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    • 1. 发明申请
    • Chromane Substituted Benzimidazole Derivatives
    • 色烷取代的苯并咪唑衍生物
    • US20070142448A1
    • 2007-06-21
    • US11612583
    • 2006-12-19
    • Takeshi HanazawaHiroki Koike
    • Takeshi HanazawaHiroki Koike
    • A61K31/4184C07D405/02C07D407/02
    • C07D405/12C07D409/12
    • This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5, R6, R7 and R8 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.
    • 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,R 6,R 7和R SUP 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(例如但不限于胃肠道) 胃食管反流疾病(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。
    • 2. 发明授权
    • Chromane substituted benzimidazole derivatives
    • 苯并二氢苯并咪唑衍生物
    • US07723321B2
    • 2010-05-25
    • US11612583
    • 2006-12-19
    • Takeshi HanazawaHiroki Koike
    • Takeshi HanazawaHiroki Koike
    • A61K31/4184C07D405/02C07D407/02
    • C07D405/12C07D409/12
    • This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5, R6, R7 and R8 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.
    • 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 3,R 4,R 5,R 6,R 7和R 8各自如本文所述, 可接受的盐和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(例如但不限于胃肠疾病,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,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,过度激素 ,气道障碍或哮喘。
    • 3. 发明授权
    • Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    • US07915448B2
    • 2011-03-29
    • US12578061
    • 2009-10-13
    • Takeshi HanazawaMisato HiranoTadashi InoueSatoshi NagayamaKazunari NakaoYuji ShishidoHirotaka Tanaka
    • Takeshi HanazawaMisato HiranoTadashi InoueSatoshi NagayamaKazunari NakaoYuji ShishidoHirotaka Tanaka
    • C07C311/03A61K31/18
    • C07C61/28C07C61/40C07C311/08C07C317/44C07C323/62C07C2601/02C07D213/26C07D213/56C07D213/74C07D213/76
    • This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6) alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof.
    • 9. 发明申请
    • Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    • US20060211741A1
    • 2006-09-21
    • US11384127
    • 2006-03-17
    • Takeshi HanazawaMisato HiranoTadashi InoueSatoshi NagayamaKazunari NakaoYuji ShishidoHirotaka Tanaka
    • Takeshi HanazawaMisato HiranoTadashi InoueSatoshi NagayamaKazunari NakaoYuji ShishidoHirotaka Tanaka
    • A61K31/4412A61K31/18C07D213/75
    • C07C61/28C07C61/40C07C311/08C07C317/44C07C323/62C07C2601/02C07D213/26C07D213/56C07D213/74C07D213/76
    • This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6-membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; 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.