CN111278828A - 巴瑞替尼磷酸盐的新晶型及其制备方法 - Google Patents

巴瑞替尼磷酸盐的新晶型及其制备方法 Download PDF

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CN111278828A
CN111278828A CN201980005068.XA CN201980005068A CN111278828A CN 111278828 A CN111278828 A CN 111278828A CN 201980005068 A CN201980005068 A CN 201980005068A CN 111278828 A CN111278828 A CN 111278828A
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degrees
crystalline form
phosphate
crystal form
ray powder
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CN111278828B (zh
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雷鑫
简振鹏
潘家君
黄芳芳
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Guangdong HEC Pharmaceutical
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Sunshine Lake Pharma 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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Abstract

本发明提供了巴瑞替尼磷酸盐的新晶型及其制备方法，属于药物化学领域。所述晶型为晶型α或晶型β。所述晶型α的XRPD图含有如下2θ(误差±0.2度)值的特征峰：12.45,14.65,15.47,16.34,17.47,20.45,22.07,24.22,25.58,26.64,28.50,29.86度；所述晶型β的XRPD图含有如下2θ(误差±0.2度)值的特征峰：3.84,8.17,12.76,16.84,19.05,21.85,24.73度。所述晶型α，晶型β均具有较好的溶解性或稳定性，有利于储存、转移、生产工艺中操作，适于制备成制剂。

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PCT国内申请，说明书已公开。

Claims (16)

  1. PCT国内申请，权利要求书已公开。
CN201980005068.XA 2018-01-09 2019-01-07 巴瑞替尼磷酸盐的新晶型及其制备方法 Active CN111278828B (zh)

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CN201810017714 2018-01-09
CN2018100177141 2018-01-09
PCT/CN2019/070596 WO2019137325A1 (zh) 2018-01-09 2019-01-07 巴瑞替尼磷酸盐的新晶型及其制备方法

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015166434A1 (en) * 2014-05-01 2015-11-05 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
CN105601635A (zh) * 2016-02-01 2016-05-25 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐的a晶型、h晶型和i晶型及其制备方法
CN105693731A (zh) * 2016-01-26 2016-06-22 上海宣创生物科技有限公司 巴瑞克替尼a晶型及其制备方法
WO2016141891A1 (zh) * 2015-03-11 2016-09-15 苏州晶云药物科技有限公司 Jak抑制剂的晶型及其制备方法
CN107200742A (zh) * 2016-03-18 2017-09-26 罗欣生物科技（上海）有限公司 一种巴瑞克替尼磷酸盐晶体及其制备方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2016816A3 (cs) * 2016-12-21 2018-07-04 Zentiva, K.S. Krystalické formy 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrilu s kyselinou fosforečnou a způsob jejich přípravy

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015166434A1 (en) * 2014-05-01 2015-11-05 Sun Pharmaceutical Industries Limited Crystalline form of baricitinib
WO2016141891A1 (zh) * 2015-03-11 2016-09-15 苏州晶云药物科技有限公司 Jak抑制剂的晶型及其制备方法
CN105693731A (zh) * 2016-01-26 2016-06-22 上海宣创生物科技有限公司 巴瑞克替尼a晶型及其制备方法
CN105601635A (zh) * 2016-02-01 2016-05-25 上海宣创生物科技有限公司 巴瑞克替尼磷酸盐的a晶型、h晶型和i晶型及其制备方法
CN107200742A (zh) * 2016-03-18 2017-09-26 罗欣生物科技（上海）有限公司 一种巴瑞克替尼磷酸盐晶体及其制备方法

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