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1. 发明申请

WO2007072146A1 CHROMANE SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS ACID PUMP INHIBITORS 审中-公开
标题翻译： CHROMANE取代苯并咪唑及其作为酸泵抑制剂使用
公开(公告)号：WO2007072146A1
公开(公告)日：2007-06-28
申请号：PCT/IB2006/003605
申请日：2006-12-06
申请人： PFIZER JAPAN INC. , PFIZER INC. , HANAZAWA, Takeshi , KOIKE, Hiroki
发明人： HANAZAWA, Takeshi , KOIKE, Hiroki
IPC分类号： C07D405/12 , C07D409/12 , A61K31/4184 , A61P1/04
CPC分类号： C07D405/12 , C07D409/12
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or NH, and -A-B- is -0-CH 2 -, -CH 2 -O-, -S-CH 2 - or -CH 2 -S- or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds In the treatment of a condition mediated by acid pump antagonistic activity such as; but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID- induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non- erosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivatioπ, airway disorders or asthma.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中X是O或NH，-AB-是-O-CH 2 - ， - CH- 2 -O - ， - S-CH 2 - 或-CH 2 -S-或其药学上可接受的盐，以及含有这些化合物的组合物和使用的这种化合物在治疗由酸泵介导的病症拮抗活性如; 胃肠道疾病，胃食管疾病，胃食管反流病（GERD），消化性溃疡，胃溃疡，十二指肠溃疡，NSAID诱导的溃疡，胃炎，幽门螺杆菌感染，消化不良，功能性消化不良，佐林格 - 埃里森综合征，非侵蚀性反流疾病（NERD），内脏痛，胃灼热，恶心，食管炎，吞咽困难，超嗜热病，呼吸道疾病或哮喘。

2. 发明申请

WO2006097817A1 N- (N-SULFONYLAMINOMETHYL) CYCLOPROPANECARBOXAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：用于治疗疼痛的N-（N-磺酰氨基乙基）环磷酰胺酰胺衍生物
公开(公告)号：WO2006097817A1
公开(公告)日：2006-09-21
申请号：PCT/IB2006/000557
申请日：2006-03-07
申请人： PFIZER JAPAN INC. , PFIZER, INC. , HANAZAWA, Takeshi , HIRANO, Misato , INOUE, Tadashi , NAGAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
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）化合物或其药学上可接受的盐或溶剂化物。这些化合物可用于治疗由哺乳动物中VR1受体过度活化引起的疼痛等疼痛引起的疾病状况。本发明还提供包含上述化合物的药物组合物。

3. 发明申请

WO2006095263A1 SUBSTITUTED N-SULFONYLAMINOPHENYLETHYL-2-PHENOXY ACETAMIDE COMPOUNDS 审中-公开
标题翻译：取代的N-磺酰氨基苯乙烯基-2-苯氧基乙酰胺化合物
公开(公告)号：WO2006095263A1
公开(公告)日：2006-09-14
申请号：PCT/IB2006/000539
申请日：2006-02-24
申请人： PFIZER JAPAN INC. , PFIZER INC. , HANAZAWA, Takeshi , HIRANO, Misato , INOUE, Tadashi , NAHAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
发明人： HANAZAWA, Takeshi , HIRANO, Misato , INOUE, Tadashi , NAHAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07D295/08 , C07D311/58 , C07C311/08 , A61K31/4453 , A61K31/353 , A61K31/18 , A61P25/00
CPC分类号： C07C311/08
摘要： This invention provides a compound of the formula (I), wherein R 1 represents (C 1 -C 6 )alkyl; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkyl; R 3 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 C 6 )alkyllsulfonyl, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 ) alkyl] 2 N-; R 4 represents a halogen atom, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 )alkyl] 2 N-; R 5 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkyIsulfonyl, [(C 1 -C 6 )alkyl]NH-, [(C 1 -C 6 ) alkyl] 2 N-, H 2 N-(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy, H 2 N-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, or [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; and *indicates a chiral centre; 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 compound.
摘要翻译：本发明提供式（I）化合物，其中R 1代表（C 1 -C 6 -C 6）烷基; R 2表示氢原子，卤素原子，羟基，（C 1 -C 6 -C 6）烷基，（C 1 -C 6）（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6）（C 1 -C 6）烷氧基 - （C 1 -C 6 -C 6）烷基或卤代（C 1 -C 6 - ç_{6 ）烷基; R 3表示卤素原子，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - （C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，C 1 -C 6 - （C 1 -C 6）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 -C 6）烷氧基，卤代（C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6）烷硫基，（C 1 -C 6 -C 6）烷基亚磺酰基，（C _{2 N-; R 5表示卤素原子，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - （C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，C 1 -C 6 - （C 1 -C 6）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 -C 6）烷氧基，卤代（C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6）烷硫基，（C 1 -C 6 -C 6）烷基亚磺酰基，（C _{1 -C _{6 ）烷基] _{2 N（ç_{1 -C _{6 ）烷氧基 - （C _{1 < / SUB> -C _{6 ）烷基; 和*表示手性中心; 或其药学上可接受的盐或溶剂合物。这些化合物可用于治疗由哺乳动物VR1受体过度活化引起的疼痛等疼痛引起的疾病状况。本发明还提供了包含上述化合物的药物组合物。}}}}}}}}}

