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1. 发明授权

US08609676B2 4, 5, 6-trisubstituted pyrimidine derivatives as factor IXa inhibitors 有权
标题翻译： 4,5,6,6-三取代嘧啶衍生物作为因子IXa抑制剂
公开(公告)号：US08609676B2
公开(公告)日：2013-12-17
申请号：US13388628
申请日：2010-08-03
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , William J. Greenlee , Keith Eagan , Zhuyan Guo , Martin C. Clasby , Yan Xia , Charles L. Jayne , Michael Dwyer , Kartik M. Keertikar , Tin-Yau Chan , Li Wang
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , William J. Greenlee , Keith Eagan , Zhuyan Guo , Martin C. Clasby , Yan Xia , Charles L. Jayne , Michael Dwyer , Kartik M. Keertikar , Tin-Yau Chan , Li Wang
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
摘要翻译：本发明涉及式（I）的新型杂环化合物：（化学式应在此插入，如本文摘要中所示）本文公开的式（I），或其药学上可接受的盐，溶剂合物，酯，前药或其立体异构体。还公开了包含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栓塞性疾病的方法。

2. 发明授权

US08153664B2 Bicyclic and tricyclic derivatives as thrombin receptor antagonists 有权
标题翻译：双环和三环衍生物作为凝血酶受体拮抗剂
公开(公告)号：US08153664B2
公开(公告)日：2012-04-10
申请号：US11865793
申请日：2007-10-02
申请人： Samuel Chackalamannil , Mariappan V. Chelliah , Yuguang Wang , Yan Xia
发明人： Samuel Chackalamannil , Mariappan V. Chelliah , Yuguang Wang , Yan Xia
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。

3. 发明申请

US20110301112A1 FUSED RING THROMBIN RECEPTOR ANTAGONISTS 有权
标题翻译：融合环硫蛋白受体拮抗剂
公开(公告)号：US20110301112A1
公开(公告)日：2011-12-08
申请号：US13188520
申请日：2011-07-22
申请人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
发明人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
IPC分类号： A61K31/4439 , A61K31/7076 , A61K31/4365 , A61K31/727 , A61P7/02 , A61P9/10 , A61P9/12 , A61P9/06 , A61P9/04 , A61P7/04 , A61P25/06 , A61P15/10 , A61P29/00 , A61P1/16 , A61P13/12 , A61P11/00 , A61P1/00 , A61P19/04 , A61P25/00 , A61P19/10 , A61P13/10 , A61P3/10 , A61P35/00 , A61P25/28 , A61P11/06 , A61P27/06 , A61P27/02 , A61P17/06 , A61P1/02 , A61P7/10 , C07D413/14
CPC分类号： C07D405/06 , C07D498/04
摘要： Fused-ring, 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, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, 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：具有下式的稠环，杂环取代的三环或所述化合物的药学上可接受的盐或溶剂合物，异构体或外消旋混合物，其中表示任选的双键，并且其中An，En，Mn，Gn，Jn，R 3，n 7，R 8 本文定义了R9，R10，R11，R32，R33，X，Y，B和Het，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以及治疗与血栓形成，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。

4. 发明授权

US08022088B2 Substituted bicyclic and tricyclic thrombin receptor antagonists 有权
标题翻译：取代的双环和三环凝血酶受体拮抗剂
公开(公告)号：US08022088B2
公开(公告)日：2011-09-20
申请号：US11769018
申请日：2007-06-27
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
IPC分类号： A01N43/40 , A61K31/44 , C07D405/00
CPC分类号： C07D405/06
摘要： Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined 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 agents is also claimed.
摘要翻译：其中代表任选的双键的取代的双环和三环修饰的烟草衍生物，或其药学上可接受的盐或溶剂化物，其中En，Fn，Gn，Zn，Jn，X，R3，R9，R10，R11，R32 本文定义的R33，B和Het以及含有它们的药物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。还声称与其他药剂组合治疗。

5. 发明申请

US20110059958A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 有权
公开(公告)号：US20110059958A1
公开(公告)日：2011-03-10
申请号：US12744736
申请日：2009-12-03
申请人： Hidemitsu Nishida , Fumihiko Saitoh , Tomokazu Hirabayashi , Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Yan Xia
发明人： Hidemitsu Nishida , Fumihiko Saitoh , Tomokazu Hirabayashi , Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Yan Xia
IPC分类号： A61K31/5377 , C07D413/12 , A61P7/02 , A61P9/10 , A61P9/12 , C07D265/32 , C07D413/10
CPC分类号： C07D401/12 , C07D265/30 , C07D265/32 , C07D267/10 , C07D279/06 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate 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.

