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1. 发明授权

EP2069302B1 SUBSTITUTED PYRIDYLMETHYL BICYCLOCARBOXYAMIDE COMPOUNDS 有权
标题翻译：取代PYRIDYLMETHYLBICYCLOCARBOXYAMIDVERBINDUNGEN
公开(公告)号：EP2069302B1
公开(公告)日：2010-08-25
申请号：EP07804935.0
申请日：2007-09-10
申请人： Pfizer Inc.
发明人： NAGAYAMA, Satoshi , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07D213/40 , C07D401/12 , A61K31/4406 , A61K31/4409 , A61K31/444 , A61P25/04 , A61P25/02
CPC分类号： C07D213/40 , C07D401/12
摘要： This invention provides a compound of the formula (I): wherein A1 is N and A2 is CR7, or A1 is CR7 and A2 is N; Y1, Y2 and Y3 are each independently CH or N, Y4 and Y5 are each independently CR8 or N, with the proviso that when one of Y1, Y2, Y3, Y4 and Y5 is N, the others are not N; R1 and R2 are each independently hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; R3 and R8 are each independently hydrogen, halogen, hydroxy, (C1-C6)alkyl, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R4 is halogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)aIkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsuIfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-; and R5, R6 and R7 are each independently hydrogen, halogen, (C1-C6)alkyl, hydroxy(C1-C6)alkyI, or (C1-C6)alkoxy; or a pharmaceutically acceptable salt, solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.

2. 发明公开

EP1861359A1 N-(N-SULFONYLAMINOMETHYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF PAIN 有权
标题翻译： FüRDIE BEHANDLUNG VON SCHMERZEN GEEIGNETE N-（N-磺酰氨基乙基）环丙基碳二亚胺
公开(公告)号：EP1861359A1
公开(公告)日：2007-12-05
申请号：EP06710543.7
申请日：2006-03-07
申请人： Pfizer, Inc.
发明人： HANAZAWA, Takeshi , HIRANO, Misato , INOUE, Tadashi , NAGAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07C311/08 , C07C317/44 , C07C323/62 , C07D213/56 , C07D213/74 , C07D213/76 , A61P29/00 , A61K31/145 , A61K31/44
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compounds.
摘要翻译：本发明提供式（I）的化合物：其中变量A，B，D，E和R 1至R 11如说明书中所定义。

3. 发明授权

EP0566592B1 Pyrimido-benzothiazines with lipoxygenase inhibitory action 失效
标题翻译：嘧啶并苯并噻嗪与脂氧合酶的抑制作用。
公开(公告)号：EP0566592B1
公开(公告)日：1994-09-14
申请号：EP92901466.0
申请日：1991-12-16
申请人： PFIZER INC.
发明人： SHIMADA, Kaoru , SHISHIDO, Yuji
IPC分类号： C07D513/04 , A61K31/54
CPC分类号： C07D513/04
摘要： This invention relates to novel pyrimido-benzothiazine derivative compounds. The compounds of the present invention inhibit the action of the lipoxygenase enzyme and are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals. This invention also relates to pharmaceutical compositions comprising such compounds.

4. 发明公开

EP2024272A2 AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME 审中-公开
标题翻译： AMIDDERIVATE ALS IONENKANALLIGANDEN SOWIE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND VERWENDUNGSVERFAHRENDAFÜR
公开(公告)号：EP2024272A2
公开(公告)日：2009-02-18
申请号：EP07794735.6
申请日：2007-05-10
申请人： Renovis, Inc. , Pfizer, Inc.
发明人： SHISHIDO, Yuji , NAKAO, Kazunari , NAGAYAMA, Satoshi , TANAKA, Hirotaka , DUNCTON, Matthew, Alexander James , COX, Matthew , KINCAID, John , SAHASRABUDHE, Kiran , ESTIARTE-MARTINEZ, Maria de Los Angeles
IPC分类号： B82B1/00 , A61K31/497
CPC分类号： C07D215/48 , C07C311/08 , C07C2601/02 , C07D205/04 , C07D215/54 , C07D217/26 , C07D231/12 , C07D239/94 , C07D241/44 , C07D295/155 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/12 , C07D471/04 , C07D498/04 , C07D498/12
摘要： Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
摘要翻译：公开了具有由下式表示的式的化合物：式（I）。化合物可以制备为药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例，疼痛，炎症，创伤性损伤等。

