Processes for preparing ASK1 inhibitors

US9771328B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9771328-B2
Application numberUS-201715413154-A
CountryUS
Kind codeB2
Filing dateJan 23, 2017
Priority dateDec 23, 2014
Publication dateSep 26, 2017
Grant dateSep 26, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.

First claim

Opening claim text (preview).

What is claimed is: 1. Crystalline 5-(4-cyclopropyl-1H-imidazol-1-1-2-fluoro-4-methylbenzoic acid hydrochloride (Compound of formula (D-a) Form II) characterized by an X-ray powder diffractogram comprising the following peaks: 8.7, 12.1, 25.7, and 26.3° 2θ±0.2° 2θ, as determined on a diffractometer using Cu—K□ radiation at a wavelength of 1.5406 Å. 2. Compound of formula (D-a) Form II according to claim 1 , wherein the diffractogram comprises additional peaks at 17.3, 19.0, 22.4, 28.6, and 29.7° 2θ±0.2° 2θ. 3. Compound of formula (D-a) Form II according to claim 1 , wherein the diffractogram is substantially as shown in FIG. 4 . 4. Compound of formula (D-a) Form II according to claim 1 , characterized by a differential scanning calorimetry (DSC) curve that comprises an endotherm at about 217° C. 5. Compound of formula (D-a) Form II according to claim 1 , wherein the DSC curve is substantially as shown in FIG. 5 .

Assignees

Inventors

Classifications

  • Drugs for disorders of the cardiovascular system · CPC title

  • for hyperglycaemia, e.g. antidiabetics · CPC title

  • Immunosuppressants, e.g. drugs for graft rejection · CPC title

  • Antihypertensives · CPC title

  • Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

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What does patent US9771328B2 cover?
The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.
Who is the assignee on this patent?
Gilead Sciences Inc
What technology area does this patent fall under?
Primary CPC classification C07D233/64. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Sep 26 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).