公开(公告)号：US20220064147A1

公开(公告)日：2022-03-03

申请号：US17413882

申请日：2019-12-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： Antonella Converso ,  Abdellatif El Marrouni ,  Ashley Forster ,  Jessica L. Frie ,  David N. Hunter ,  Scott D. Kuduk ,  Helen J. Mitchell ,  Philippe Nantermet ,  Deyou Sha ,  William Daniel Shipe ,  Cheng Wang ,  Deping Wang

IPC: C07D403/06 ,  A61K45/06

Abstract: The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

公开(公告)号：US20220062284A1

公开(公告)日：2022-03-03

申请号：US17411341

申请日：2021-08-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： Antonella Converso ,  Abdellatif El Marrouni ,  Anthony W. Shaw ,  David N. Hunter ,  Ashley Forster ,  Cheng Wang ,  Yunlong Zhang

IPC: A61K31/513 ,  A61K45/06 ,  C07D403/06 ,  C07D401/06 ,  A61P31/18

Abstract: The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

公开(公告)号：US10272077B2

公开(公告)日：2019-04-30

申请号：US15830131

申请日：2017-12-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: C07D471/10 ,  A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

公开(公告)号：US09499541B2

公开(公告)日：2016-11-22

申请号：US14505255

申请日：2014-10-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman ,  Heather E. Stevenson

IPC: A01N43/42 ,  A61K31/44 ,  C07D211/00 ,  C07D213/00 ,  C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00 ,  C07D471/04 ,  A61K31/506 ,  C07D487/04

CPC classification number: C07D471/04 ,  A61K31/506 ,  C07D487/04

Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺二氢化茚衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US20150005330A1

公开(公告)日：2015-01-01

申请号：US14485259

申请日：2014-09-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: C07D471/20

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺氮杂茚衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US20170027925A1

公开(公告)日：2017-02-02

申请号：US15293569

申请日：2016-10-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A61K31/4545

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists ofCGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺氮杂茚衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US09499545B2

公开(公告)日：2016-11-22

申请号：US14485259

申请日：2014-09-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A01N43/42 ,  A61K31/44 ,  C07D211/00 ,  C07D213/00 ,  C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00 ,  C07D471/20 ,  A61K31/435 ,  C07D471/10

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

公开(公告)号：US20150031716A1

公开(公告)日：2015-01-29

申请号：US14505255

申请日：2014-10-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman ,  Heather E. Stevenson

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/506 ,  C07D487/04

Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺二氢化茚衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US20220242847A1

公开(公告)日：2022-08-04

申请号：US17611448

申请日：2020-05-18

Applicant: Antonella CONVERSO ,  Abdellatif EL MARROUNI ,  Ashley FORSTER ,  Jessica L. FRIE ,  David N. HUNTER ,  Cheng WANG ,  Deping WANG ,  Merck Sharp & Dohme Corp.

Inventor： Antonella Converso ,  Abdellatif El Marrouni ,  Ashley Forster ,  Jessica L. Frie ,  David N. Hunter ,  Cheng Wang ,  Deping Wang

IPC: C07D401/06 ,  C07D401/14 ,  A61K45/06 ,  A61K31/506 ,  A61P31/18

Abstract: The present disclosure is directed to pyridinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

公开(公告)号：US20190275024A1

公开(公告)日：2019-09-12

申请号：US16396056

申请日：2019-04-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A61K31/4545 ,  C07D471/20 ,  A61K31/438 ,  A61K31/435 ,  C07D471/10

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 such diseases in which CGRP is involved.