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公开(公告)号：US09221834B2
公开(公告)日：2015-12-29
申请号：US13881896
申请日：2011-10-25
Applicant: Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
Inventor： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
IPC: A61K31/4439 , A61K31/506 , A61K31/5377 , A61K31/4545 , A61K31/497 , A61K31/444 , C07D491/08 , C07D417/14 , C07D413/14 , A61K31/42 , A61K45/06 , C07D413/06
CPC classification number: C07D491/08 , A61K31/42 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/06 , C07D413/14 , C07D417/14 , A61K2300/00
Abstract: 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 compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
Abstract translation: 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，A3是取代的苯基或茚满基。 式（I）。
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公开(公告)号：US20130331372A1
公开(公告)日：2013-12-12
申请号：US13881896
申请日：2011-10-25
Applicant: Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
Inventor： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
IPC: C07D491/08 , A61K31/5377 , A61K31/4545 , A61K31/444 , A61K31/497 , C07D417/14 , C07D413/14 , A61K45/06 , A61K31/4439 , A61K31/506
CPC classification number: C07D491/08 , A61K31/42 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/06 , C07D413/14 , C07D417/14 , A61K2300/00
Abstract: 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 compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
Abstract translation: 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，A3是取代的苯基或茚满基。 式（I）。
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3.发明申请
公开(公告)号：US20110178059A1
公开(公告)日：2011-07-21
申请号：US13073190
申请日：2011-03-28
Applicant: Amjad ALI , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
Inventor： Amjad ALI , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li
IPC: A61K31/421 , C07D263/04 , C07D417/02 , A61K31/427 , C07D413/02 , A61K31/454 , A61K31/4439 , A61K31/506 , A61P9/10
CPC classification number: C07D263/20 , C07D263/24 , C07D413/04 , C07D413/10 , C07D417/10 , C07D417/14
Abstract: 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.
Abstract translation: 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：US07652049B2
公开(公告)日：2010-01-26
申请号：US11173295
申请日：2005-07-01
Applicant: Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
Inventor： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC: C07D263/20 , A61K31/4015
CPC classification number: C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: Compounds having the structures 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 or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
Abstract translation: 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。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US20090124689A1
公开(公告)日：2009-05-14
申请号：US12083183
申请日：2006-10-13
Applicant: Yi-Heng Chen , Zhijian Lu , Peter J. Sinclair
Inventor： Yi-Heng Chen , Zhijian Lu , Peter J. Sinclair
IPC: A61K31/24 , C07C269/00
CPC classification number: C07C271/22
Abstract: Compounds having a biphenyl group substituted with a phenyl or heteroaromatic group, as shown in 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:
Abstract translation: 包含被苯基或杂芳基取代的联苯基的化合物，如式I所示，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：
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公开(公告)号：US20080119476A1
公开(公告)日：2008-05-22
申请号：US11631821
申请日：2005-07-01
Applicant: Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
Inventor： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC: A61K31/422 , A61K31/40 , A61K31/4166 , A61K31/427 , A61K31/4439 , A61K31/501 , A61P9/10 , C07D233/32 , C07D263/20 , C07D417/10 , C07D417/04 , C07D413/10 , C07D413/04 , C07D401/04 , C07D285/10 , C07D233/44 , C07D207/24 , A61K31/506 , A61K31/497 , A61K31/433 , A61K31/4168 , A61K31/421
CPC classification number: C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: Compounds having the structures 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 or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
Abstract translation: 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。在式I化合物中，B或 R 2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH 2 - 2连接到环上或连接到环上。
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公开(公告)号：US20220259188A1
公开(公告)日：2022-08-18
申请号：US17614732
申请日：2020-06-01
Applicant: Hua ZHOU , John J. ACTON, III , Michael J. ARDOLINO , Yi-Heng CHEN , Peter H. FULLER , Anmol GULATI , Rebecca Elizabeth JOHNSON , William P. KAPLAN , Solomon D. KATTAR , Mitchell H. KEYLOR , Derun LI , Kaitlyn Marie LOGAN , Min LU , Gregori J. MORRIELLO , Santhosh F. NEELAMKAVIL , Barbara PIO , Nunzio SCIAMMETTA , Vladimir SIMOV , Jing SU , Luis TORRES , Xin YAN , Merck Sharp & Dohme Corp.
