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公开(公告)号：US09487504B2
公开(公告)日：2016-11-08
申请号：US14409147
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Jongwon Lim , Michael H. Reutershan , John Michael Ellis , Kaleen Konrad Childers , Anthony Donofrio , Michael D. Altman , Andrew M. Haidle , Anna Zabierek , Matthew Christopher , Jonathan Grimm , Jason Burch , Maria Emilia Di Francesco , Alessia Petrocchi , Christian Beaulieu , Vouy Linh Truong , Alan B. Northrup , Marc Blouin
IPC: C07D403/12 , C07D403/14 , C07D401/14
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14
Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
Abstract translation: 本发明提供了式I的新型咪唑类似物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20150175575A1
公开(公告)日：2015-06-25
申请号：US14409147
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Jongwon Lim , Michael H. Reutershan , John Michael Ellis , Kaleen Konrad Childers , Anthony Donofrio , Michael D. Altman , Andrew M. Haidle , Anna Zabierek , Matthew Christopher , Jonathan Grimm , Jason Burch , Maria Emilia Di Francesco , Alessia Petrocchi , Christian Beaulieu , Vouy Linh Truong , Alan B. Northrup , Marc Blouin
IPC: C07D403/12 , C07D401/14
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14
Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
Abstract translation: 本发明提供了式I的新型咪唑类似物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US09994587B2
公开(公告)日：2018-06-12
申请号：US15123111
申请日：2015-03-02
Applicant: MERCK CANADA INC.
Inventor： 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: C07D498/10 , C07D265/30 , A61K31/5375 , C07D413/12 , A61K31/5377 , C07D417/14 , C07D413/14 , C07D487/04 , C07D471/04 , C07D413/06 , C07D265/36 , A61K31/5386 , A61K45/06
CPC classification number: 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
Abstract: 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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公开(公告)号：US20170217986A1
公开(公告)日：2017-08-03
申请号：US15123111
申请日：2015-03-02
Applicant: 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.
Inventor： 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: 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 classification number: 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
Abstract: 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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公开(公告)号：US20160296527A1
公开(公告)日：2016-10-13
申请号：US15104782
申请日：2014-12-17
Applicant: MERCK SHARP & DOHME CORP. , MERCK CANADA INC.
Inventor： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Helen Juteau , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Christian Nadeau , Daniel Simard , Satyanarayana Tummanapalli , Vouy Linh Truong , Karine M. Villeneuve , Peter D. Williams
IPC: A61K31/5377 , C07D413/14 , C07D471/04 , C07D487/04 , A61K45/06 , C07D413/04
CPC classification number: A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Abstract translation: 本发明涉及5-杂芳基吗啉衍生物及其用于抑制HIV蛋白酶，HIV复制的抑制，HIV预防感染，HIV感染治疗以及预防，治疗和延迟的用途 艾滋病的发病或进展。 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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Patent Agency Ranking
公开(公告)号：US09737545B2
公开(公告)日：2017-08-22
申请号：US15104782
申请日：2014-12-17
Applicant: MERCK SHARP & DOHME CORP. , MERCK CANADA INC.
Inventor： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Helen Juteau , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Christian Nadeau , Daniel Simard , Satyanarayana Tummanapalli , Vouy Linh Truong , Karine M. Villeneuve , Peter D. Williams
IPC: A61K31/5377 , C07D417/04 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/04 , C07D265/30 , C07D413/14
CPC classification number: A61K31/5377 , A61K45/06 , C07D265/30 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives 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. 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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公开(公告)号：US20160311786A1
公开(公告)日：2016-10-27
申请号：US15104510
申请日：2014-12-17
Applicant: MERCK SHARP & DOHME CORP. , MERCK CANADA INC.
Inventor： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Satyanarayana Tummanapalli , Vouy Linh Truong , Peter D. Williams
IPC: C07D265/30 , A61K45/06 , C07D413/12 , A61K31/5377 , C07D471/04 , C07D417/14 , C07D487/04 , C07D417/12 , C07D513/04 , A61K31/5375 , C07D413/14
CPC classification number: C07D265/30 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives 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. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Abstract translation: 本发明涉及2,5,6-取代的吗啉衍生物及其在抑制HIV蛋白酶，HIV复制抑制，HIV感染预防，HIV感染治疗和预防治疗中的应用 ，并延迟艾滋病的发病或进展。 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：US20150191461A1
公开(公告)日：2015-07-09
申请号：US14409133
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Michelle R. Machacek , Michael D. Altman , Eric T. Romeo , Dilrukshi Vitharana , Brandon Cash , Tony Siu , Matthew Christopher , Solomon D. Kattar , Andrew M. Haidle , Kaleen Konrad Childers , Matthew L. Maddess , Michael H. Reutershan , Yves Ducharme , David J. Guerin , Kerrie Spencer , Christian Beaulieu , Vouy Linh Truong , Daniel Guay , Alan B. Northrup , Brandon M. Taoka , Jongwon Lim , Christian Fischer , John W. Butcher , Ryan D. Otte , Binyuan Sun , John Michael Ellis
IPC: C07D471/04 , C07D401/14 , C07D413/14 , C07D409/14 , C07D403/14 , C07D403/12
CPC classification number: C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
Abstract translation: 本发明提供了式I的新型吡唑衍生物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US09834526B2
公开(公告)日：2017-12-05
申请号：US15104510
申请日：2014-12-17
Applicant: MERCK SHARP & DOHME CORP. , MERCK CANADA INC.
Inventor： John A. McCauley , Christian Beaulieu , David Jonathan Bennett , Christopher J. Bungard , Sheldon Crane , Thomas J. Greshock , Katharine M. Holloway , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Satyanarayana Tummanapalli , Vouy Linh Truong , Peter D. Williams
IPC: A61K31/535 , C07D265/28 , C07D265/30 , A61K45/06 , A61K31/5375 , A61K31/5377 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
CPC classification number: C07D265/30 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives 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. 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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公开(公告)号：US09242984B2
公开(公告)日：2016-01-26
申请号：US14409133
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Michelle R. Machacek , Michael D. Altman , Eric T. Romeo , Dilrukshi Vitharana , Brandon Cash , Tony Siu , Hua Zhou , Matthew Christopher , Solomon D. Kattar , Andrew M. Haidle , Kaleen Konrad Childers , Matthew L. Maddess , Michael H. Reutershan , Yves Ducharme , David J. Guerin , Kerrie Spencer , Christian Beaulieu , Vouy Linh Truong , Daniel Guay , Alan B. Northrup , Brandon M. Taoka , Jongwon Lim , Christian Fischer , John W. Butcher , Ryan D. Otte , Binyuan Sun , John Michael Ellis
IPC: C07D401/00 , A61K31/00 , C07D471/04 , C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/14
CPC classification number: C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
Abstract translation: 本发明提供了式I的新型吡唑衍生物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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