5. 发明公开

EP1893583A1 SUBSTITUTED ARYLOXY-N-BICYCLOMETHYL ACETAMIDE COMPOUNDS AS VR1 ANTAGONISTS 有权
标题翻译：取代的芳氧基的N- BICYCLOMETHYLACETAMIDVERBINDUNGEN AS VR1拮抗剂
公开(公告)号：EP1893583A1
公开(公告)日：2008-03-05
申请号：EP06744787.0
申请日：2006-05-22
申请人： Pfizer, Inc.
发明人： INOUE, Tadashi , KAWASHIMA, Tadashi , NAGAYAMA, Satoshi , SHISHIDO, Yuji
IPC分类号： C07D235/26 , C07D209/34 , C07D263/58 , C07D231/56 , C07D235/06 , C07D249/18 , C07D277/62 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61P29/00 , A61K31/404
CPC分类号： C07D277/62 , C07D209/34 , C07D231/56 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58
摘要： This invention provides a compound of the formula (I): wherein A=B=D represents NR10-C(O)-NR9, S-C(O)-NR9, NR9-C(O)-S, NR9-C(O)-O, CR10-C(O)-NR9, 0-C(O)-NR9, NR10-C(O)-CR9, NR10-NR9-C(O), C(O)-NR9-NR10, NR10-N=CR9, N=N-CR9, NR10-CR9=N, N=CR9-NR10, NR10-N=N, N=N-NR10, S-CR9=N or N=CR9-S; X1 represents CR1 or N; X2 and X3 each independently represents CR8 or N; R1, R6, R8, R9 and R10 each independently represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C1,-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)aikoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R2, R3, R4, and R5 each independently represents hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6) alkyl, or hydroxy(C1-C6)alkyl; and R7 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-; or a pharmaceutically acceptable salt thereof, provided that: (i) when A=B=D represents NR10-N=N or N=N-NR10, then R2 represents (C1-C6)alkyl, halogen, halo(C1-C6) alkyl or hydroxy(C1-C6)alkyl; or (ii) when A=B=D represents NR10-N=N or N=N-NR10, and R2 represents (C1-C6)alkyl, then R7 represents halogen, (C1-C6)alkyl, (C1-C6)aIkOXy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

6. 发明公开

EP0861235A1 SUBSTITUTED BENZYLAMINOPIPERIDINE COMPOUNDS 失效
标题翻译：取代的苯甲酰氨基哌啶化合物
公开(公告)号：EP0861235A1
公开(公告)日：1998-09-02
申请号：EP96914375.0
申请日：1996-06-10
申请人： PFIZER INC.
发明人： SATAKE, Kunio , SHISHIDO, Yuji , WAKABAYASHI, Hiroaki
IPC分类号： A61K , C07D , G06F9 , A61K31 , A61P1 , A61P13 , A61P25 , A61P29 , A61P31 , A61P43 , C07D211 , C07D405 , G06F7
CPC分类号： C07D211/56
摘要： This invention provides a compound of formula (I) and its pharmaceutically acceptable salts, wherein R is halo C1-C8 alkyl, halo C2-C8 alkenyl, halo C2-C8 alkynyl or halo C1-C8 alkyl substituted by hydroxy or C1-C8 alkoxy; R1 is hydrogen, halo or C¿1?-C6 alkoxy; or R and R?1¿, together with the two carbon atoms shared between the benzene ring and the R and R1, complete a fused C¿4?-C6 cycloalkyl wherein one carbon atom is optionally replaced by oxygen and wherein one or two of the carbon atoms are optionally substituted by up to five substituents selected from halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are of use in treating a gastrointestinal disorder, a central nervous system (CNS) disorder, an inflammatory disease, emesis, urinary incontinence, pain, migraine, sunburn, diseases, disorders and adverse conditions caused by Helicobacter pylori, or angiogenesis especially CNS disorders in a mammalian subject, especially humans.
摘要翻译：本发明提供了式（I）化合物及其药学上可接受的盐，其中R为被羟基或C 1 -C 8烷氧基取代的卤代C 1 -C 8烷基，卤代C 2 -C 8烯基，卤代C 2 -C 8炔基或卤代C 1 -C 8烷基 ; R 1是氢，卤素或C 1 -C 6烷氧基; 或者R 1和R 2与苯环与R 1和R 1之间共有的两个碳原子一起形成稠合的C 4 -C 6环烷基，其中一个碳原子任选地被氧代替，并且其中一个或两个碳原子任选被至多五个选自卤素，C 1 -C 6烷基和卤代C 1 -C 6烷基的取代基取代; X是C1-C6烷氧基，卤代C1-C6烷氧基，苯氧基或卤素; Ar是任选被卤素取代的苯基。这些化合物可用于治疗由幽门螺杆菌引起的胃肠疾病，中枢神经系统（CNS）疾病，炎性疾病，呕吐，尿失禁，疼痛，偏头痛，晒伤，疾病，病症和不良疾病或血管生成，特别是CNS 哺乳动物受试者特别是人类的疾病。

