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公开(公告)号:US20160214997A1
公开(公告)日:2016-07-28
申请号:US14914843
申请日:2014-08-25
申请人: Amjad ALI , 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 , MERCK SHARP & DOHME CORP.
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
CPC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.
摘要翻译: 本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。
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公开(公告)号:US08648058B2
公开(公告)日:2014-02-11
申请号:US13577797
申请日:2011-02-10
申请人: Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lin Yan
发明人: Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lin Yan
IPC分类号: A61K31/655 , C07C245/24
CPC分类号: C07C291/00 , C07C291/08 , C07C2601/08 , C07D249/04
摘要: A compound of formula I, wherein R1-R7 are defined herein, or stereoisomers therof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using these compounds for treating hypertension.
摘要翻译: 式I化合物,其中R 1 -R 7在本文中定义,或其立体异构体,或其药学上可接受的盐,或其立体异构体的药学上可接受的盐,以及使用这些化合物治疗高血压的方法。
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3.
公开(公告)号:US08440702B2
公开(公告)日:2013-05-14
申请号:US13073190
申请日:2011-03-28
申请人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
发明人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
IPC分类号: A61K31/4166 , A61K31/44 , C07D413/10
CPC分类号: C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10 , C07D417/10 , C07D417/14
摘要: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
摘要翻译: 具有式I结构的化合物,包括化合物的药学上可接受的盐,是CETP抑制剂,可用于升高HDL-胆固醇,降低LDL-胆固醇,以及用于治疗或预防动脉粥样硬化。 化合物具有通过单键连接的3个环状基团,例如三苯基,其直接连接到式I的环或连接在位置B.
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公开(公告)号:US20130059823A1
公开(公告)日:2013-03-07
申请号:US13698444
申请日:2011-05-16
申请人: Amjad Ali , Lin Yan , Pei Huo , Ravi Nargund
发明人: Amjad Ali , Lin Yan , Pei Huo , Ravi Nargund
IPC分类号: A61K31/655 , A61P9/12 , C07C245/02
CPC分类号: C07C291/02 , C07B59/001 , C07C2601/14
摘要: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is (CR1R2)nC(O)OR16, wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.
摘要翻译: 具有结构(I)的化合物或其药学上可接受的盐,其中R 3是氢,氘,-OH,-OC 1-6烷基或卤素; R8是氢,氘或C1-6烷基; R 11和R 12独立地是氢,-C 1-6烷基,-OH,-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基, - (CH 2)1-2 OH或-OC 1-6烷基,或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子,其中所述环是未取代的或被卤素或-C 1-6烷基单取代,二取代或三取代; R15是(CR1R2)nC(O)OR16,其中n是0,1或2,-C(O)NHCH(R17)OR16或-C(O)NHCH(R17)C(O)NHCH(R18) (O)OR16; R16是氢,C1-6烷基或(CH2)1-2N + R19R20R21; R 1,R 2,R 4,R 5,R 6,R 7,R 9,R 10,R 17,R 18,R 19,R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。
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公开(公告)号:US08293777B2
公开(公告)日:2012-10-23
申请号:US12629419
申请日:2009-12-02
申请人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
发明人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
IPC分类号: A61K31/34 , A61K31/41 , C07D249/00 , C07D409/02
CPC分类号: C07D403/10 , C07D235/08 , C07D257/04 , C07D409/06
摘要: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译: 具有其中R为血管紧张素受体拮抗剂活性基团且Y为Y的结构的化合物选自R 1选自-O-C 1-6烷基,-O-芳基,-O- 杂芳基,-O-C 3-8环烷基,-C 1-6烷基, - 芳基, - 杂芳基和-C 3-8环烷基; R2和R3独立地选自氢和C 1-4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。
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公开(公告)号:US20120238608A1
公开(公告)日:2012-09-20
申请号:US13483213
申请日:2012-05-30
申请人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
