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1.
公开(公告)号:US20080090830A1
公开(公告)日:2008-04-17
申请号:US11865793
申请日:2007-10-02
IPC分类号: A61K31/4427 , A61K31/435 , A61K31/443 , A61K31/4439 , A61K31/502 , A61P1/00 , A61P11/00 , A61P15/00 , A61P17/00 , A61P35/00 , A61P9/00 , C07D221/06 , C07D401/06 , C07D413/02 , C07D487/00
CPC分类号: C07D401/06 , C07D417/06
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bonds the dotted line is optionally a bond or no bonds resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failures and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 异构体或外消旋混合物的下式的杂环取代三环或其药学上可接受的盐或溶剂合物,其中表示可选的双键,虚线可选地是一个键或没有导致双键或单键的键,如允许 通过化合价要求,其中E,A,GM,Het,B,X,R 3,R 10,R 11, 本文定义了SUP 32和33 SS,其余取代基如说明书中所定义,以及含有它们的药物组合物和治疗与血栓形成有关的疾病的方法 ,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心脏衰竭和癌症。 还要求与其它心血管药物联合治疗。
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公开(公告)号:US20070270439A1
公开(公告)日:2007-11-22
申请号:US11774358
申请日:2007-07-06
申请人: Samuel Chackalamannil , Martin Clasby , William Greenlee , Yuguang Wang , Yan Xia , Enrico Veltri , Mariappan Chelliah
发明人: Samuel Chackalamannil , Martin Clasby , William Greenlee , Yuguang Wang , Yan Xia , Enrico Veltri , Mariappan Chelliah
IPC分类号: A61K31/4427 , A61K31/506 , A61P29/00 , A61P35/00 , A61P9/00 , A61P9/02 , A61P9/06 , A61P9/10 , A61P9/12 , C07D221/00 , C07D239/26
CPC分类号: C07D405/06 , C07D405/14 , C07D417/14
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 具有下式的杂环取代的三环或其药学上可接受的盐,其中:虚线表示任选的单键; “img id =”custom-character-00001“he =”2.79mm“wi =”7.03mm“file =”US20070270439A1-20071122-P00002.TIF“img-content =”character“img-format =”tif“/> 表示可选的双键; n为0-2; Q是环烷基,任选被R 13和R 14取代; R 13和R 14独立地选自(C 1 -C 6 -C 6)烷基,(C
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公开(公告)号:US20070179187A1
公开(公告)日:2007-08-02
申请号:US11733635
申请日:2007-04-10
申请人: Samuel Chackalamannil , Martin Clasby , William Greenlee , Yuguang Wang , Yan Xia , Enrico Veltri , Mariappan Chelliah
发明人: Samuel Chackalamannil , Martin Clasby , William Greenlee , Yuguang Wang , Yan Xia , Enrico Veltri , Mariappan Chelliah
IPC分类号: A61K31/4433 , C07D405/02
CPC分类号: C07D405/06 , C07D405/14 , C07D417/14
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 具有下式的杂环取代的三环或其药学上可接受的盐,其中:虚线表示任选的单键; “img id =”custom-character-00001“he =”3.13mm“wi =”7.37mm“file =”US20070179187A1-20070802-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示可选的双键,n为0-2; Q是环烷基,任选被R 13和R 14取代; R 13和R 14独立地选自(C 1 -C 6 -C 6)烷基,(C
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公开(公告)号:US20070197628A1
公开(公告)日:2007-08-23
申请号:US11653558
申请日:2007-01-16
申请人: Samuel Chackalamannil , Mariappan Chelliah , Martin Clasby , Keith Eagen , Jack Scott , Yuguang Wang , Yan Xia , William Greenlee
发明人: Samuel Chackalamannil , Mariappan Chelliah , Martin Clasby , Keith Eagen , Jack Scott , Yuguang Wang , Yan Xia , William Greenlee
IPC分类号: A61K31/4035 , C07D209/46
CPC分类号: C07D209/46 , C07C233/31 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/90 , C07D209/44 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
摘要翻译: 具有式(I)的通式结构的化合物或其药学上可接受的盐,溶剂化物或酯可用于治疗疾病,病症或病症如肥胖,代谢紊乱,成瘾,中枢神经系统疾病, 心血管疾病,呼吸系统疾病和胃肠道疾病。
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公开(公告)号:US20050267155A1
公开(公告)日:2005-12-01
申请号:US11137283
申请日:2005-05-25
申请人: Mariappan Chelliah , Samuel Chackalamannil , Yan Xia , Martin Clasby , William Greenlee , Yuguang Wang , Enrico Veltri , Wenxue Wu , Michael Graziano , Teddy Kosoglou , Madhu Chintala
发明人: Mariappan Chelliah , Samuel Chackalamannil , Yan Xia , Martin Clasby , William Greenlee , Yuguang Wang , Enrico Veltri , Wenxue Wu , Michael Graziano , Teddy Kosoglou , Madhu Chintala
IPC分类号: A61K31/443 , A61K31/4433 , A61P9/00 , A61P11/00 , A61P25/28 , C07D405/06 , C07D405/08 , C07D493/04 , C07D45/02
