CN112424202B - 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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CN112424202B
CN112424202B CN201980037275.3A CN201980037275A CN112424202B CN 112424202 B CN112424202 B CN 112424202B CN 201980037275 A CN201980037275 A CN 201980037275A CN 112424202 B CN112424202 B CN 112424202B
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compound
crystal form
cancer
ray powder
salt
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CN112424202A (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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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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)

Priority Applications (1)

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CN202111208432.8A CN113861191B (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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CNPCT/CN2018/092194 2018-06-21
CN2018092194 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) US12043622B2 (https=)
EP (1) EP3812386A4 (https=)
JP (1) JP7430656B2 (https=)
KR (1) KR102768666B1 (https=)
CN (2) CN112424202B (https=)
AU (1) AU2019290722B2 (https=)
BR (1) BR112020026052A2 (https=)
EA (1) EA202190036A1 (https=)
IL (1) IL279579B2 (https=)
MX (1) MX2020013847A (https=)
PH (1) PH12020552236A1 (https=)
SG (1) SG11202012858QA (https=)
TW (1) TWI786303B (https=)
WO (1) WO2019242719A1 (https=)

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CN117222411B (zh) * 2021-03-24 2026-03-27 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
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
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

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

Family Cites Families (3)

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WO2017005900A1 (en) 2015-07-08 2017-01-12 F. Hoffmann-La Roche Ag ARYL SULTAM DERIVATIVES AS RORc MODULATORS
WO2017102796A1 (en) 2015-12-16 2017-06-22 F. Hoffmann-La Roche Ag HETEROARYL AMIDE SULTAM DERIVATIVES AS RORc MODULATORS
TWI646094B (zh) 2016-06-01 2019-01-01 大陸商貝達藥業股份有限公司 Crystal form of inhibitory protein kinase active compound and application thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016015604A1 (en) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. Compounds as cdk small-molecule inhibitors and uses thereof
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CDK4/6抑制剂abemaciclib合成工艺的优化;鄢龙 等;《武汉工程大学学报》;20180430;第40卷(第2期);第149-155页 *
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;Yan Wang，et al.;《Bioorganic & Medicinal Chemistry Letters》;20180131;第28卷;第974-978页 *

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EP3812386A4 (en) 2022-03-30
IL279579A (en) 2021-03-01
CA3104365A1 (en) 2019-12-26
JP2021529175A (ja) 2021-10-28
EP3812386A1 (en) 2021-04-28
BR112020026052A2 (pt) 2021-03-23
AU2019290722B2 (en) 2023-12-21
IL279579B (en) 2022-10-01
IL279579B2 (en) 2023-02-01
KR102768666B1 (ko) 2025-02-17
CN113861191A (zh) 2021-12-31
KR20210024004A (ko) 2021-03-04
CN112424202A (zh) 2021-02-26
PH12020552236A1 (en) 2021-06-28
TW202016114A (zh) 2020-05-01
CN113861191B (zh) 2023-09-19
US12043622B2 (en) 2024-07-23
MX2020013847A (es) 2021-04-28
AU2019290722A1 (en) 2021-01-28
TWI786303B (zh) 2022-12-11
WO2019242719A1 (zh) 2019-12-26
JP7430656B2 (ja) 2024-02-13
SG11202012858QA (en) 2021-02-25
US20210261546A1 (en) 2021-08-26
EA202190036A1 (ru) 2021-03-24

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