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21. 发明申请

US20100292192A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 有权
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：US20100292192A1
公开(公告)日：2010-11-18
申请号：US12812547
申请日：2009-01-08
申请人： Amjad Ali , Michael Man-Chu Lo , Christopher Franklin , Brent R. Whitehead
发明人： Amjad Ali , Michael Man-Chu Lo , Christopher Franklin , Brent R. Whitehead
IPC分类号： A61K31/655 , C07C245/24 , A61P9/12 , A61P7/10
CPC分类号： C07D403/10 , C07D235/20 , C07D257/04 , C07D401/14 , C07D409/06
摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;Z is —O— or —(CR14R15)_; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N═N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y选自和：2）-C（R 1 H）OC（O）X（（CR 12 R 13） - （CHR 10）m - （CH 2）n -Z-（CH 2）q - （CHR 11）r - （CR 16 R 17）） - R 5; Z是-O-或 - （CR14R15）_; m，n，p，q和r独立地选自0和1组成的组; X是-O-或 - （CR 18 R 19） - ; R1选自氢，C1-4烷基，芳基和C1-4烷基芳基; R5是-O-N = N（O）-NR3R4; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

22. 发明授权

US11046714B2 2,2-difluorodioxolo A2A receptor antagonists 有权
公开(公告)号：US11046714B2
公开(公告)日：2021-06-29
申请号：US14914843
申请日：2014-08-25
申请人： Merck Sharp & Dohme Corp. , Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
发明人： Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
IPC分类号： C07D519/00 , C07D491/147
摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

23. 发明授权

US10329289B2 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor 有权
公开(公告)号：US10329289B2
公开(公告)日：2019-06-25
申请号：US15386009
申请日：2016-12-21
申请人： Jianming Bao , Xiaolei Gao , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Debra L. Ondeyka , Andrew W. Stamford , Fengqi Zhang
发明人： Jianming Bao , Xiaolei Gao , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Debra L. Ondeyka , Andrew W. Stamford , Fengqi Zhang
IPC分类号： C07D471/04 , C07F9/22 , C07D519/00 , C07D491/048 , C07D471/08 , C07D491/052 , A61K31/437 , A61P25/00
摘要： The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

24. 发明申请

US20120232039A1 PRIMARY AMINE DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES 有权
标题翻译：主要的氨基二氮杂环戊烷杂环衍生物
公开(公告)号：US20120232039A1
公开(公告)日：2012-09-13
申请号：US13412032
申请日：2012-03-05
申请人： Amjad ALI , Michael Man-Chu Lo , Brent Whitehead , Shrenik K. Shah , Lin Yan , Timothy J. Henderson , Zack Zhiqiang Guo
发明人： Amjad ALI , Michael Man-Chu Lo , Brent Whitehead , Shrenik K. Shah , Lin Yan , Timothy J. Henderson , Zack Zhiqiang Guo
IPC分类号： A61K31/655 , A61P9/12 , C07C245/24
CPC分类号： C07D211/46 , C07D207/12 , C07D207/273 , C07D207/48 , C07D211/96 , C07D223/08 , C07D309/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/12
摘要： A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有用于治疗高血压，肺动脉高压（PAH），充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病的结构的化合物。

25. 发明申请

US20120208838A1 DIURETICS 有权
公开(公告)号：US20120208838A1
公开(公告)日：2012-08-16
申请号：US13504581
申请日：2010-10-22
申请人： Amjad Ali , Christopher Franklin , Ravi Nargund , Michael Man-Chu Lo , Lin Yan , Pei Huo
发明人： Amjad Ali , Christopher Franklin , Ravi Nargund , Michael Man-Chu Lo , Lin Yan , Pei Huo
IPC分类号： A61K31/4355 , A61P9/12 , C07D491/048
CPC分类号： C07D491/048
摘要： A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构（I）的化合物，其中R选自1）和2）或其药学上可接受的盐，以及使用该化合物治疗高血压的方法。

