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公开(公告)号:EP1048655B1
公开(公告)日:2004-09-01
申请号:EP98957145.0
申请日:1998-12-03
发明人: NAKAZATO, Atsuro , OKUBO, Taketoshi , KUMAGAI, Toshihito , CHAKI, Shigeyuki , TOMISAWA, Kazuyuki , NAGAMINE, Masashi , GOTOH, Makoto , YOSHIDA, Masanori
IPC分类号: C07D215/54 , C07D215/56 , C07D241/44 , C07D491/056 , A61K31/47 , A61K31/495 , C07D401/06
CPC分类号: C07D401/06 , C07D215/54 , C07D241/44
摘要: 1,2-Dihydro-2-oxoquinoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein Ar represents pyridyl or group represented by general formula (II) (wherein X?3 and X4¿ are the same or different and each represents hydrogen, halogeno, C¿1-5? alkyl, C1-5 alkoxy, hydroxy, or trifluoromethyl); Y represents nitrogen, CH, or C(OH); R?1 and R2¿ are the same or different and each represents hydrogen, C¿1-10? alkyl, C3-15 alkoxyalkyl, or C3-15 alkylaminoalkyl or R?1 and R2¿ form a cycloamino group together with the adjacent nitrogen atom; X?1 and X2¿ are the same or different and each represents hydrogen, C¿1-5? alkyl, C1-5 alkoxy, or halogeno or X?1 and X2¿ together represent alkylenedioxy; and n is an integer of 1 to 3.
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公开(公告)号:EP2003131A1
公开(公告)日:2008-12-17
申请号:EP07740490.3
申请日:2007-03-30
发明人: OKUBO, Taketoshi , KUMAGAI, Toshihito , ISHII, Takaaki , NAKAMURA, Toshio , ABE, Kumi , AMADA, Yuri , ISHIZAKA, Tomoko , SUN, Xiang-Min , SEKIGUCHI, Yoshinori , SASAKO, Shigetada , SHIMIZU, Takanori , NAGATSUKA, Takayuki
IPC分类号: C07D401/12 , A61K31/4365 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/553 , A61P1/14 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/36 , A61P35/00 , A61P43/00
CPC分类号: C07D401/12
摘要: Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC 4 receptor antagonistic effect.
摘要翻译: 公开了由式[I]表示的氨基吡咯烷化合物或其药学上可接受的盐。 化合物或盐可用作模式障碍如抑郁症,焦虑症,厌食症,恶病质,疼痛和药物依赖性的预防/治疗剂,其作用依赖于MC4受体拮抗作用。
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公开(公告)号:EP1176146B1
公开(公告)日:2005-06-08
申请号:EP00907999.7
申请日:2000-03-10
IPC分类号: C07D473/34 , C07D487/04 , C07D211/78 , C07D207/34 , A61K31/52 , A61K31/519 , A61P43/00 , A61P25/24 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/30 , A61P25/08 , A61P1/00 , A61P7/10 , A61P9/10 , A61P9/12 , A61P17/02 , A61P29/00 , A61P37/02
CPC分类号: A61K31/519 , C07D473/00 , C07D487/04
摘要: Carbamoyl tetrahydropyridine derivatives represented by general formula (1) and being efficacious against CRF-related diseases; medicinally acceptable salts of the same; and intermediates for the preparation thereof, wherein R?1 and R2¿ are each independently hydrogen, C¿1?-C5 alkyl, or the like; Y?1-Y2 is (R4)C=C(R5), (R6¿)C=N, N=N, (R7)N-CO, or N=C(R?8); X1, X2 and X3¿ are each independently hydrogen, halogeno, or the like; R?3, R4, R5 and R6¿ are each independently hydrogen or alkyl; R7 is hydrogen, C¿1?-C5 alkyl, or the like; and R?8¿ is hydrogen or carbamoyl.
