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1. 发明申请

US20090105253A1 Triazole Derivative and Use Thereof 失效
标题翻译：三唑衍生物及其用途
公开(公告)号：US20090105253A1
公开(公告)日：2009-04-23
申请号：US11887936
申请日：2006-04-06
申请人： Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
发明人： Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
IPC分类号： A61K31/5377 , C07D249/06 , C07D413/12 , A61K31/4192
CPC分类号： C07D249/06 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D411/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.
摘要翻译：本发明涉及含有式（I）表示的化合物的凝血酶受体拮抗剂，其中R1a，R1b和R2各自为氢原子，任选取代的烃基，任选取代的杂环基或任选取代的烷氧基，R 3 是由式-NHCOR4，-NHSO2R5，-NHCON（R6a）（R6b），-NHCOOR7或-CONHR8表示的基团，其中R4，R5，R6a，R6b，R7和R8各自为氢原子，任选取代的烃基，任选取代的杂环基等），环A是任选进一步具有取代基的单环芳环，R 1a和R 1b任选地彼此键合以形成任选取代的含氮非芳族杂环，或盐或其前药。本发明的凝血酶受体拮抗剂具有凝血酶受体（特别是PAR-1）拮抗作用，可用于预防或治疗PAR-1介导的病理状态或疾病。

2. 发明授权

US07803822B2 Triazole derivative and use thereof 失效
标题翻译：三唑衍生物及其用途
公开(公告)号：US07803822B2
公开(公告)日：2010-09-28
申请号：US11887936
申请日：2006-04-06
申请人： Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
发明人： Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D249/06 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D411/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.
摘要翻译：本发明涉及含有式（I）表示的化合物的凝血酶受体拮抗剂，其中R1a，R1b和R2各自为氢原子，任选取代的烃基，任选取代的杂环基或任选取代的烷氧基，R 3 是由式-NHCOR4，-NHSO2R5，-NHCON（R6a）（R6b），-NHCOOR7或-CONHR8表示的基团，其中R4，R5，R6a，R6b，R7和R8各自为氢原子，任选取代的烃基，任选取代的杂环基等），环A是任选进一步具有取代基的单环芳环，R 1a和R 1b任选地彼此键合以形成任选取代的含氮非芳族杂环或盐或其前药。本发明的凝血酶受体拮抗剂具有凝血酶受体（特别是PAR-1）拮抗作用，可用于预防或治疗PAR-1介导的病理状态或疾病。

3. 发明申请

US20130331409A1 CONDENSED HETEROCYCLIC COMPOUND 有权
标题翻译：稠化的杂环化合物
公开(公告)号：US20130331409A1
公开(公告)日：2013-12-12
申请号：US14002439
申请日：2012-03-15
申请人： Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
发明人： Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
IPC分类号： C07D471/14 , C07D471/04
CPC分类号： C07D471/14 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异的PDE10A抑制作用的化合物及其用途。化合物是由下式（I）表示的化合物：其中各符号如本说明书中所定义，或其盐。

4. 发明授权

US08563575B2 Fused heterocyclic compounds 有权
公开(公告)号：US08563575B2
公开(公告)日：2013-10-22
申请号：US13166212
申请日：2011-06-22
申请人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
发明人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.

5. 发明授权

US08846713B2 Fused heterocyclic compounds as phosphodiesterases (PDEs) inhibitors 有权
标题翻译：稠合杂环化合物作为磷酸二酯酶（PDEs）抑制剂
公开(公告)号：US08846713B2
公开(公告)日：2014-09-30
申请号：US13806352
申请日：2011-06-22
申请人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata
发明人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata
IPC分类号： C07D401/14 , A61K31/437 , A61K31/4439 , A61K31/444
CPC分类号： A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
摘要翻译：本发明提供具有PDE抑制作用的化合物，其可用作预防或治疗由式（I）表示的精神分裂症等的药剂：

6. 发明申请

US20130172328A1 FUSED HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASES (PDES) INHIBITORS 有权
标题翻译：熔融杂环化合物作为磷酸二氢钾（PDES）抑制剂
公开(公告)号：US20130172328A1
公开(公告)日：2013-07-04
申请号：US13806352
申请日：2011-06-22
申请人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki , John F. Quinn , Joseph Raker , Fatoumata Camara , Yi Wang
发明人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki , John F. Quinn , Joseph Raker , Fatoumata Camara , Yi Wang
IPC分类号： C07D471/04 , C07D498/04 , C07D473/00 , C07D519/00
CPC分类号： A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
摘要翻译：本发明提供具有PDE抑制作用的化合物，其可用作预防或治疗由式（I）表示的精神分裂症等的药剂：

7. 发明授权

US09029388B2 Condensed heterocyclic compound 有权
标题翻译：缩合杂环化合物
公开(公告)号：US09029388B2
公开(公告)日：2015-05-12
申请号：US14002439
申请日：2012-03-15
申请人： Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
发明人： Takahiko Taniguchi , Jun Kunitomo , Masato Yoshikawa , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Haruhi Kamisaki , Shinkichi Suzuki , Kasei Miura
IPC分类号： C07D471/14 , C07D471/04 , C07D519/00
CPC分类号： C07D471/14 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异的PDE10A抑制作用的化合物及其用途。化合物是由下式（I）表示的化合物：其中各符号如本说明书中所定义，或其盐。

