Merck Sharp + Dohme Corp.

Annapurna Bio, Inc.

Haifeng Tang

Alexander Pasternak

Fa-Xiang Ding

Jinlong Jiang

Barbara A Pio

Shawn P Walsh

Shuzhi Dong

Jessica Frie

Aurash Shahripour

Xin Gu

Lihu Yang

Jing Su

Harry R Chobanian

Yan Guo

Takao Suzuki

Weidong Pan

Xianhai Huang

Zhe Nie

Zhicai Wu

Dooseop Kim

Zhi-Cai Shi

Wanying Sun

Weiguo Liu

Yuping Zhu

Tesfaye Biftu

William K Hagmann

Guoqing Li

Helen Y Chen

Li Xiao

Christina B Madsen-Duggan

John P Caldwell

Marc A Labroli

Kevin Michael Belyk

Haiqun Tang

Sookhee Nicole Ha

Dexi Yang

Min K Park

Timothy Allen Blizzard

Paul E Finke

Changyou Zhou

Songnian Lin

Anthony K Ogawa

Timothy A Blizzard

Qinghong Fu

Reynalda Keh Dejesus

Mihir Mandal

Shu-Wei Yang

Nardos H Teumelsan

Michael Allen Hanson

Yang Yu

Brian Cato

Reynalda De Jesus

Sarah Boyce

Reynalda K DeJesus

Reynalda DeJesus

Ginny Dai Ho

Yi Zang

Christine Yang

Zheng Tan

Hongwu Wang

Dipshikha Biswas

Sandra J Koseoglu

Sang Ho Lee

Terry Roemer

Christopher Michael Tan

Hao Wang

Charles J Gill

Clare London

Linda Brockunier

Christopher W Plummer

Zhiqiang Zhao

Jacqueline D Hicks

Jianping Pan

Yuhua Huang

Zhiqiang Guo

Katherine Young

Ming Wang

Cangming Yang

Ronald Dale Ferguson, Ii

Hong Dong Chu

Rudrajit Mal

Matthew Lombardo

Candido Gude

Zack Zhiqiang Guo

Min Ge

Zhifa Pu

David N Hunter

Jinlong Jian

Alex Pasternak

Eric Dean Cline

Sunita Malkani

Ronald Dale Ferguson

Min Park

Kevin M Belyk

Reynalda Dejesus

Reynalda K Dejesus

Ronald Dale Ii Ferguson

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

Compounds and compositions for treating conditions associated with APJ receptor activity

Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic.

Oxazolidinones as TarO inhibitors

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor; gene symbol 'APLNR'). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor, gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition. Non-limiting examples of such diseases, disorders, or conditions include: (i) cardiovascular disease; (ii) metabolic disorders; (iii) diseases, disorders, and conditions associated with vascular pathology; and (iv) organ failure; (v) diseases, disorders, and conditions associated with infections (e.g., microbial infections); and (vi) diseases, disorders, or conditions that are sequela or comorbid with any of the foregoing or any disclosed herein. More particular non-limiting examples of such diseases, disorders, or conditions include pulmonary hypertension (e.g., PAH); heart failure; type II diabetes; renal failure; sepsis; and systemic hypertension.

The present invention relates to monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic. 

Chromane monobactam compounds for the treatment of bacterial infections

The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, Q, A, M, W, Rand Rare as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.

Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a &#x3b2;-lactam antibiotic. 

Oxazolidinones as taro inhibitors

The present invention provides compounds of Formula I (I) 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 chronic kidney disease and conditions associated with excessive salt and water retention. 

Inhibitors of the renal outer medullary potassium channel

The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, L, M, W, X, Y, Z, Rand Rare as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds. 

Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

The present invention provides compounds of Formula I 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 chronic kidney disease and conditions associated with excessive salt and water retention.

The present invention relates to compounds of formula I that are metallo-&#x3b2;-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with &#x3b2;-lactam antibiotics for overcoming resistance. 

Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors

Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as 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 chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included. 

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Metuchen, NJ, United States of America

Haifeng Tang