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1. 发明授权

US5889006A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US5889006A
公开(公告)日：1999-03-30
申请号：US700628
申请日：1996-08-08
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W. Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02 , C07D403/02 , C07D403/14
CPC分类号： C07D405/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物）其中R，R 1，R 2，R 3，R 4，R 21，R 27 R28，X，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱性拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

2. 发明授权

US6043255A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US6043255A
公开(公告)日：2000-03-28
申请号：US266079
申请日：1999-03-10
申请人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
发明人： Derek B. Lowe , Wei K. Chang , Joseph A. Kozlowski , Joel G. Berger , Robert McQuade , Allen Barnett , Margaret Sherlock , Wing Tom , Sundeep Dugar , Lian-Yong Chen , John W Clader , Samuel Chackalamannil , Yuguang Wang , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice , Wayne Vaccaro , Michael J. Green , Margaret E. Browne , Theodros Asberom , Craig D. Boyle
IPC分类号： C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/02
CPC分类号： C07D405/14 , C07D211/24 , C07D211/32 , C07D239/34 , C07D257/04 , C07D295/03 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D405/12 , C07D409/14 , C07C2101/14
摘要： Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和制备方法。还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

3. 发明授权

US06969719B2 Polycyclic guanine phosphodiesterase V inhibitors 失效
标题翻译：多环鸟嘌呤磷酸二酯酶V抑制剂
公开(公告)号：US06969719B2
公开(公告)日：2005-11-29
申请号：US10227778
申请日：2002-08-26
申请人： Theodros Asberom , Yueqing Hu , Dmitri Pissarnitski , Ruo Xu , Yuguang Wang , Samuel Chackalamannil , John W. Clader , Andrew William Stamford
发明人： Theodros Asberom , Yueqing Hu , Dmitri Pissarnitski , Ruo Xu , Yuguang Wang , Samuel Chackalamannil , John W. Clader , Andrew William Stamford
IPC分类号： A61K31/519 , A61K45/00 , A61P1/04 , A61P1/14 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/28 , A61P27/06 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/14 , C07D487/20 , A61K31/527
CPC分类号： C07D487/14
摘要： A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological disorders: A representative example is:
摘要翻译：具有式（I.1）或（II.1）的多环鸟嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其可用于治疗性功能障碍和其他生理障碍：代表性的例子是：

4. 发明授权

US5977138A Ether muscarinic antagonists 失效
标题翻译：醚类毒蕈碱拮抗剂
公开(公告)号：US5977138A
公开(公告)日：1999-11-02
申请号：US910616
申请日：1997-08-13
申请人： Yuguang Wang , Wei K. Chang , Sundeep Dugar , Samuel Chackalamannil
发明人： Yuguang Wang , Wei K. Chang , Sundeep Dugar , Samuel Chackalamannil
IPC分类号： A61K45/06 , C07D211/46 , C07D211/96 , C07D405/12 , C07D405/14 , C07D409/14 , A61K31/445 , C07D401/04
CPC分类号： C07D405/12 , A61K45/06 , C07D211/46 , C07D211/96 , C07D405/14 , C07D409/14
摘要： 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or an isomer, pharmaceutically acceptable salt, ester or solvate thereof, whereinX is a bond, --O--, --S--, --SO--, --SO.sub.2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O-- CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 -C.sub.6 alkyl)-, --C(C.sub.1 -C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --O--C(O)NR.sup.17 --, --NR.sup.17 C(O)--O--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --;R is cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl;R.sup.2 is H, alkyl, optionally substituted cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted piperidinyl; and the remaining variables are as defined in the specification, are disclosed. Compounds of formula I are useful for treating cognitive disorders such as Alzheimer's disease. Also disclosed are pharmaceutical compositions, methods of preparation and combinations of compounds of formula I with ACh'ase inhibitors.
摘要翻译： 1,4-二取代的式I的哌啶毒蕈碱拮抗剂或其异构体，药学上可接受的盐，酯或溶剂化物，其中X是键，-O - ， - S - ， - SO - ， - SO 2 - ， - ，-C（OR 7）2 - ， - CH 2 -O - ， - CH 2 - ， - CH = CH - ， - CH 2 - ， - CH（C 1 -C 6烷基） - ， - CONR 17 - ， - NR 17 CO - ， - OC（O）NR 17 - ， - NR 17 C（O）-O-，-SO 2 NR 17 - 或-NR 17 SO 2 - R是环烷基，任选取代的苯基或任选取代的吡啶基; R2是H，烷基，任选取代的环烷基，环烯基，叔丁氧羰基或任选取代的哌啶基; 并且其余变量如说明书中所定义。式I化合物可用于治疗认知障碍如阿尔茨海默病。还公开了药物组合物，制备方法和式I化合物与ACh酶抑制剂的组合。

5. 发明授权

US07531544B2 Xanthine phosphodiesterase V inhibitors 失效
公开(公告)号：US07531544B2
公开(公告)日：2009-05-12
申请号：US11852638
申请日：2007-09-10
申请人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
IPC分类号： A61K31/522 , A61P9/12 , A61P15/10 , C07D473/04 , C07D473/06 , C07D473/08
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:

6. 发明授权

US06821978B2 Xanthine phosphodiesterase V inhibitors 失效
标题翻译：黄嘌呤磷酸二酯酶V抑制剂
公开(公告)号：US06821978B2
公开(公告)日：2004-11-23
申请号：US09940760
申请日：2001-08-28
申请人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig D. Boyle , Andrew W. Stamford
IPC分类号： A61K31505
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:
摘要翻译：具有式（I）的黄嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其特别用于治疗男性（勃起）和女性性功能障碍等生理障碍：例如，本发明的代表性化合物是：

7. 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。

8. 发明授权

US07888369B2 Oxazoloisoquinoline derivatives as thrombin receptor antagonists 有权
标题翻译：恶唑啉异喹啉衍生物作为凝血酶受体拮抗剂
公开(公告)号：US07888369B2
公开(公告)日：2011-02-15
申请号：US11642170
申请日：2006-12-20
申请人： Samuel Chackalamannil , Yuguang Wang
发明人： Samuel Chackalamannil , Yuguang Wang
IPC分类号： C07D491/14 , A61K31/4355 , A61P7/02 , A61P9/10 , A61P9/12 , A61P9/06 , A61P9/00 , A61P9/02
CPC分类号： C07D487/04 , C07D471/04
摘要： This application provides for oxazolisoquinoline derivatives of the formula or a pharmaceutically acceptable salt of said compound wherein: B is —CH═CH—; M is —C(R1)(R2)—; and the remaining substituents are as defined in the specification 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. This application also provides for combination therapy with the compounds of Ib or pharmaceutically acceptable salts thereof with other cardiovascular agents.
摘要翻译：本申请提供了下式的恶唑啉喹啉衍生物或所述化合物的药学上可接受的盐，其中：B是-CH = CH-; M是-C（R 1）（R 2） - ; 并且其余的取代基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。本申请还提供了将Ib化合物或其药学上可接受的盐与其它心血管药物组合治疗。

9. 发明申请

US20080090830A1 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：US20080090830A1
公开(公告)日：2008-04-17
申请号：US11865793
申请日：2007-10-02
申请人： Samuel Chackalamannil , Mariappan Chelliah , Yuguang Wang , Yan Xia
发明人： Samuel Chackalamannil , Mariappan Chelliah , Yuguang Wang , Yan Xia
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。

10. 发明授权

US07304078B2 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
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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