26. 发明授权

US08106034B2 Angiotensin II receptor antagonists 有权
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US08106034B2
公开(公告)日：2012-01-31
申请号：US12864448
申请日：2009-01-29
申请人： Amjad Ali , Michael Man-Chu Lo
发明人： Amjad Ali , Michael Man-Chu Lo
IPC分类号： A61K31/655 , C07C291/08 , A61P9/12
CPC分类号： C07D403/14 , C07D401/14
摘要： A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR1R20)1-7R5, or —C(O)(CR1R20)1-7R5; R1 and R20 are independently selected from the group consisting of hydrogen or C1-4 alkyl; R5 is —O—N═N(O)—NR3R4; and R3 and R4 are independently selected from the group consisting of —CH2CH2OH, —CH2CH2OCH3, —C1-4 alkyl, unsubstituted or substituted C1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC1-4 alkyl, or R3 and R4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.
摘要翻译：具有结构的化合物，其中R是血管紧张素受体阻断基团Y是 - （CR1R20）1-7R5或-C（O）（CR1R20）1-7R5; R 1和R 20独立地选自氢或C 1-4烷基; R5是-O-N = N（O）-NR3R4; 并且R 3和R 4独立地选自-CH 2 CH 2 OH，-CH 2 CH 2 OCH 3，-C 1-4烷基，未取代或取代的C 1-6烯基，未取代或取代的吗啉代，氨基，未取代或取代的苄基，未取代或取代的苯基，未取代的或取代的芳基C 1-4烷基，或R 3和R 4与它们所连接的氮原子一起形成选自下列的环或其立体异构体或其药学上可接受的盐，或其药学上可接受的盐其立体异构体，其可用于治疗高血压。

27. 发明申请

US20110230532A1 NITROOXY CYCLOALKANE DERIVATIVES 有权
公开(公告)号：US20110230532A1
公开(公告)日：2011-09-22
申请号：US13130473
申请日：2009-07-27
申请人： Amjad Ali , Robert K. Baker , Kathleen M. Rupprecht , Michael Man-Chu Lo , Brent Whitehead
发明人： Amjad Ali , Robert K. Baker , Kathleen M. Rupprecht , Michael Man-Chu Lo , Brent Whitehead
IPC分类号： A61K31/41 , A61K31/215 , A61K31/24 , A61K31/16 , A61K31/075 , C07D257/04 , C07C69/76 , C07C69/74 , C07C237/24 , C07C205/44 , A61P9/12
CPC分类号： C07D257/04 , C07D249/12
摘要： A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构的化合物，其中Y选自-C（O）OR 2，-C（O）NHR 8，-C（CH 2）1-2OR 3，OH及其药学上可接受的盐，以及使用该化合物治疗高血压。

28. 发明授权

US07880014B2 Angiotensin II receptor antagonists 有权
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US07880014B2
公开(公告)日：2011-02-01
申请号：US12000247
申请日：2007-12-11
申请人： Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
发明人： Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
IPC分类号： C07D257/00 , C07D403/00
CPC分类号： C07D403/10
摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5-; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y1-Y2-Y3-Y4-Y5-; Y1是C（R1R2）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-OC（O）C 1-4烷基; Y2是O或CH2; Y 3是C（O）或CH 2; Y4是O或CH2; Y 5是 - （CH 2）1-2 - （X）0-1 - （CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

29. 发明申请

US20100152259A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：US20100152259A1
公开(公告)日：2010-06-17
申请号：US12516482
申请日：2007-12-11
申请人： Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
发明人： Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
IPC分类号： C07D403/10 , A61K31/4184 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R an angiotensin receptor antagonist active group, Y is Y1—Y2—Y3—Y4—Y5. Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R为血管紧张素受体拮抗剂活性基团，Y为Y1-Y2-Y3-Y4-Y5。 Y1是C（R1R2）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1-4烷基; Y2是O或CH2; Y 3是C（O）或CH 2; Y4是O或CH2; Y 5是 - （CH 2）1-2 - （X）0-1-CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

30. 发明公开

US20230322785A1 ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY 审中-公开
公开(公告)号：US20230322785A1
公开(公告)日：2023-10-12
申请号：US18015387
申请日：2022-07-21
申请人： Christopher W. BOYCE , Thomas H. GRAHAM , Andrew J. HOOVER , Xianhai HUANG , Rognze KUANG , Jae-Hun KIM , Joseph M. KELLY , Michael Man-Chu LO , Jing SU , Dong XIAO , Xiaohong ZHU , Merck Sharp & Dohme LLC
发明人： Amjad Ali , Christopher W. Boyce , Jared N. Cumming , Duane DeMong , Thomas H. Graham , Subrahmanyam Gudipati , Andrew J. Hoover , Xianhai Huang , Rongze Kuang , Jae-Hun Kim , Joseph M. Kelly , Yeon-Hee Lim , Michael Man-Chu Lo , Jesus Moreno , Jing Su , Heping Wu , Dong Xiao , Younong Yu , Xiaohong Zhu
IPC分类号： C07D487/04 , C07K16/28 , A61P35/00
CPC分类号： C07D487/04 , A61P35/00 , C07K16/2896
摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

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