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    Piperidine derivative, process for producing the same, and use
    1.
    发明申请
    Piperidine derivative, process for producing the same, and use 失效
    哌啶衍生物，其制备方法和用途

    公开(公告)号：US20060167052A1

    公开(公告)日：2006-07-27

    申请号：US10516252

    申请日：2003-05-29

    申请人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai ,  Masayuki Yamashita

    发明人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai ,  Masayuki Yamashita

    IPC分类号： A61K31/454 ,  C07D403/02

    CPC分类号： C07D405/14 ,  C07D211/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

    摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally lo substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and 15 when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

    摘要翻译： 本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选地 取代烃基，酰基或任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是 任选取代的芳环，条件是当Z是被氧代基取代的亚甲基时，R 1不是甲基，而当Z是被甲基取代的亚甲基时，R 1是环B 是取代的芳香环或其盐，其是对速激肽受体具有优异拮抗作用的新型哌啶衍生物，并且可用作药物，特别是用于预防和/或治疗尿频和/或 尿失禁

    Piperidine derivative, process for producing the same, and use
    2.
    发明授权
    Piperidine derivative, process for producing the same, and use 失效
    哌啶衍生物，其制备方法和用途

    公开(公告)号：US07622487B2

    公开(公告)日：2009-11-24

    申请号：US10516252

    申请日：2003-05-29

    申请人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai

    发明人： Yoshinori Ikeura ,  Tadatoshi Hashimoto ,  Naoki Tarui ,  Junya Shirai

    IPC分类号： A61K31/445 ,  C07D403/12

    CPC分类号： C07D405/14 ,  C07D211/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

    摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group, X is an oxygen atom or an optionally substituted imino group, Z is an optionally substituted methylene group, Ring A is an optionally further substituted piperidine ring, and Ring B is an optionally substituted aromatic ring, provided that when Z is a methylene group substituted with an oxo group, R1 is not a methyl group, and when Z is a methylene group substituted with a methyl group, Ring B is a substituted aromatic ring, or a salt thereof, which is a novel piperidine derivative having excellent antagonistic action for a tachykinin receptor and useful as a medicament, particularly an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

    摘要翻译： 本发明提供由下式表示的化合物：其中Ar是芳基，芳烷基或芳族杂环基，其各自可以被取代，R 1是氢原子，任选取代的烃基，酰基或 任选取代的杂环基，X是氧原子或任选取代的亚氨基，Z是任选取代的亚甲基，环A是任选进一步取代的哌啶环，环B是任选取代的芳环，条件是当Z 是被氧基取代的亚甲基，R1不是甲基，当Z是被甲基取代的亚甲基时，环B是取代的芳香环或其盐，它是具有 用于速激肽受体的优异拮抗作用，可用作药物，特别是用于预防和/或治疗尿频和/或尿失禁的药剂。

    Nitrogen-containing heterocyclic compound and use thereof
    5.
    发明申请
    Nitrogen-containing heterocyclic compound and use thereof 有权
    含氮杂环化合物及其用途

    公开(公告)号：US20090156572A1

    公开(公告)日：2009-06-18

    申请号：US12314015

    申请日：2008-12-02

    申请人： Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    发明人： Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    IPC分类号： A61K31/397 ,  C07D413/12 ,  A61K31/5377 ,  C07D401/12 ,  A61K31/4545 ,  C07D417/14 ,  A61K31/541 ,  C07D401/14 ,  A61K31/497 ,  C07D487/04 ,  A61K31/4985

    CPC分类号： C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

    摘要翻译： 本发明涉及一种由下式表示的化合物：其中环A为任选具有取代基的含氮杂环，环B为任选具有取代基的芳环，环C为任选具有取代基的环状基团 R 1为氢原子，任选具有取代基的烃基，酰基，任选具有取代基的杂环基或任选具有取代基的氨基，R2为任选卤代的C1 -6烷基，m和n各自为0至5的整数，m + n为2至5的整数，并且是单键或双键，或其盐等。 由于该化合物具有优异的速激肽受体拮抗作用，并且可用作预防或治疗诸如下尿路疾病，胃肠道疾病，中枢神经系统疾病等各种疾病的药剂。

    Piperidine derivative and use thereof
    6.
    发明申请
    Piperidine derivative and use thereof 审中-公开
    哌啶衍生物及其用途

    公开(公告)号：US20070149570A1

    公开(公告)日：2007-06-28

    申请号：US11701380

    申请日：2007-02-02

    申请人： Yoshinori Ikeura ,  Junya Shirai ,  Takeshi Yoshikawa ,  Nobuki Sakauchi

    发明人： Yoshinori Ikeura ,  Junya Shirai ,  Takeshi Yoshikawa ,  Nobuki Sakauchi

    IPC分类号： C07D211/56 ,  A61K31/445

    CPC分类号： C07D211/58 ,  C07D405/12

    摘要： The present invention relates to a compound represented by the formula: wherein Ar is a phenyl group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom, a C1-6 alkyl group optionally having substituent(s) or a C3-6 cycloalkyl group optionally having substituent(s), Z is a methylene group optionally having a C1-6 alkyl group, ring A is a piperidine ring optionally further having substituent(s), ring B and ring C are benzene rings optionally further having substituent(s), and R2 optionally form a ring together with the adjacent substituent on the ring B, except the compounds represented by the formula: or a salt thereof. The compound of the present invention has a superior tachykinin receptor antagonistic action, particularly a substance P receptor antagonistic action, and is useful as a pharmaceutical agent, for example, tachykinin receptor antagonist, an agent for the prophylaxis or treatment of lower urinary tract symptoms, gastrointestinal diseases or central nerve diseases.

