氟苯基)-4-[外-6-间硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
19. 1-(4-氟苯基)-4-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
20. 1-(4-氟苯基)-4-[外-6-对氰基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
21. 1-(4-氟苯基)-4-[外-6-噻吩-3-基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
22. 1-(4-氟苯基)-4-[外-6-吡啶-3-基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
23. 1-(4-氟苯基)-3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙-1-酮
24. 1-(二-4-氟苯基)-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁烷
25. 1-(二-4-氟苯基)-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁烷
26. 1-(4-氟苯基)-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
27. 1-(4-氟苯基)-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
28. 1-(4-氟苯基)-4-[外-6,7-二苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
29. 1-苯基-4-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
30. 1-苯基-4-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
31. 1-(4-氟苯基)-4-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
32. 1-(4-氟苯基)-4-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
33. 1-(4-氟苯基)-4-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-醇
34. 1-(4-氟苯基)-4-[外-6-对氨基苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁-1-酮
35.N-(3-[外-6-苯基3-氮杂二环[3.2.0]庚烷-3-基]丙基)-4-氟苯甲酰胺
36. 1-(3-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)苯甲酰胺
37. 1-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氟苯甲酰胺
38.N-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
39.N-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基-4-氟苯甲酰胺
40.N-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基苯甲酰胺
41. 1-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基-4-异丙基苯甲酰胺
42.N-(3-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-4-氯苯甲酰胺
43.N-(2-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氯苯甲酰胺
44.N-(3-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-3-甲氧基苯甲酰胺
45.N-(3-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-3-硝基苯甲酰胺
46.N-(3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-4-氟苯甲酰胺
47.N-(3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)苯甲酰胺
48.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氟苯甲酰胺
49.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
50.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基-4-氟苯甲酰胺
51.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基苯甲酰胺
52.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基-4-异丙基苯甲酰胺
53.N-(3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-4-氯苯甲酰胺
54.N-(3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-3-甲氧基苯甲酰胺
55.N-(3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基)-3-硝基苯甲酰胺
56.N-(2-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氯苯甲酰胺
57.N-(2-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氯苯甲酰胺
58.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-2-羟基苯甲酰胺
59.N-(2-[外-6-间羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氯苯甲酰胺
60.外-3-正丁基-6-苯基-3-氮杂二环[3.2.0]庚烷
61.外-3-甲基-6-苯基-3-氮杂二环[3.2.0]庚烷
62.外-3-甲基-6-对氟苯基-3-氮杂二环[3.2.0]庚烷
63.外-3-正丙基-6-对氟苯基-3-氮杂二环[3.2.0]庚烷
64.外-3-甲基-6,7-二苯基-3-氮杂二环[3.2.0]庚烷
65.外-3-正丙基-6-间羟基苯基-3-氮杂二环[3.2.0]庚烷
66.外-3-烯丙基-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷
67.外-3-(3,4-二甲氧基)苯乙基-6-苯基-3-氮杂二环[3.2.0]庚烷
68.外-3-(3,4-二甲氧基)苯乙基-6-对氟苯基-3-氮杂二环[3.2.0]庚烷
69.外-3-(3,4-二羟基)苯乙基-3-氮杂二环[3.2.0]庚烷
70.外-3-苯乙基-6-对氟苯基-3-氮杂二环[3.2.0]庚烷
71. 6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
72.(+)-6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
73.(-)-6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
74. 6-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
75. 6-β-[外-6,7-二苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
76. 6-β-[外-6,7-二(对氟苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
77. 6-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
78. 6-β-[外-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
79. 6-β-[外-6-间羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
80. 6-β-(2-[外-6-对氨基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
81. 6-β-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
82. 6-β-[外-6-对甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
83. 6-β-[外-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
84. 6-β-[外-6-间氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
85. 6-β-[外-6-对羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
86. 6-β-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
87. 6-β-[外-6-(对叔丁基苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
88. 6-β-[内-6-(对叔丁基苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
89. 6-β-[外-6-(3,4-二氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
90. 6-β-[外-6-(3,4-二甲氧基苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
91. 6-β-[外-6-对氰基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
92. 6-β-[外-6-(3,4-二羟基苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
93. 6-β-[外-6-(邻氟苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
94. 6-β-[外-6-噻吩-3-基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
95. 6-β-[外-6-(5-氯噻吩-2-基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
96. 6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-2,3-二氢-5H-噻唑并[3,2-a]嘧啶-5-酮
97. 6-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-2,3-二氢-5H-噻唑并[3,2-a]嘧啶-5-酮
