CN109548403A - Galunisertib的晶型及其制备方法和用途 - Google Patents

Galunisertib的晶型及其制备方法和用途 Download PDF

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Publication number
CN109548403A
CN109548403A CN201780028843.4A CN201780028843A CN109548403A CN 109548403 A CN109548403 A CN 109548403A CN 201780028843 A CN201780028843 A CN 201780028843A CN 109548403 A CN109548403 A CN 109548403A
Authority
CN
China
Prior art keywords
crystal form
present
crystal
galunisertib
moist
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201780028843.4A
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English (en)
Inventor
陈敏华
张炎锋
陈宇浩
高慧
陆飞
张晓宇
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Crystal Pharmaceutical Suzhou Co Ltd
Original Assignee
Crystal Pharmaceutical Suzhou Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Crystal Pharmaceutical Suzhou Co Ltd filed Critical Crystal Pharmaceutical Suzhou Co Ltd
Publication of CN109548403A publication Critical patent/CN109548403A/zh
Pending legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Galunisertib的晶型A及其制备方法和用途，该晶型具有良好的稳定性和溶解性、较低的引湿性等有利性能，对未来该药物的优化和开发具有重要价值。

Description

PCT国内申请，说明书已公开。

Claims (6)

  1. PCT国内申请，权利要求书已公开。
CN201780028843.4A 2016-07-07 2017-07-21 Galunisertib的晶型及其制备方法和用途 Pending CN109548403A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610533326 2016-07-07
PCT/CN2017/092233 WO2018006870A1 (zh) 2016-07-07 2017-07-21 Galunisertib的晶型及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN109548403A true CN109548403A (zh) 2019-03-29

Family

ID=60912012

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780028843.4A Pending CN109548403A (zh) 2016-07-07 2017-07-21 Galunisertib的晶型及其制备方法和用途

Country Status (3)

Country Link
US (1) US10604528B2 (zh)
CN (1) CN109548403A (zh)
WO (1) WO2018006870A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11111248B2 (en) 2017-03-17 2021-09-07 Hangzhou Solipharma Co., Ltd. Crystal form of 2-(6-methyl-pyridin-2-yl)-3-yl-[6-amido-quinolin-4-yl]-5,6-dihydro-4H-pyrrolo[1,2-B]pyrazole, preparation method therefor and pharmaceutical composition thereof
WO2019042383A1 (zh) * 2017-08-31 2019-03-07 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
WO2019137027A1 (zh) * 2018-01-12 2019-07-18 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
WO2023244132A1 (en) * 2022-06-17 2023-12-21 Saúde Viável, S.A. Galunisertib for use in the treatment of androgenic alopecia

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1714090A (zh) * 2002-11-22 2005-12-28 伊莱利利公司 喹啉基－吡咯并吡唑化合物
CN110582497A (zh) * 2017-03-17 2019-12-17 杭州领业医药科技有限公司 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的晶型及其制备方法和药物组合物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6627646B2 (en) * 2001-07-17 2003-09-30 Sepracor Inc. Norastemizole polymorphs
BRPI0613639A2 (pt) * 2005-07-22 2012-02-22 Lilly Co Eli composto, composição farmacêutica, uso do composto, e, processo para produzir um composto

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1714090A (zh) * 2002-11-22 2005-12-28 伊莱利利公司 喹啉基－吡咯并吡唑化合物
CN110582497A (zh) * 2017-03-17 2019-12-17 杭州领业医药科技有限公司 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的晶型及其制备方法和药物组合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JEFFRY K. NIEMEIER ET AL.: "Application of Kinetic Modeling and Competitive Solvent Hydrolysis in the Development of a Highly Selective Hydrolysis of a Nitrile to an Amide", 《ORG. PROCESS RES. DEV.》 *

Also Published As

Publication number Publication date
WO2018006870A1 (zh) 2018-01-11
US10604528B2 (en) 2020-03-31
US20190241572A1 (en) 2019-08-08

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