4. 发明申请

WO2006103503A1 SUBSTITUTED ARYLOXOETHYL CYCLOPROPANECARBOXAMIDE COMPOUNDS AS VR1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为VR1受体拮抗剂的取代的芳基乙氧基环丙酰氧基化合物
公开(公告)号：WO2006103503A1
公开(公告)日：2006-10-05
申请号：PCT/IB2006/000585
申请日：2006-03-15
申请人： PFIZER JAPAN INC. , PFIZER INC. , HANAZAWA, Takeshi , NAGAYAMA, Satoshi , NAKAO, Kazumari , TANAKA, Hirotaka
发明人： HANAZAWA, Takeshi , NAGAYAMA, Satoshi , NAKAO, Kazumari , TANAKA, Hirotaka
IPC分类号： C07C233/61 , C07D213/50 , C07D233/00 , A61K31/165 , A61K31/4164 , A61K31/44 , A61P29/00
CPC分类号： C07C233/61 , C07C2601/02 , C07D213/50 , C07D233/56 , C07D233/64
摘要： This invention provides a compound of the formula (I): (I) These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor, such as 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：（I）这些化合物可用于治疗由哺乳动物中的VR1受体过度活化引起的疾病，例如疼痛等。本发明还提供了包含上述化合物的药物组合物。

5. 发明申请

WO2008114123A1 SPIRO BENZIMIDAZOLE DERIVATIVES AS ACID PUMP INHIBITORS 审中-公开
标题翻译：作为酸泵抑制剂的SPIRO苯并咪唑衍生物
公开(公告)号：WO2008114123A1
公开(公告)日：2008-09-25
申请号：PCT/IB2008/000643
申请日：2008-03-12
申请人： RAQUALIA PHARMA INC. , HANAZAWA, Takeshi , JINNO, Madoka , KOIKE, Hiroki , MORITA, Mikio , MURATA, Yoshihisa
发明人： HANAZAWA, Takeshi , JINNO, Madoka , KOIKE, Hiroki , MORITA, Mikio , MURATA, Yoshihisa
IPC分类号： C07D491/107 , A61K31/4188 , A61P1/04
CPC分类号： C07D491/107
摘要： This invention relates to compounds of the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and A are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
摘要翻译：本发明涉及式（I）化合物：（I）或其药学上可接受的盐，其中：R1，R2，R3，R4，R5，R6，R7，R8和A各自如本文所述或药学上可接受的盐和含有这些化合物的组合物及其治疗和使用方法，包括用于治疗由酸泵拮抗活性介导的病症的化合物，所述活性例如但不限于胃肠道疾病，胃食管疾病，胃食管反流病（GERD ），咽喉反流病，消化性溃疡，胃溃疡，十二指肠溃疡，NSAID诱导的溃疡，胃炎，幽门螺杆菌感染，消化不良，功能性消化不良，佐林格 - 埃利森综合征，非侵蚀性反流病（NERD），内脏痛，癌症，胃灼热，恶心，食管炎，吞咽困难，过度激活，气道障碍或哮喘。

