Cyclerion Therapeutics, Inc.

Ironwood Pharmaceuticals, Inc.

Microbia, Inc.

Timothy Claude Barden

Ara Mermerian

Paul A Renhowe

Rajesh R Iyengar

Takashi Nakai

Glen Robert Rennie

G-Yoon Jamie Im

Mark G Currie

Joon Jung

Thomas Wai-Ho Lee

Karthik Iyer

James Edward Sheppeck

Nicholas Robert Perl

Xiang Y Yu

Joel D Moore

Colleen Hudson

Kimberly Kafadar Long

George Todd Milne

Lei Jia

James Jia

John Jeffrey Talley

Kevin Sprott

Charles Kim

Jane Yang

Angelika Fretzen

G Todd Milne

Brian Cali

James Philip Pearson

Song Xue

Daniel P Zimmer

Vishnu Vardhan Reddy Karnati

Robert C Livingston

Wayne C Schairer

Kim Tang

Peter Germano

Wayne Schairer

Craig N Zimmerman

Barbara B Chen

Peter Scott Yorgey

Yueh-Tyng Chien

Nicholas Perl

Bo Peng

Wilmin Bartolini

Jing-Jing Yang

Jeffrey Segal

Regina Lundrigan-Soucy

Eduardo Martinez

Regina Lundigran

Regina Lundrigan

Nisha Perez

Stephen Antonelli

Paul Allen Renhowe

Paul Allan Renhowe

Mark Currie

The present disclosure relates to novel processes for the preparation of compounds useful as stimulators of soluble guanylate cyclase (sGC). These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula (I), including Compound (I), Compound (IA) and Compound (IB), in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.

Processes for preparation of soluble guanylate cyclase stimulators

Compounds of Formulae I' and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed. 

sGC stimulators

The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula (I). 

SGC stimulators

The present patent application discloses the compounds according to Formula (I) shown below, or pharmaceutically acceptable salts thereof wherein J, n, R, R, R, R, R, m and X as defined herein. 

Phosphorus prodrugs of pyrazolo-substituted pyrimidine sGC stimulators

The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable. The compounds are of Formula I: 

The present patent application discloses at least the compounds according to Formula I' shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, ring E, J, n, J, J, X, Z, Z, R, R, Y, R, o and W are as defined herein.

The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. Compounds of the invention are described in Table 1.

FAAH inhibitors

Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.

2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators

A compound of Formula (I): or a pharmaceutically acceptable salt of the compound. Also described are pharmaceutical formulations thereof and methods of using the same.

NONOate derivatives and uses thereof

Growing community of inventors

Salem, MA, United States of America

Timothy Claude Barden