CPC分类号: C07D493/04 , C07D405/06
摘要: A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is —O— or —NR6— when the double-dashed line represents a single bond; X is H, —OH or —NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译: 公开了由结构式表示的化合物及其药学上可接受的盐和溶剂,其中:R 10和R 34之间的环碳之间的单点划线是 附表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或不存在键; 当双点划线表示单键时,X是-O-或-NR 6 - 当双点划线表示不存在的键时,X是H,-OH或-NHR 20; 和其他参数如本文所定义。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体的结合物的药物组合物和组合。
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公开(公告)号:US20060223808A1
公开(公告)日:2006-10-05
申请号:US11392324
申请日:2006-03-29
IPC分类号: A61K31/4747 , A61K31/502 , C07D413/02
CPC分类号: C07D263/52 , C07D413/08
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, En, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 异构体或外消旋混合物的下式的杂环取代三环或其药学上可接受的盐或溶剂化物,其中表示可选的双键,虚线是可选的键或无键,导致双重 债券或单一债券,如价格要求所允许的,并且其中A N,N,N,N, N,N,N,N,R 9,R 10, 在本文中定义,其余取代基如本说明书中所定义,其中R 11,R 32,R 32和/ ,以及含有它们的药物组合物和治疗与血栓形成,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心力衰竭, 和癌症。 还要求与其它心血管药物联合治疗。
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公开(公告)号:US20060079684A1
公开(公告)日:2006-04-13
申请号:US11243708
申请日:2005-10-05
IPC分类号: C07D413/02 , C07D405/02
CPC分类号: C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/10
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein A, B, G, M, X, J, n, Het, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 式中的杂环取代三环或所述化合物,异构体或外消旋混合物的药学上可接受的盐或溶剂化物,其中表示可选的双键,虚线是可选的键或无键,导致双重 键或单键,如价格要求所允许的,并且其中A,B,G,M,X,J,n,Het,R 3,R 10, 本文定义了R 11,R 32和R 33,并且其余的取代基如说明书中所定义,以及药物 含有它们的组合物和通过施用所述化合物治疗与血栓形成,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心力衰竭和癌症相关的疾病的方法。 还要求与其它心血管药物联合治疗。
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8.
公开(公告)号:US08153664B2
公开(公告)日:2012-04-10
申请号:US11865793
申请日:2007-10-02
IPC分类号: C07D401/06 , A61K31/4439 , A61P7/02 , A61P7/12 , A61P9/10 , A61P29/00 , A61P19/02 , A61P3/10 , A61P3/14 , A61P11/06 , A61P11/08
CPC分类号: C07D401/06 , C07D417/06
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 所述式的杂环取代三环或所述化合物,异构体或外消旋混合物的药学上可接受的盐或溶剂合物,其中代表任选的双键,虚线任选是键或无键,导致双键或单键, 如价格要求所允许的,其中E,A,GM,Het,B,X,R 3,R 10,R 11,R 32和R 33在本文中定义,其余取代基如说明书中所定义,以及药物 含有它们的组合物和通过施用所述化合物治疗与血栓形成,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心力衰竭和癌症相关的疾病的方法。 还要求与其它心血管药物联合治疗。
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公开(公告)号:US07304078B2
公开(公告)日:2007-12-04
申请号:US10412982
申请日:2003-04-14
申请人: Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
发明人: Samuel Chackalamannil , William J. Greenlee , Yuguang Wang , Wenxue Wu , Enrico P. Veltri , Yan Xia
IPC分类号: A61K31/443 , C07D405/02
CPC分类号: C07D405/06 , C07D405/14 , C07D417/14
摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0–2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1–C6)alkyl, (C3–C8)cycloalkyl, —OH, (C1–C6)alkoxy, R27-aryl(C1–C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3–6 atoms; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译: 式中的杂环取代三环
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公开(公告)号:US07897601B2
公开(公告)日:2011-03-01
申请号:US11653558
申请日:2007-01-16
申请人: Samuel Chackalamannil , Mariappan V. Chelliah , Martin C. Clasby , Keith A. Eagen , Jack D. Scott , Yuguang Wang , Yan Xia , William J. Greenlee
发明人: Samuel Chackalamannil , Mariappan V. Chelliah , Martin C. Clasby , Keith A. Eagen , Jack D. Scott , Yuguang Wang , Yan Xia , William J. Greenlee
IPC分类号: A61K31/454 , A61K31/4035 , A61K31/5377 , C07D209/46 , C07D295/04 , C07D401/04
CPC分类号: C07D209/46 , C07C233/31 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/90 , C07D209/44 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
摘要翻译: 具有式(I)的通式结构的化合物或其药学上可接受的盐,溶剂化物或酯可用于治疗疾病,病症或病症如肥胖,代谢紊乱,成瘾,中枢神经系统疾病, 心血管疾病,呼吸系统疾病和胃肠道疾病。
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