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1. WO2018153364 - OSALMID CRYSTAL FORM II, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF

Publication Number WO/2018/153364
Publication Date 30.08.2018
International Application No. PCT/CN2018/077185
International Filing Date 26.02.2018
IPC
C07C 231/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
08from amides by reaction at nitrogen atoms of carboxamide groups
C07C 231/24 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
22Separation; Purification; Stabilisation; Use of additives
24Separation; Purification
C07C 235/64 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
58with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring
64having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
CPC
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07C 231/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
08from amides by reaction at nitrogen atoms of carboxamide groups
C07C 231/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
22Separation; Purification; Stabilisation; Use of additives
24Separation; Purification
C07C 235/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
58with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
64having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
Applicants
  • 中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]/[CN]
Inventors
  • 朱维良 ZHU, Weiliang
  • 徐志建 XU, Zhijian
  • 李波 LI, Bo
  • 张勇 ZHANG, Yong
Agents
  • 北京金信知识产权代理有限公司 KINGSOUND & PARTNERS
Priority Data
201710108969.427.02.2017CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) OSALMID CRYSTAL FORM II, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF
(FR) FORME II DU CRISTAL D'OSALMIDE, SON PROCÉDÉ DE PRÉPARATION ET SES APPLICATIONS
(ZH) 柳胺酚晶型II、其制备方法及其应用
Abstract
(EN) Disclosed are an osalmid crystal form II, a preparation method therefor, and applications thereof. An XRPD indicated by an 2θ angle, of the crystal form has characteristic peaks at the diffraction angels 7.527±0.2, 13.653±0.2, 14.644±0.2, 15.037±0.2, 19.62±0.2, 20.092±0.2, 20.454±0.2, 22.618±0.2, 24.45±0.2, 25.226±0.2, 26.288±0.2, 26.638±0.2, 28.516±0.2, 29.373±0.2, 29.723±0.2, 31.605±0.2, 35.794±0.2 and 38.104±0.2. The crystalline form has excellent physicochemical properties and drug forming performance, has a simple preparation method, lower crystal form hygroscopicity, good stability and good reproducibility.
(FR) L'invention concerne une forme II du cristal d'osalmide, son procédé de préparation et ses applications. Selon l'invention, une XRPD indiquée par un angle 2θ, de la forme cristalline a des pics caractéristiques aux angles de diffraction 7,527±0,2, 13,653±0,2, 14,644±0,2, 15,037±0,2, 19,62±0,2, 20,092±0,2, 20,454±0,2, 22,618±0,2, 24,45±0,2, 25,226±0,2, 26,288±0,2, 26,638±0,2, 28,516±0,2, 29,373±0,2, 29,723±0,2, 31,605±0,2, 35,794±0,2 et 38,104±0,2. La forme cristalline a d'excellentes propriétés physicochimiques et une excellente performance de formation de médicament, présente un procédé de préparation simple, une basse hygroscopicité de forme cristalline, une bonne stabilité et une bonne reproductibilité.
(ZH) 公开了柳胺酚晶型II、其制备方法及其应用。该晶型以2θ角度表示的XRPD在衍射角7.527±0.2、13.653±0.2、14.644±0.2、15.037±0.2、19.62±0.2、20.092±0.2、20.454±0.2、22.618±0.2、24.45±0.2、25.226±0.2、26.288±0.2、26.638±0.2、28.516±0.2、29.373±0.2、29.723±0.2、31.605±0.2、35.794±0.2、38.104±0.2处具有特征峰。该晶型具有优良的理化性质和成药性能,制备方法简单,晶型吸湿性小,具有良好的稳定性,重现性好能。
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