CO2018005854A2 - Inhibidores de la proteína quinasa, método de preparación y uso médico de los mismos - Google Patents
Inhibidores de la proteína quinasa, método de preparación y uso médico de los mismosInfo
- Publication number
- CO2018005854A2 CO2018005854A2 CONC2018/0005854A CO2018005854A CO2018005854A2 CO 2018005854 A2 CO2018005854 A2 CO 2018005854A2 CO 2018005854 A CO2018005854 A CO 2018005854A CO 2018005854 A2 CO2018005854 A2 CO 2018005854A2
- Authority
- CO
- Colombia
- Prior art keywords
- compounds
- present
- preparation
- medical use
- mesomer
- Prior art date
Links
Classifications
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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
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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
- A61K31/505—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- 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
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- 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)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
La presente invención proporciona compuestos como se muestran en la fórmula I o un tautómero, un mesómero, un racemato, un enantiómero, un diastereómero, un compuesto deuterado, un profármaco o una mezcla de los mismos, o una sal o solvato farmacéuticamente aceptable de los compuestos como se muestran en la fórmula I o un tautómero, un mesómero, un racemato, un enantiómero, un diastereómero, un compuesto deuterado, un profármaco o una mezcla de los mismos, en donde R1 a R7 son como se definen en la descripción. La presente invención también proporciona un método de preparación y un uso médico de los compuestos. Los compuestos de la presente invención tienen una actividad superior o equivalente al fármaco candidato LY2835219 actualmente bajo ensayos clínicos de fase III, y algunos de los compuestos muestran mejor selectividad. Además, los compuestos preferidos exhiben buena absorción y buena distribución hematoencefálica cuando se administran por vía oral. Los compuestos de la presente invención se muestran prometedores para su desarrollo como nuevos fármacos para el tratamiento de enfermedades asociadas con la proliferación celular, particularmente tumores cerebrales, proporcionando nuevas opciones para médicos y pacientes.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510856641.1A CN106810536A (zh) | 2015-11-30 | 2015-11-30 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| PCT/CN2016/107455 WO2017092635A1 (zh) | 2015-11-30 | 2016-11-28 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2018005854A2 true CO2018005854A2 (es) | 2018-06-20 |
Family
ID=58796287
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2018/0005854A CO2018005854A2 (es) | 2015-11-30 | 2018-06-06 | Inhibidores de la proteína quinasa, método de preparación y uso médico de los mismos |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US11091476B2 (es) |
| EP (1) | EP3385262B1 (es) |
| JP (2) | JP6921101B2 (es) |
| KR (1) | KR20180083421A (es) |
| CN (3) | CN106810536A (es) |
| AU (1) | AU2016365366B2 (es) |
| BR (1) | BR112018010879A2 (es) |
| CA (1) | CA3002884A1 (es) |
| CO (1) | CO2018005854A2 (es) |
| DK (1) | DK3385262T3 (es) |
| ES (1) | ES2928169T3 (es) |
| HU (1) | HUE060152T2 (es) |
| IL (1) | IL259711B (es) |
| MA (1) | MA42341B2 (es) |
| MX (1) | MX2018006370A (es) |
| PH (1) | PH12018550049A1 (es) |
| PT (1) | PT3385262T (es) |
| RU (1) | RU2749437C2 (es) |
| UA (1) | UA124001C2 (es) |
| WO (1) | WO2017092635A1 (es) |
| ZA (1) | ZA201803531B (es) |
Families Citing this family (16)
| 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 |
| US11440912B2 (en) | 2017-10-27 | 2022-09-13 | Fresenius Kabi Oncology Ltd | Process for the preparation of ribociclib and its salts |
| MX2020008559A (es) | 2018-02-15 | 2021-01-08 | Nuvation Bio Inc | Compuestos heterocíclicos como inhibidores de la quinasa. |
| WO2019170055A1 (zh) * | 2018-03-05 | 2019-09-12 | 上海海和药物研究开发有限公司 | 具有cdk4/6激酶抑制活性的化合物、其药用组合物和用途 |
| SG11202108004VA (en) * | 2019-01-29 | 2021-08-30 | Beta Pharma Inc | 2h-indazole derivatives as therapeutic agents for brain cancers and brain metastases |
| WO2020253865A1 (zh) | 2019-06-21 | 2020-12-24 | 甘李药业股份有限公司 | Cdk4/6抑制剂、及其盐和中间体的制备方法 |
