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公开(公告)号：US09315475B2
公开(公告)日：2016-04-19
申请号：US14021930
申请日：2013-09-09
申请人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
发明人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D265/30 , C07D487/04 , C07D493/04 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07F7/08
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US10450309B2
公开(公告)日：2019-10-22
申请号：US15769079
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Phieng Siliphaivanh , Kerrie Spencer , Satyanarayana Tummanapalli
IPC分类号： A61K31/35 , A61P3/10 , C07D311/22 , C07D311/58 , C07D405/14 , C07D417/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US20180291017A1
公开(公告)日：2018-10-11
申请号：US15768097
申请日：2016-11-28
申请人： Yongxin HAN , Phieng SILIPHAIVANH , Kerrie SPENCER , Satyanarayana TUMMANAPALLI , Merck Sharp & Dohme Corp.
IPC分类号： C07D417/14 , A61P3/10
CPC分类号： C07D417/14 , A61K9/2054 , A61P3/10
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US20180305342A1
公开(公告)日：2018-10-25
申请号：US15767371
申请日：2016-11-28
申请人： Yongxin HAN , Jongwon LIM , Phieng SILIPHAIVANH , Kerrie SPENCER , Satyanarayana TUMMANAPALLI , Merck Sharp & Dohme Corp.
IPC分类号： C07D405/06 , C07D311/22 , C07D417/06 , C07D413/06
CPC分类号： C07D405/06 , A61K9/2054 , A61K31/353 , C07D311/22 , C07D413/06 , C07D417/06
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension. Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US10336733B2
公开(公告)日：2019-07-02
申请号：US15767371
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Jongwon Lim , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： C07D417/06 , C07D413/06 , C07D311/22 , C07D405/06 , A61K31/353 , A61K9/20
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US10370368B2
公开(公告)日：2019-08-06
申请号：US15768097
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： A61K9/20 , A61P3/10 , C07D417/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US20170217986A1
公开(公告)日：2017-08-03
申请号：US15123111
申请日：2015-03-02
申请人： John A. MCCAULEY , David Johathan BENNETT , Christopher J. BUNGARD , Thomas J. GRESHOCK , M. Katharine HOLLOWAY , Peter D. WILLIAMS , Christian BEAULIEU , Sheldon CRANE , Stephanie LESSARD , Daniel MCKAY , Carmela MOLINARO , Oscar Miguel MORADEI , Vijayasaradhi SIVALENKA , Vouy Linh TRUONG , Satyanarayana TUMMANAPALLI , Merck Canada Inc.
发明人： John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Thomas J. Greshock , M. Katharine Holloway , Peter D. Williams , Christian Beaulieu , Sheldon Crane , Stephanie Lessard , Daniel Mckay , Carmela Molinaro , Oscar Miguel Moradei , Vijayasaradhi Sivalenka , Vouy Linh Truong , Satyanarayana Tummanapalli
IPC分类号： C07D498/10 , A61K31/5375 , C07D413/12 , A61K31/5377 , C07D417/14 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/06 , C07D265/36 , A61K31/5386 , C07D265/30 , C07D413/14
CPC分类号： C07D498/10 , A61K31/5375 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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