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公开(公告)号:US20180162874A1
公开(公告)日:2018-06-14
申请号:US15579115
申请日:2016-06-20
申请人: Gregori J. MORRIELLO , Lehua CHANG , Ashley FORSTER , Yili CHEN , Michael P. DWYER , Richard BERGER , Ming WANG , Kausik K. NADA , Jaime L. BUNDA , William D. SHIPE , Merck Sharp & Dohme Corp.
发明人: Gregori J. Morriello , Michael P. Dwyer , Lehua Chang , Yili Chen , Ming Wang , Ashley Forster , Richard Berger , Kausik k Nanda , Jaime L Bunda , William D Shipe
IPC分类号: C07D498/04 , C07D473/34 , A61P25/18 , A61P25/16 , A61P25/28
CPC分类号: C07D498/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/28 , C07D473/34 , C07D487/04
摘要: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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公开(公告)号:US20140329798A1
公开(公告)日:2014-11-06
申请号:US14358241
申请日:2012-11-09
发明人: Scott Edmondson , Zhiyong Hu , Ping Liu , Gregori J. Morriello , Jason W. Szewczyk , Bowei Wang , Liping Wang , Harold B. Wood , Cheng Zhu , Yuping Zhu , Zhiqiang Guo
IPC分类号: C07D513/04 , C07D239/42 , C07D405/12 , C07D409/12 , C07D498/04 , C07D487/04 , C07D403/14 , C07D401/14 , C07D403/12 , C07D471/04
CPC分类号: C07D513/04 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included
摘要翻译: 披露式(I)的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法
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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
申请人: 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.
发明人: 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分类号: 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
摘要: 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:US10647727B2
公开(公告)日:2020-05-12
申请号:US15579115
申请日:2016-06-20
申请人: Merck Sharp & Dohme Corp. , Gregori J. Morriello , Michael P. Dwyer , Lehua Chang , Yili Chen , Ming Wang , Ashley Forster , Richard Berger , Kausik K. Nanda , Jamie L. Bunda , William D. Shipe
发明人: Gregori J. Morriello , Lehua Chang , Ashley Forster , Richard Berger , Kausik K. Nanda , William D. Shipe
IPC分类号: C07D487/04 , C07D498/04 , C07D473/34 , A61P25/06 , A61P25/28 , A61P25/18 , A61P25/16
摘要: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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公开(公告)号:US10138255B2
公开(公告)日:2018-11-27
申请号:US15124635
申请日:2015-03-06
发明人: Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号: A61K31/554 , C07D513/08 , A61K45/06
摘要: The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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公开(公告)号:US09018224B2
公开(公告)日:2015-04-28
申请号:US14358241
申请日:2012-11-09
发明人: Scott Edmondson , Zhiyong Hu , Ping Liu , Gregori J. Morriello , Jason W. Szewczyk , Bowei Wang , Liping Wang , Harold B. Wood , Cheng Zhu , Yuping Zhu , Zhiqiang Guo
IPC分类号: A01N43/54 , A61K31/505 , C07D513/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D239/42 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12
CPC分类号: C07D513/04 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译: 披露式(I)的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。
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公开(公告)号:US09840478B2
公开(公告)日:2017-12-12
申请号:US14908421
申请日:2014-07-29
发明人: Peter D. Williams , John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Kartik M. Keertikar , H. Marie Loughran , Jessie J. Manikowski , Gregori J. Morriello , Dong-Ming Shen , Edward C. Sherer , Jurgen Schultz , Sherman T. Waddell , Catherine M. Wiscount , Nicolas Zorn , Xin-Jie Chu , Satyanarayana Tummanapalli , Vijayasaradhi Sivalenka , Bin Hu , Tao Ji , Bin Zhong
IPC分类号: C07D241/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/14
CPC分类号: C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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公开(公告)号:US20170073354A1
公开(公告)日:2017-03-16
申请号:US15124635
申请日:2015-03-06
申请人: Jurgen SCHULZ , Peter D. WILLIAMS , John A. MCCAULEY , Christopher J. BUNGARD , David Jonathan BENNETT , Sherman T. WADDELL , Gregori J. MORRIELLO , Lehua CHANG , Michael P. DWYER , Katharine M. HOLLOWAY , Alejandro CRESPO , Xin-Jie CHU , Catherine WISCOUNT , Marie H. LOUGHRAN , Jesse J. MANIKOWSKI , Kartik M. KEERTIKAR , Bin HU , Bin ZHONG , Tao JI , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd.
发明人: Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号: C07D513/08 , A61K31/554 , A61K45/06
CPC分类号: C07D513/08 , A61K31/554 , A61K45/06
摘要: The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
摘要翻译: 本发明涉及含有该化合物的式I药物组合物的化合物及其在抑制HIV蛋白酶,抑制HIV复制,预防HIV感染,HIV感染治疗和预防, 治疗和延迟艾滋病的发病或进展。
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公开(公告)号:US20160159752A1
公开(公告)日:2016-06-09
申请号:US14908421
申请日:2014-07-29
发明人: Peter D. Williams , John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Kartik M. Keertikar , H. Marie Loughran , Jessie J. Manikowski , Gregori J. Morriello , Dong-Ming Shen , Edward C. Sherer , Jurgen Schultz , Sherman T. Waddell , Catherine M. Wiscount , Nicolas Zorn , Xin-Jie Chu , Satyanarayana Tummanapalli , Vijayasaradhi Sivalenka , Bin Hu , Tao Ji , Bin Zhong
IPC分类号: C07D241/04 , C07D401/12 , C07D417/14 , C07D405/14 , C07D413/14 , C07D401/06 , C07D405/12
CPC分类号: C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
摘要翻译: 本发明涉及哌嗪衍生物,包含它们的药物组合物及其在抑制HIV蛋白酶,HIV复制抑制,HIV预防感染,HIV感染治疗和预防治疗中的用途 ,并延迟艾滋病的发病或进展。
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公开(公告)号:US20230023066A1
公开(公告)日:2023-01-26
申请号:US17769814
申请日:2020-10-20
申请人: Mitchell H. KEYLOR , Michael j. ARDOLINO , Ryan W. CHAU , Peter H. FULLER , Anmol GULATI , Rebecca Elizabeth JOHNSON , Solomon D. KATTAR , Kaila A. MARGREY , Gregori J. MOREIELLO , Santhosh F. NEELAMKAVIL , Xin YAN , Elsie C. YU , Cayetena Carmela ZARATE SAEZ , Merck Sharp & Dohme Corp.
发明人: Mitchell H. Keylor , Michael J. Ardolino , Ryan W. Chau , Peter H. Fuller , Anmol Gulati , Rebecca Elizabeth Johnson , Solomon D. Kattar , Kaila A. Margrey , Gregori J. Morriello , Santhosh F. Neelamkavil , Xin Yan , Elsie C. Yu , Cayetana Carmela Zarate Saez
IPC分类号: C07D403/14 , C07D405/14 , C07D403/12 , C07D417/14 , C07D401/14 , C07D413/14 , C07D409/14
摘要: The present invention is directed to substituted certain N-(heteroaryl)quinazolin-2-amine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein J, R3, and R4, 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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