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    Substituted Aryloxymethyl Bicyclicmethyl Acetamide Compounds
    3.
    发明申请
    Substituted Aryloxymethyl Bicyclicmethyl Acetamide Compounds 失效

    公开(公告)号：US20060270682A1

    公开(公告)日：2006-11-30

    申请号：US11421242

    申请日：2006-05-31

    申请人： Tadashi Inoue ,  Satoshi Nagayama ,  Yuji Shishido

    发明人： Tadashi Inoue ,  Satoshi Nagayama ,  Yuji Shishido

    IPC分类号： A61K31/501 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4184 ,  A61K31/4192

    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, O—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)alkoxy, 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)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—. 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.

    Substituted pyridylmethyl bicycliccarboxyamide compounds
    4.
    发明授权
    Substituted pyridylmethyl bicycliccarboxyamide compounds 失效
    取代的吡啶基甲基双环羧酰胺化合物

    公开(公告)号：US08178558B2

    公开(公告)日：2012-05-15

    申请号：US12439888

    申请日：2007-09-10

    申请人： Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka

    发明人： Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka

    IPC分类号： A61K31/47 ,  C07D213/56

    CPC分类号： C07D213/40 ,  C07D401/12

    摘要： This invention relates to novel substituted pyridylmethyl bicyclocarboxamide compounds and to their use in therapy. These compounds are particularly useful as modulators of the VR1 (Type I Vanilloid) receptor, and are 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.

    摘要翻译： 本发明涉及新型取代的吡啶基甲基双环胺化合物及其在治疗中的用途。 这些化合物特别可用作VR1（I型香草素）受体的调节剂，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，盆腔超敏反应 ，膀胱疾病，炎症等，在哺乳动物，特别是人类中。

    Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
    7.
    发明申请
    Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists 失效

    公开(公告)号：US20060100460A1

    公开(公告)日：2006-05-11

    申请号：US11270780

    申请日：2005-11-09

    申请人： Tadashi Inoue ,  Satoshi Nagayama ,  Kazunari Nakao

    发明人： Tadashi Inoue ,  Satoshi Nagayama ,  Kazunari Nakao

    IPC分类号： C07D211/26 ,  A61K31/445 ,  A61K31/18 ,  C07C311/19

    CPC分类号： C07C311/08 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/10 ,  C07D295/096 ,  C07D311/16

    摘要： This invention provides a compound of the formula (I): wherein R1 represents a (C1-C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group or a (C1-C6) alkoxy group; R3, R4, R5 and R6 each independently represents a hydrogen atom, a (C1-C6) alkyl, or a halogen atom; R7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group optionally substituted with a piperidino group, a (C-1-C6)alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C1-C6)alkoxy group, a (C1-C6)alkoxy-(C1-C6)alkyl group, a (C1-C6)alkoxy-(C1-C6)alkoxy group, a halo (C1-C6)alkyl group, a (C1-C6)alkylthio group, a (C1-C6)alkylsulfinyl group or a (C1-C6)alkylsulfonyl group; R5 represents a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a hydroxy(C1-C6)alkoxy group, a (C1-C6)alkoxy-(C1-C6)alkyl group or a (C1-C6)alkoxy-(C1-C6)alkoxy group; or R7 and R8, when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C1-C6)alkyl group, a (C1-C6)alkoxy group and a hydroxy(C1-C6)alkyl group; and R9 represents a hydrogen atom or a halogen atom; 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 as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula (I).

    Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    8.
    发明授权
    Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效

    公开(公告)号：US07915448B2

    公开(公告)日：2011-03-29

    申请号：US12578061

    申请日：2009-10-13

    申请人： Takeshi Hanazawa ,  Misato Hirano ,  Tadashi Inoue ,  Satoshi Nagayama ,  Kazunari Nakao ,  Yuji Shishido ,  Hirotaka Tanaka

    发明人： Takeshi Hanazawa ,  Misato Hirano ,  Tadashi Inoue ,  Satoshi Nagayama ,  Kazunari Nakao ,  Yuji Shishido ,  Hirotaka Tanaka

    IPC分类号： C07C311/03 ,  A61K31/18

    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): 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.