Merck Sharp + Dohme Corp.

The Scripps Research Institute

Expansion Therapeutics, Inc.

Timothy Allen Blizzard

Barbara A Pio

Helen Y Chen

Harry R Chobanian

Candido Gude

Tesfaye Biftu

William K Hagmann

Hubert B Josien

Bin Hu

Shawn P Walsh

Purakkattle J Biju

Zhengxia Chen

Mingxiang Cui

Jared N Cumming

Ravi P Nargund

Alexander Pasternak

Qun Dang

Jack D Scott

Haifeng Tang

Bing Li

Linus S Lin

Yan Guo

Christopher W Plummer

Jessica Frie

William J Greenlee

Joseph P Vacca

Jinlong Jiang

Feroze Ujjainwalla

Zhicai Wu

Ping Liu

Fa-Xiang Ding

Dooseop Kim

Songnian Lin

John S Debenham

Cheng Zhu

Zhi-Cai Shi

Bowei Wang

Derun Li

Shuzhi Dong

Richard Berger

Michael A Ellis

Brian T Campbell

Jiayi Xu

Kevin Michael Belyk

Matthew D Disney

Anilkumar G Nair

Meibi Dai

Aurash Shahripour

Mihir Mandal

Nelo R Rivera

Libo Xu

Zhiyong Hu

Bart Harper

Jason W Szewczyk

Rui Zhang

Matthew John Clements

Ming Wang

Dann Parker

Andy Jennings

Jason Eugene Imbriglio

Jinglai Hao

Ian Mangion

Brian Cato

Jane Yang Wu

Jeffrey Donald Hermes

Zack Zhiqiang Guo

Michael Shevlin

Sunita V Dewnani

Byron Dubois

Suzanne Rzuczek

Alexei Pushechnikov

Seongkon Kim

Reynalda K DeJesus

Reynalda De Jesus

Rebecca T Ruck

Christopher J Mortko

Zaihong Zhang

Ying Lv

Lili Tian

John Ndungu

Johnny Zhaoning Zhu

Frank P Dininno

Jerry Dwain Ii Morgan

Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.

Bis-benzimidazole compounds and methods of using the same

In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R, ring A, R, m, -L-, ring B, R, n, q, ring C, R, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. 

C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use

The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity. 

Isoquinoline derivatives as MGAT2 inhibitors

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 

Antidiabetic tricyclic compounds

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 

Antidiabetic substituted heteroaryl compounds

In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R, R, ring A, R, m, L, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. 

C-6 spirocarbocyclic iminothiadiazine dioxides as BACE inhibitors, compositions, and their use

The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is &#x2014;O&#x2014;, &#x2014;N(R), &#x2014;C(R)(R) or &#x2014;C(O)&#x2014;; and Y is &#x2014;O&#x2014;, &#x2014;N(R), &#x2014;C(R)(R) or &#x2014;C(O)&#x2014; and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD. 

Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists

This invention relates to compounds of Formula I-VI having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

Inhibitors of the Renal Outer Medullary Potassium channel

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 

Thrombin inhibitors

The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. 

Inhibitors of the renal outer medullary potassium channel

Substituted bicyclic beta-lactams of Formula I: (I), are &#x3b2;-lactamase inhibitors, wherein a, X, Rand Rare defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with &#x3b2;-lactam antibiotics. In particular, the compounds can be employed with a &#x3b2;-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to &#x3b2;-lactam antibiotics due to the presence of the &#x3b2;-lactamases.

&#x3b2;-lactamase inhibitors

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Princeton, NJ, United States of America

Timothy Allen Blizzard