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1. 发明申请

US20060167052A1 Piperidine derivative, process for producing the same, and use 失效
标题翻译：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

2. 发明授权

US07622487B2 Piperidine derivative, process for producing the same, and use 失效
标题翻译：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。

3. 发明申请

US20060241145A1 Piperidine derivative crystal, process for producing the same, and use 审中-公开
标题翻译：哌啶衍生物晶体，其制备方法和用途
公开(公告)号：US20060241145A1
公开(公告)日：2006-10-26
申请号：US11407209
申请日：2006-04-20
申请人： Yoshinori Ikeura , Tadatoshi Hashimoto , Junya Shirai , Yoshikawa Takeshi , Hiroshi Nakatani , Mitsuhisa Yamano , Masahiro Mizuno , Hiroyuki Irie
发明人： Yoshinori Ikeura , Tadatoshi Hashimoto , Junya Shirai , Yoshikawa Takeshi , Hiroshi Nakatani , Mitsuhisa Yamano , Masahiro Mizuno , Hiroyuki Irie
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D211/74 , C07D211/56 , C07D401/12 , C07D401/14
摘要： The present invention provides a piperidine derivative having antagonistic action for tachykinin receptors and the like, a crystal thereof, and an agent for the prophylaxis or treatment of diseases including lower urinary tract disease and the like, which contains the derivative. Specifically, the present invention provides an optically active compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof.
摘要翻译：本发明提供对速激肽受体等具有拮抗作用的哌啶衍生物及其结晶，以及含有该衍生物的预防或治疗包括下尿路疾病等的疾病的药剂。具体地，本发明提供由式（I）表示的光学活性化合物：其中每个符号如说明书中所定义，及其盐。

4. 发明申请

US20060142337A1 Piperidine derivative and use thereof 审中-公开
标题翻译：哌啶衍生物及其用途
公开(公告)号：US20060142337A1
公开(公告)日：2006-06-29
申请号：US11358070
申请日：2006-02-22
申请人： Yoshinori Ikeura , Tadatoshi Hashimoto , Haruyuki Nishida , Junya Shirai , Nobuki Sakauchi
发明人： Yoshinori Ikeura , Tadatoshi Hashimoto , Haruyuki Nishida , Junya Shirai , Nobuki Sakauchi
IPC分类号： C07D211/54 , A61K31/445
CPC分类号： C07D211/46 , C07D211/58 , C07D211/62 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound represented by the formula: wherein Ar is an aryl group optionally having substituents, R is a C1-6 alkyl group, R1 is a hydrogen atom, a hydrocarbon group optionally having substituents, an acyl group or a heterocyclic group optionally having substituents, X is an oxygen atom or an imino group optionally having substituents, ring A is a piperidine ring optionally further having substituents, and ring B is a benzene ring having substituents, or a salt thereof, and an agent for the prophylaxis or treatment of lower urinary tract abnormality and the like, which contains the compound.
摘要翻译：本发明提供由下式表示的化合物：其中Ar是任选具有取代基的芳基，R是C 1-6烷基，R 1是氢任选具有取代基的烃基，任选具有取代基的酰基或杂环基，X是任选具有取代基的氧原子或亚氨基，环A是任选还具有取代基的哌啶环，环B是苯具有取代基的环或其盐，以及含有该化合物的预防或治疗下尿路异常等的药剂。

5. 发明申请

US20090156572A1 Nitrogen-containing heterocyclic compound and use thereof 有权
标题翻译：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。

6. 发明申请

US20070149570A1 Piperidine derivative and use thereof 审中-公开
标题翻译：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。

7. 发明授权

US08470816B2 Nitrogen-containing heterocyclic compound and use thereof 有权
标题翻译：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。

8. 发明申请

US20090186874A1 Carboxamide derivative and use thereof 审中-公开
标题翻译：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。

9. 发明授权

US09156837B2 Heterocyclic compound 有权
标题翻译：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。

10. 发明授权

US08158617B2 Fused heterocyclic compound and use thereof 有权
标题翻译：稠合杂环化合物及其用途
公开(公告)号：US08158617B2
公开(公告)日：2012-04-17
申请号：US12227333
申请日：2007-05-15
申请人： Junya Shirai , Tomokazu Kusumoto , Hiroyuki Nagamiya
发明人： Junya Shirai , Tomokazu Kusumoto , Hiroyuki Nagamiya
IPC分类号： A61P13/02 , A61P3/04 , A61P15/02 , A61P21/00 , A61P43/00 , A61K31/553 , A61K31/55 , C07D498/04
CPC分类号： A61K31/553 , A61B5/04882 , A61B5/202 , A61B5/205 , A61K31/00 , A61K31/4353 , A61N1/36007 , C07D223/16 , C07D487/04 , C07D498/04 , C07D519/00 , G01N33/942
摘要： The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.
摘要翻译：本发明涉及含有下式表示的化合物的5-羟色胺5-HT 2C受体活化剂，其中环A是任选具有取代基的5-或6-元芳族杂环，环B为7-至9-元其中m和n（m，n）的组合是（1,2），（2,1），（2,2），（3,1），（ 3,2）或（4,1）或其盐或其前药，以及具有5-羟色胺5-HT 2C受体激活作用的稠合杂环化合物等。

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