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A kind of crystal form of bisulfate salt of jak kinase inhibitor and preparation method thereof

A crystal form and anti-solvent technology, which is applied in the field of preparing drugs for the treatment and/or prevention of arthritis diseases, and can solve problems such as poor solubility of crystal forms

Active Publication Date: 2021-01-15
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above crystal forms all have the defect of poor solubility, and it is necessary to explore further to find a crystal form with better solubility

Method used

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  • A kind of crystal form of bisulfate salt of jak kinase inhibitor and preparation method thereof
  • A kind of crystal form of bisulfate salt of jak kinase inhibitor and preparation method thereof
  • A kind of crystal form of bisulfate salt of jak kinase inhibitor and preparation method thereof

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Embodiment Construction

[0028] In the specification and claims of the present application, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. However, for a better understanding of the present invention, definitions and explanations of some related terms are provided below. In addition, when the definitions and explanations of terms provided in this application are inconsistent with the meanings commonly understood by those skilled in the art, the definitions and explanations of terms provided in this application shall prevail.

[0029] The "ketone solvent" in the present invention refers to a compound in which a carbonyl group (-C(O)-) is connected to two hydrocarbon groups. According to the different hydrocarbon groups in the molecule, ketones can be divided into aliphatic ketones, alicyclic ketones, aromatic ketones, Saturated and unsaturated ketones, specific examples include but not limited to: acetone, me...

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Abstract

The present invention relates to a crystal form of bisulfate of a JAK kinase inhibitor and a preparation method therefor. Specifically, the present invention relates to a crystal form III of (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazole-5-base)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-base)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate, and a preparation method therefor. The crystal form III of a compound represented by formula (I) in the present invention has good crystal stability, and a used crystallization solvent has low toxicity and low residue, and can be better used in clinical treatment.

Description

technical field [0001] The present invention relates to (3aR, 5s, 6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3- d] pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide hydrogen sulfate III crystal form and its preparation method, its application in pharmaceutical compositions and the III Use of the crystal form and the composition in the preparation of medicines for treating and / or preventing arthritis diseases. Background technique [0002] Arthritis is the most common chronic disease in the world. There are many causes of arthritis and different causes of joint damage. Currently, Tofacitinib (CP-690550) is a new oral JAK pathway inhibitor developed by Pfizer. Tofacitinib is the first-in-class drug for the treatment of rheumatoid arthritis. Based on the structure of Tofacitinib, WO2013091539 discloses a series of JAK kinase inhibitor compounds with in vivo and in vitro activity and high absorption. [0003] Patent application WO201419...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P19/02A61P29/00
CPCA61K31/519A61P19/02A61P29/00C07D487/04
Inventor 张全良刘兵高晓晖边林
Owner JIANGSU HENGRUI MEDICINE CO LTD
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