6. 发明申请

US20070244163A1 Fused Ring Thrombin Receptor Antagonists 有权
标题翻译：融合环凝血酶受体拮抗剂
公开(公告)号：US20070244163A1
公开(公告)日：2007-10-18
申请号：US11734057
申请日：2007-04-11
申请人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
发明人： Yan Xia , Mariappan V. Chelliah , Samuel Chackalamannil
IPC分类号： A61K31/4439 , C07D491/02
CPC分类号： C07D405/06 , C07D498/04
摘要： Fused-ring, 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, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, 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：熔融环，具有下式的杂环取代的三环或所述化合物的药学上可接受的盐或溶剂合物，异构体或外消旋混合物，其中表示可选的双键，并且其中A N，N， M，N，N，N，N，N，N，N，N， R 8，R 9，R 10，R 11，R 32，R 12，本文中定义了R32，X，Y，B和Het，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。还要求与其它心血管药物联合治疗。

7. 发明授权

US06894065B2 Thrombin receptor antagonists 有权
公开(公告)号：US06894065B2
公开(公告)日：2005-05-17
申请号：US10457256
申请日：2003-06-09
申请人： Samuel Chackalamannil , Mariappan V. Chelliah , Yan Xia
发明人： Samuel Chackalamannil , Mariappan V. Chelliah , Yan Xia
IPC分类号： A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/497 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D521/00 , A61K31/4427 , C07D215/00 , C07D237/02
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： Heterocyclic-substituted compounds of the formula or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is —(CH2)n—; wherein R10 is absent; or wherein R3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—, optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is H, —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, ═NOR17, (H, H), (H, OH), (H, SH), (H, C1-C6 alkoxy) or (H, substituted-amino); R22 and R23 are independently —OH, —OC(O)R30, OC(O)NR30R31, or optionally substituted alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl, cycloalkyl, cycloalkenyl, carbonyl, amino, alkoxy, alkenyloxy, alkynyloxy, heterocycloalkyloxy, cycloalkyloxy, or cycloalkenyloxy; or R22 and R10, or R23 and R11, can form a carbocyclic or heterocyclic ring; and the remaining variables are as described in the specification. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.

8. 发明申请

US20120157403A1 BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为血红蛋白受体拮抗剂的双相和三环衍生物
公开(公告)号：US20120157403A1
公开(公告)日：2012-06-21
申请号：US13404462
申请日：2012-02-24
申请人： Samuel Chackalamannil , Mariappan V. Chelliah , Yuguang Wang , Yan Xia
发明人： Samuel Chackalamannil , Mariappan V. Chelliah , Yuguang Wang , Yan Xia
IPC分类号： A61K31/7076 , C07D401/08 , C07D417/08 , C07D413/08 , C07D409/08 , A61K31/4439 , A61K31/443 , A61K31/5025 , A61K31/4436 , A61K31/473 , A61K31/517 , A61K31/498 , A61K31/4725 , A61K31/4709 , A61K31/616 , A61K31/4365 , A61K31/727 , A61P7/02 , A61P9/10 , A61P9/12 , A61P9/00 , A61P9/06 , A61P9/04 , A61P13/12 , A61P15/00 , A61P29/00 , A61P1/16 , A61P11/00 , A61P1/00 , A61P37/06 , A61P25/00 , A61P19/10 , A61P13/10 , A61P3/10 , A61P35/00 , A61P25/28 , A61P27/06 , A61P11/06 , A61P27/02 , A61P17/06 , A61P1/02 , C07D405/08
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。

9. 发明申请

US20120136016A1 4, 5, 6-TRISUBSTITUTED PYRIMIDINE DERIVATIVES AS FACTOR IXA INHIBITORS 有权
标题翻译：作为因子IXA抑制剂的4,5,6-取代的吡嗪衍生物
公开(公告)号：US20120136016A1
公开(公告)日：2012-05-31
申请号：US13388628
申请日：2010-08-03
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , William J. Greenlee , Keith Eagen , Zhuyan Guo , Martin C. Clasby , Yan Xia , Charles L. Jayne , Michael Dwyer , Kartick M. Keertikar , Tin-Yau Chan , Li Wang
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , William J. Greenlee , Keith Eagen , Zhuyan Guo , Martin C. Clasby , Yan Xia , Charles L. Jayne , Michael Dwyer , Kartick M. Keertikar , Tin-Yau Chan , Li Wang
IPC分类号： A61K31/505 , C07D403/04 , A61P7/02 , C07D403/12 , C07D401/12 , C07D239/47 , C07D239/60
CPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
摘要翻译：本发明涉及式（I）的新型杂环化合物：（化学式应在此插入，如本文摘要中所示）本文公开的式（I），或其药学上可接受的盐，溶剂合物，酯，前药或其立体异构体。还公开了包含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栓塞性疾病的方法。

10. 发明申请

US20090069383A1 Thrombin Receptor Antagonists 审中-公开
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US20090069383A1
公开(公告)日：2009-03-12
申请号：US12261545
申请日：2008-10-30
申请人： Samuel Chackalamannil , Mariappan V. Chelliah , Yan Xia
发明人： Samuel Chackalamannil , Mariappan V. Chelliah , Yan Xia
IPC分类号： A61K31/443 , C07D405/06 , A61P7/00 , A61P9/00 , A61P35/00 , A61P29/00 , A61P11/00
CPC分类号： C07D417/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14
摘要： A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译：公开了一系列由结构式表示的化合物及其药学上可接受的异构体，盐，溶剂化物和多晶型物。还公开了含有所述化合物的药物组合物及其作为大麻素受体的凝血酶受体拮抗剂和粘合剂的用途。

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