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.

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.

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.

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。

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.

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。