CN109311891A - 作为jak抑制剂的吡咯并嘧啶化合物的结晶 - Google Patents

作为jak抑制剂的吡咯并嘧啶化合物的结晶 Download PDF

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Publication number
CN109311891A
CN109311891A CN201780037131.9A CN201780037131A CN109311891A CN 109311891 A CN109311891 A CN 109311891A CN 201780037131 A CN201780037131 A CN 201780037131A CN 109311891 A CN109311891 A CN 109311891A
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formulas
compound shown
crystallization
crystalline
compound
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CN201780037131.9A
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CN109311891B (zh
Inventor
周舟
张爱明
张喜全
姚华东
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Capital Pharmaceutical Holdings Beijing Co ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • 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
    • 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

Abstract

本申请属于医药化学领域。具体而言，本申请涉及作为JAK抑制剂的吡咯并嘧啶化合物(式I)的结晶A和结晶B，还涉及结晶A和结晶B的制备方法、包含结晶A或结晶B的结晶组合物、包含结晶A或结晶B或其结晶组合物的药物组合物以及它们的医药用途。本申请的结晶A和结晶B具有纯度高、结晶度高、稳定性好等优点。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN201780037131.9A 2016-06-16 2017-06-15 作为jak抑制剂的吡咯并嘧啶化合物的结晶 Active CN109311891B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2016104359474 2016-06-16
CN201610435947.4A CN107759600A (zh) 2016-06-16 2016-06-16 作为jak抑制剂的吡咯并嘧啶化合物的结晶
PCT/CN2017/088429 WO2017215630A1 (zh) 2016-06-16 2017-06-15 作为jak抑制剂的吡咯并嘧啶化合物的结晶

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CN109311891A true CN109311891A (zh) 2019-02-05
CN109311891B CN109311891B (zh) 2020-09-04

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CN201780037131.9A Active CN109311891B (zh) 2016-06-16 2017-06-15 作为jak抑制剂的吡咯并嘧啶化合物的结晶

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US (1) US10626118B2 (zh)
EP (1) EP3473626B1 (zh)
JP (1) JP6986032B2 (zh)
KR (1) KR102523564B1 (zh)
CN (2) CN107759600A (zh)
AU (1) AU2017284702B2 (zh)
CA (1) CA3026602A1 (zh)
ES (1) ES2886910T3 (zh)
RU (1) RU2746045C2 (zh)
TW (1) TWI753918B (zh)
WO (1) WO2017215630A1 (zh)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107759600A (zh) 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
CN107513069A (zh) * 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
CN113242859B (zh) 2018-12-24 2023-04-14 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物的治疗用途及其固体药物组合物
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021180093A1 (zh) * 2020-03-09 2021-09-16 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物的治疗噬血细胞综合征的用途
WO2022268083A1 (zh) * 2021-06-21 2022-12-29 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物及其药物组合物治疗慢性移植物抗宿主病的用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103214483A (zh) * 2005-12-13 2013-07-24 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
CN105777754A (zh) * 2014-12-16 2016-07-20 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009003913A (es) * 2006-10-27 2009-04-24 Signal Pharm Llc Formas solidas que comprenden 4-[9-(tetrahidro-furano-3-il)-8-(2,4 ,6-trifluoro-fenilamino)-9h-purin-2-ilamino]-ciclohexan-1-ol, composiciones de las mismas, y su uso.
EP2740731B1 (en) * 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
US20130310340A1 (en) * 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
EP3183253B1 (en) 2014-08-21 2018-06-27 ratiopharm GmbH Salt of (r)-3-(4-(7h-pyrrolo [2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3-cyclopentylpropanenitrile with benzenesulfonic acid
CN107759600A (zh) 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103214483A (zh) * 2005-12-13 2013-07-24 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
CN105777754A (zh) * 2014-12-16 2016-07-20 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物

Also Published As

Publication number Publication date
AU2017284702A1 (en) 2019-01-24
CN107759600A (zh) 2018-03-06
KR20190017977A (ko) 2019-02-20
KR102523564B1 (ko) 2023-04-19
TWI753918B (zh) 2022-02-01
RU2018145948A (ru) 2020-07-16
CA3026602A1 (en) 2017-12-21
RU2746045C2 (ru) 2021-04-06
ES2886910T3 (es) 2021-12-21
US20190330215A1 (en) 2019-10-31
JP6986032B2 (ja) 2021-12-22
US10626118B2 (en) 2020-04-21
AU2017284702B2 (en) 2021-05-06
CN109311891B (zh) 2020-09-04
JP2019521980A (ja) 2019-08-08
EP3473626A1 (en) 2019-04-24
WO2017215630A1 (zh) 2017-12-21
EP3473626A4 (en) 2020-02-19
EP3473626B1 (en) 2021-08-04
RU2018145948A3 (zh) 2020-10-16
TW201800413A (zh) 2018-01-01

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