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公开(公告)号:US08980916B2
公开(公告)日:2015-03-17
申请号:US14353359
申请日:2012-10-24
IPC分类号: A61K45/06 , A61K31/5377 , A61K31/4725 , A61K31/4439 , A61K31/4375 , C07D471/04 , C07D413/12 , C07D413/14 , C07D401/12
CPC分类号: C07D401/12 , A61K31/4375 , A61K31/4439 , A61K31/4725 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译: 本发明提供本文所述的式(I)化合物或其药学上可接受的盐。 本发明还提供包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防血栓形成,栓塞,高凝状态或纤维变化的方法。
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公开(公告)号:US08557766B2
公开(公告)日:2013-10-15
申请号:US13444595
申请日:2012-04-11
申请人: Munetaka Ohkouchi
发明人: Munetaka Ohkouchi
CPC分类号: C07D275/03 , A61K31/425 , A61K31/427 , A61K31/435 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4985 , A61K31/502 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/10 , C07D491/107 , C07D491/20
摘要: [Object]To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of Solving the Problem]A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
摘要翻译: 本发明提供一种GPR40活化剂,其含有作为活性成分的具有GPR40激动剂作用的新化合物,化合物的盐,化合物或其盐的溶剂化物,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 解决问题的手段式(I)的化合物:(其中p为0〜4; j为0〜2; k为0〜1;环A为芳基,杂环基,环烷基 ,环烯基,螺环基;环B为芳基,杂芳基; X为0或-NR7-,R1〜R7和L为特定基团),化合物的盐或溶剂化物 化合物或盐。
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公开(公告)号:US08476287B2
公开(公告)日:2013-07-02
申请号:US13392350
申请日:2010-12-24
IPC分类号: A61K31/506 , A61K31/425 , A61K31/4436 , A61K31/4535 , C07D239/24 , C07D275/02 , C07D417/02
CPC分类号: C07D275/03 , A61K9/1623 , A61K9/2018 , A61K9/4858 , C07D417/12 , C07D417/14
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of solving the problem]A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups),a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: [问题]提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 解决问题的方法式(I)的化合物:(其中n为0〜2; p为0〜4; j为0〜3; k为0〜2,环A为 任选被L取代或被L取代的杂环基;环B是苯环,吡啶环或嘧啶环; X是O,S,-NR7-,R1至R7是特定基团) ,化合物的盐或盐或化合物的溶剂合物。
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公开(公告)号:US08455500B2
公开(公告)日:2013-06-04
申请号:US13504749
申请日:2010-10-29
申请人: Akihiro Okano , Munetaka Ohkouchi
发明人: Akihiro Okano , Munetaka Ohkouchi
IPC分类号: A61K31/505 , A61K31/4427 , A61K31/42 , C07D413/02 , C07D413/00 , C07D261/06 , C07D239/24
CPC分类号: C07D261/12 , C07D413/12
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of Solving the Problem]A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: [问题]提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 解决问题的方法式(I)的化合物:(其中p为0〜4; j为0〜3; k为0〜2,环A为特定的环状基团,环B为苯 环,吡啶环或嘧啶环; X是-CH 2 - ,O,-S(O)i - (i是0至2)或-NR 7 - ; R 1至R 6是特定基团), 化合物或盐或化合物的溶剂化物。
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公开(公告)号:US09072758B2
公开(公告)日:2015-07-07
申请号:US14114017
申请日:2012-04-11
IPC分类号: C07D279/02 , C07D285/10 , C07D285/16 , C07D417/12 , C07D417/14 , A61K31/69 , A61K31/425 , A61K31/4439 , A61K31/54 , A61K31/541 , A61K31/549 , A61K45/06 , C07D275/03 , C07F5/04 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/48
CPC分类号: C07D275/03 , A61K9/145 , A61K9/1652 , A61K9/2018 , A61K9/485 , A61K31/425 , A61K31/4439 , A61K31/4985 , A61K31/54 , A61K31/541 , A61K31/549 , A61K31/69 , A61K45/06 , C07D279/02 , C07D285/10 , C07D285/16 , C07D417/12 , C07D417/14 , C07F5/04
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like.[Means of solving the problem]A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A′″ is a benzene ring, a pyridine ring; ring B′ is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: 本发明提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为有效成分的GPR40活化剂,特别是胰岛素促分泌素和 糖尿病,肥胖症等的预防和/或治疗剂。 [解决问题的方法]式(III)的化合物:其中f为0〜2,g为1〜4,j为0〜3,k为0〜2,n为0〜2,p为0 至4; h为0至3; q1为0至3; q2为0或1; r1为0至2(条件是q1 + q2 + r1为0至5); J1a为-CR11a,N; J2是-CR12aR12b-,-CR12c-; T是-CH2-,O,-S(O)i-(i是0-2的整数)或-NR7-; X是O,S或-NR7- 环A'“为苯环,吡啶环,环B'为苯环,吡啶环,嘧啶环,R1〜R14为特定基团),化合物的盐或其溶剂合物 盐或化合物。
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公开(公告)号:US20140057871A1
公开(公告)日:2014-02-27
申请号:US14114017
申请日:2012-04-11
IPC分类号: A61K31/69 , A61K31/4439 , C07D275/03 , A61K31/425 , C07D285/16 , A61K45/06 , C07D279/02 , A61K31/54 , A61K31/541 , C07D285/10 , C07D417/14 , C07F5/04 , C07D417/12 , A61K31/549
