Thomas J Graham, 436931 Jackson Dr, San Diego, CA 92119

2022040, Dec 22, 2022

Sep 18, 2020

17/761433

- Rahway NJ, US
Thomas H. Graham - Somerville MA, US
Xiaoshen Ma - Boston MA, US
Zahid Hussain - Dayton NJ, US
Mihir Mandal - Westfield NJ, US
Symon Gathiaka - Waltham MA, US
Yongxin Han - Needham MA, US
David L. Sloman - Newton MA, US

C07D 471/04
A61P 35/00

Provided are compounds of Formula (I)or a pharmaceutically acceptable salt thereof, wherein Y, CY, R, R, R, R, R, R, R, R, R, and the subscripts m, n, and q are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treatment of cancer. Also provided are pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. Also provided are methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

2023005, Feb 23, 2023

Nov 26, 2019

17/294836

Yonglian ZHANG - Kenilworth NJ, US
Amjad ALI - Kenilworth NJ, US
Jared CUMMING - Winchester MA, US
Duane DEMONG - Boston MA, US
Qiaolin DENG - Kenilworth NJ, US
Thomas H. GRAHAM - Boston MA, US
Elisabeth HENNESSY - Boston MA, US
Matthew A. LARSEN - Boston MA, US
Kun LIU - Boston MA, US
Ping LIU - Boston MA, US
Umar Faruk MANSOOR - Boston MA, US
Jianping PAN - Kenilworth NJ, US
Christopher W. PLUMMER - Kenilworth NJ, US
Aaron SATHER - Boston MA, US
Uma SWAMINATHAN - Boston MA, US
Huijun WANG - Westfield NJ, US
- Rahway NJ, US

Merck Sharp & Dohme Corp. - Rahway NJ

A61K 31/519
A61K 39/395
C07D 471/04
C07D 519/00
A61K 31/55

In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2and/or A2receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2receptor and/or the adenosine A2receptor.

2021039, Dec 23, 2021

Nov 15, 2019

17/292511

Zachary G. BRILL - Boston MA, US
Amjad ALI - Kenilworth NJ, US
Jared CUMMING - Winchester MA, US
Duane DEMONG - Boston MA, US
Qiaolin DENG - Kenilworth NJ, US
Thomas H. GRAHAM - Boston MA, US
Rongze KUANG - Kenilworth NJ, US
Yeon-Hee LIM - South San Francisco CA, US
Christopher W. PLUMMER - Kenilworth NJ, US
Jenny Lorena RICO DUQUE - Boston MA, US
Huijun WANG - Kenilworth NJ, US
Yonglian ZHANG - Kenilworth NJ, US
Kake ZHAO - Kenilworth NJ, US
- Rahway NJ, US

Merck Sharp & Dohme Corp. - Rahway NJ

C07D 487/04
C07K 16/28

In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R, R, and Rare as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

2021012, Apr 29, 2021

Oct 27, 2020

17/081477

- Rahway NJ, US
Symon Gathiaka - Waltham MA, US
Yongxin Han - Needham MA, US
Xiaoshen Ma - Boston MA, US
Ryan D. Otte - Natick MA, US
David L. Sloman - Newton MA, US
Thomas H. Graham - Somerville MA, US
Timothy Henderson - Natick MA, US
Elizabeth Hennessy - Weston MA, US
Anandan Palani - Needham MA, US

C07D 498/22
A61P 35/00
A61K 31/519
C07D 471/22
C07D 519/00

The disclosure provides compounds of Formula (I)or a pharmaceutically acceptable salt thereof, wherein W, W, Y, Z, M, L, C, C, R, R, R, R, R, R, Rand the subscripts m, n, q, and r are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

2019033, Oct 31, 2019

Nov 13, 2017

16/461902

Thomas H. Graham - Boston MA, US
Wensheng LIU - Edison NJ, US
Clare TUDGE - Chatham NJ, US
Andreas VERRAS - New York NY, US
Jinlong JIANG - Kenilworth NJ, US
- Rahway NJ, US

Merck Sharp & Dohme Corp. - Rahway NJ

C07D 515/08
C07D 409/12
C07D 401/12
C07D 403/12
C07D 231/56
C07D 405/12
C07D 487/04
C07D 417/12
C07D 413/12
C07D 409/14

The present invention relates to a compound represented by formula I′: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

2019027, Sep 12, 2019

Nov 13, 2017

16/461880

Thomas H. GRAHAM - Boston MA, US
Jinlong JIANG - Kenilworth NJ, US
Clare TUDGE - Chatham NJ, US
- Rahway NJ, US

Merck Sharp & Dohme Corp. - Rahway NJ

C07D 409/12
A61P 1/16
C07D 209/08
C07D 401/12
C07D 413/12
C07D 409/14

The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

2018019, Jul 12, 2018

May 20, 2016

15/575433

- Rahway NJ, US
Thomas H. Graham - Quincy MA, US
Sherman T. Waddell - Westfield NJ, US
John A. McCauley - Maple Glen PA, US
Andrew W. Stamford - Chatham NJ, US
John M. Sanders - Hatfield PA, US
Lihong Hu - Shanghai, CN
Jiaqiang Cai - Shanghai, CN
Lianyun Zhao - Shanghai, CN

MERCK SHARP & DOHME CORP. - Rahway NJ

C07D 491/147
A61K 31/4375
A61P 31/18
C07D 471/14

The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R, R, R, R, R, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.

2016010, Apr 21, 2016

Apr 18, 2014

14/892754

- Rahway NJ, US
Timothy J. Hartingh - Blue Bell PA, US
Izzat T. Raheem - Doylestown PA, US
John Schreier - Harleysville PA, US
John Sisko - Lansdale PA, US
John Wai - Harleysville PA, US
Thomas H. Graham - Scotch Plains NJ, US
Lihong Hu - Shanghai, CN
Xuanjia Peng - Shanghai, CN

Merck Sharp & Dohme Corp. - Rahway NJ

C07D 498/16
A61K 45/06
A61K 31/4985
A61K 31/5383
C07D 471/16

The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R-R, A, X and n are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.