CO2021002651A2 - Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met - Google Patents
Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y metInfo
- Publication number
- CO2021002651A2 CO2021002651A2 CONC2021/0002651A CO2021002651A CO2021002651A2 CO 2021002651 A2 CO2021002651 A2 CO 2021002651A2 CO 2021002651 A CO2021002651 A CO 2021002651A CO 2021002651 A2 CO2021002651 A2 CO 2021002651A2
- Authority
- CO
- Colombia
- Prior art keywords
- tam
- met kinase
- pyrazolo
- kinase inhibitors
- pyridine compounds
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- FPYJSJDOHRDAMT-KQWNVCNZSA-N 1h-indole-5-sulfonamide, n-(3-chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1h-pyrrol-2-yl]methylene]-2,3-dihydro-n-methyl-2-oxo-, (3z)- Chemical compound C=1C=C2NC(=O)\C(=C/C3=C(C(C(=O)N4CCN(C)CC4)=C(C)N3)C)C2=CC=1S(=O)(=O)N(C)C1=CC=CC(Cl)=C1 FPYJSJDOHRDAMT-KQWNVCNZSA-N 0.000 title 1
- 150000005230 pyrazolo[3,4-b]pyridines Chemical class 0.000 title 1
- 229940125895 MET kinase inhibitor Drugs 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- A61K31/435—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
- A61K31/506—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Plural Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
La presente invención se refiere a compuestos de la Fórmula I: I y estereoisómeros, tautómeros y sales de los mismos farmacéuticamente aceptables, en donde R1, R2, R9, X1 y G son como se definen en la presente, los cuales son inhibidores de una o más cinasas TAM y/o cinasa c-Met, y son útiles en el tratamiento y prevención de enfermedades las cuales pueden ser tratadas con un inhibidor de cinasa TAM y/o un inhibidor de cinasa c-Met.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862724829P | 2018-08-30 | 2018-08-30 | |
| US201962858686P | 2019-06-07 | 2019-06-07 | |
| PCT/US2019/048701 WO2020047184A1 (en) | 2018-08-30 | 2019-08-29 | PYRAZOLO[3,4-b]PYRIDINE COMPOUNDS AS INHIBITORS OF TAM AND MET KINASES |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2021002651A2 true CO2021002651A2 (es) | 2021-03-08 |
Family
ID=67928919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2021/0002651A CO2021002651A2 (es) | 2018-08-30 | 2021-02-26 | Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US11104676B2 (es) |
| EP (1) | EP3843850B1 (es) |
| JP (2) | JP6970859B2 (es) |
| KR (1) | KR20210049898A (es) |
| CN (1) | CN112930215A (es) |
| AU (3) | AU2019330017B2 (es) |
| BR (1) | BR112021002722A2 (es) |
| CA (1) | CA3110502C (es) |
| CL (1) | CL2021000467A1 (es) |
| CO (1) | CO2021002651A2 (es) |
| CR (1) | CR20210098A (es) |
| CU (1) | CU20210015A7 (es) |
| DO (1) | DOP2021000038A (es) |
| EC (1) | ECSP21012498A (es) |
| IL (1) | IL281127B2 (es) |
| MA (1) | MA53487A (es) |
| MX (1) | MX2021001952A (es) |
| NI (1) | NI202100007A (es) |
| PE (1) | PE20211779A1 (es) |
| PH (1) | PH12021500017A1 (es) |
| SG (1) | SG11202101148UA (es) |
| TW (1) | TW202024071A (es) |
| UY (1) | UY38349A (es) |