98. 6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,3,7-三甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
99. 6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-5H-噻唑并[3,2-a]嘧啶-5-酮
100. 6-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-5H-噻唑并[3,2-a]嘧啶-5-酮
101. 7-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
102. 7-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
103. 7-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
104. 7-β-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
105. 7-β-[外-6-对甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
106. 7-β-[外-6-间羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2H,6H-嘧啶并[2,1-b][1,3]噻嗪-6-酮
107. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
108.(+)-3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
109.(-)-3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
110. 3-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
111. 3-β-[外-6-间氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
112. 3-β-[外-6-对氰基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
113. 3-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
114. 3-β-[外-6-对羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
115. 3-β-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
116. 3-β-[外-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
117. 3-β-[外-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
118. 3-β-[内-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
119. 3-β-[外-6-间羟基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
120. 3-β-[外-6-对氨基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
121. 3-β-[外-6-对碘苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
122. 3-β-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
123. 3-β-[外-6-(3,4-二氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
124. 3-β-[外-6-(3,4-二羟基苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
125. 3-β-[外-6-(3,5-二氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
126. 3-β-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
127. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲基-2,4-(1H,3H)喹唑啉二酮
128. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-氯-2,4-(1H,3H)喹唑啉二酮
129. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-氟-2,4-(1H,3H)喹唑啉二酮
130. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-5-氯-2,4-(1H,3H)喹唑啉二酮
131. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-氟-2,4-(1H,3H)喹唑啉二酮
132. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-甲基-2,4-(1H,3H)喹唑啉二酮
133. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-8-甲氧基-2,4-(1H,3H)喹唑啉二酮
134. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-三氟甲基-2,4-(1H,3H)喹唑啉二酮
135. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-硝基-2,4-(1H,3H)喹唑啉二酮
136. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-硝基-2,4-(1H,3H)喹唑啉二酮
137. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-氨基-2,4-(1H,3H)喹唑啉二酮
138. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-氨基-2,4-(1H,3H)喹唑啉二酮
139. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6-羟基-2,4-(1H,3H)喹唑啉二酮
140. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-5-氯2,4-(1H,3H)喹唑啉二酮
141. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,7-二甲氧基-2,4-(1H,3H)喹唑啉二酮
142. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,8-二氯-2,4-(1H,3H)喹唑啉二酮
143. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,7,8-三甲氧基-2,4-(1H,3H)喹唑啉二酮
144. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1-甲基-2,4-(1H,3H)喹唑啉二酮
145. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1-乙基-2,4-(1H,3H)喹唑啉二酮
146. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1-烯丙基-2,4-(1H,3H)喹唑啉二酮
147. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1-苄基-2,4-(1H,3H)喹唑啉二酮
148. 3-γ-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丙基-2,4-(1H,3H)喹唑啉二酮
149. 3-δ-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]丁基-2,4-(1H,3H)喹唑啉二酮
150. 3-β-[外-6-(2-噻吩基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
151. 3-β-[外-6-(5-氯-2-噻吩基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
152. 3-β-[外-6-(3-噻吩基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
153. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1H-噻吩并[3,2-d]嘧啶-2,4-二酮
154. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1H-噻吩并[2,3-d]嘧啶-2,4-二酮
155. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1H-噻吩并[3,4-d]嘧啶-2,4-二酮
156. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1-甲基-1H,3H-吡啶并[2,3-d]嘧啶-2,4-二酮
157. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-3H-喹唑啉-4-酮
158. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲氧基-3H-喹唑啉-4-酮
159. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮二盐酸盐
160. 3-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
161. 3-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
162. 3-β-[外-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
163. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,6-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
164. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,7-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
165. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,8-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
166. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,9-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
167. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,6,8-三甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
168. 3-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,7-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
169. 3-β-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,7-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
170. 3-β-[外-6-苯基--3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,8-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
171. 3-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,9-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
172. 3-β-[外-6-(5-氯噻吩-2-基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
173. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
174. 3-β-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
175. 3-β-[外-6-对甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-6,7,8,9-四氢-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
176. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-4H-嘧啶并[1,2-a]嘧啶-4-酮
177. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-7-氯-4H-嘧啶并[1,2-a]嘧啶-4-酮
178. 6-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-7-甲基-1H,5H-咪唑并[1,2-a]嘧啶-5-酮
179. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基-7,8-二氢-4H,6H-吡咯并[1,2-a]嘧啶-4-酮
180. 2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基苯并咪唑
181. 1-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基苯并咪唑
182. 1-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2,3-二氢苯并咪唑-2-酮
183. 2-[外-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基苯并咪唑
184. 3-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基吲哚,熔点:193-195℃(盐酸盐)
185. 3-β-(2-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基吲哚
186. 3-β-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基吲哚,熔点:104-105℃(盐酸盐)
187. 3-β-[外-6-间甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基吲哚
188. 2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-3,4-二氢喹唑啉-4-酮
189. 2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-3,4-二氢喹唑啉-4-硫酮
190. 2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-3,4-二氢喹唑啉-4-酮
191. 2-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-3,4-二氢喹唑啉-4-酮
192. 2-[外-6-邻甲氧基苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-3,4-二氢喹唑啉-4-酮
193. 2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-4-羟基-6-甲基嘧啶
194. 6-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基-2-甲基-4-羟基嘧啶
195. 6-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基尿嘧啶
196. 6-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]甲基尿嘧啶
197. 6-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1,2,3,4-四氢-1,3-二甲基-2,4-二氧代嘧啶
198. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-6-甲基-2,4-二氧代嘧啶
199. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-1,6-二甲基-2,4-二氧代嘧啶
200. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-3,6-二甲基-2,4-二氧代嘧啶
201. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-3,6-二甲基-2,4-二硫代嘧啶
202. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-1,3,6-三甲基-2,4-二氧代嘧啶
203. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-1,2,3,4-四氢-6-氨基-1-甲基-2,4-二氧代嘧啶
204. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-氨基-6-甲基-4(3H)嘧啶酮
205. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-氨基-3,6-二甲基-4(3H)嘧啶酮
206. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
207. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3-乙基-6-甲基-4(3H)嘧啶酮
208. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-氨基-3-乙基-6-甲基-4(3H)嘧啶酮
209. 5-β-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
210. 5-β-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
211. 5-β-[外-6-邻氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
212. 5-β-[外-6-对三氟甲基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
213. 5-β-[外-6-对氰基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
214. 5-β-[外-6-间氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
215. 5-β-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基-2-甲基氨基-4-甲氧基-6-甲基嘧啶
216. 3-β-[外-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
217. 3-β-[内-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
218. 3-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
219. 3-β-[外-6-对三氟甲基苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-6-氟-2,4-(1H,3H)喹唑啉二酮
220. 3-β-[外-6-间氯苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
221. 3-β-[外-6-对甲氧基苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-6-甲基-2,4-(1H,3H)喹唑啉二酮
222. 5-β-[外-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
223. 5-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
224. 1-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2(3H)苯并咪唑酮
225. 5-β-[外-6-对硝基苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
226. 5-β-[外-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
227. 5-β-[内-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
228. 3-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
229. 1-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基二氢吲哚-2-酮
230. 6-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
231. 1-β-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2(1H)喹诺酮(Chinolon)
232. 3-β-[7-苯基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
233. 3-β-[7-对氟苯基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
234. 5-β-[7-对氟苯基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨乙基-3,6-二甲基-4(3H)嘧啶酮