6. 发明申请

WO2007031860A1 INDANE SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS ACID PUMP INHIBITORS 审中-公开
标题翻译：茚胺取代苯并咪唑及其作为酸性抑制剂的用途
公开(公告)号：WO2007031860A1
公开(公告)日：2007-03-22
申请号：PCT/IB2006/002553
申请日：2006-09-08
申请人： PFIZER JAPAN INC. , PFIZER INC. , HANAZAWA, Takeshi , KOIKE, Hiroki , SAKAKIBARA, Sachiko
发明人： HANAZAWA, Takeshi , KOIKE, Hiroki , SAKAKIBARA, Sachiko
IPC分类号： C07D235/08 , C07D403/06 , A61K31/4184 , A61K31/496 , A61P1/04
CPC分类号： C07D403/06 , C07D235/08
摘要： This invention relates to compounds of the formula (I): a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug, wherein: A, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by acid pump antagonisitic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
摘要翻译：本发明涉及式（I）化合物：其前药或所述化合物或所述前药的药学上可接受的盐，其中：A，X，R 1，R 2， R 3，R 3，R 4，R 5，R 6，R 7， SUP，R 8和R 9各自如本文所述或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在治疗病症中的用途由酸泵拮抗活性介导，例如但不限于胃肠道疾病，胃食管疾病，胃食管反流病（GERD），消化性溃疡，胃溃疡，十二指肠溃疡，NSAID诱发的溃疡，胃炎，幽门螺杆菌感染，消化不良功能性消化不良，佐林格 - 埃利森综合征，非侵蚀性反流病（NERD），内脏痛，胃灼热，恶心，食管炎，吞咽困难，过度激活，气道障碍或哮喘。

7. 发明申请

WO2007129188A1 CYCLOPROPANECARBOXAMIDE COMPOUND 审中-公开
标题翻译：环磷酰胺化合物
公开(公告)号：WO2007129188A1
公开(公告)日：2007-11-15
申请号：PCT/IB2007/001143
申请日：2007-04-27
申请人： PFIZER JAPAN INC. , PFIZER INC. , HANAZAWA, Takeshi , NAGAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
发明人： HANAZAWA, Takeshi , NAGAYAMA, Satoshi , NAKAO, Kazunari , SHISHIDO, Yuji , TANAKA, Hirotaka
IPC分类号： C07D213/24 , A61K31/435 , A61P29/00
CPC分类号： C07D213/24
摘要： This invention relates to novel substituted N-(N-sulfonylaminoarylmethyl)cyclopropanecarboxamide compound and to their use in therapy. This invention provides 2-(6-tert-butylpyridin-3-yl)-N-((1R)-1-{3,5-difluoro-4-[(methylsulfonyl)amino]phenyl}ethyl)-2-methylcyclopropanecarboxamide, or a pharmaceutically acceptable salt or solvate thereof. This compound is particularly useful as an antagonist of the VR1 (Type I Vanilloid) receptor, and is thus useful for the treatment of pain, neuralgia, neuropathies, nerve injury, burns, migraine, carpal tunnel syndrome, fibromyalgia, neuritis, sciatica, pelvic hypersensitivity, bladder disease, inflammation, or the like in mammals, especially humans. The present invention also relates to a pharmaceutical composition comprising the above compound.
摘要翻译：本发明涉及新的取代的N-（N-磺酰基氨基芳基甲基）环丙烷甲酰胺化合物及其在治疗中的用途。本发明提供2-（6-叔丁基吡啶-3-基）-N - （（1R）-1- {3,5-二氟-4 - [（甲基磺酰基）氨基]苯基}乙基）-2-甲基环丙烷甲酰胺，或其药学上可接受的盐或溶剂合物。该化合物特别可用作VR1（I型香草素）受体的拮抗剂，因此可用于治疗疼痛，神经痛，神经病，神经损伤，烧伤，偏头痛，腕管综合征，纤维肌痛，神经炎，坐骨神经痛，骨盆哺乳动物，特别是人类中的超敏反应，膀胱疾病，炎症等。本发明还涉及包含上述化合物的药物组合物。

