公开(公告)号：US20060106050A1

公开(公告)日：2006-05-18

申请号：US11311083

申请日：2005-12-19

申请人： Samuel Chakalamannil ,  Mariappan Chelliah ,  Martin Clasby ,  Yan Xia

发明人： Samuel Chakalamannil ,  Mariappan Chelliah ,  Martin Clasby ,  Yan Xia

IPC分类号： A61K31/4741 ,  C07D491/02

CPC分类号： C07D491/04 ,  C07D493/04 ,  C07D495/04

摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is —COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or —COOH and/or —SO3H substituted alkyl; R1, R2, R3, R9, R10 and R11 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.

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：n 1和n 2个独立地为0-2; Het是任选取代的单，双或三环杂芳族基团; B是烷基或任选取代的烯基; R 22是-COR 23或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R 23是卤代烷基; 烯基; 卤代烯基 炔基; 任选取代的环烷基 环烷基 - 烷基; 芳基; 芳烷基 杂芳基; 杂环烷基; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 9， R 11如本说明书中所定义; 以及含有它们的药物组合物以及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。

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

公开(公告)号：US20140057836A1

公开(公告)日：2014-02-27

申请号：US13960343

申请日：2013-08-06

申请人： Thomas BARA ,  Sathesh Bhat ,  Dipshika Biswas ,  Linda Brockunier ,  Duane Burnette ,  Samuel Chackalamannil ,  Mariappan Vasu Cheliah ,  Austin Chen ,  Martin Clasby ,  Vince J. Colandrea ,  Zhuyan Guo ,  Yongxin Han ,  Charles Jayne ,  Hubert Josien ,  Karen Marcantonio ,  Shouwu Miao ,  Santhosh Neelamkavil ,  Patrick Pinto ,  Murali Rajogopalan ,  Unmesh Shah ,  Francisco Velazquez ,  Srikanth Venkatraman ,  Yan Xia

发明人： Thomas BARA ,  Sathesh Bhat ,  Dipshika Biswas ,  Linda Brockunier ,  Duane Burnette ,  Samuel Chackalamannil ,  Mariappan Vasu Cheliah ,  Austin Chen ,  Martin Clasby ,  Vince J. Colandrea ,  Zhuyan Guo ,  Yongxin Han ,  Charles Jayne ,  Hubert Josien ,  Karen Marcantonio ,  Shouwu Miao ,  Santhosh Neelamkavil ,  Patrick Pinto ,  Murali Rajogopalan ,  Unmesh Shah ,  Francisco Velazquez ,  Srikanth Venkatraman ,  Yan Xia

IPC分类号： C07K5/08 ,  A61K45/06 ,  A61K38/06

CPC分类号： C07K5/08 ,  A61K38/06 ,  A61K45/06 ,  C07D419/00 ,  C07D491/22

摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

摘要翻译： 本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

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

公开(公告)号：US20060135526A1

公开(公告)日：2006-06-22

申请号：US11311195

申请日：2005-12-19

申请人： Martin Clasby ,  Samuel Chackalamannil ,  Bernard Neustadt ,  Xiaobang Gao

发明人： Martin Clasby ,  Samuel Chackalamannil ,  Bernard Neustadt ,  Xiaobang Gao

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

摘要翻译： 公开了具有结构式I的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - 。 R 1是烷基或环烷基; R 2是氢，卤素或-CN; R 3是氢或烷基; R 4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基，任选取代的芳基烷基或任选取代的杂芳基烷基取代的杂环烷基; 或R 3和R 4，形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。 还公开了化合物在治疗帕金森病中的用途，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合组分的试剂盒的用途。

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。

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。