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    Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
    2.
    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 N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
    3.
    发明授权
    Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists 失效

    公开(公告)号：US07214824B2

    公开(公告)日：2007-05-08

    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： C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00

    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 (C1–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; R8 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 N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists
    4.
    发明申请
    Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists 失效

    公开(公告)号：US20060205980A1

    公开(公告)日：2006-09-14

    申请号：US11372706

    申请日：2006-03-10

    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： C07C311/46

    CPC分类号： C07C311/08

    摘要： This invention provides a compound of the formula (I): wherein R1 represents (C1-C6)alkyl; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl or halo(C1-C6)alkyl; R3 represents a halogen atom, (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, (C1-C6)alkylsulfonyl, [(C1-C6)alkyl]NH—, or [(C1-C6)alkyl]2N—; R4 represents a halogen atom, (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—; R5 represents a halogen atom, (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, (C1-C6)alkylsulfonyl, [(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, or [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)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.

    Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    6.
    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.

    Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
    7.
    发明申请
    Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效

    公开(公告)号：US20060211741A1

    公开(公告)日：2006-09-21

    申请号：US11384127

    申请日：2006-03-17

    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： A61K31/4412 ,  A61K31/18 ,  C07D213/75

    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, (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.

    Substituted Aryloxymethyl Bicyclicmethyl Acetamide Compounds
    8.
    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.