| WO (1) | WO2020047184A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210049862A (ko) * | 2018-08-24 | 2021-05-06 | 난징 트렌스테라 바이오사이언스즈 컴퍼니 리미티드 | 일종의 신형 퀴놀린 유도체 억제제 |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和失調症之化合物 |
| EP4029862A4 (en) * | 2019-09-06 | 2023-10-04 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | CONNECTION WITH AXL AND C-MET KINASE INHIBITORY ACTIVITY, THEIR PREPARATION AND USE |
| WO2021057782A1 (zh) * | 2019-09-24 | 2021-04-01 | 南京药捷安康生物科技有限公司 | 杂环衍生物及其用途 |
| JP7181325B2 (ja) * | 2020-03-03 | 2022-11-30 | アレイ バイオファーマ インコーポレイテッド | がんを処置するための方法 |
| EP4319748A1 (en) * | 2021-04-09 | 2024-02-14 | Tachyon Therapeutics, Inc. | Treatment of cancer with kdm4 inhibitors |
| WO2023002360A1 (en) | 2021-07-22 | 2023-01-26 | Pfizer Inc. | Solid forms and formulations of an inhibitor of tam and c-met kinases |
| IT202100022682A1 (it) * | 2021-09-01 | 2023-03-01 | Luigi Frati | Derivati pirimidinici e loro uso nel trattamento di tumori |
| CN115850301A (zh) * | 2021-09-24 | 2023-03-28 | 中山医诺维申新药研发有限公司 | 吡唑酮类化合物及其组合物和用途 |
| CA3236956A1 (en) * | 2021-11-05 | 2023-05-11 | Haihe Biopharma Co., Ltd. | Solid dispersion, preparation method therefor, and solid formulation comprising same |
| WO2023078408A1 (zh) * | 2021-11-05 | 2023-05-11 | 上海海和药物研究开发股份有限公司 | 含met受体酪氨酸激酶抑制剂的药物组合及应用 |
| US11753395B2 (en) | 2021-12-16 | 2023-09-12 | Kinnate Biopharma Inc. | Inhibitors of MET kinase |
| WO2023125803A1 (zh) * | 2021-12-29 | 2023-07-06 | 北京鞍石生物科技有限责任公司 | 杂芳环氮氧化合物及其制备方法和应用 |
| US11945785B2 (en) | 2021-12-30 | 2024-04-02 | Biomea Fusion, Inc. | Pyrazine compounds as inhibitors of FLT3 |
| CN116768868B (zh) * | 2023-08-15 | 2023-12-08 | 云南省药物研究所 | 一种哒嗪酮硫代衍生物及其制备方法和应用 |
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| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US20050288290A1 (en) | 2004-06-28 | 2005-12-29 | Borzilleri Robert M | Fused heterocyclic kinase inhibitors |
| JP5368701B2 (ja) | 2004-07-02 | 2013-12-18 | エクセリクシス、インコーポレイテッド | ｃ−Ｍｅｔモジュレーター及び使用方法 |
| PE20061119A1 (es) | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| JP2009529047A (ja) * | 2006-03-07 | 2009-08-13 | アレイ バイオファーマ、インコーポレイテッド | ヘテロ二環系ピラゾール化合物およびその使用 |
| CN102816175B (zh) | 2011-06-09 | 2015-12-16 | 上海汇伦生命科技有限公司 | 一种杂环并吡啶酮类化合物,其中间体、制备方法和用途 |
| WO2013032797A2 (en) * | 2011-08-26 | 2013-03-07 | New Hope R & D Bioscience, Inc. | Oxetane 3,3-dicarboxamide compounds and methods of making and using same |
| JP2014534949A (ja) * | 2011-09-19 | 2014-12-25 | ジェネンテック， インコーポレイテッド | Ｃ−ｍｅｔアンタゴニストおよびｂ−ｒａｆアンタゴニストを含む組合せ処置 |
| KR20140090678A (ko) * | 2011-11-14 | 2014-07-17 | 세파론, 인코포레이티드 | AXL 및 c-MET 키나제 억제제로서의 우라실 유도체 |
| JP2016527274A (ja) | 2013-08-02 | 2016-09-08 | イグナイタ インコーポレイテッド | ＡＸＬ／ｃＭＥＴ阻害剤を単独または他の薬剤と組み合わせて用いて各種がんを治療する方法 |
| HUE037579T2 (hu) * | 2013-12-26 | 2018-09-28 | Ignyta Inc | Pirazolo[1,5-a]piridin-származékok és módszerek alkalmazásukra |
| WO2016004272A1 (en) | 2014-07-02 | 2016-01-07 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| CA2954862A1 (en) | 2014-07-31 | 2016-02-04 | Novartis Ag | Combination therapy |
