CN112424202A - 抑制cdk4/6活性化合物的晶型及其应用 - Google Patents

抑制cdk4/6活性化合物的晶型及其应用 Download PDF

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CN112424202A
CN112424202A CN201980037275.3A CN201980037275A CN112424202A CN 112424202 A CN112424202 A CN 112424202A CN 201980037275 A CN201980037275 A CN 201980037275A CN 112424202 A CN112424202 A CN 112424202A
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compound
crystalline form
cancer
disease
ray powder
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CN112424202B (zh
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王义乾
张春辉
王家炳
丁列明
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Betta Pharmaceuticals 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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

Abstract

本发明涉及结构式(I)所示的(R)‑N‑(5‑((4‑乙基哌嗪‑1‑基)甲基)吡啶‑2‑基)‑5‑氟‑4‑(6‑氟‑1‑甲基‑1,2,3,4‑四氢苯并[4,5]咪唑并[1,2‑a]吡啶‑8‑基)嘧啶‑2‑胺(化合物I)的盐型或其晶型，本发明还涉及化合物I的盐型和/或其晶型的制备方法，含有所述盐型和/或晶型的药物组合物，以及它们在制备治疗疾病、病症或病状的药物中的应用或用于治疗疾病、病症或病状的治疗方法。

Description

PCT国内申请，说明书已公开。

Claims (28)

  1. PCT国内申请，权利要求书已公开。
CN201980037275.3A 2018-06-21 2019-06-21 抑制cdk4/6活性化合物的晶型及其应用 Active CN112424202B (zh)

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CN2018092194 2018-06-21
CNPCT/CN2018/092194 2018-06-21
PCT/CN2019/092239 WO2019242719A1 (zh) 2018-06-21 2019-06-21 抑制cdk4/6活性化合物的晶型及其应用

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US (1) US20210261546A1 (zh)
EP (1) EP3812386A4 (zh)
JP (1) JP7430656B2 (zh)
KR (1) KR20210024004A (zh)
CN (2) CN113861191B (zh)
AU (1) AU2019290722B2 (zh)
BR (1) BR112020026052A2 (zh)
CA (1) CA3104365A1 (zh)
EA (1) EA202190036A1 (zh)
IL (1) IL279579B2 (zh)
MX (1) MX2020013847A (zh)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023131179A1 (zh) * 2022-01-05 2023-07-13 贝达药业股份有限公司 苯并咪唑衍生物或其盐在治疗白血病中的用途

Families Citing this family (2)

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CN117222411A (zh) * 2021-03-24 2023-12-12 贝达药业股份有限公司 药物组合、包含其的试剂盒及其用途
CN115872923B (zh) * 2022-12-29 2023-04-28 成都泰和伟业生物科技有限公司 一种化合物及其制备方法

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CN104592251A (zh) * 2015-01-23 2015-05-06 中国药科大学 4-(稠杂环取代氨基)-1h-吡唑-3-甲酰胺类化合物及其用途
WO2016015604A1 (en) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. Compounds as cdk small-molecule inhibitors and uses thereof
WO2016173505A1 (en) * 2015-04-28 2016-11-03 Shanghai Fochon Pharmaceutical Co., Ltd. Certain protein kinase inhibitor
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CN107690431A (zh) * 2015-07-08 2018-02-13 豪夫迈·罗氏有限公司 作为RORc调节剂的芳基磺内酰胺衍生物
WO2017102796A1 (en) * 2015-12-16 2017-06-22 F. Hoffmann-La Roche Ag HETEROARYL AMIDE SULTAM DERIVATIVES AS RORc MODULATORS
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CN104592251A (zh) * 2015-01-23 2015-05-06 中国药科大学 4-(稠杂环取代氨基)-1h-吡唑-3-甲酰胺类化合物及其用途
WO2016173505A1 (en) * 2015-04-28 2016-11-03 Shanghai Fochon Pharmaceutical Co., Ltd. Certain protein kinase inhibitor
CN106608879A (zh) * 2015-10-27 2017-05-03 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
WO2018113771A1 (en) * 2016-12-22 2018-06-28 Betta Pharmaceuticals Co., Ltd Benzimidazole derivatives, preparation methods and uses theirof
WO2019035008A1 (en) * 2017-08-15 2019-02-21 Beijing Xuanyi Pharmasciences Co., Ltd. INHIBITORS OF CDK4 / 6 AND THEIR USE

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YAN WANG，ET AL.: "Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity r", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *
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EP3812386A1 (en) 2021-04-28
EA202190036A1 (ru) 2021-03-24
BR112020026052A2 (pt) 2021-03-23
JP2021529175A (ja) 2021-10-28
KR20210024004A (ko) 2021-03-04
CN113861191A (zh) 2021-12-31
MX2020013847A (es) 2021-04-28
CN113861191B (zh) 2023-09-19
CN112424202B (zh) 2021-09-17
SG11202012858QA (en) 2021-02-25
AU2019290722B2 (en) 2023-12-21
AU2019290722A1 (en) 2021-01-28
CA3104365A1 (en) 2019-12-26
IL279579A (en) 2021-03-01
IL279579B2 (en) 2023-02-01
WO2019242719A1 (zh) 2019-12-26
IL279579B (en) 2022-10-01
EP3812386A4 (en) 2022-03-30
TWI786303B (zh) 2022-12-11
JP7430656B2 (ja) 2024-02-13
PH12020552236A1 (en) 2021-06-28
US20210261546A1 (en) 2021-08-26
TW202016114A (zh) 2020-05-01

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