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1. 发明申请

WO2003064425A1 N-SUBSTITUTED SPIROPIPERIDINE COMPOUNDS AS LIGANDS FOR ORL-1 RECEPTOR 审中-公开
标题翻译： N-取代的螺吡啶化合物作为ORL-1受体的配体
公开(公告)号：WO2003064425A1
公开(公告)日：2003-08-07
申请号：PCT/IB2003/000203
申请日：2003-01-16
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITO, Fumitaka , KOIKE, Hiroki , MORITA, Asato
发明人： ITO, Fumitaka , KOIKE, Hiroki , MORITA, Asato
IPC分类号： C07D487/06
CPC分类号： C07D401/06 , C07D487/06 , C07D487/10 , C07D491/10
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, ester or ether thereof, wherein R 1 through R 12 are independently hydrogen or the like; X 1 and X 2 are independently CH 2 or the like; R 13 is hydrogen or the like; or R 12 and R 13 taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R 14 and R 15 are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.
摘要翻译：式（I）化合物或其药学上可接受的盐，酯或醚，其中R 1至R 12独立地为氢等; X 1和X 2独立地是CH 2等; R 13是氢等; 或R 12和R 13与分离所述取代基的喹啉环的三个环原子一起形成杂环; R 14和R 15是氢等，或这些基团一起形成氧代; 虚线表示单键或双键。这些化合物是ORL-1受体的配体，特别是用于所述受体的拮抗剂。

2. 发明申请

WO2005080317A2 THERAPEUTIC AMIDE DERIVATIVES 审中-公开
标题翻译：治疗酰胺衍生物
公开(公告)号：WO2005080317A2
公开(公告)日：2005-09-01
申请号：PCT/IB2005/000258
申请日：2005-02-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
发明人： KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
IPC分类号： C07C235/00
CPC分类号： C07C235/48 , C07C2601/14 , C07D207/34 , C07D209/34 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/227 , C07D215/48 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/26 , C07D237/04 , C07D237/24 , C07D249/04 , C07D263/38 , C07D277/68 , C07D303/22 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/06 , C07D405/12
摘要： The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: A and B independently represent CH 2 or O, with the proviso that A and B are not simultaneously O; Cy represents one of the following Formula (II) optionally substituted by one to three groups selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, C 1-6 alkylamino and amino; R 1 and R 2 are independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl and C 3-8 cycloalkyl; n represents an integer from 0-4; X is hydrogen, hydroxy, halogen or C 1-6 alkoxy; Y is oxy, thio, a 1-4 membered alkylene, a 2-4 membered alkylene ether, 2-4 membered alkylene thioether or an oxyethyleneoxy group, optionally substituted by 1 to 4 groups independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy and C 1-6 haloalkyl; Z is CH or N; and p represents an integer from 0-5 when Z is CH or 0-4 when Z is N; when p represents 2 or more, two of R 2 s may be taken together with the carbon atoms to which they are attached to form a 5-8 membered cycloalkyl ring to processes for the preparation of, intermediates used in the preparation of, compositions containing such compounds and the uses of such compounds as antagonists of the NMDA NR2B receptor.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：A和B独立地表示CH 2或O，条件是A和B不同时为O; Cy表示任选被一至三个选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6烷基氨基和氨基的基团取代的下式（II）之一。 R 1和R 2独立地选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基和C 3-8环烷基; n表示0-4的整数; X是氢，羟基，卤素或C 1-6烷氧基; Y是氧基，硫代，1-4元亚烷基，2-4元亚烷基醚，2-4元亚烷基硫醚或氧化乙烯氧基，任选被1至4个独立地选自羟基，卤素，C 1-6烷基， C 1-6烷氧基和C 1-6卤代烷基; Z是CH或N; 当Z为CH时，p表示0-5的整数，Z为N时为0〜4的整数。当p表示2或更多时，R 2中的两个可以与它们所连接的碳原子一起形成5-8元环烷基环，以制备用于制备中间体的中间体，含有这些化合物的组合物以及这些化合物作为NMDA NR2B受体的拮抗剂的用途。

3. 发明申请

WO2004089366A1 BICYCLIC COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：双环化合物作为NR2B受体拮抗剂
公开(公告)号：WO2004089366A1
公开(公告)日：2004-10-21
申请号：PCT/IB2004/001177
申请日：2004-04-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
发明人： ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
IPC分类号： A61K31/4184
CPC分类号： C07D239/94 , C07D209/08 , C07D215/12 , C07D215/26 , C07D231/56 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/26 , C07D261/20 , C07D263/56 , C07D471/04
摘要： This invention provides a compound of the formula (I) wherein R 1 and R 2 independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物，其中R 1和R 2独立地表示氢原子等; X表示共价键或类似物：A表示具有8至12个环原子的双环，芳族，饱和或部分不饱和的杂环或碳环基团; B表示苯基或具有5〜6个环原子的杂芳基等：这些化合物可用于治疗NMDA NR2B受体过度活化引起的疾病状况，例如哺乳动物的疼痛等。本发明还提供了包含上述化合物的药物组合物。

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