发明人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
IPC分类号: A61K31/4178 , A61P9/12 , C07D493/04
CPC分类号: C07D403/10 , C07D235/20 , C07D257/04 , C07D409/06 , C07D493/04
摘要: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译: 具有其中R为例如Y的结构的化合物选自1)R5,2)-C(R1R2)(C(R3R4))0-1Y1R5和3)-C(R1R2) - O-Y1R5; R 1,R 2,R 3和R 4独立地选自氢和C 1-4烷基; R5是 Y1选自C(O)-O-和P(O)(OR 6)-O-; R6为氢或CH3,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。
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公开(公告)号:US08193365B2
公开(公告)日:2012-06-05
申请号:US12815146
申请日:2010-06-14
申请人: Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi
发明人: Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi
IPC分类号: C07D261/02 , C07D209/04 , C07D307/93 , A01N57/26 , A01N57/00
CPC分类号: A61K31/343 , A61K31/381 , A61K31/404 , A61K31/42 , A61K31/44 , A61K31/4412 , A61K31/455 , A61K31/47 , A61K31/472 , A61K38/00 , A61K45/06 , C07C233/16 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/32 , C07C311/04 , C07C311/08 , C07C317/32 , C07D209/08 , C07D213/54 , C07D215/12 , C07D217/02 , C07D261/08 , C07D271/10 , C07D307/14 , C07D307/79 , C07D333/20 , C07D333/22 , C07D333/28 , A61K2300/00
摘要: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
摘要翻译: 式I化合物,包括化合物的药学上可接受的盐,是CETP抑制剂,可用于培养HDL-胆固醇,降低LDL-胆固醇,以及治疗或预防动脉粥样硬化。 在式1化合物中,A1和A2各自为芳环,5-6元杂环,稠合于杂环的芳环,稠合于杂环的苯环或环烷基环。
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公开(公告)号:US20110218177A1
公开(公告)日:2011-09-08
申请号:US13121972
申请日:2009-09-21
申请人: Sander G. Mills , Amjad Ali , Cameron Smith
发明人: Sander G. Mills , Amjad Ali , Cameron Smith
IPC分类号: A61K31/661 , C07C219/22 , A61K31/265 , C07C329/06 , C07F9/06 , C07F9/38 , A61K31/662 , A61P3/00 , A61P3/06
CPC分类号: A61K31/42 , C07C219/22 , C07C219/28 , C07C229/36 , C07C329/06 , C07C2601/14 , C07F9/091 , C07F9/093 , C07F9/094
摘要: The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.
摘要翻译: 式I的化合物是具有中心恶唑烷酮环的CETP抑制剂的前药。 通过消除HX,在给予患者后,化合物环化形成恶唑烷酮环。
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9.
公开(公告)号:US07915271B2
公开(公告)日:2011-03-29
申请号:US12087290
申请日:2006-12-29
申请人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
发明人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
IPC分类号: A61K31/4166 , A61K31/44 , A61K31/506 , C07D239/34 , C07D413/10 , C07D263/06
CPC分类号: C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10 , C07D417/10 , C07D417/14
摘要: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
摘要翻译: 具有式I结构的化合物,包括化合物的药学上可接受的盐,是CETP抑制剂,可用于升高HDL-胆固醇,降低LDL-胆固醇,以及用于治疗或预防动脉粥样硬化。 化合物具有通过单键连接的3个环状基团,例如三苯基,其直接连接到式I的环或连接在位置B.
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公开(公告)号:US07910592B2
公开(公告)日:2011-03-22
申请号:US12087185
申请日:2006-12-29
申请人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li , Christopher F. Thompson
发明人: Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li , Christopher F. Thompson
IPC分类号: A61K31/497 , A61K31/427 , A61K31/422 , A61K31/506 , C07D239/02 , C07D241/02 , C07D401/02 , C07D277/02 , C07D263/02
CPC分类号: C07D413/06 , C07D263/24
摘要: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
摘要翻译: 具有式(I)结构的化合物,包括化合物的药学上可接受的盐,是CETP抑制剂,可用于培养HDL-胆固醇,降低LDL-胆固醇,以及用于治疗或预防动脉粥样硬化。 在式(I)的化合物中,B是苯基以外的环状基团,B在与B与式(I)的结构的其余部分连接的位置的邻位的位置具有环状取代基。 式(I)的5元环除了B之外还具有第二个环状取代基。
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