235. 3-β-[外-6-对氟苯基-3-氮杂二环[3.1.0]已烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
236. 3-β-[外-6-苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
237. 3-β-[6,6-二苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
238. 5-β-[外-6-对氟苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
239. 6-β-[外-6-间氯苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
240. 3-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
241. 5-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
242. 6-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
243. 1-β-[6-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2(3H)苯并咪唑酮
244. 1-β-[-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基二氢吲哚-2-酮
245. 1-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2(1H)喹诺酮
246. 3-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
247. 5-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
248. 6-β-[外-6-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
249. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基二氢吲哚-2-酮
250. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2(1H)喹诺酮
251. 3-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
252. 5-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
253. 6-β-[内-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
254. 1-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基二氢吲哚-2-酮
255. 1-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2(1H)喹诺酮
256. 3-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
257. 5-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
258. 6-β-[外-7-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
259. 1-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基二氢吲哚-2-酮
260. 1-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基-2(1H)喹诺酮
261. 3-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
262. 5-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
263. 3-β-[内-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
264. 5-β-[内-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
265. 3-β-[内-6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
266. 5-β-[内-6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
267. 3-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
268. 5-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
269. 1-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2(3H)苯并咪唑酮
270. 1-β-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基二氢吲哚-2-酮
271. 3-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
272. 5-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
273. 3-β-[6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
274. 5-β-[6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
275. 3-β-[6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
276. 5-β-[6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
277. 1-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2(3H)苯并咪唑酮
278. 1-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基二氢吲哚-2-酮
279. 1-β-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基-2(1H)喹诺酮
280. 3-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮(Chinazolidon)
281. 5-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
282. 3-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2-甲基-4H-吡啶并[1.2-a]嘧啶-4-酮
283. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2(1H)喹诺酮
284. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2(3H)苯并咪唑酮
285. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基二氢吲哚-2-酮
286. 3-β-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
287. 5-β-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
288. 3-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
289. 5-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
290. 3-β-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
291. 5-β-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
292. 6-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-7-甲基-5H-噻唑并[3.2-a]嘧啶-5-酮
293. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2(3H)苯并咪唑酮
294. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基二氢吲哚-2-酮
295. 1-β-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2(1H)喹诺酮
296. 3-β-[外-7-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
297. 5-β-[外-7-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
298. 3-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
299. 5-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
300. 3-β-[7-对氟苯基-3-氮杂二环[4.3.0]壬-1-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
301. 5-β-[7-苯基-3-氮杂二环[4.3.0]壬-1-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
302. 5-β-[7-对氟苯基-3-氮杂二环[4.3.0]壬-1-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
303. 3-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
304. 5-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
305. 1-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2(3H)苯并咪唑酮
306. 1-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基二氢吲哚-2-酮
307. 1-β-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基-2(1H)喹诺酮
308. 3-β-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
309. 5-β-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
310. 3-β-[外/内-6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2,4-(1H,3H)喹唑啉二酮
311. 5-β-[外/内-6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基-2-甲基氨基-3,6-二甲基-4(3H)嘧啶酮
