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CN115708409A - 一种化合物的盐、其晶型以及制备方法与应用 - Google Patents

一种化合物的盐、其晶型以及制备方法与应用 Download PDF

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Publication number
CN115708409A
CN115708409A CN202080045649.9A CN202080045649A CN115708409A CN 115708409 A CN115708409 A CN 115708409A CN 202080045649 A CN202080045649 A CN 202080045649A CN 115708409 A CN115708409 A CN 115708409A
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degrees
cancer
salt
crystalline form
fluoro
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尹磊
姚郑林
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Gan and Lee Pharmaceuticals Co Ltd
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Gan and Lee Pharmaceuticals Co Ltd
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Application filed by Gan and Lee Pharmaceuticals Co Ltd filed Critical Gan and Lee Pharmaceuticals Co Ltd
Publication of CN115708409A publication Critical patent/CN115708409A/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
    • C07D401/14—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
    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

化合物5‑氟‑4‑(7'‑氟‑2'‑甲基螺[环戊烷‑1,3'‑吲哚]‑5'‑基)‑氮‑(5‑(1‑甲基哌啶‑4‑基)吡啶‑2‑基)嘧啶‑2‑胺的富马酸盐、马来酸盐及已二酸盐、琥珀酸盐及多个晶型，以及其制备方法与应用被公开，已证实上述盐或其晶型可以更好地替代5‑氟‑4‑(7'‑氟‑2'‑甲基螺[环戊烷‑1,3'‑吲哚]‑5'‑基)‑氮‑(5‑(1‑甲基哌啶‑4‑基)吡啶‑2‑基)嘧啶‑2‑胺，克服其在包括溶解性、食物效应风险大及稳定性等方面的缺陷，同时具有较低的吸湿性，具有极大的应用价值。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN202080045649.9A 2019-06-21 2020-06-22 一种化合物的盐、其晶型以及制备方法与应用 Pending CN115708409A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910542355 2019-06-21
CN2019105423556 2019-06-21
PCT/CN2020/097482 WO2020253875A1 (zh) 2019-06-21 2020-06-22 一种化合物的盐、其晶型以及制备方法与应用

Publications (1)

Publication Number Publication Date
CN115708409A true CN115708409A (zh) 2023-02-21

Family

ID=74040655

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080045649.9A Pending CN115708409A (zh) 2019-06-21 2020-06-22 一种化合物的盐、其晶型以及制备方法与应用

Country Status (16)

Country Link
US (1) US20220168302A1 (zh)
EP (1) EP3988546A4 (zh)
JP (1) JP2022538076A (zh)
KR (1) KR20220041090A (zh)
CN (1) CN115708409A (zh)
AR (1) AR119184A1 (zh)
AU (1) AU2020296048A1 (zh)
BR (1) BR112021025944A2 (zh)
CA (1) CA3144546A1 (zh)
CL (1) CL2021003438A1 (zh)
CO (1) CO2022000502A2 (zh)
IL (1) IL289231A (zh)
MX (1) MX2022000051A (zh)
PH (1) PH12021553151A1 (zh)
WO (1) WO2020253875A1 (zh)
ZA (1) ZA202200964B (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022042738A1 (zh) * 2020-08-31 2022-03-03 甘李药业股份有限公司 一种含cdk4/6抑制剂的药物组合物
WO2022242563A1 (zh) * 2021-05-17 2022-11-24 甘李药业股份有限公司 一种cdk4/6抑制剂的医药用途
EP4696689A1 (en) * 2023-04-04 2026-02-18 Suzhou Kintor Pharmaceuticals, Inc. Salt form and crystal form of chiral heterocyclic compound having hedgehog pathway antagonist activity

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106810536A (zh) * 2015-11-30 2017-06-09 甘李药业股份有限公司 一种蛋白激酶抑制剂及其制备方法和医药用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20022332A3 (cs) * 2000-01-07 2003-01-15 Transform Pharmaceuticals, Inc. Sestava vzorků

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106810536A (zh) * 2015-11-30 2017-06-09 甘李药业股份有限公司 一种蛋白激酶抑制剂及其制备方法和医药用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LEI YIN等: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 144, pages 1 - 28, XP055766971 *

Also Published As

Publication number Publication date
CA3144546A1 (en) 2020-12-24
PH12021553151A1 (en) 2022-07-25
AU2020296048A1 (en) 2022-02-10
CO2022000502A2 (es) 2022-01-28
US20220168302A1 (en) 2022-06-02
MX2022000051A (es) 2022-05-24
EP3988546A1 (en) 2022-04-27
IL289231A (en) 2022-02-01
KR20220041090A (ko) 2022-03-31
EP3988546A4 (en) 2023-05-17
WO2020253875A1 (zh) 2020-12-24
JP2022538076A (ja) 2022-08-31
BR112021025944A2 (pt) 2022-02-08
ZA202200964B (en) 2022-08-31
AR119184A1 (es) 2021-12-01
CL2021003438A1 (es) 2022-09-30

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