    摘要翻译： 本发明涉及由下式表示的化合物：其中Ar是任选具有取代基的苯基，R 1是氢原子，任选具有取代基的烃基， 酰基或任选具有取代基的杂环基，R 2是氢原子，任选具有取代基的C 1-6烷基或C 任选具有取代基的3-6个环烷基，Z是任选具有C 1-6 - 烷基的亚甲基，环A是任选进一步具有 取代基，环B和环C是任选进一步具有取代基的苯环，并且R 2任选地与环B上的相邻取代基一起形成环，除了由式 式：或其盐。 本发明的化合物具有优异的速激肽受体拮抗作用，特别是P受体拮抗作用，可用作药剂，例如速激肽受体拮抗剂，预防或治疗下尿路症状的药剂， 胃肠道疾病或中枢神经疾病。

    Nitrogen-containing heterocyclic compound and use thereof
    7.
    发明授权
    Nitrogen-containing heterocyclic compound and use thereof 有权
    含氮杂环化合物及其用途

    公开(公告)号：US08470816B2

    公开(公告)日：2013-06-25

    申请号：US12314015

    申请日：2008-12-02

    申请人： Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    发明人： Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    IPC分类号： A61K31/5355 ,  A61K31/445 ,  A61K31/444 ,  A61K31/40 ,  C07D413/04 ,  C07D401/04 ,  C07D211/56 ,  C07D207/14

    CPC分类号： C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

    摘要翻译： 本发明涉及一种由下式表示的化合物：其中环A为任选具有取代基的含氮杂环，环B为任选具有取代基的芳环，环C为任选具有取代基的环状基团 R 1为氢原子，任选具有取代基的烃基，酰基，任选具有取代基的杂环基或任选具有取代基的氨基，R2为任选卤代的C1 -6烷基，m和n分别为0〜5的整数，m + n为2〜5的整数，为单键或双键，或其盐等。 由于该化合物具有优异的速激肽受体拮抗作用，并且可用作预防或治疗诸如下尿路疾病，胃肠道疾病，中枢神经系统疾病等各种疾病的药剂。

    Carboxamide derivative and use thereof
    8.
    发明申请
    Carboxamide derivative and use thereof 审中-公开
    羧酰胺衍生物及其用途

    公开(公告)号：US20090186874A1

    公开(公告)日：2009-07-23

    申请号：US10584949

    申请日：2005-01-13

    申请人： Yoshinori Ikeura ,  Junya Shirai

    发明人： Yoshinori Ikeura ,  Junya Shirai

    IPC分类号： A61K31/55 ,  C07D211/60 ,  A61K31/445 ,  A61K31/44 ,  C07D213/81 ,  C07D401/02 ,  C07D401/12 ,  C07D223/04 ,  C07D401/00 ,  A61K31/4545

    CPC分类号： C07D223/06 ,  C07D211/62 ,  C07D211/78

    摘要： The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an aromatic ring optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is an optionally halogenated C1-6 alkyl group, Y is a methylene group optionally having substituent(s), m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof. The compound of the present invention has a superior tachykinin receptor antagonistic action, particularly an SP receptor antagonistic action, and is useful as a pharmaceutical agent, for example, a tachykinin receptor antagonist, an agent for the prophylaxis or treatment of an abnormality of lower urinary tract functions, a digestive organ disease or a central nerve disease, and the like.

    摘要翻译： 本发明涉及由下式表示的化合物：其中环A为任选还具有取代基的含氮杂环，环B和环C各自为任选具有取代基的芳环，R 1为氢原子 ，任选具有取代基的烃基，任选具有取代基的酰基或杂环基，Z是任选卤代的C 1-6烷基，Y是任选具有取代基的亚甲基，m和 n分别为0〜5的整数，m + n为2〜5的整数，＆lt; img id =“CUSTOM-CHARACTER-00001”he =“2.46mm”wi =“6.35mm”file =“US20090186874A1- 20090723-P00001.TIF“img-content =”character“img-format =”tif“/>是单键或双键，或其盐。 本发明的化合物具有优异的速激肽受体拮抗作用，特别是SP受体拮抗作用，可用作药剂，例如速激肽受体拮抗剂，预防或治疗下尿异症的药物 道功能，消化器官疾病或中枢神经疾病等。

    Heterocyclic compound
    9.
    发明授权
    Heterocyclic compound 有权
    杂环化合物

    公开(公告)号：US09156837B2

    公开(公告)日：2015-10-13

    申请号：US14235992

    申请日：2012-07-27

    申请人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    发明人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

    IPC分类号： C07D277/30 ,  C07D277/56 ,  C07D211/90 ,  C07D417/12 ,  C07D471/04 ,  C07D401/12 ,  C07D277/24 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

    CPC分类号： C07D471/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

    摘要： A heterocyclic compound having an RORγt inhibitory activity, which is a compound of formula (I) or a salt thereof is provided. The compound has ring A, which is an optionally substituted cyclic group and is bound to a pyrazole ring though Q. Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene. R1 is a substituent. Ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2. R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group.

    摘要翻译： 提供具有RORγt抑制活性的杂环化合物，其为式（I）化合物或其盐。 该化合物具有环A，其为任选取代的环状基团，并且通过Q键合至吡唑环。Q为键，任选取代的C 1-10亚烷基，任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基。 R1是取代基。 环B是噻唑环，异噻唑环或二氢噻唑环，除了R2之外，它们各自任选进一步被取代基取代。 R 2是任选取代的环羰基-C 1-6烷基，任选取代的氨基羰基-C 1-6烷基，任选取代的环C 1-6烷基，任选取代的环C 1-6烷基氨基羰基， 任选取代的氨基羰基-C 2-6烯基，任选取代的C 1-6烷基羰基氨基-C 1-6烷基，任选取代的环 - 氨基羰基，任选取代的环羰基或任选取代的非芳族杂环基。