公开(公告)号：US09353101B2

公开(公告)日：2016-05-31

申请号：US14398165

申请日：2013-04-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： John J. Acton, III ,  Feng Ye ,  Petr Vachal ,  Deyou Sha ,  James F. Dropinski ,  Lin Chu ,  Debra Ondeyka ,  Alexander J. Kim ,  Vincent J. Colandrea ,  Yi Zang ,  Fengqi Zhang ,  Guizhen Dong

IPC: C07D417/14 ,  C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/444 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高人类患者的HDL-胆固醇和降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。

公开(公告)号：US20150111866A1

公开(公告)日：2015-04-23

申请号：US14398165

申请日：2013-04-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： John J. Acton, III ,  Feng Ye ,  Petr Vachal ,  Deyou Sha ,  James F. Dropinski ,  Lin Chu ,  Debra Ondeyka ,  Alexander J. Kim ,  Vincent J. Colandrea ,  Yi Zang ,  Fengqi Zhang ,  Guizhen Dong

IPC: C07D417/14 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/444 ,  C07D413/14 ,  A61K31/506

CPC classification number: C07D417/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14

Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高人类患者的HDL-胆固醇和降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。

公开(公告)号：US20200206350A1

公开(公告)日：2020-07-02

申请号：US16644107

申请日：2018-08-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： Lin Chu ,  Nathalie Y. Toussaint ,  Dong Xiao ,  Petr Vachal ,  Ramesh S. Kashi ,  Annette Bak

IPC: A61K47/22 ,  C07K16/28 ,  A61K47/26 ,  C07D233/64 ,  C07C279/14 ,  C07C235/12 ,  C07C229/36 ,  A61K47/18

Abstract: The present invention relates to pegylated amino acid compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3A, R3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.