7. 发明授权

EP1861359B1 N-(N-SULFONYLAMINOMETHYL)CYCLOPROPANECARBOXAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF PAIN 有权
标题翻译：疼痛SUITABLE N-（N- sulfonylaminomethyl）环丙烷羧酸酰胺衍生物的治疗
公开(公告)号：EP1861359B1
公开(公告)日：2012-11-14
申请号：EP06710543.7
申请日：2006-03-07
申请人： Pfizer Inc.
发明人： HANAZAWA, Takeshi , HIRANO, Misato , INOUE, Tadashi , NAGAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07C311/08 , C07C317/44 , C07C323/62 , C07D213/56 , C07D213/74 , C07D213/76 , A61P29/00 , A61K31/145 , A61K31/44
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76

8. 发明授权

EP1893583B1 SUBSTITUTED ARYLOXY-N-BICYCLOMETHYL ACETAMIDE COMPOUNDS AS VR1 ANTAGONISTS 有权
标题翻译：作为VR1拮抗剂的取代的芳氧基-N-二甲基乙酰乙酰胺化合物
公开(公告)号：EP1893583B1
公开(公告)日：2012-04-04
申请号：EP06744787.0
申请日：2006-05-22
申请人： Pfizer Inc.
发明人： INOUE, Tadashi , KAWASHIMA, Tadashi , NAGAYAMA, Satoshi , SHISHIDO, Yuji
IPC分类号： C07D235/26 , C07D209/34 , C07D263/58 , C07D231/56 , C07D235/06 , C07D249/18 , C07D277/62 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61P29/00 , A61K31/404
CPC分类号： C07D277/62 , C07D209/34 , C07D231/56 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58
摘要： This invention provides a compound of the formula (I): wherein A=B=D represents NR10-C(O)-NR9, S-C(O)-NR9, NR9-C(O)-S, NR9-C(O)-O, CR10-C(O)-NR9, 0-C(O)-NR9, NR10-C(O)-CR9, NR10-NR9-C(O), C(O)-NR9-NR10, NR10-N=CR9, N=N-CR9, NR10-CR9=N, N=CR9-NR10, NR10-N=N, N=N-NR10, S-CR9=N or N=CR9-S; X1 represents CR1 or N; X2 and X3 each independently represents CR8 or N; R1, R6, R8, R9 and R10 each independently represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C1,-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)aikoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R2, R3, R4, and R5 each independently represents hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6) alkyl, or hydroxy(C1-C6)alkyl; and R7 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-; or a pharmaceutically acceptable salt thereof, provided that: (i) when A=B=D represents NR10-N=N or N=N-NR10, then R2 represents (C1-C6)alkyl, halogen, halo(C1-C6) alkyl or hydroxy(C1-C6)alkyl; or (ii) when A=B=D represents NR10-N=N or N=N-NR10, and R2 represents (C1-C6)alkyl, then R7 represents halogen, (C1-C6)alkyl, (C1-C6)aIkOXy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy(C1-C6)alkoxy, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供了式（I）化合物：其中A = B = D表示NR 10 -C（O）-NR 9，SC（O）-NR 9，NR 9 -C（O）-S，NR 9 -C（O）（O）-NR9，NR10-C（O）-CR9，NR10-NR9-C（O），C（O）-NR9-NR10，NR10- N = CR9，N = N-CR9，NR10-CR9 = N，N = CR9-NR10，NR10-N = N，N = N-NR10，S-CR9 = N或N = CR9- X1代表CR1或N; X2和X3各自独立地表示CR8或N; （C1-C6）烷基，（C1-C6）烷氧基，羟基（C1-C6）烷氧基，（C1-C6）烷氧基 - （C1-C6）烷基，（C 1 -C 6）烷硫基，（C 1 -C 6）烷基亚磺酰基或（C 1 -C 6）烷基磺酰基;（C 1 -C 6）烷氧基 - （C 1 -C 6）烷氧基 - （C 1 -C 6）烷基，卤素，卤代（C 1 -C 6）烷基或羟基（C 1 -C 6）烷基; R 2，R 3，R 4和R 5各自独立地表示氢。（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，羟基（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷基，（C 1 -C 6）烷氧基，[（C 1 -C 6）烷基] NH-或[（C 1 -C 6）烷基] 2 N- 条件是：（i）当A = B = D时，表示NR10-N = N或N = N-NR10，则R2表示（C1-C6）烷基，卤素，卤代（C1- 烷基或羟基（C 1 -C 6）烷基; 或（ii）当A = B = D时，表示NR10-N = N或N = N-NR10，且R2表示（C1-C6）烷基时，则R7表示卤素，（C1- C6）烷基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，[（C 1 -C 6）烷基] NH-或[ C1-C6）烷基] 2 N-。这些化合物可用于治疗由VR1受体的过度激活引起的疾病状态，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。

