NOVEL PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF SOLUBLE GUANYLATE CYCLASE STIMULATORS

WIPO Patent Application WO/2019/140095

A1

The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I 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.

WALLACE DEBRA JANE (US)
ZHOU FENGER (US)
WANG YUGUANG (US)
NAKAI TAKASHI (US)
KARNATI VISHNU VARDHAN REDDY (US)
SCHAIRER WAYNE C (US)
KISSEL WILLAIM (US)
XUE SONG (US)
HASHASH AHMAD (US)

PCT/US2019/013060

July 18, 2019

January 10, 2019

Click for automatic bibliography generation  

CYCLERION THERAPEUTICS INC (US)

C07D413/14; C07C237/06; C07D239/34; C07D263/06

WO2017095697A1	2017-06-08
WO2016044447A1	2016-03-24

US20170137439A1

2017-05-18

TAKASHI NAKAI ET AL: "Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans", ACS MEDICINAL CHEMISTRY LETTERS, vol. 7, no. 5, 12 May 2016 (2016-05-12), pages 465 - 469, XP055406060, ISSN: 1948-5875, DOI: 10.1021/acsmedchemlett.5b00479
"Handbook of Chemistry and Physics", 1994
THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
"March's Advanced Organic Chemistry", 2001, JOHN WILEY & SONS

DAVIS, Steven, G. et al. (US)

View/Download PDF      PDF Help

Previous Patent: CARDIAC RESYNCHRONIZATION THERAPY DIAGNOSTICS

Next Patent: HEADSET WITH ADJUSTABLE MICROPHONE SUPPORT AND METHOD FOR ADJUSTING MICROPHONE