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1. 发明申请

US20080275085A1 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：US20080275085A1
公开(公告)日：2008-11-06
申请号：US12081926
申请日：2008-04-23
申请人： Junya Shirai , Shinji Morimoto , Hideyuki Sugiyama , Nobuki Sakauchi , Takeshi Yoshikawa
发明人： Junya Shirai , Shinji Morimoto , Hideyuki Sugiyama , Nobuki Sakauchi , Takeshi Yoshikawa
IPC分类号： A61K31/4545 , C07D401/04 , A61P1/00 , A61K31/445
CPC分类号： C07D211/60 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula: wherein R1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R2 is methyl or cyclopropyl; R3 is a hydrogen atom or methyl; R4 is a chlorine atom or trifluoromethyl; R5 is a chlorine atom or trifluoromethyl; and a group represented by the formula: is a group represented by the formula: wherein R6 is a hydrogen atom, methyl, ethyl or isopropyl; R7 is a hydrogen atom, methyl or a chlorine atom; and R8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.
摘要翻译：本发明提供了一种新的哌啶衍生物和含有它的速激肽受体拮抗剂，以及由下式表示的化合物：其中R 1是氨基甲酰基甲基，甲基磺酰基乙基羰基等; R 2是甲基或环丙基; R 3是氢原子或甲基; R 4是氯原子或三氟甲基; R 5是氯原子或三氟甲基; 并且由下式表示的基团是由下式表示的基团：其中R 6是氢原子，甲基，乙基或异丙基; R 7是氢原子，甲基或氯原子; R 8是氢原子，氟原子，氯原子或甲基; 或3-甲基噻吩-2-基及其盐。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US07982044B2 Iminopyridine derivatives and use thereof 有权
标题翻译：亚氨基吡啶衍生物及其用途
公开(公告)号：US07982044B2
公开(公告)日：2011-07-19
申请号：US13022563
申请日：2011-02-07
申请人： Masato Yoshida , Nobuki Sakauchi
发明人： Masato Yoshida , Nobuki Sakauchi
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , C07D401/10 , C07D413/10
摘要： The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译：本发明旨在提供具有α1D肾上腺素能受体拮抗作用的亚氨基吡啶衍生物化合物，其可用作预防或治疗下尿路疾病等。本发明提供由下式表示的化合物，其中每个符号如说明书中所定义，或其盐。

7. 发明申请

US20120088748A1 HETEROCYCLIC COMPOUNDS 失效
标题翻译：杂环化合物
公开(公告)号：US20120088748A1
公开(公告)日：2012-04-12
申请号：US13253293
申请日：2011-10-05
申请人： Yuji Ishichi , Masami Yamada , Taku Kamei , Ikuo Fujimori , Yoshihisa Nakada , Tomoya Yukawa , Nobuki Sakauchi , Yusuke Ohba , Tetsuya Tsukamoto
发明人： Yuji Ishichi , Masami Yamada , Taku Kamei , Ikuo Fujimori , Yoshihisa Nakada , Tomoya Yukawa , Nobuki Sakauchi , Yusuke Ohba , Tetsuya Tsukamoto
IPC分类号： A61K31/553 , C07D413/14 , C07D413/04 , C07D413/10 , C07D417/12 , C07D413/12 , C07D417/04 , C07D417/14 , C07D498/08 , C07D475/02 , A61P25/24 , A61P25/22 , A61P25/00 , A61P15/12 , A61P29/00 , A61P13/00 , C07D267/10
CPC分类号： C07D267/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/08
摘要： Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof.
摘要翻译：提供具有单胺再摄取抑制活性的化合物，其由式（I）表示，其中环A是任选取代的6元芳环，环B是环A上的取代基任选地键合以与环一起形成 A，任选取代的9元或10元芳族稠环，以及其它符号如说明书中所定义，或其盐。

8. 发明授权

US07985862B2 Iminopyridine derivatives and use thereof 失效
公开(公告)号：US07985862B2
公开(公告)日：2011-07-26
申请号：US13022537
申请日：2011-02-07
申请人： Masato Yoshida , Nobuki Sakauchi
发明人： Masato Yoshida , Nobuki Sakauchi
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , C07D401/10 , C07D413/10
摘要： The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

9. 发明申请

US20110124876A1 IMINOPYRIDINE DERIVATIVES AND USE THEREOF 有权
公开(公告)号：US20110124876A1
公开(公告)日：2011-05-26
申请号：US13022563
申请日：2011-02-07
申请人： Masato Yoshida , Nobuki Sakauchi
发明人： Masato Yoshida , Nobuki Sakauchi
IPC分类号： C07D213/73
CPC分类号： C07D213/82 , C07D401/10 , C07D413/10
摘要： The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like.The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.

10. 发明申请

US20110124875A1 IMINOPYRIDINE DERIVATIVES AND USES THEREOF 失效
标题翻译：亚氨基吡啶衍生物及其用途
公开(公告)号：US20110124875A1
公开(公告)日：2011-05-26
申请号：US13022556
申请日：2011-02-07
申请人： Masato YOSHIDA , Nobuki Sakauchi
发明人： Masato YOSHIDA , Nobuki Sakauchi
IPC分类号： C07D211/84
CPC分类号： C07D213/82 , C07D401/10 , C07D413/10
摘要： The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like.The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译：本发明旨在提供具有α1D肾上腺素能受体拮抗作用的亚氨基吡啶衍生物化合物，其可用作预防或治疗下尿路疾病等。本发明提供由下式表示的化合物，其中每个符号如说明书中所定义，或其盐。

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