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31. 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。

32. 发明授权

US08003803B2 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：US08003803B2
公开(公告)日：2011-08-23
申请号：US11734057
申请日：2007-04-11
申请人： Yan Xia , Samuel Chackalamannil
发明人： Yan Xia , Samuel Chackalamannil
IPC分类号： C07D263/00 , C07D413/00
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。

33. 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。

34. 发明授权

US07442712B2 Constrained himbacine analogs as thrombin receptor antagonists 有权
标题翻译：约束吗啡类似物作为凝血酶受体拮抗剂
公开(公告)号：US07442712B2
公开(公告)日：2008-10-28
申请号：US11137283
申请日：2005-05-25
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia , Martin C. Clasby , William J. Greenlee , Yuguang Wang , Enrico P. Veltri , Wenxue Wu , Michael P. Graziano , Teddy Kosoglou , Madhu Chintala
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia , Martin C. Clasby , William J. Greenlee , Yuguang Wang , Enrico P. Veltri , Wenxue Wu , Michael P. Graziano , Teddy Kosoglou , Madhu Chintala
IPC分类号： A61K31/44 , C07D409/00
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。

35. 发明申请

US20070232635A1 Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists 有权
标题翻译：可用作凝血酶受体拮抗剂的单环和二环吗啡衍生物
公开(公告)号：US20070232635A1
公开(公告)日：2007-10-04
申请号：US11728672
申请日：2007-03-27
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
IPC分类号： A61K31/44 , C07D213/57 , C07D211/70
CPC分类号： C07D213/24 , C07D213/57 , C07D405/06
摘要： Monocyclic and bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein Gn, Jn, R3, R8, 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：具有下式的单环和二环的烟草衍生物或所述化合物的药学上可接受的盐或溶剂合物，其中表示可选的双键，并且其中G N， R 3，R 3，R 8，R 9，R 10，R 11，本文定义了本文定义的SUP，R 32，B和Het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，心力衰竭和癌症。还声称与其他药剂组合治疗。

36. 发明申请

US20070179187A1 THROMBIN RECEPTOR ANTAGONISTS 有权
标题翻译：硫蛋白受体拮抗剂
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

37. 发明授权

US06897216B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06897216B2
公开(公告)日：2005-05-24
申请号：US10448854
申请日：2003-05-30
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： A61K31/505 , A61K31/519 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - 。 Y是-N（R 2）CH 2 CH 2，N（R 3） - ， - OCH 2， N 2 - （CH 2） - ， - O - ， - S - ， - CH 2 S- ， - （CH 2）2 -NH-或任选取代的m和n为2-3，Q为氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ， - R 0 -OC（O） - ，R 7 -N（R 8）-C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（-NOR 2） - ; 或当Q为CH时，苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8和/或在说明书中定义的它们在治疗帕金森病中的用途，单独使用或与治疗帕金森病的其它药物组合，以及包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

38. 发明授权

US6063847A Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US6063847A
公开(公告)日：2000-05-16
申请号：US197442
申请日：1998-11-23
申请人： Samuel Chackalamannil , Theodros Asberom , Yan Xia , Dario Doller , Martin C. Clasby , Michael F. Czarniecki
发明人： Samuel Chackalamannil , Theodros Asberom , Yan Xia , Dario Doller , Martin C. Clasby , Michael F. Czarniecki
IPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/04 , C07D493/10 , A61K31/44 , A61K31/423 , A61K31/47 , C02D213/60
CPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/04 , C07D493/10
摘要： Heterocyclic-substituted tricyclics of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond;the double dotted line represents an optional single bond;n is 0-2;Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl;Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group;B is --(CH.sub.2).sub.n3 --, wherein n.sub.3 is 0-5, --CH.sub.2 --O--, --CH.sub.2 S--, --CH.sub.2 --NR.sup.6 --, --C(O)NR.sup.6 --. --NR.sup.6 C(O)--, ##STR2## optionally substituted alkenyl or optionally substituted alkynyl; X is --O-- or --NR.sup.6 -- when the double dotted line represents a single bond, or X is --OH or --NHR.sup.20 when the bond is absent;Y is .dbd.O, .dbd.S, (H, H), (H, OH) or (H, C.sub.1 -C.sub.6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is .dbd.O, (H, H), (H, OH), (H, SH) or (H, C.sub.1 -C.sub.6 alkoxy);R.sup.15 is absent when the double dotted line represents a single bond and is H, --NR.sup.18 R.sup.19, or --OR.sup.17 when the bond is absent; or Y is ##STR3## and R.sup.15 is H or C.sub.1 -C.sub.6 alkyl; 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：单个虚线表示任选的双键; 双点划线表示可选的单键; n为0-2; Q是任选取代的环烷基，杂环烷基，芳基或杂芳基; Het是任选取代的单，双或三环杂芳族基团; B是 - （CH 2）n3-，其中n3是0-5，-CH2-O-，-CH2S-，-CH2-NR6-， - C（O）NR6-。 -NR 6 C（O） - ，任选取代的烯基或任选取代的炔基; 当双点划线表示单键时，X是-O-或-NR6-，或者当不存在键时X是-OH或-NHR 20; 当双点划线表示单键时，Y为= O，= S，（H，H），（H，OH）或（H，C 1 -C 6烷氧基），或当不存在键时，Y为= （H，H），（H，OH），（H，SH）或（H，C 1 -C 6烷氧基）; 当双重虚线表示单键并且当不存在键时，R 15不存在且为H，-NR 18 R 19或-OR 17; 或Y为R 15为H或C 1 -C 6烷基; 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。

39. 发明授权

US08987242B2 Morpholinone compounds as factor IXA inhibitors 有权
标题翻译：吗啉酮化合物作为因子IXA抑制剂
公开(公告)号：US08987242B2
公开(公告)日：2015-03-24
申请号：US12791464
申请日：2010-06-01
申请人： Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Tomokazu Hirabayashi , Santhosh Neelamkavil , Hidemitsu Nishida , Fumihiko Saitoh , Unmesh Shah , Yan Xia
发明人： Samuel Chackalamannil , Tin-Yau Chan , Mariappan V. Chelliah , Martin C. Clasby , Michael Dwyer , William J. Greenlee , Tomokazu Hirabayashi , Santhosh Neelamkavil , Hidemitsu Nishida , Fumihiko Saitoh , Unmesh Shah , Yan Xia
IPC分类号： A61K31/535 , A01N43/00 , A61K31/33 , C07D413/12 , A61K31/397 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/7088 , A61K39/395 , A61K45/06 , C07D265/32 , C07D413/10 , C07D413/14 , C07D417/10
CPC分类号： C07D413/12 , A61K31/397 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/7088 , A61K39/395 , A61K45/06 , C07D265/32 , C07D413/10 , C07D413/14 , C07D417/10 , A61K2300/00
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.
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或溶剂合物。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，高凝状态或纤维化改变的方法。

40. 发明授权

US08642582B2 Morpholinone compounds as factor IXa inhibitors 有权
标题翻译：吗啉酮化合物作为因子IXa抑制剂
公开(公告)号：US08642582B2
公开(公告)日：2014-02-04
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： A61K31/535
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.
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或溶剂合物。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，高凝状态或纤维化改变的方法。

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