CN110582497A - 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 - Google Patents

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 Download PDF

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CN110582497A
CN110582497A CN201780090261.9A CN201780090261A CN110582497A CN 110582497 A CN110582497 A CN 110582497A CN 201780090261 A CN201780090261 A CN 201780090261A CN 110582497 A CN110582497 A CN 110582497A
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solvent
crystalline form
stirring
crystallization
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CN110582497B (zh
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盛晓红
盛晓霞
汪晶
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SOLIPHARMA LLC
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    • 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
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    • 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

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Abstract

本发明涉及式(I)所示的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(Galunisertib或LY2157299)的晶型，与Galunisertib已知的固体形式相比，本发明的晶型在溶解度、吸湿性、晶型稳定性、形貌等方面具有优势。本发明还涉及所述Galunisertib晶型的制备方法，其药物组合物及其在制备用于预防和/或治疗与TGF‑β有关的疾病中的用途。

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN201780090261.9A 2017-03-17 2017-03-17 Galunisertib的晶型及其制备方法和药物组合物 Active CN110582497B (zh)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109548403A (zh) * 2016-07-07 2019-03-29 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途

Families Citing this family (2)

* 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
WO2022235621A1 (en) * 2021-05-03 2022-11-10 Thirona Bio, Inc. Methods for treating a pulmonary disease with an alk-5 (tgf beta r1) inhibitor

Citations (3)

* 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
US7872020B2 (en) * 2005-07-22 2011-01-18 Eli Lilly And Company TGF-β inhibitors
CN102711799A (zh) * 2009-11-10 2012-10-03 纽约市哥伦比亚大学理事会 用于创伤治疗的组合物和方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109548403A (zh) 2016-07-07 2019-03-29 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途
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

Patent Citations (3)

* 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
US7872020B2 (en) * 2005-07-22 2011-01-18 Eli Lilly And Company TGF-β inhibitors
CN102711799A (zh) * 2009-11-10 2012-10-03 纽约市哥伦比亚大学理事会 用于创伤治疗的组合物和方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHENGHUA JIN等: "Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY》 *
JEFFRY K. NIEMEIER等: "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》 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109548403A (zh) * 2016-07-07 2019-03-29 苏州科睿思制药有限公司 Galunisertib的晶型及其制备方法和用途

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US20200399272A1 (en) 2020-12-24
US11111248B2 (en) 2021-09-07
WO2018165979A1 (zh) 2018-09-20

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