CN113874362A - 喹唑啉酮类化合物的晶型及其制备方法 - Google Patents

喹唑啉酮类化合物的晶型及其制备方法 Download PDF

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Publication number
CN113874362A
CN113874362A CN202080035113.9A CN202080035113A CN113874362A CN 113874362 A CN113874362 A CN 113874362A CN 202080035113 A CN202080035113 A CN 202080035113A CN 113874362 A CN113874362 A CN 113874362A
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China
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degrees
pi3k
formula
compound
crystal form
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CN202080035113.9A
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English (en)
Inventor
黄婧婕
殷毅杰
姚婷
于涛
吴成德
董加强
施斌
唐伟
杨文谦
王铁林
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Luoxin Health Technology Development Beijing Co ltd
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Luoxin Health Technology Development Beijing Co ltd
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Publication of CN113874362A publication Critical patent/CN113874362A/zh
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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
    • C07D401/02—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 two hetero rings
    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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

Abstract

本发明涉及一种作为PI3Kα抑制剂的化合物式(I)的晶型及其制备方法，并涉及其在制备治疗实体瘤的药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN202080035113.9A 2019-05-13 2020-05-13 喹唑啉酮类化合物的晶型及其制备方法 Pending CN113874362A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201910394653 2019-05-13
CN2019103946535 2019-05-13
CN2019104237112 2019-05-21
CN201910423711 2019-05-21
PCT/CN2020/089972 WO2020228729A1 (zh) 2019-05-13 2020-05-13 喹唑啉酮类化合物的晶型及其制备方法

Publications (1)

Publication Number Publication Date
CN113874362A true CN113874362A (zh) 2021-12-31

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CN202080035113.9A Pending CN113874362A (zh) 2019-05-13 2020-05-13 喹唑啉酮类化合物的晶型及其制备方法

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US (1) US20220213060A1 (zh)
EP (1) EP3971175A4 (zh)
JP (1) JP2022533151A (zh)
KR (1) KR20220008313A (zh)
CN (1) CN113874362A (zh)
WO (1) WO2020228729A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113501819B (zh) * 2021-07-09 2024-02-02 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) 吡啶并咪唑取代的喹唑啉酮衍生物及其合成方法和应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106146500A (zh) * 2015-03-26 2016-11-23 江苏豪森药业集团有限公司 5-氟-3-苯基-2-[(1s)-1-(9h-嘌呤-6-基氨基)丙基]-4(3h)-喹唑啉酮晶型及其制备方法
CN107955019A (zh) * 2016-10-17 2018-04-24 广东众生药业股份有限公司 一种egfr抑制剂的盐型、晶型及其制备方法
CN108239067A (zh) * 2016-12-27 2018-07-03 沈阳药科大学 喹唑啉酮类衍生物及其制备方法和用途
US20180319799A1 (en) * 2015-12-16 2018-11-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pyrido[1,2-a]pyrimidone analog, crystal form thereof, intermediate thereof and preparation method therefor

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA104147C2 (uk) 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
JP2021503447A (ja) * 2017-11-13 2021-02-12 羅欣薬業（上海）有限公司Ｌｕｏｘｉｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ （Ｓｈａｎｇｈａｉ） Ｃｏ．， Ｌｔｄ． キナゾリノン類化合物及びその使用

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106146500A (zh) * 2015-03-26 2016-11-23 江苏豪森药业集团有限公司 5-氟-3-苯基-2-[(1s)-1-(9h-嘌呤-6-基氨基)丙基]-4(3h)-喹唑啉酮晶型及其制备方法
US20180319799A1 (en) * 2015-12-16 2018-11-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Pyrido[1,2-a]pyrimidone analog, crystal form thereof, intermediate thereof and preparation method therefor
CN107955019A (zh) * 2016-10-17 2018-04-24 广东众生药业股份有限公司 一种egfr抑制剂的盐型、晶型及其制备方法
CN108239067A (zh) * 2016-12-27 2018-07-03 沈阳药科大学 喹唑啉酮类衍生物及其制备方法和用途

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HAO ZHANG ET AL.: "Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 23, pages 7765 - 7776, XP029342484, DOI: 10.1016/j.bmc.2015.11.027 *
YAN-HUA FAN ER AL.: "Design, synthesis, and biological evaluation of novel 3-substituted imidazo[1, 2-a]pyridine and quinazolin-4(3H)-one derivatives as PI3Kα inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》, vol. 139, pages 95 - 106, XP055607860, DOI: 10.1016/j.ejmech.2017.07.074 *

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EP3971175A1 (en) 2022-03-23
JP2022533151A (ja) 2022-07-21
US20220213060A1 (en) 2022-07-07
KR20220008313A (ko) 2022-01-20
WO2020228729A1 (zh) 2020-11-19
EP3971175A4 (en) 2022-11-09

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