8. 发明申请

WO2006095263A8 SUBSTITUTED N-SULFONYLAMINOPHENYLETHYL-2-PHENOXY ACETAMIDE COMPOUNDS 审中-公开
标题翻译：取代的N-磺酰氨基苯乙烯基-2-苯氧基乙酰胺化合物
公开(公告)号：WO2006095263A8
公开(公告)日：2007-11-08
申请号：PCT/IB2006000539
申请日：2006-02-24
申请人： PFIZER JAPAN INC , PFIZER , HANAZAWA TAKESHI , HIRANO MISATO , INOUE TADASHI , NAGAYAMA SATOSHI , NAKAO KAZUNARI , SHISHIDO YUJI , TANAKA HIROTAKA
发明人： HANAZAWA TAKESHI , HIRANO MISATO , INOUE TADASHI , NAGAYAMA SATOSHI , NAKAO KAZUNARI , SHISHIDO YUJI , TANAKA HIROTAKA
IPC分类号： C07D295/08 , A61K31/18 , A61K31/353 , A61K31/4453 , A61P25/00 , C07C311/08 , C07D311/58
CPC分类号： C07C311/08
摘要： This invention provides a compound of the formula (I), wherein R 1 represents (C 1 -C 6 )alkyl; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkyl; R 3 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 C 6 )alkyllsulfonyl, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 ) alkyl] 2 N-; R 4 represents a halogen atom, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl]NH-, or [(C 1 -C 6 )alkyl] 2 N-; R 5 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyll, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkyIsulfonyl, [(C 1 -C 6 )alkyl]NH-, [(C 1 -C 6 ) alkyl] 2 N-, H 2 N-(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy, H 2 N-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-NH-(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, or [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; and *indicates a chiral centre; 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 compound.
摘要翻译：本发明提供式（I）化合物，其中R 1表示（C 1 -C 6 -C 6）烷基; R 2表示氢原子，卤素原子，羟基，（C 1 -C 6 -C 6）烷基，（C 1 -C 6）（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6） C 1 -C 6烷氧基 - （C 1 -C 6 -C 6）烷基或卤代（C 1 -C 6 - ç_{6 ）烷基; R 3表示卤素原子，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - （C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，）烷氧基 - （C 1 -C 6 -C 6）烷氧基，卤素（C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6）烷硫基，（C 1 -C 6 -C 6）烷基亚磺酰基，（C _{2 N-; R 5表示卤素原子，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - （C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，（C 1 -C 6）烷基，）烷氧基 - （C 1 -C 6 -C 6）烷氧基，卤素（C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6）烷硫基，（C 1 -C 6 -C 6）烷基亚磺酰基，（C _{C 6 -C 6烷基） C 1 -C 6烷基] N 2 - ， - N - （C 1 -C 6） C 1 -C 6烷氧基，（C 1 -C 6 -C 6）烷基-NH-（C 1 -C 6） -C 6 -C 6烷氧基，[（C 1 -C 6 -C 6）烷基] N 2 N（C < C 1 -C 6 -C 6烷氧基，H 2 N - （C 1 -C 6））烷氧基 - （C 1 -C 6 -C 6）烷基，（C 1 -C 6 -C 6）烷基-NH - （C 1 -C 6 -C 6）烷氧基 - （C 1 -C 6 -C 6）烷基或[（ ç_{1 -C _{6 ）烷基] _{2 N（ç_{1 -C _{6 ）烷氧基 - （C _{1 < / SUB> -C _{6 ）烷基; 和*表示手性中心; 或其药学上可接受的盐或溶剂合物。这些化合物可用于治疗由哺乳动物中VR1受体过度活化引起的疼痛等疼痛引起的疾病状况。本发明还提供了包含上述化合物的药物组合物。}}}}}}}}}}

9. 发明申请

WO2006097817A9 N- (N-SULFONYLAMINOMETHYL) CYCLOPROPANECARBOXAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：用于治疗疼痛的N-（N-磺酰基氨基甲基）环丙烷氨基甲酰胺衍生物
公开(公告)号：WO2006097817A9
公开(公告)日：2006-12-07
申请号：PCT/IB2006000557
申请日：2006-03-07
申请人： PFIZER JAPAN INC , PFIZER , HANAZAWA TAKESHI , HIRANO MISATO , INOUE TADASHI , NAGAYAMA SATOSHI , NAKAO KAZUNARI , SHISHIDO YUJI , TANAKA HIROTAKA
发明人： HANAZAWA TAKESHI , HIRANO MISATO , INOUE TADASHI , NAGAYAMA SATOSHI , NAKAO KAZUNARI , SHISHIDO YUJI , TANAKA HIROTAKA
IPC分类号： C07C311/08 , A61K31/145 , A61K31/44 , A61P29/00 , C07C317/44 , C07C323/62 , C07D213/56 , C07D213/74 , C07D213/76
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：本发明提供了式（I）化合物或其药学上可接受的盐或溶剂化物。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。

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