312. 1-β-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基二氢吲哚-2-酮
313. 6-β-[6-苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基-7-甲基-5H-噻唑并[3,2-a]嘧啶-5-酮
314.N-(2-[外-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)-4-氟苯甲酰胺
315.N-(2-[内-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)-4-氟苯甲酰胺
316.N-(2-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)-4-氟苯甲酰胺
317.N-(2-[外-6-对三氟甲基苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
318.N-(2-[外-6-间氯苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
319.N-(2-[外-6-对甲氧基苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)-4-氯苯甲酰胺
320.N-(2-[外-6-苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)萘-1-甲酰胺
321. 1-(4-氟苯基)-4-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]丁-1-酮
322. 1-(4-氟苯基)-4-[外-6-对氟苯基-7-甲基-1,5-顺式-3,7-二氮杂二环[3.3.0]辛烷-3-基]丁-1-醇
323.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)苯甲酰胺
324. 1-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)萘
325. 1-(4-氟苯基)-4-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-酮
326. 1-(4-氟苯基)-4-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-醇
327.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-2-(N-甲基)氨基苯甲酰胺
328.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-5-氯噻吩-2-基甲酰胺
329.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)茚-3-甲酰胺
330.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-4-氟苯甲酰胺
331.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)萘-1-甲酰胺
332. 1-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)萘
333. 1-(4-氟苯基)-4-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]丁-1-酮
334.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)苯甲酰胺
335.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)茚-3-甲酰胺
336.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)萘-1-甲酰胺
337.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)-4-氟苯甲酰胺
338.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)-3-氯-1-苯并噻吩-2-基甲酰胺
339. 1-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)萘
340. 1-(4-氟苯基)-4-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]丁-1-酮
341. 1-(4-氟苯基)-4-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]丁-1-醇
342.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)-2-(N-甲基)氨基苯甲酰胺
343.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)-5-氯噻吩-2-基甲酰胺
344.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)苯甲酰胺
345.N-(2-[6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)-3-氯-1-苯并噻吩-2-基甲酰胺
346.N-(2-[6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)萘-1-甲酰胺
347.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)茚-3-甲酰胺
348.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-6-烯-3-基]乙基)萘-1-甲酰胺
349. 1-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)萘
350. 1-(4-氟苯基)-4-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-酮
351. 1-(4-氟苯基)-4-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-醇
352.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]-2-(N-甲基)氨基苯甲酰胺
353.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)苯甲酰胺
354.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-5-氯噻吩-2-基甲酰胺
355.N-(2-[内-6-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-4-氟苯甲酰胺
356.N-(2-[内-6-对三氟甲基苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)茚-3-甲酰胺
357. 2-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)萘
358.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)苯甲酰胺
359.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)-2-(N-甲基)氨基苯甲酰胺
360.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-7-烯-3-基]乙基)萘-1-甲酰胺
361. 1-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)萘
362. 1-(4-氟苯基)-4-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]丁-1-酮
363.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)苯甲酰胺
364.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)-5-氯噻吩-2-基甲酰胺
365.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)-3-氯-1-苯并噻吩-2-基甲酰胺
366.N-(2-[外-7-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)茚-3-甲酰胺
367.N-(2-[外-7-苯基-1,5-顺式-3-氮杂二环[4.3.0]壬-8-烯-3-基]乙基)萘-1-甲酰胺
368. 1-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)萘
369. 1-(4-氟苯基)-4-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-酮
370. 1-(4-氟苯基)-4-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]丁-1-醇
371.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-2-(N-甲基)氨基苯甲酰胺
372.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)苯甲酰胺
373.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)-5-氯噻吩-2-基甲酰胺
374.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)萘-1-甲酰胺
375.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[4.3.0]壬烷-3-基]乙基)茚-3-甲酰胺
376. 1-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基)萘
377. 1-(4-氟苯基)-4-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]丁-1-酮
378.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基)苯甲酰胺
379.N-(2-[6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛-6-烯-3-基]乙基)萘-1-甲酰胺
380. 1-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘
381. 1-(4-氟苯基)-4-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]丁-1-醇
382.N-(2-[外-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
383.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘-1-甲酰胺
384.N-(2-[外-6-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)茚-3-甲酰胺
