Cyclerion Therapeutics, Inc.

William Kissel

Takashi Nakai

Song Xue

Ahmad Hashash

Vishnu Vardhan Reddy Karnati

Wayne C Schairer

Fenger Zhou

Yuguang Wang

Debra Jane Wallace

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.

Processes and intermediates for the preparation of soluble guanylate cyclase stimulators

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.

The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as simulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said simulators. 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. 

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Cambridge, MA, United States of America

William Kissel