9. 发明公开

EP2069302A1 SUBSTITUTED PYRIDYLMETHYL BICYCLOCARBOXYAMIDE COMPOUNDS 有权
标题翻译：取代的吡啶甲基双环碳酰胺化合物
公开(公告)号：EP2069302A1
公开(公告)日：2009-06-17
申请号：EP07804935.0
申请日：2007-09-10
申请人： Pfizer Inc.
发明人： NAGAYAMA, Satoshi , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07D213/40 , C07D401/12 , A61K31/4406 , A61K31/4409 , A61K31/444 , A61P25/04 , A61P25/02
CPC分类号： C07D213/40 , C07D401/12
摘要： This invention provides a compound of the formula (I): wherein A1 is N and A2 is CR7, or A1 is CR7 and A2 is N; Y1, Y2 and Y3 are each independently CH or N, Y4 and Y5 are each independently CR8 or N, with the proviso that when one of Y1, Y2, Y3, Y4 and Y5 is N, the others are not N; R1 and R2 are each independently hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; R3 and R8 are each independently hydrogen, halogen, hydroxy, (C1-C6)alkyl, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R4 is halogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)aIkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsuIfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH- or [(C1-C6)alkyl]2N-; and R5, R6 and R7 are each independently hydrogen, halogen, (C1-C6)alkyl, hydroxy(C1-C6)alkyI, or (C1-C6)alkoxy; or a pharmaceutically acceptable salt, solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供了式（I）化合物：其中A 1是N且A 2是CR 7，或者A 1是CR 7且A 2是N; Y1，Y2和Y3各自独立地为CH或N，Y4和Y5各自独立地为CR8或N，条件是当Y1，Y2，Y3，Y4和Y5中的一个为N时，其余不为N; R 1和R 2各自独立地为氢，卤素，（C 1 -C 6）烷基，卤代（C 1 -C 6）烷基或羟基（C 1 -C 6）烷基; （C 1 -C 6）烷基，羟基（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷氧基 - （C 1 -C 6）烷硫基，（C 1 -C 6）烷基亚磺酰基或（C 1 -C 6）烷基磺酰基; （C 1 -C 6）烷基，（C 3 -C 6）环烷基，卤代（C 1 -C 6）烷基，羟基（C 1 -C 6）烷基，卤代C 1 -C 6烷氧基，羟基C 1 -C 6烷氧基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷基，（C 1 -C 6）烷氧基 - （C 1 -C 6）烷氧基，卤代C 1 -C 6烷基磺酰基，卤代C 1 -C 6烷基亚磺酰基，烷硫基，[（C1-C6）烷基] NH-或[（C1-C6）烷基] 2N-; （C 1 -C 6）烷基，羟基（C 1 -C 6）烷基或（C 1 -C 6）烷氧基;和R 5，R 6和R 7各自独立地为氢，卤素，或其药学上可接受的盐，溶剂合物。这些化合物可用于治疗由哺乳动物中VR1受体的过度激活引起的疾病，如疼痛等。本发明还提供了包含上述化合物的药物组合物。

10. 发明授权

EP0861235B1 SUBSTITUTED BENZYLAMINOPIPERIDINE COMPOUNDS 失效
标题翻译：取代BENZYLAMINOPIPERLOIN CONNECTIONS
公开(公告)号：EP0861235B1
公开(公告)日：2001-11-07
申请号：EP96914375.9
申请日：1996-06-10
申请人： PFIZER INC.
发明人： SATAKE, Kunio , SHISHIDO, Yuji , WAKABAYASHI, Hiroaki
IPC分类号： C07D211/56 , A61K31/445
CPC分类号： C07D211/56
摘要： This invention provides a compound of formula (I) and its pharmaceutically acceptable salts, wherein R is halo C1-C8 alkyl, halo C2-C8 alkenyl, halo C2-C8 alkynyl or halo C1-C8 alkyl substituted by hydroxy or C1-C8 alkoxy; R1 is hydrogen, halo or C¿1?-C6 alkoxy; or R and R?1¿, together with the two carbon atoms shared between the benzene ring and the R and R1, complete a fused C¿4?-C6 cycloalkyl wherein one carbon atom is optionally replaced by oxygen and wherein one or two of the carbon atoms are optionally substituted by up to five substituents selected from halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are of use in treating a gastrointestinal disorder, a central nervous system (CNS) disorder, an inflammatory disease, emesis, urinary incontinence, pain, migraine, sunburn, diseases, disorders and adverse conditions caused by Helicobacter pylori, or angiogenesis especially CNS disorders in a mammalian subject, especially humans.

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