385. 1-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘
386. 1-(4-氟苯基)-4-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]丁-1-酮
387.N-(2-[内-6-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
388.N-(2-[内-6-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘-1-甲酰胺
389. 1-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘
390. 1-(4-氟苯基)-4-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]丁-1-酮
391.N-(2-[外-7-对氟苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
392.N-(2-[外-7-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)萘-1-甲酰胺
393.N-(2-[外-7-苯基-1,5-顺式-3-氮杂二环[3.3.0]辛烷-3-基]乙基)茚-3-甲酰胺
394.N-(2-[外-6-对氟苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基)-4-氟苯甲酰胺
395.N-(2-[外-6-苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基)-5-氯噻吩-2-基甲酰胺
396.N-(2-[6,6-二苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基)萘-1-基甲酰胺
397.N-(2-[外-6-对氟苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基)-3-氯-1-苯并噻吩-2-基甲酰胺
398.N-(2-[外-6-间氯苯基-3-氮杂二环[3.1.0]己烷-3-基]乙基)-4-氯苯甲酰胺
399.1-(2-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)萘
400.N-(2-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)苯甲酰胺
401.N-(2-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)萘-1-甲酰胺
402.N-(2-[6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)茚-3-甲酰胺
403. 1-(2-[外/内-6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)萘
404.N-(2-[外/内-6-对氟苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛烷-3-基]乙基)苯甲酰胺
405. 1-(2-[6-苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)萘
406.N-(2-[6-苯基-1,5-顺式-8-氧杂-3,7-二氮杂二环[3.3.0]辛-6-烯-3-基]乙基)苯甲酰胺
407.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯磺酰胺
408.N-(2-[外-6-苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯磺酰胺
409.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-N-甲基苯磺酰胺
410.N-(2-[外-6-(5-氯噻吩-2-基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氟苯磺酰胺
411. 3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1-苯氧基丙烷
412. 2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1-对氟苯氧基乙烷
413. 3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1-(1-萘基氧基)丙烷
414. 3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1-对叔丁基苯氧基丙烷
415. 3-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]-1-对氟苯氧基丙烷
416.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)硫代苯甲酰胺
417.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氟硫代苯甲酰胺
418.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氯硫代苯甲酰胺
419.O-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酸酯
420.O-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-氟苯甲酸酯
421.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1H-苯并[cd]吲哚-2-酮
422.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1H-苯并[cd]吲哚-2-酮
423.N-(2-[外-6-间氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1H-苯并[cd]吲哚-2-酮
424.N-(2-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1H-苯并[cd]吲哚-2-酮
425. 3,3-二甲基-1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)二氢吲哚-2-酮
426. 3,3-二甲基-1-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)二氢吲哚-2-酮
427. 3,3-二甲基-1-(2-[外-6-间氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)二氢吲哚-2-酮
428. 1-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-3,3,5-三甲基二氢吲哚-2-酮
429. 3,4-二氯-N-(2-[外-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
430. 2,5-二氟-N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
431. 2-氨基-N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
432. 2-氨基-N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
433.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-2-甲基氨基苯甲酰胺
434.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-2-甲基氨基苯甲酰胺
435. 3-氨基-N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
436. 4-氨基-N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯甲酰胺
437.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)噻吩-2-甲酰胺
438. 5-氯-N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)噻吩-2-甲酰胺
439. 5-氯-N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)噻吩-2-甲酰胺
440. 5-氯-N-(2-[外-6-(5-氯-2-噻吩基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基)噻吩-2-甲酰胺
441.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯并[b]呋喃-2-甲酰胺
442. 3-氯-N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯并[b]噻吩-2-甲酰胺
443. 3-氯-N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯并[b]噻吩-2-甲酰胺
444. 3-氯-N-(2-[外-6-对硝基苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯并[b]噻吩-2-甲酰胺
445.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)茚-3-甲酰胺
446.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)茚-3-甲酰胺
447.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)环丙烷甲酰胺
448.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)环戊烷甲酰胺
449.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)环戊烷甲酰胺
450.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)环己烷甲酰胺
451.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)环己烷甲酰胺
452.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)萘-1-甲酰胺
453.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)吲哚-2-甲酰胺
454.N-(2-[外-6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)吲哚-3-甲酰胺
455.外-6-对氟苯基-3-[2-(1-萘基)乙基]-3-氮杂二环[3.2.0]庚烷
456.外-6-对氯苯基-3-[2-(1-萘基)乙基]-3-氮杂二环[3.2.0]庚烷
457.外-6-间氯苯基-3-[2-(1-萘基)乙基]-3-氮杂二环[3.2.0]庚烷
458.外-6-(5-氯-2-噻吩基)-3-[2-(1-萘基)乙基]-3-氮杂二环[3.2.0]庚烷
459.外-6-对氟苯基-3-[2-(2-萘基)乙基]-3-氮杂二环[3.2.0]庚烷
