CN110582279A - 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]吡唑的共晶，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]吡唑的共晶，其制备方法和药物组合物 Download PDF

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CN110582279A
CN110582279A CN201780090404.6A CN201780090404A CN110582279A CN 110582279 A CN110582279 A CN 110582279A CN 201780090404 A CN201780090404 A CN 201780090404A CN 110582279 A CN110582279 A CN 110582279A
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crystal
monohydrate
succinic acid
fumaric acid
pyrrolo
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CN110582279B (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
    • C07D401/00—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
    • C07D401/14—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 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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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)与共晶形成物形成的共晶，与Galunisertib已知的固体形式相比，本发明的共晶在稳定性、溶解度等方面具有优势。本发明还涉及所述共晶的晶型及其制备方法，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 (21)

  1. PCT国内申请，权利要求书已公开。
CN201780090404.6A 2017-03-21 2017-03-21 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]吡唑的共晶，其制备方法和药物组合物 Active CN110582279B (zh)

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PCT/CN2017/077459 WO2018170724A1 (zh) 2017-03-21 2017-03-21 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]吡唑的共晶，其制备方法和药物组合物

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CN110582279B CN110582279B (zh) 2023-07-14

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WO2018170724A1 (zh) 2017-03-21 2018-09-27 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]吡唑的共晶，其制备方法和药物组合物

Citations (4)

* 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
CN102424681A (zh) * 2011-10-24 2012-04-25 华东师范大学 酰基四氢-β-咔啉类化合物及其衍生物、用途及其制备方法
WO2014072517A1 (en) * 2012-11-12 2014-05-15 Institució Catalana De Recerca I Estudis Avançats Methods and kits for the prognosis of colorectal cancer
WO2016123573A1 (en) * 2015-01-30 2016-08-04 President And Fellows Of Harvard College Peritumoral and intratumoral materials for cancer therapy

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7872020B2 (en) 2005-07-22 2011-01-18 Eli Lilly And Company TGF-β inhibitors
WO2018170724A1 (zh) 2017-03-21 2018-09-27 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]吡唑的共晶，其制备方法和药物组合物

Patent Citations (4)

* 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
CN102424681A (zh) * 2011-10-24 2012-04-25 华东师范大学 酰基四氢-β-咔啉类化合物及其衍生物、用途及其制备方法
WO2014072517A1 (en) * 2012-11-12 2014-05-15 Institució Catalana De Recerca I Estudis Avançats Methods and kits for the prognosis of colorectal cancer
WO2016123573A1 (en) * 2015-01-30 2016-08-04 President And Fellows Of Harvard College Peritumoral and intratumoral materials for cancer therapy

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
徐萍等: "《药物化学》", 31 March 2008, 北京大学医学出版社 *

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WO2018170724A1 (zh) 2018-09-27
US20200017470A1 (en) 2020-01-16
CN110582279B (zh) 2023-07-14
US10995083B2 (en) 2021-05-04

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