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1. WO2020001460 - PHARMACEUTICALLY ACCEPTABLE SALT, CRYSTAL FORM OF AZABICYCLO SUBSTITUTED TRIAZOLE DERIVATIVE AND PREPARATION METHOD

Publication Number WO/2020/001460
Publication Date 02.01.2020
International Application No. PCT/CN2019/092940
International Filing Date 26.06.2019
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4196
1,2,4-Triazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
C07D 401/14 (2006.01)
C07D 405/14 (2006.01)
A61K 31/44 (2006.01)
A61K 31/4196 (2006.01)
A61P 15/00 (2006.01)
CPC
A61K 31/4196
A61K 31/44
A61P 15/00
C07D 401/14
C07D 405/14
Applicants
  • 江苏恒瑞医药股份有限公司 JIANGSU HENGRUI MEDICINE CO., LTD. [CN/CN]; 中国江苏省连云港市 经济技术开发区昆仑山路7号 No. 7 Kunlunshan Road Economic and Technological Development Zone Lianyungang, Jiangsu 222047, CN
  • 上海恒瑞医药有限公司 SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD [CN/CN]; 中国上海市 闵行经济技术开发区文井路279号 No. 279 Wenjing Road Economic and Technological Development Zone, Minhang District Shanghai 200245, CN
Inventors
  • 王林 WANG, Lin; CN
  • 邵启云 SHAO, Qiyun; CN
  • 冯君 FENG, Jun; CN
  • 贺峰 HE, Feng; CN
  • 曹笑立 CAO, Xiaoli; CN
  • 杜振兴 DU, Zhenxing; CN
Agents
  • 上海弼兴律师事务所 SHANGHAI BESHINING LAW OFFICE; 中国上海市 小木桥路681号外经大厦21楼 21st Floor SFECO Mansion 681 Xiaomuqiao Road Shanghai 200032, CN
Priority Data
201810676344.227.06.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PHARMACEUTICALLY ACCEPTABLE SALT, CRYSTAL FORM OF AZABICYCLO SUBSTITUTED TRIAZOLE DERIVATIVE AND PREPARATION METHOD
(FR) SEL PHARMACEUTIQUEMENT ACCEPTABLE, FORME CRISTALLINE D'UN DÉRIVÉ DE TRIAZOLE SUBSTITUÉ PAR AZABICYCLO ET PROCÉDÉ DE PRÉPARATION
(ZH) 氮杂双环基取代的三唑类衍生物的可药用盐、晶型及制备方法
Abstract
(EN)
Provided are a pharmaceutically acceptable salt, a crystal form of an azabicyclo substituted triazole derivative and a preparation method therefor. In particular, provided are a pharmaceutically acceptable salt, a crystal form of a compound 1-(2-chloro-4-fluorophenyl)-3-(5-(methoxymethyl)-4-(6-methoxypyridine-3-yl)-4H-1,2,4-triazol-3-yl)-3-azabicyclo[3.1.0]hexane as shown in formula A, and a preparation method therefor. Relative to free bases, the pharmaceutically acceptable salt of the compound has a higher purity and an even better chemical stability, and is of great significance for developing a drug suitable for industrial production and having a good biological activity. (A)
(FR)
L'invention concerne un sel pharmaceutiquement acceptable, une forme cristalline d'un dérivé de triazole substitué par azabicyclo et un procédé de préparation associé. En particulier, l'invention concerne un sel pharmaceutiquement acceptable, une forme cristalline d'un composé 1-(2-chloro-4-fluorophényl)-3-(5-(méthoxyméthyl)-4-(6-méthoxypyridine-3-yl)-4H-1,2,4-triazol-3-yl)-3-azabicyclo[3.1.0]hexane comme représenté par la formule A, et un procédé de préparation associé. Le sel pharmaceutiquement acceptable du composé selon l'invention, par comparaison à des bases libres, a une pureté plus élevée et une stabilité chimique encore meilleure, et est d'une grande importance pour développer un médicament approprié pour une production industrielle et ayant une bonne activité biologique. (A)
(ZH)
本披露中提供了氮杂双环基取代的三唑类衍生物的可药用盐、晶型及制备方法。具体而言,本披露中提供了式A所示化合物1-(2-氯-4-氟苯基)-3-(5-(甲氧基甲基)-4-(6-甲氧基吡啶-3-基)-4H-1,2,4-三唑-3-基)-3-氮杂双环[3.1.0]己烷的可药用盐、晶型及制备方法。相对于自由碱而言,该化合物可药用盐具有更高的纯度,更为优异的化学稳定性,对开发适合工业生产且生物活性良好的药物具有重要意义。(A)
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