Inventor： Hua Zhou , John J. Acton, III , Michael J. Ardolino , Yi-Heng Chen , Peter H. Fuller , Anmol Gulati , Rebecca Elizabeth Johnson , William P. Kaplan , Solomon D. Kattar , Mitchell H. Keylor , Derun Li , Kaitlyn Marie Logan , Min Lu , Gregori J. Morriello , Santhosh F. Neelamkavil , Barbara Pio , Nunzio Sciammetta , Vladimir Simov , Jing Su , Luis Torres , Xin Yan
IPC: C07D405/14 , C07D487/08 , C07D409/14 , C07D403/04 , C07D403/14 , C07D498/04 , C07D498/08 , C07D487/10 , C07D401/14 , C07D471/10 , C07D491/107 , C07D471/04 , C07D487/04 , A61P25/16
Abstract: The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6-disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
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公开(公告)号：US09695198B2
公开(公告)日：2017-07-04
申请号：US14652150
申请日：2013-12-16
Applicant: Cameron James Smith , Edward Sherer , Louis-Charles Campeau , James Balkovec , William John Greenlee , Derun Li , Liangqin Guo , Tin-Yau Chan , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , John Qiang Tan , Tomokazu Hirabayashi , Mika Sekioka , MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD.
Inventor： Cameron James Smith , Edward Sherer , Louis-Charles Campeau , James Balkovec , William John Greenlee , Derun Li , Liangqin Guo , Tin-Yau Chan , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , John Qiang Tan , Tomokazu Hirabayashi , Mika Sekioka
IPC: C07D413/14 , C07D417/06 , C07D498/04 , C07D513/04 , C07D413/12 , C07D471/04 , C07D413/06
CPC classification number: C07D513/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D498/04
Abstract: The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
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公开(公告)号：US20150368269A1
公开(公告)日：2015-12-24
申请号：US14652150
申请日：2013-12-16
Applicant: Tomokazu HIRABAYASHI , Mika KATSUNO , Cameron James SMITH , Edward SHERER , Louis-Charles CAMPEAU , James BALKOVEC , William John GREENLEE , Derun LI , Liangqin GUO , Tin Yan CHAN , Yi-Heng CHEN , Yili CHEN , Samuel CHACKALAMANNIL , John Qiang TAN , MERCH SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD.
Inventor： Cameron James Smith , Edward Sherer , Louis-Charles Campeau , James Balkovec , William John Greenlee , Derun Li , Liangqin Guo , Tin-Yau Chan , Yi-Heng Chen , Yili Chen , Samuel Chackalamannil , John Qiang Tan , Tomokazu Hirabayashi , Mika Sekioka
IPC: C07D513/04 , C07D417/06 , C07D413/06 , C07D498/04 , C07D471/04
CPC classification number: C07D513/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D471/04 , C07D498/04
Abstract: The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
Abstract translation: 本发明提供式（I）化合物，其中A为杂环环系，B为杂环环系或芳环系，以及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的方法 血栓形成，栓塞，高凝状态或纤维化变化。
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公开(公告)号：US20170174693A1
公开(公告)日：2017-06-22
申请号：US15384429
申请日：2016-12-20
Applicant: Raphaelle Berger , Yi-Heng Chen , Guoqing Li , Joie Garfunkle , Hong-Dong Li , Shouwu Miao , Subharekha Raghavan , Cameron J. Smith , John Stelmach , Alan Whitehead , Rui Zhang , Yong Zhang , Jianmin Fu , Gang Ji , Falong Jiang
Inventor： Raphaelle Berger , Yi-Heng Chen , Guoqing Li , Joie Garfunkle , Hong-Dong Li , Shouwu Miao , Subharekha Raghavan , Cameron J. Smith , John Stelmach , Alan Whitehead , Rui Zhang , Yong Zhang , Jianmin Fu , Gang Ji , Falong Jiang
IPC: C07D487/04 , A61K31/519 , C07D519/00 , A61K45/06
CPC classification number: C07D487/04 , A61K31/519 , A61K45/06 , C07D519/00
Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