460.外-6-对氟苯基-3-[1-萘基甲基]-3-氮杂二环[3.2.0]庚烷
461.外-6-对氟苯基-3-[2-萘基甲基]-3-氮杂二环[3.2.0]庚烷
462. 4-(6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基)-1-(噻吩-2-基)丁烷-1-酮
463. 4-(6-对氯苯基-3-氮杂二环[3.2.0]庚烷-3-基)-1-(噻吩-2-基)丁烷-1-酮
464.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-4-苯基吡咯烷-2-酮
465.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)苯并噁唑啉-2-酮
466.N-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)异二氢吲哚酮
467. 1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)吲唑
468. 1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1,8-萘磺酸内酰胺
469. 4-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)-1,4-苯并噁嗪-3-酮
470. 1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)喹喔啉-2(1H)-酮
471. 1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)二氢吲哚-2-酮
472. 1-(2-[外-6-对氟苯基-3-氮杂二环[3.2.0]庚烷-3-基]乙基)螺[环丙烷-1′,3-二氢吲哚-2-酮]
473. 3,6-二甲基-2-甲基氨基-5-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3H-嘧啶-4-酮
474. 3,6-二甲基-2-甲基氨基-5-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3H-嘧啶-4-酮
475. 3,6-二甲基-2-甲基氨基-5-[2-(外-6-(5-氯-1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3H-嘧啶-4-酮
476. 3,6-二甲基-2-甲基氨基-5-[2-(外-6-(6-氯-2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3H-嘧啶-4-酮
477. 3,6-二甲基-2-甲基氨基-5-[2-(外-6-(9-菲基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3H-嘧啶-4-酮
478. 7-甲基-6-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基)-5H-噻唑并[3,2-a]嘧啶-5-酮
479. 3-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H,3H-喹唑啉-2,4-二酮
480. 3-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H,3H-喹唑啉-2,4-二酮
481. 6-氟-3-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H,3H-喹唑啉-2,4-二酮
482. 3-[2-(外-6-(5-氯-2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H,3H-喹唑啉-2,4-二酮
483. 3-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-2-甲基-4H-吡啶并[1.2-a]嘧啶-4-酮
484. 1-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-2(1H)喹诺酮
485. 1-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]二氢吲哚-2-酮
486. 1-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-2(3H)苯并咪唑酮
487. 1-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3-甲基-2(3H)苯并咪唑酮
488.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-苯甲酰胺
489.N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-苯甲酰胺
490.N-[2-(外-6-(5-氯-1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-苯甲酰胺
491. 3-[2-(1-萘基)乙基]-外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷
492. 3-[2-(1-萘基)乙基]-外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷
493. 1-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H-苯并[cd]吲哚-2-酮
494. 1-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H-苯并[cd]吲哚-2-酮
495. 3,3-二甲基-1-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1,3-二氢吲哚-2-酮
496. 3,3-二甲基-1-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1,3-二氢吲哚-2-酮
497. 3,3-二甲基-1-[2-(外-6-(6-氯-2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1,3-二氢吲哚-2-酮
498.5-氯-N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-2-噻吩甲酰胺
499. 5-氯-N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-2-噻吩甲酰胺
500.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-4-氟苯甲酰胺
501.N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-4-硝基苯甲酰胺
502.N-[2-(外-6-(6-氯-2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]苯甲酰胺
503.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-4-甲氧基苯甲酰胺
504.N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-4-羟基苯甲酰胺
505.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-3,4-二氯苯甲酰胺
506.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]萘-1-甲酰胺
507.N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]萘-1-甲酰胺
508.N-[2-(外-6-(9-菲基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]苯甲酰胺
509. 1-[2-(外-6-(6-氯-2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H-苯并[cd]吲哚-2-酮
510. 1-[2-(外-6-(9-菲基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]-1H-苯并[cd]吲哚-2-酮
511.N-[2-(外-6-(1-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]异二氢吲哚酮
512.N-[2-(外-6-(2-萘基)-3-氮杂二环[3.2.0]庚烷-3-基)乙基]异二氢吲哚酮
513.(+)-(1S,5R,6S)外-1-[2-[6-(4-氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3-甲基-2H-1,3-二氢苯并咪唑-2-酮
514.(+)-(1S,5R,6S)外-1-[2-[6-(4-氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3-乙基-2H-1,3-二氢苯并咪唑-2-酮
515.(+)-(1S,5R,6S)外-1-[2-[6-(4-氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3-正丙基-2H-1,3-二氢苯并咪唑-2-酮
516.(+)-(1S,5R,6S)外-2-[2-[6-(4-氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3,3-二甲基-2,3-二氢-1,2-苯并异噻唑1,1-二氧化物
517.(+)-(1S,5R,6S)外-2-[2-[6-(4-氯苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-2,3-二氢-1,2-苯并异噻唑1,1-二氧化物
518.(+)-(1S,5R,6S)外-2-[2-[6-(4-氟苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3,3-二甲基-2,3-二氢-1,2-苯并异噻唑1,1-二氧化物
519.(+)-(1S,5R,6S)外-2-[2-[6-(4-氟苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-3,3-二乙基-2,3-二氢-1,2-苯并异噻唑1,1-二氧化物
520.(+)-(1S,5R,6S)外-2-[2-[6-(4-氟苯基)-3-氮杂二环[3.2.0]庚烷-3-基]乙基]-2,3-二氢-1,2-苯并异噻唑1,1-二氧化物
Claims (4)
其中
B是可以含有双键的4元、5元或6元环,
R1是苯基、萘基、菲基或噻吩基,所述基团分别可未取代或者被卤素原子、C1-4-烷基、三氟甲基、羟基、C1-4-烷氧基、氨基、一甲基氨基、二甲基氨基、氰基或硝基单取代或二取代,
n是数字0、1、2、3或4,且
R3是氢原子、羟基或苯基,所述苯基未取代或者被氟、氯或溴原子取代,
R4是氢原子,或者
R3与R4一起为氧原子,
R5是苯基、萘基或噻吩基,所述基团分别可未取代或者被氟原子、氯原子、溴原子、羟基、硝基、氨基、C1-4-链烷酰基氨基、C1-4-烷基氨基、C1-4-烷基或甲氧基单取代或二取代,
R6是氢原子或甲基,
R7是苯基、萘基、苯并呋喃基、苯并噻吩基、噻吩基、吲哚基、N-甲基吲哚基或茚基,所述基团分别可未取代或者被氟原子、氯原子、溴原子、C1-4-烷基、羟基、甲氧基、硝基、氰基、三氟甲基、氨基或二-C1-4-烷基氨基单取代或二取代,或者R7是C3-7-环烷基,
R8是氢原子或氟或氯原子或C1-4-烷基、甲氧基或氨基,