8. 发明授权

US08778944B2 Pyridazinone compounds 有权
标题翻译：哒嗪酮化合物
公开(公告)号：US08778944B2
公开(公告)日：2014-07-15
申请号：US13543207
申请日：2012-07-06
申请人： Takahiko Taniguchi , Akira Kawada , John F. Quinn , Jun Kunitomo , Masato Yoshikawa , Makoto Fushimi
发明人： Takahiko Taniguchi , Akira Kawada , John F. Quinn , Jun Kunitomo , Masato Yoshikawa , Makoto Fushimi
IPC分类号： A61K31/50 , A61K31/501
CPC分类号： C07D403/04 , A61K9/2059 , C07D401/14 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
摘要翻译：本发明提供具有PDE抑制作用的化合物，其可用作预防或治疗精神分裂症等的药物。式（I0）的化合物，其中R1表示取代基; R2表示氢原子或取代基; R3表示氢原子或取代基; 环A表示可被取代的芳环，环B表示可被取代的5元杂芳环或其盐。

9. 发明申请

US20130172292A1 FUSED HETEROCYCLIC COMPOUNDS 有权
标题翻译：熔融杂环化合物
公开(公告)号：US20130172292A1
公开(公告)日：2013-07-04
申请号：US13814073
申请日：2011-08-03
申请人： Joseph Raker , Takahiko Taniguchi , Masato Yoshikawa , Tomoaki Hasui , Jun Kunitomo
发明人： Joseph Raker , Takahiko Taniguchi , Masato Yoshikawa , Tomoaki Hasui , Jun Kunitomo
IPC分类号： C07D471/04 , C07D471/14 , C07D519/00
CPC分类号： C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′-(Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.
摘要翻译：本发明提供了具有PDE 10A抑制作用的化合物，其可用作预防或治疗精神分裂症等的药物。由式（1'）表示的化合物：其中环A'表示任选取代的吡啶环，任选取代的哒嗪环，嘧啶环或吡嗪环，R1'表示（1）其中R1a'表示任选取代的苯基或任选取代的5至10元杂环基，环B2表示键，-S - ， - O-，-CO-，任选取代的亚甲基或-NR a' - （R a '表示氢原子或任选取代的C 1-6烷基），并且环B1'表示任选进一步取代的6至10元芳族烃环或任选进一步取代的5至10元芳族杂环，或者可选地，L'和R 1a'可以一起形成任选取代的双环或三环稠合杂环基，或（2），其中，R 1b'表示任选取代的苯基，或任选取代的5-至10- 环B2'表示任选取代的苯环，任选取代的吡啶环，任选取代的嘧啶环，任选取代的吡嗪环或任选取代的哒嗪环，环D'表示任选进一步取代的5-或6-元环，R 2' 表示氢原子或取代基，X'表示= N-或= CRb' - （Rb'表示氢原子或取代基）， - - - 表示Rb'和R2'可以一起形成与它们各自相邻的碳原子和氮原子，当X'= CRb'或其盐时，任选取代的5-至7-元环。

10. 发明申请

US20100069351A1 SPIRO COMPOUND AND USE THEREOF 有权
标题翻译： SPIRO化合物及其用途
公开(公告)号：US20100069351A1
公开(公告)日：2010-03-18
申请号：US12449320
申请日：2008-02-05
申请人： Takahiko Taniguchi , Kenichi Miyata , Osamu Kubo
发明人： Takahiko Taniguchi , Kenichi Miyata , Osamu Kubo
IPC分类号： A61K31/397 , C07D237/02 , A61K31/50 , C07D265/12 , A61K31/537 , C07D239/72 , A61K31/527 , C07D245/04 , A61P3/00 , A61P9/00
CPC分类号： C07D401/04 , C07D409/14 , C07D417/14 , C07D471/10 , C07D487/10 , C07D491/107 , C07D498/10
摘要： The present invention aims to provide a novel SCD inhibitor.The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.
摘要翻译：本发明旨在提供一种新型的SCD抑制剂。本发明涉及包含由式（I）表示的化合物的SCD抑制剂，其中R是任选取代的环状基团或任选取代的氨基甲酰基，条件是R不是任选取代的7-吡啶并[2,3-d] 嘧啶基; 环A是任选进一步取代的哒嗪环; R 1，R 2，R 3，R 4，R 11，R 12，R 13和R 14各自独立地为氢原子或取代基，或R 1和R 11组合，R 2和R 12组合，R 3和R 13组合，或R 4和R 14组合任选地形成氧代基团，或者R 2和R 4组合任选地形成键或亚烷基交联; m和n各自独立地为0〜2的整数。环B是任选取代的环，条件是与螺环碳原子相邻的构成环B的两个原子不是同时为氧原子，或其盐或其前药。

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