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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.

3. 发明授权

US08148363B2 Heterocyclic compounds as factor IXA inhibitors 有权
标题翻译：杂环化合物作为因子IXA抑制剂
公开(公告)号：US08148363B2
公开(公告)日：2012-04-03
申请号：US12993607
申请日：2009-05-18
申请人： Martin C. Clasby , William J. Greenlee , Yan Xia , Tin-Yau Chan , Mariappan V. Chelliah , Samuel Chackalamannil , Haiyan Pu , Keith A. Eagen , Henry Vaccaro , Brian A. McKittrick , Liyuan Wang , Xiaobang Gao
发明人： Martin C. Clasby , William J. Greenlee , Yan Xia , Tin-Yau Chan , Mariappan V. Chelliah , Samuel Chackalamannil , Haiyan Pu , Keith A. Eagen , Henry Vaccaro , Brian A. McKittrick , Liyuan Wang , Xiaobang Gao
IPC分类号： A61K31/55 , A61K31/4184 , A61K31/5377 , A61K31/4192 , A61K31/454 , A61K31/4439 , A61K31/422 , A61K31/506 , A61K31/496 , A61P7/02 , C07D403/14 , C07D413/14 , C07D403/04 , C07D401/14
CPC分类号： C07D487/04 , C07D231/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel heterocyclic compounds of Formulae I-III; 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-III的新型杂环化合物; 如本文所公开的或其药学上可接受的盐，溶剂化物，酯，前药或立体异构体。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。

4. 发明授权

US07897601B2 Cannabinoid receptor modulators 失效
标题翻译：大麻素受体调节剂
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。

5. 发明授权

US06326380B1 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US06326380B1
公开(公告)日：2001-12-04
申请号：US09545720
申请日：2000-04-07
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： A61K3147
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 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 —(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 —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, (H, H), (H, OH), (H, SH) or (H, C1-C6 alkoxy); R15 is absent when the double dotted line represents a single bond and is H, —NR18R19, or —OR17 when the bond is absent; or Y is or and R15 is H or C1-C6 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：式2的杂环取代的三环或其药学上可接受的盐，其中：单点线表示任选的双键;双点划线表示任选的单键; n为0-2; Q为任选取代的环烷基，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）NR 6 - ，-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为-O-或-NR6-，或X为-OH或-NHR20 当双键虚线表示单键时，当不存在键时，Y为= O，= S，（H，H），（H，OH）或（H，C 1 -C 6烷氧基），Y为= O，（H，H），（H，OH），（H，SH）或（H，C1-C6烷氧基）;当双点表示单键且为H时， NR18R19或-OR17，当该键不存在时; 或Y为或R 15为H或C 1 -C 6烷基;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，心力衰竭和癌症相关的疾病的方法通过施用所述化合物。

6. 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。

7. 发明申请

US20110135650A1 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：US20110135650A1
公开(公告)日：2011-06-09
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： A61K39/395 , C07D413/12 , A61K31/5377 , C07D295/10 , A61K31/5375 , C07D413/10 , C07D413/14 , C07D413/04 , C07D401/12 , A61K31/496 , C07D279/12 , A61K31/54 , A61K31/397 , A61K31/7088 , A61P7/02 , A61P9/00
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。

8. 发明授权

US07741318B2 Pyrazolo [1,5-A]pyrimidine adenosine A2a receptor antagonists 有权
标题翻译：吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US07741318B2
公开(公告)日：2010-06-22
申请号：US11311195
申请日：2005-12-19
申请人： Martin C. Clasby , Samuel Chackalamannil , Bernard R. Neustadt , Xiaobang Gao
发明人： Martin C. Clasby , Samuel Chackalamannil , Bernard R. Neustadt , Xiaobang Gao
IPC分类号： C07D243/08 , C07D295/02 , C07D295/16 , C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/497 , A61K31/5513 , A61P25/16
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 - ; R1是烷基或环烷基; R2是氢，卤素或-CN; R3是氢或烷基; R4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基取代的杂环烷基，任选取代的芳基烷基或任选取代的杂芳基烷基; 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。

9. 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。

10. 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。

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