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1. 发明申请

US20130102605A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：US20130102605A1
公开(公告)日：2013-04-25
申请号：US13642958
申请日：2011-04-21
申请人： Peng Liang , Morihiro Mitsuya , Yoshio Ogino , Changhe Qi , Hidekazu Takahashi , Paul Tempest , Jiabing Wang , Yuguang Wang , Zhenzhen Wang , Shaohua Zhang , Nanyan Zhou , Jiuxiang Zhu
发明人： Peng Liang , Morihiro Mitsuya , Yoshio Ogino , Changhe Qi , Hidekazu Takahashi , Paul Tempest , Jiabing Wang , Yuguang Wang , Zhenzhen Wang , Shaohua Zhang , Nanyan Zhou , Jiuxiang Zhu
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14 , C07D487/08
摘要： The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的噻唑。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

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。

4. 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。

5. 发明授权

US07713999B2 Thrombin receptor antagonists 有权
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US07713999B2
公开(公告)日：2010-05-11
申请号：US11733635
申请日：2007-04-10
申请人： Samuel Chackalamannil , Martin C. Clasby , William J. Greenlee , Yuguang Wang , Yan Xia , Enrico P. Veltri , Mariappan V. Chelliah
发明人： Samuel Chackalamannil , Martin C. Clasby , William J. Greenlee , Yuguang Wang , Yan Xia , Enrico P. Veltri , Mariappan V. Chelliah
IPC分类号： A61K31/443 , C07D307/78
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; 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）烷基，（C 3 -C 8）环烷基，-OH，（C 1 -C 6）烷氧基，R 27 - 芳基（C 1 -C 6）烷基，杂芳基，杂芳基烷基，杂环基，杂环基烷基，卤素和卤代烷基; 或R 13和R 14一起形成3-6个原子的螺环或异环环，Het是单或双环任选取代的杂芳基; 和B是键，亚烷基或任选取代的亚烯基或亚炔基，其中剩余的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，动脉粥样硬化，再狭窄有关的疾病的方法，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。

6. 发明申请

US20070254952A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20070254952A1
公开(公告)日：2007-11-01
申请号：US11736722
申请日：2007-04-18
申请人： Yuguang Wang , Samuel Chackalamannil , Yuriko Root
发明人： Yuguang Wang , Samuel Chackalamannil , Yuriko Root
IPC分类号： A61K31/277 , A61K31/138 , A61K31/075
CPC分类号： A61K31/03 , A61K31/10 , C07C43/225 , C07C255/54 , C07C255/58 , C07C2601/08
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable salts or solvates thereof, wherein: Ar1 is a chlorophenyl group, Ar2 is a dichlorophenyl group, R1 is a —(CH2)m—X—(CH2)n—R2 group, X is a —NH—, —O—, —C(O)— or —S(O)2— group, and R2 is a substituted phenyl group. These compounds are CB1 receptor modulators. Also disclosed are methods of treating CB1 modulated diseases or conditions such as the metabolic syndrome.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：Ar 1是氯苯基，Ar 2是二氯苯基， 1是 - （CH 2 CH 2）m -X-（CH 2）n - R 2基团，X是-NH-，-O-，-C（O） - 或-S（O）2 - ， - 2是取代的苯基。这些化合物是CB1受体调节剂。还公开了治疗CB1调节的疾病或诸如代谢综合征的病症的方法。

7. 发明申请

US20070197628A1 Cannabinoid receptor modulators 失效
标题翻译：大麻素受体调节剂
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。

8. 发明申请

US20060007152A1 Computer finger mouse 审中-公开
标题翻译：电脑手指鼠标
公开(公告)号：US20060007152A1
公开(公告)日：2006-01-12
申请号：US11172761
申请日：2005-07-02
申请人： Yuguang Wang
发明人： Yuguang Wang
IPC分类号： G09G5/08
CPC分类号： G06F3/03543 , G06F2203/0333
摘要： A computer finger mouse includes a concave structure for embrace the fingertips of a hand in a relaxed positions. The concave structure allows the mouse be held and manipulated by the fingertips of a hand only. A hand holding and manipulating the computer finger mouse is in a naturally relaxed and curled position, without requiring static twisting of the hand, wrist, or forearm. As a result, fatigue, discomfort, and pain are minimized or eliminated even after a long period of continuous use.
摘要翻译：计算机手指鼠标包括凹形结构，用于在轻松的位置包围手的指尖。凹形结构允许鼠标被手的指尖保持和操纵。握住和操纵计算机手指鼠标的手处于自然松弛和卷曲的位置，而不需要手，手腕或前臂的静态扭转。结果，即使在长时间的连续使用之后，疲劳，不适和疼痛也被最小化或消除。

9. 发明申请

US20050267155A1 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：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。

10. 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。

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