摘要翻译: 通式(1)表示的氨基甲酰基四氢吡啶衍生物对CRF相关疾病有效; 药物可接受的盐; 和用于制备它们的中间体,其中R 1和R 2各自独立地为氢,C 1 -C 5烷基等; (R 4)C = C(R 5),(R 6)C = N,N = N,(R 7)N -CO或N = C(R 8)。 X 1,X 2和X 3各自独立地为氢,卤代等; R 3,R 4,R 5和R 6各自独立地为氢或烷基; R 7是氢,C 1 -C 5烷基等; 而R 8是氢或氨基甲酰基。
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公开(公告)号:EP1176146A1
公开(公告)日:2002-01-30
申请号:EP00907999.7
申请日:2000-03-10
IPC分类号: C07D473/34 , C07D487/04 , C07D211/78 , C07D207/34 , A61K31/52 , A61K31/519 , A61P43/00 , A61P25/24 , A61P25/22 , A61P25/28 , A61P25/16 , A61P25/30 , A61P25/08 , A61P1/00 , A61P7/10 , A61P9/10 , A61P9/12 , A61P17/02 , A61P29/00 , A61P37/02
CPC分类号: A61K31/519 , C07D473/00 , C07D487/04
摘要: Carbamoyl tetrahydropyridine derivatives represented by the formula:
[in the formula, R 1 and R 2 are identical or different, and each represents a hydrogen atom, a C 1 -C 5 alkyl group, or the like; Y 1 -Y 2 represents (R 4 )C=C(R 5 ), (R 6 )C=N, N=N, (R 7 )N-CO, or N=C(R 8 ); X 1 , X 2 , and X 3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R 3 , R 4 , R 5 , and R 6 are identical or different, and each represents a hydrogen atom or an alkyl group; R 7 represents a hydrogen atom, a C 1 -C 5 alkyl group, or the like; and R 8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided.
The derivatives described above are effective for diseases which are believed to involve CRF.摘要翻译: 由下式表示的氨基甲酰基四氢吡啶衍生物[式中,R1和R2相同或不同,且各自表示氢原子,C1-C5烷基等; Y1-Y2表示(R4)C = C(R5),(R6)C = N,N = N,(R7)N-CO或N = C(R8)。 X 1,X 2和X 3相同或不同,并且各自表示氢原子,卤素原子等; R3,R4,R5和R6相同或不同,并且各自表示氢原子或烷基; R7代表氢原子,C1-C5烷基等; 并且R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐,以及用于其制备的中间体。 上述衍生物对于认为涉及CRF的疾病是有效的。
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公开(公告)号:EP1048655A1
公开(公告)日:2000-11-02
申请号:EP98957145.0
申请日:1998-12-03
发明人: NAKAZATO, Atsuro , OKUBO, Taketoshi , KUMAGAI, Toshihito , CHAKI, Shigeyuki , TOMISAWA, Kazuyuki , NAGAMINE, Masashi , GOTOH, Makoto , YOSHIDA, Masanori
IPC分类号: C07D215/54 , C07D215/56 , C07D241/44 , C07D491/056 , A61K31/47 , A61K31/495
CPC分类号: C07D401/06 , C07D215/54 , C07D241/44
摘要: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula:
wherein Ar is a pyridyl group or a group represented by the formula:
(wherein X 3 and X 4 are the same or different, and are each a hydrogen atom, a halogen atom, a C 1-5 alkyl group, a C 1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R 1 and R 2 are the same or different, and are each a hydrogen atom, a C 1-10 alkyl group, a C 3-15 alkoxyalkyl group or a C 3-15 alkylaminoalkyl group, or R 1 and R 2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X 1 and X 2 are the same or different, and are each a hydrogen atom, a C 1-5 alkyl group, a C 1-5 alkoxy group or a halogen atom, or X 1 and X 2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.摘要翻译: 由下式表示的1,2-二氢-2-氧代喹啉衍生物:其中Ar为吡啶基或由下式表示的基团:其中X 3和X 4相同 或不同,并且各自为氢原子,卤素原子,C 1-5烷基,C 1-5烷氧基,羟基或三氟甲基),Y为氮原子,CH或C(OH) R 1和R 2相同或不同,各自为氢原子,C 1-10烷基,C 3-15烷氧基烷基或C 3-15烷基氨基烷基,或R 1和R 2 与它们所连接的氮原子一起形成环状氨基,X 1和X 2相同或不同,分别为氢原子,C 1-5烷基, C 1-5烷氧基或卤原子,或X 1和X 2一起形成亚烷基二氧基,n为1〜3的整数。 或其药学上可接受的盐。
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