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1. WO2020228642 - CRYSTALLIZATION OF SMAC MIMIC USED AS IAP INHIBITOR AND PREPARATION METHOD THEREOF

Publication Number WO/2020/228642
Publication Date 19.11.2020
International Application No. PCT/CN2020/089437
International Filing Date 09.05.2020
IPC
C07K 5/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
C07D 403/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4045 2006.01
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 正大天晴药业集团股份有限公司 CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. [CN]/[CN]
Inventors
  • 刘迎春 LIU, Yingchun
  • 徐招兵 XU, Zhaobing
  • 胡利红 HU, Lihong
  • 丁照中 DING, Charles Z.
  • 朱兴训 ZHU, Xingxun
  • 陈曙辉 CHEN, Shuhui
Agents
  • 北京林达刘知识产权代理事务所(普通合伙) LINDA LIU & PARTNERS
Priority Data
201910389970.810.05.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) CRYSTALLIZATION OF SMAC MIMIC USED AS IAP INHIBITOR AND PREPARATION METHOD THEREOF
(FR) CRISTALLISATION D'UN MIMÉTIQUE DE SMAC UTILISÉ EN TANT QU'INHIBITEUR D'IAP ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种用作IAP抑制剂的SMAC模拟物的结晶及其制备方法
Abstract
(EN)
Provided are a crystallization of an SMAC mimic used as an IAP inhibitor and a preparation method thereof; also comprised is the use of said crystallization in the preparation of a drug for treating cancer benefiting from cIAP1 inhibition. The compound of formula (I) has high crystallization stability and low hygroscopicity, and has advantages in terms of physical properties, safety, and metabolic stability, and has high drug value.
(FR)
L'invention concerne une cristallisation d'un mimétique de SMAC utilisé en tant qu'inhibiteur d'IAP et son procédé de préparation; l'utilisation de ladite cristallisation dans la préparation d'un médicament pour le traitement du cancer bénéficiant d'une inhibition de cIAP1. Le composé de formule (I) présente une stabilité de cristallisation élevée et une faible hygroscopicité, et présente des avantages en termes de propriétés physiques, de sécurité et de stabilité métabolique, et a une valeur médicamenteuse élevée.
(ZH)
一种用作IAP抑制剂的SMAC模拟物的结晶及其制备方法,还包括所述结晶在制备治疗受益于cIAP1抑制的癌症的药物中的用途。所述式(I)化合物的结晶稳定性高、吸湿性小,在物理性质、安全性和代谢稳定性方面具有优势,有较高的成药价值。
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