R9是氢原子或甲基,且
R10是氢原子或甲基,或者
R9和R10与环碳原子一起形成螺环丙烷环,
R11是氢原子、羟基、C1-4-烷基或C1-4-烷氧基,或者与相邻碳原子一起为C=O-或C=S基,
X和Y是碳原子、CH、CH2、NH或C1-4-烷基-N或氮原子,
Z为直接键,或者Z是CO、CS、或CH或CH2,其中所述CH或CH2上的氢原子可被羟基、氨基或C1-4-烷氧基或卤素原子代替,且
A是氢原子、羟基、氨基、巯基、C1-4-烷基氨基、二-C1-4-烷基氨基、C1-4-烷硫基或C1-4-烷氧基,或者与相邻碳原子一起为C=O,或者
A是与Y结合的C3-C4-亚烷基,所述亚烷基可包含-个或两个非累积双键,并且其中的一个CH或CH2可被氮原子或硫原子或NH或N-CH3代替,并且该环可被氟原子、氯原子、甲基、甲氧基、硝基或氨基单取代,或者当该环是苯环时,其可以被氟原子、氯原子、甲基、三氟甲基、硝基、羟基、甲氧基、氨基、一甲基氨基或二甲基氨基单取代、二取代或三取代,
并且其中含有X、Y和Z的环可在1-位氮原子上携带C1-4-烷基、烯丙基或苄基,并且可含有1-3个非累积双键。
2.权利要求1的应用,其中所述应用是在制备用于治疗成瘾性疾病的药物中的应用。
3.权利要求1或2的应用,其中所述应用是在制备用于治疗可卡因成瘾的药物中的应用。
4.权利要求1或2的应用,其中所述应用是在制备用于治疗安非他明和类似于安非他明的物质成瘾的药物中的应用。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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DE19854147.3 | 1998-11-24 | ||
DE19854147A DE19854147A1 (de) | 1998-11-24 | 1998-11-24 | Verwendung von N-substituierten Azabicycloalkan-Derivaten zur Verwendung bei der Bekämpfung der Cocainsucht |
Publications (1)
Publication Number | Publication Date |
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CN1328455A true CN1328455A (zh) | 2001-12-26 |
Family
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CN99813559A Pending CN1328455A (zh) | 1998-11-24 | 1999-11-12 | N-取代的氮杂二环烷衍生物在治疗中枢神经系统疾病中的应用 |
Country Status (21)
Country | Link |
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EP (1) | EP1133293A1 (zh) |
JP (1) | JP2002530333A (zh) |
KR (1) | KR20010080535A (zh) |
CN (1) | CN1328455A (zh) |
AR (1) | AR021502A1 (zh) |
AU (1) | AU1775300A (zh) |
BG (1) | BG105549A (zh) |
BR (1) | BR9915589A (zh) |
CA (1) | CA2352526A1 (zh) |
CZ (1) | CZ20011796A3 (zh) |
DE (1) | DE19854147A1 (zh) |
HK (1) | HK1040933A1 (zh) |
HR (1) | HRP20010472A2 (zh) |
HU (1) | HUP0104416A3 (zh) |
IL (1) | IL143181A0 (zh) |
NO (1) | NO20012538L (zh) |
PL (1) | PL348758A1 (zh) |
SK (1) | SK7112001A3 (zh) |
TR (1) | TR200101476T2 (zh) |
WO (1) | WO2000030639A1 (zh) |
ZA (1) | ZA200103976B (zh) |
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EP1836183A2 (en) | 2004-12-13 | 2007-09-26 | Galileo Pharmaceuticals, Inc. | Spiro derivatives as lipoxygenase inhibitors |
GB0812310D0 (en) | 2008-07-03 | 2008-08-13 | Syngenta Ltd | Novel herbicides |
WO2014111837A1 (en) * | 2013-01-15 | 2014-07-24 | Novartis Ag | Use of alpha 7 nicotinic acetylcholine receptor agonists |
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WO1989004311A1 (en) * | 1987-11-12 | 1989-05-18 | American Home Products Corporation | Polycyclicamines with psychotropic activity |
DE4427648A1 (de) * | 1994-08-04 | 1996-02-08 | Basf Ag | N-Stubstituierte 3-Azabicyclo[3,2,0,]heptan-Derivate, ihre Herstellung und Verwendung |
DE4341403A1 (de) * | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
DE4427647A1 (de) * | 1994-08-04 | 1996-02-08 | Basf Ag | N-substituierte Azabicycloheptan-Derivate, ihre Herstellung und Verwendung |
-
1998
- 1998-11-24 DE DE19854147A patent/DE19854147A1/de not_active Withdrawn
-
1999
- 1999-11-12 TR TR2001/01476T patent/TR200101476T2/xx unknown
- 1999-11-12 AU AU17753/00A patent/AU1775300A/en not_active Abandoned
- 1999-11-12 BR BR9915589-3A patent/BR9915589A/pt not_active IP Right Cessation
- 1999-11-12 JP JP2000583522A patent/JP2002530333A/ja active Pending
- 1999-11-12 HU HU0104416A patent/HUP0104416A3/hu unknown
- 1999-11-12 IL IL14318199A patent/IL143181A0/xx unknown
- 1999-11-12 KR KR1020017006445A patent/KR20010080535A/ko not_active Application Discontinuation
- 1999-11-12 SK SK711-2001A patent/SK7112001A3/sk unknown
- 1999-11-12 PL PL99348758A patent/PL348758A1/xx not_active Application Discontinuation
- 1999-11-12 EP EP99960974A patent/EP1133293A1/de not_active Withdrawn
- 1999-11-12 WO PCT/EP1999/008734 patent/WO2000030639A1/de not_active Application Discontinuation
- 1999-11-12 CA CA002352526A patent/CA2352526A1/en not_active Abandoned
- 1999-11-12 CN CN99813559A patent/CN1328455A/zh active Pending
- 1999-11-12 CZ CZ20011796A patent/CZ20011796A3/cs unknown
- 1999-11-24 AR ARP990105979A patent/AR021502A1/es unknown
-
2001
- 2001-05-16 ZA ZA200103976A patent/ZA200103976B/en unknown
- 2001-05-23 NO NO20012538A patent/NO20012538L/no not_active Application Discontinuation
- 2001-05-30 BG BG105549A patent/BG105549A/xx unknown
- 2001-06-21 HR HR20010472A patent/HRP20010472A2/hr not_active Application Discontinuation
-
2002
- 2002-04-12 HK HK02102768.4A patent/HK1040933A1/zh unknown
Also Published As
Publication number | Publication date |
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WO2000030639A1 (de) | 2000-06-02 |
AU1775300A (en) | 2000-06-13 |
CZ20011796A3 (cs) | 2002-05-15 |
ZA200103976B (en) | 2002-05-16 |
DE19854147A1 (de) | 2000-05-25 |
BR9915589A (pt) | 2001-08-07 |
HK1040933A1 (zh) | 2002-06-28 |
JP2002530333A (ja) | 2002-09-17 |
PL348758A1 (en) | 2002-06-03 |
HUP0104416A2 (hu) | 2002-04-29 |
SK7112001A3 (en) | 2001-12-03 |
BG105549A (en) | 2001-12-29 |
EP1133293A1 (de) | 2001-09-19 |
IL143181A0 (en) | 2002-04-21 |
HUP0104416A3 (en) | 2002-11-28 |
NO20012538D0 (no) | 2001-05-23 |
KR20010080535A (ko) | 2001-08-22 |
TR200101476T2 (tr) | 2001-10-22 |
AR021502A1 (es) | 2002-07-24 |
HRP20010472A2 (en) | 2003-04-30 |
CA2352526A1 (en) | 2000-06-02 |
NO20012538L (no) | 2001-07-04 |
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