CPC分类号: C07D275/03 , A61K9/145 , A61K9/1652 , A61K9/2018 , A61K9/485 , A61K31/425 , A61K31/4439 , A61K31/4985 , A61K31/54 , A61K31/541 , A61K31/549 , A61K31/69 , A61K45/06 , C07D279/02 , C07D285/10 , C07D285/16 , C07D417/12 , C07D417/14 , C07F5/04
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like.[Means of solving the problem]A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A′″ is a benzene ring, a pyridine ring; ring B′ is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: 本发明提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 糖尿病,肥胖症等的预防和/或治疗剂。 [解决问题的方法]式(III)的化合物:其中f为0〜2,g为1〜4,j为0〜3,k为0〜2,n为0〜2,p为0 至4; h为0至3; q1为0至3; q2为0或1; r1为0至2(条件是q1 + q2 + r1为0至5); J1a为-CR11a,N; J2是-CR12aR12b-,-CR12c-; T是-CH2-,O,-S(O)i-(i是0-2的整数)或-NR7-; X是O,S或-NR7- 环A“为苯环,吡啶环,环B'为苯环,吡啶环,嘧啶环,R1〜R14为特定基团),化合物的盐或溶剂化物 盐或化合物。
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公开(公告)号:US20120220772A1
公开(公告)日:2012-08-30
申请号:US13504749
申请日:2010-10-29
申请人: Akihiro Okano , Munetaka Ohkouchi
发明人: Akihiro Okano , Munetaka Ohkouchi
IPC分类号: C07D261/12 , C07D413/12
CPC分类号: C07D261/12 , C07D413/12
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of solving the problem]A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: [问题]提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 [解决问题的方法]式(I)的化合物(其中p为0〜4; j为0〜3; k为0〜2,环A为特定的环状基团,环B为苯 环,吡啶环或嘧啶环; X是-CH 2 - ,O,-S(O)i - (i是0至2)或-NR 7 - ; R 1至R 6是特定基团), 化合物或盐或化合物的溶剂化物。
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公开(公告)号:US09040525B2
公开(公告)日:2015-05-26
申请号:US13877626
申请日:2011-10-11
IPC分类号: C07D279/02 , A61K31/541 , C07D277/04 , C07D275/02 , C07D285/10 , C07D285/16 , C07D417/12 , A61K31/425 , A61K31/433 , A61K31/4439 , A61K31/549 , A61K45/06 , C07D285/34 , C07D417/14
CPC分类号: C07D417/12 , A61K31/4152 , A61K31/425 , A61K31/433 , A61K31/4439 , A61K31/54 , A61K31/541 , A61K31/549 , A61K45/06 , C07D275/02 , C07D275/03 , C07D277/04 , C07D279/02 , C07D285/10 , C07D285/16 , C07D285/34 , C07D417/14
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of Solving the Problem]A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: 本发明提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 解决问题的方法式(1)的化合物:(其中n为0〜2; p为0〜4; h为0〜3; j为0〜3; k为0〜2;环B 是芳基或杂芳基; X是O,S或-NR7-; J1是-CR11aR11b-或-NR11c-; J2是-CR12aR12b-或-NR12c-,R1至R12c是特定基团),a 化合物的盐或盐或化合物的溶剂化物。
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公开(公告)号:US20130203739A1
公开(公告)日:2013-08-08
申请号:US13877626
申请日:2011-10-11
IPC分类号: C07D277/04 , A61K31/549 , A61K31/4439 , A61K31/433 , A61K45/06 , C07D285/34 , C07D279/02 , C07D417/14 , C07D417/12 , A61K31/541 , A61K31/425
CPC分类号: C07D417/12 , A61K31/4152 , A61K31/425 , A61K31/433 , A61K31/4439 , A61K31/54 , A61K31/541 , A61K31/549 , A61K45/06 , C07D275/02 , C07D275/03 , C07D277/04 , C07D279/02 , C07D285/10 , C07D285/16 , C07D285/34 , C07D417/14
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of solving the problem]A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: 本发明提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 [解决问题的方法]式(1)的化合物:(其中n为0〜2; p为0〜4; h为0〜3; j为0〜3; k为0〜2;环B 是芳基或杂芳基; X是O,S或-NR7-; J1是-CR11aR11b-或-NR11c-; J2是-CR12aR12b-或-NR12c-,R1至R12c是特定基团),a 化合物的盐或盐或化合物的溶剂化物。
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公开(公告)号:US20120157459A1
公开(公告)日:2012-06-21
申请号:US13392350
申请日:2010-12-24
IPC分类号: A61K31/4985 , A61K31/425 , C07D417/12 , A61K31/4439 , A61K31/506 , A61K31/427 , C07D417/14 , A61K31/454 , A61K31/4545 , A61K31/40 , A61K31/403 , A61K31/522 , A61K31/496 , A61P3/10 , C07D275/03
CPC分类号: C07D275/03 , A61K9/1623 , A61K9/2018 , A61K9/4858 , C07D417/12 , C07D417/14
摘要: [Problem]To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases.[Means of solving the problem]A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups),a salt of the compound, or a solvate of the salt or the compound.
摘要翻译: [问题]提供具有GPR40激动剂作用的新化合物,化合物的盐,盐或化合物等的溶剂合物作为活性成分的GPR40活化剂,特别是胰岛素促分泌素和 用于预防和/或治疗糖尿病,肥胖或其它疾病的药物。 解决问题的方法式(I)的化合物:(其中n为0〜2; p为0〜4; j为0〜3; k为0〜2,环A为 任选被L取代或被L取代的杂环基;环B是苯环,吡啶环或嘧啶环; X是O,S,-NR7-,R1至R7是特定基团) ,化合物的盐或盐或化合物的溶剂合物。
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