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    • 6. 发明授权
      US07915448B2 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
    • Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    • US07915448B2
    • 2011-03-29
    • US12578061
    • 2009-10-13
    • Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
    • Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
    • C07C311/03 , A61K31/18
    • C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20060211741A1 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
    • Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    • US20060211741A1
    • 2006-09-21
    • US11384127
    • 2006-03-17
    • Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
    • Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
    • A61K31/4412 , A61K31/18 , C07D213/75
    • C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明申请
      US20090318497A1 SUBSTITUTED PYRIDYLMETHYL BICYCLICCARBOXYAMIDE COMPOUNDS 失效
    • SUBSTITUTED PYRIDYLMETHYL BICYCLICCARBOXYAMIDE COMPOUNDS
    • 取代的吡啶基甲基双酚A羧酸化合物
    • US20090318497A1
    • 2009-12-24
    • US12439888
    • 2007-09-10
    • Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka
    • Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka
    • A61K31/44 , C07D213/56 , C07D401/12 , A61K31/4709
    • C07D213/40 , C07D401/12
    • 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)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, 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)alkyl, 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.
    • 本发明提供式（I）化合物：其中A1为N，A2为CR7，或A1为CR7，A2为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，其他不为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; R 3和R 8各自独立地为氢，卤素，羟基，（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，卤代（C 1 -C 6）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; R4是卤素，（C1-C6）烷基，（C3-C6）环烷基，卤代（C1-C6）烷基，羟基（C1-C6）烷基，卤代（C1-C6）烷氧基，羟基（C1-C6）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， 烷基硫基，[（C1-C6）烷基] NH-或[（C1-C6）烷基] 2N-; 并且R 5，R 6和R 7各自独立地为氢，卤素，（C 1 -C 6）烷基，羟基（C 1 -C 6）烷基或（C 1 -C 6）烷氧基; 或其药学上可接受的盐，溶剂化物。 这些化合物可用于治疗哺乳动物VR1受体过度活化（如疼痛等）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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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