| GB201509338D0 (en) | 2015-05-29 | 2015-07-15 | Bergenbio As | Combination therapy |
| KR101829998B1 (ko) | 2015-11-04 | 2018-02-19 | 롬엔드하스전자재료코리아유한회사 | 착색 감광성 수지 조성물 및 이를 이용한 차광성 스페이서 |
| SG10202009423QA (en) * | 2016-03-28 | 2020-11-27 | Incyte Corp | Pyrrolotriazine compounds as tam inhibitors |
| US20190269666A1 (en) | 2016-07-29 | 2019-09-05 | Eli Lilly And Company | Combination therapy with merestinib and anti-pd-l1 or anti-pd-1 inhibitors for use in the treatment of cancer |
| CN109689056A (zh) | 2016-08-01 | 2019-04-26 | 亚尼塔公司 | 用于治疗癌症的组合 |
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| CN108250200A (zh) | 2016-12-28 | 2018-07-06 | 中国科学院上海药物研究所 | 一种具有Axl抑制活性的化合物及其制备和应用 |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| CN111372925B (zh) | 2017-11-24 | 2022-09-02 | 南京明德新药研发有限公司 | 作为c-MET/AXL抑制剂的尿嘧啶类化合物 |
| WO2019113190A1 (en) | 2017-12-07 | 2019-06-13 | Array Biopharma Inc. | Bicyclic fused pyridine compounds as inhibitors of tam kinases |
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2019
- 2019-08-28 UY UY0001038349A patent/UY38349A/es unknown
- 2019-08-29 TW TW108131145A patent/TW202024071A/zh unknown
- 2019-08-29 BR BR112021002722-0A patent/BR112021002722A2/pt not_active Application Discontinuation
- 2019-08-29 EP EP19766425.3A patent/EP3843850B1/en active Active
- 2019-08-29 IL IL281127A patent/IL281127B2/en unknown
- 2019-08-29 CR CR20210098A patent/CR20210098A/es unknown
- 2019-08-29 AU AU2019330017A patent/AU2019330017B2/en active Active
- 2019-08-29 KR KR1020217009262A patent/KR20210049898A/ko active IP Right Grant
- 2019-08-29 PE PE2021000248A patent/PE20211779A1/es unknown
- 2019-08-29 JP JP2021510177A patent/JP6970859B2/ja active Active
- 2019-08-29 WO PCT/US2019/048701 patent/WO2020047184A1/en active Application Filing
- 2019-08-29 MX MX2021001952A patent/MX2021001952A/es unknown
- 2019-08-29 CN CN201980071473.1A patent/CN112930215A/zh active Pending
- 2019-08-29 CU CU2021000015A patent/CU20210015A7/es unknown
- 2019-08-29 SG SG11202101148UA patent/SG11202101148UA/en unknown
- 2019-08-29 US US16/555,432 patent/US11104676B2/en active Active
- 2019-08-29 CA CA3110502A patent/CA3110502C/en active Active
- 2019-08-29 MA MA053487A patent/MA53487A/fr unknown
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2021
- 2021-02-09 NI NI202100007A patent/NI202100007A/es unknown
- 2021-02-23 PH PH12021500017A patent/PH12021500017A1/en unknown
- 2021-02-23 EC ECSENADI202112498A patent/ECSP21012498A/es unknown
- 2021-02-24 CL CL2021000467A patent/CL2021000467A1/es unknown
- 2021-02-26 CO CONC2021/0002651A patent/CO2021002651A2/es unknown
- 2021-02-26 DO DO2021000038A patent/DOP2021000038A/es unknown
- 2021-07-15 US US17/376,571 patent/US11780835B2/en active Active
- 2021-10-29 JP JP2021177253A patent/JP7337133B2/ja active Active
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2022
- 2022-05-03 AU AU2022202946A patent/AU2022202946B2/en active Active
- 2022-08-25 AU AU2022221514A patent/AU2022221514B2/en not_active Expired - Fee Related
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