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1. WO2022001820 - CRYSTALLINE FORM OF HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

Publication Number WO/2022/001820
Publication Date 06.01.2022
International Application No. PCT/CN2021/102068
International Filing Date 24.06.2021
IPC
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/437 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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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)
A61P 11/14 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
14Antitussive agents
A61P 13/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 11/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
Applicants
  • 武汉朗来科技发展有限公司 WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD. [CN]/[CN]
Inventors
  • 王亮 WANG, Liang
  • 娄军 LOU, Jun
  • 洪华云 HONG, Huayun
  • 郭晓丹 GUO, Xiaodan
  • 钱丽娜 QIAN, Lina
  • 张轶涵 ZHANG, Yihan
  • 陈永凯 CHEN, Yongkai
  • 王朝东 WANG, Chaodong
Agents
  • 上海弼兴律师事务所 SHANGHAI BESHINING LAW OFFICE
Priority Data
202010610052.629.06.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) CRYSTALLINE FORM OF HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
(FR) FORME CRISTALLINE D'UN COMPOSÉ HÉTÉROCYCLIQUE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 杂环类化合物的晶型及其制备方法和应用
Abstract
(EN) Provided are a crystalline form of a compound represented by formula A, the crystalline form being crystalline form I, crystalline form II, crystalline form III, crystalline form IV, crystalline form V, crystalline form VI, crystalline form VII, crystalline form VIII or crystalline form IX, a preparation method therefor, a composition thereof, and an application thereof in the preparation of a P2X3 receptor antagonist or an application thereof in the preparation of drugs preventing and/or treating pains, urinary tract illness or respiratory system illness. The compound has high P2X3 antagonist activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
(FR) L'invention concerne une forme cristalline d'un composé représenté par la formule A, la forme cristalline étant une forme cristalline I, forme cristalline II, forme cristalline III, forme cristalline IV, forme cristalline V, forme cristalline VI, forme cristalline VII, forme cristalline VIII ou forme cristalline IX, un procédé de préparation correspondant, une composition associée, et leur utilisation dans la préparation d'un antagoniste du récepteur P2X3 ou leur utilisation dans la préparation de médicaments pour la prévention et/ou le traitement de douleurs, d'une maladie des voies urinaires ou d'une maladie du système respiratoire. Le composé a une activité antagoniste de P2X3 élevée, et a une bonne sélectivité, une faible toxicité, une bonne stabilité métabolique et une faible influence sur le goût.
(ZH) 提供了一种如式A所示的化合物的晶型:所述晶型是晶型I、晶型II、晶型III、晶型IV、晶型V、晶型VI、晶型VII、晶型VIII或晶型IX,及其制备方法、组合物以及其在制备P2X3受体拮抗剂中的应用,或者在制备用于预防和/或治疗疼痛、泌尿道疾病或呼吸系统疾病的药物中的应用。所述化合物具有高的P2X3拮抗活性,且具有较好的选择性,毒性较低、代谢稳定性较好、味觉影响较小。
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