| AR119184A1 (es) * | 2019-06-21 | 2021-12-01 | Gan & Lee Pharmaceuticals | Sales de un compuesto, formas cristalinas de las sales y método de preparación y uso de las mismas |
| CN116113628A (zh) * | 2020-08-31 | 2023-05-12 | 甘李药业股份有限公司 | 一种含cdk4/6抑制剂的药物组合物 |
| JP2023554643A (ja) * | 2020-12-18 | 2023-12-28 | プレリュード・セラピューティクス・インコーポレイテッド | Ｃｄｋ阻害剤及び医薬としてのその使用 |
| CN117222636A (zh) * | 2021-04-12 | 2023-12-12 | 甘李药业股份有限公司 | 作为cdk4/6抑制剂的氘代化合物 |
| CN117337284A (zh) * | 2021-05-17 | 2024-01-02 | 甘李药业股份有限公司 | 一种cdk4/6抑制剂的医药用途 |
| WO2023040914A1 (zh) * | 2021-09-14 | 2023-03-23 | 甘李药业股份有限公司 | 一种cdk4/6抑制剂的医药用途 |
| WO2023116862A1 (zh) * | 2021-12-24 | 2023-06-29 | 江苏恒瑞医药股份有限公司 | 氢化吲哚类化合物、其制备方法及其在医药上的应用 |
| CN115093397B (zh) * | 2022-06-07 | 2023-09-05 | 自贡市第三人民医院 | 一种用于治疗肿瘤的化合物、合成方法及应用 |
| CN117658987A (zh) * | 2022-09-08 | 2024-03-08 | 上海深势唯思科技有限责任公司 | 作为plk1抑制剂的化合物及其制备方法和用途 |
| WO2024066986A1 (zh) * | 2022-09-30 | 2024-04-04 | 楚浦创制（武汉）医药科技有限公司 | 2-氨基嘧啶类化合物及其应用、药用组合物 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| PL357099A1 (en) | 2000-02-07 | 2004-07-12 | Abbott Gmbh & Co.Kg | 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors |
| GEP20063909B (en) * | 2002-01-22 | 2006-08-25 | Warner Lambert Co | 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES |
| WO2005076854A2 (en) * | 2004-02-04 | 2005-08-25 | Smithkline Beecham Corporation | Pyrimidinone compounds useful as kinase inhibitors |
| KR20080110998A (ko) | 2006-01-30 | 2008-12-22 | 엑셀리시스, 인코포레이티드 | Ｊａｋ２ 조절자로서 ４아릴２아미노피리미딘 또는 4아릴２아미노알킬피리미딘 및 이들을 포함하는 약제학적 조성물 |
| WO2008124085A2 (en) | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
| WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| AU2009214440B2 (en) | 2008-02-15 | 2014-09-25 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases |
| ES2392788T3 (es) | 2008-05-16 | 2012-12-13 | F. Hoffmann-La Roche Ag | Inhibidores de las JNK |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| UY33227A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de la cdk4/6 |
| US20130310340A1 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
| US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| 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 |
| 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 |
| CA3072766A1 (en) | 2017-09-05 | 2019-03-14 | Blackthorn Therapeutics, Inc. | 2,6-diazaspiro[3.3]hepatan-2-yl derivatives and pharmaceutical compostions thereof useful as vasopressin receptor antagonists |
| CN117222636A (zh) | 2021-04-12 | 2023-12-12 | 甘李药业股份有限公司 | 作为cdk4/6抑制剂的氘代化合物 |
-
2015
- 2015-11-30 CN CN201510856641.1A patent/CN106810536A/zh active Pending
-
2016
- 2016-11-28 CA CA3002884A patent/CA3002884A1/en active Pending
- 2016-11-28 PT PT168699452T patent/PT3385262T/pt unknown
- 2016-11-28 KR KR1020187017438A patent/KR20180083421A/ko not_active Application Discontinuation
- 2016-11-28 CN CN201680064053.7A patent/CN108290864B/zh active Active
- 2016-11-28 WO PCT/CN2016/107455 patent/WO2017092635A1/zh active Application Filing
- 2016-11-28 IL IL259711A patent/IL259711B/en unknown
- 2016-11-28 CN CN202111217526.1A patent/CN113956238B/zh active Active
- 2016-11-28 MX MX2018006370A patent/MX2018006370A/es unknown
- 2016-11-28 JP JP2018546737A patent/JP6921101B2/ja active Active
- 2016-11-28 BR BR112018010879-0A patent/BR112018010879A2/pt not_active Application Discontinuation
- 2016-11-28 RU RU2018122864A patent/RU2749437C2/ru active
- 2016-11-28 MA MA42341A patent/MA42341B2/fr unknown
- 2016-11-28 DK DK16869945.2T patent/DK3385262T3/da active
- 2016-11-28 US US15/778,812 patent/US11091476B2/en active Active
- 2016-11-28 UA UAA201806447A patent/UA124001C2/uk unknown
- 2016-11-28 HU HUE16869945A patent/HUE060152T2/hu unknown
- 2016-11-28 AU AU2016365366A patent/AU2016365366B2/en active Active
- 2016-11-28 EP EP16869945.2A patent/EP3385262B1/en active Active
- 2016-11-28 ES ES16869945T patent/ES2928169T3/es active Active
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2018
- 2018-04-23 PH PH12018550049A patent/PH12018550049A1/en unknown
- 2018-05-28 ZA ZA2018/03531A patent/ZA201803531B/en unknown
- 2018-06-06 CO CONC2018/0005854A patent/CO2018005854A2/es unknown
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2021
- 2021-06-08 JP JP2021095588A patent/JP2021138737A/ja active Pending
- 2021-07-30 US US17/444,109 patent/US11787801B2/en active Active
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