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1. 发明申请

WO2007072142A3 BENZIMIDAZOLE-5-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：苯并咪唑-5-羧酰胺衍生物
公开(公告)号：WO2007072142A3
公开(公告)日：2008-08-28
申请号：PCT/IB2006003578
申请日：2006-12-06
申请人： PFIZER JAPAN INC , PFIZER , IWAMURO YUKO , KOIKE HIROKI , MORITA MIKIO , SAKAKIBARA SACHIKO
发明人： IWAMURO YUKO , KOIKE HIROKI , MORITA MIKIO , SAKAKIBARA SACHIKO
IPC分类号： C07D235/08 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/496 , A61K31/5355 , A61K31/541 , A61P1/04 , C07D401/12 , C07D403/06 , C07D413/06 , C07D417/06
CPC分类号： C07D235/08 , C07D401/12 , C07D403/06 , C07D413/06 , C07D417/06
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R 1 , R 2 , R 3 , R 4 , A and X 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 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, hypersalivation, 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：R 1，R 2，R 3， R 4，A和X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由酸泵拮抗活性介导的病症中的用途，例如胃肠疾病，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，Zollinger-Ellison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。

2. 发明申请

WO2007072142A2 BENZIMIDAZOLE-5-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：苯并咪唑-5-羧酰胺衍生物
公开(公告)号：WO2007072142A2
公开(公告)日：2007-06-28
申请号：PCT/IB2006/003578
申请日：2006-12-06
申请人： PFIZER JAPAN INC. , PFIZER INC. , IWAMURO, Yuko , KOIKE, Hiroki , MORITA, Mikio , SAKAKIBARA, Sachiko
发明人： IWAMURO, Yuko , KOIKE, Hiroki , MORITA, Mikio , SAKAKIBARA, Sachiko
CPC分类号： C07D235/08 , C07D401/12 , C07D403/06 , C07D413/06 , C07D417/06
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R 1 , R 2 , R 3 , R 4 , A and X 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 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, hypersalivation, 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：R 1，R 2，R 3， R 4，A和X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由酸泵拮抗活性介导的病症中的用途，例如胃肠疾病，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，Zollinger-Ellison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。

3. 发明申请

WO2006134460A1 CHROMANE SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS ACID PUMP ANTAGONISTS 审中-公开
标题翻译：取代苄基苯并噻唑衍生物作为酸性尿素拮抗剂
公开(公告)号：WO2006134460A1
公开(公告)日：2006-12-21
申请号：PCT/IB2006/001567
申请日：2006-06-02
申请人： PFIZER JAPAN INC. , PFIZER INC. , KOIKE, Hiroki , SAKAKIBARA, Sachiko
发明人： KOIKE, Hiroki , SAKAKIBARA, Sachiko
IPC分类号： A61K31/4184 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , A61P1/04
CPC分类号： C07D405/12 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R 1 , R 2 , R 3 , R 4 , R 5 and 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 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, hypersalivation, 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：A，B，X，R 1，R 2，R SUP R 3，R 4，R 5和R 6，R 7，R SUP， > 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和这些化合物在治疗由酸泵拮抗活性介导的病症中的用途胃肠疾病，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，Zollinger- 埃里森综合征，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。

4. 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。

5. 发明申请

WO0244153A8 4-6-DIPHENYL PYRIDINE DERIVATIVES AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译： 4-6-二苯基吡啶衍生物作为抗炎剂
公开(公告)号：WO0244153A8
公开(公告)日：2002-11-28
申请号：PCT/EP0113338
申请日：2001-11-19
申请人： BAYER AG , MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
发明人： MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
IPC分类号： A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5365 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D498/04 , A61K31/44
CPC分类号： C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12
摘要： 4-aryl pyrimidine compounds of general formula and salts thereof:wherein X is CH or N; R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R is hydrogen, halogen, etc.; R is hydrogen, hydroxy, halogen, amino, etc.; R is hydroxy, amino, carboxy, etc. or R and R together form a ring; R is hydrogen, carbamoyl, cyano, carboxy, C1-16 alkoxycarbonyl, etc. and R is amino or C1-16 alkanoylamino or R and R together form a ring. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and act as inhibitors of IKK- beta and thus inhibit nuclear factor kappa B(NF-KB).
摘要翻译：通式为4-芳基嘧啶化合物及其盐：其中X为CH或N; R 1是氢，卤素，C 1-6烷基，C 1-6烷氧基等; R 2是氢，卤素等; R 3是氢，羟基，卤素，氨基等; R 4是羟基，氨基，羧基等，或者R 3和R 4一起形成环; R 5是氢，氨基甲酰基，氰基，羧基，C 1-6烷氧基羰基等，R 6是氨基或C 1-6烷酰基氨基或R 5和R 6一起形成环。化合物（I）或其盐具有优异的抗炎活性，并且作为IKK-β的抑制剂，从而抑制核因子κB（NF-κB）。

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