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1. WO2022007629 - CRYSTAL FORM OF UPADACITINIB, PREPARATION METHOD THEREFOR, AND USE THEREOF

Publication Number WO/2022/007629
Publication Date 13.01.2022
International Application No. PCT/CN2021/101784
International Filing Date 23.06.2021
IPC
C07D 487/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61K 31/4985 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 29/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants
  • 苏州科睿思制药有限公司 CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD. [CN]/[CN]
Inventors
  • 陈敏华 CHEN, Minhua
  • 张婧 ZHANG, Jing
Priority Data
202010653055.808.07.2020CN
202010991590.417.09.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) CRYSTAL FORM OF UPADACITINIB, PREPARATION METHOD THEREFOR, AND USE THEREOF
(FR) FORME CRISTALLINE D'UPADACITINIB, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 乌帕替尼的晶型及其制备方法和用途
Abstract
(EN) A new crystal form of upadacitinib and a preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of a JAK1 inhibitor drug and drugs for treating rheumatic arthritis, Crohn's disease, ulcerative colitis, atopic dermatitis, and psoriatic arthritis. Compared with the prior art, the crystal form of upadacitinib has one or more improved characteristics and is of great value for the optimization and development of drugs in the future.
(FR) La présente invention concerne une nouvelle forme cristalline d'upadacitinib et son procédé de préparation, une composition pharmaceutique contenant la forme cristalline, et l'utilisation de la forme cristalline dans la préparation d'un médicament à base d'inhibiteur de la JAK1 et de médicaments pour le traitement de la polyarthrite rhumatoïde, de la maladie de Crohn, de la rectocolite hémorragique, de la dermatite atopique et de l'arthrite psoriasique. La forme cristalline d'upadacitinib présente une ou plusieurs caractéristiques améliorées par rapport à l'état de la technique, et est d'une grande valeur pour l'optimisation et le développement de médicaments à l'avenir.
(ZH) 一种乌帕替尼的新晶型及其制备方法,含有该晶型的药物组合物,以及该晶型在制备JAK1抑制剂药物和治疗类风湿性关节炎、克罗恩病、溃疡性结肠炎、异位性皮炎和银屑病关节炎药物中的用途。所述乌帕替尼晶型比现有技术具有一种或多种改进的特性,对未来该药物的优化和开发具有重要价值。
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