SG11201408052WA - IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS - Google Patents
IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORSInfo
- Publication number
- SG11201408052WA SG11201408052WA SG11201408052WA SG11201408052WA SG11201408052WA SG 11201408052W A SG11201408052W A SG 11201408052WA SG 11201408052W A SG11201408052W A SG 11201408052WA SG 11201408052W A SG11201408052W A SG 11201408052WA SG 11201408052W A SG11201408052W A SG 11201408052WA
- Authority
- SG
- Singapore
- Prior art keywords
- imidazo
- compound
- kinase inhibitors
- pyridazine derivatives
- acceptable salt
- Prior art date
Links
- 150000004942 imidazo[1,2-b]pyridazines Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- VTVRXITWWZGKHV-UHFFFAOYSA-N imidazo[1,2-b]pyridazine Chemical group N1=CC=CC2=NC=CN21 VTVRXITWWZGKHV-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
- 285 - Abstract The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R , G, T, Y , Y , Y , and Y are as defined 1 1 2 3 4 herein.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012127079 | 2012-06-04 | ||
| PCT/JP2013/065328 WO2013183578A1 (en) | 2012-06-04 | 2013-06-03 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVE AS KINASE INHIBITOR |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201408052WA true SG11201408052WA (en) | 2015-01-29 |
Family
ID=49711970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201408052WA SG11201408052WA (en) | 2012-06-04 | 2013-06-03 | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AS KINASE INHIBITORS |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US9187489B2 (en) |
| EP (1) | EP2857404B1 (en) |
| JP (1) | JP5814467B2 (en) |
| KR (1) | KR101781255B1 (en) |
| CN (1) | CN104520300B (en) |
| AU (1) | AU2013272701B2 (en) |
| BR (1) | BR112014029851B1 (en) |
| CA (1) | CA2874819C (en) |
| CO (1) | CO7160119A2 (en) |
| CY (1) | CY1119607T1 (en) |
| DK (1) | DK2857404T3 (en) |
| ES (1) | ES2648228T3 (en) |
| HR (1) | HRP20171724T1 (en) |
| HU (1) | HUE037221T2 (en) |
| IL (1) | IL236075A (en) |
| IN (1) | IN2014MN02497A (en) |
| LT (1) | LT2857404T (en) |
| MX (1) | MX357021B (en) |
| MY (1) | MY170326A (en) |
| NO (1) | NO2857404T3 (en) |
| NZ (1) | NZ702574A (en) |
| PH (1) | PH12014502721A1 (en) |
| PL (1) | PL2857404T3 (en) |
| PT (1) | PT2857404T (en) |
| RS (1) | RS56625B1 (en) |
| RU (1) | RU2635917C2 (en) |
| SG (1) | SG11201408052WA (en) |
| SI (1) | SI2857404T1 (en) |
| SM (1) | SMT201700539T1 (en) |
| TW (1) | TWI585088B (en) |
| WO (1) | WO2013183578A1 (en) |
| ZA (1) | ZA201408843B (en) |
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| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
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| AR077468A1 (en) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS |
| BR112012029405B1 (en) | 2010-05-20 | 2021-01-05 | Array Biopharma Inc. | macrocyclic compounds such as trk kinase inhibitors, pharmaceutical composition, use of a compound of formula i or a pharmaceutically acceptable salt thereof, process for the preparation of a compound |
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| CA2941206C (en) * | 2014-03-27 | 2022-09-20 | Janssen Pharmaceutica Nv | Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1h-imidazo[1,2-b]pyrazole derivatives as ros1 inhibitors |
| ES2715676T3 (en) * | 2014-03-27 | 2019-06-05 | Janssen Pharmaceutica Nv | Substituted 4,5,6,7-tetrahydro-pyrazolo [1,5-a] pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo [1,5-a] [1,4] diazepine as ros1 inhibitors |
| CN106488768A (en) * | 2014-04-25 | 2017-03-08 | 埃克塞里艾克西斯公司 | Methods of treating lung adenocarcinoma |
| AU2015346046B2 (en) | 2014-11-16 | 2020-06-25 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| EP3303631A1 (en) | 2015-06-01 | 2018-04-11 | Loxo Oncology Inc. | Methods of diagnosing and treating cancer |
| MX379846B (en) | 2015-06-18 | 2025-03-11 | 89Bio Ltd | SUBSTITUTED 4-BENZYL AND 4-BENZOYL PIPERIDINE DERIVATIVES. |
| CN107847765B (en) | 2015-06-18 | 2021-05-04 | 89生物有限公司 | 1,4-Substituted piperidine derivatives |
| EP3322706B1 (en) | 2015-07-16 | 2020-11-11 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| SG11201803438XA (en) | 2015-10-26 | 2018-05-30 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| CN106854174A (en) * | 2015-12-08 | 2017-06-16 | 湖南华腾制药有限公司 | A kind of preparation method of 4 substituted piperidine derivatives |
| MX386416B (en) | 2016-04-04 | 2025-03-18 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| TN2018000338A1 (en) | 2016-04-04 | 2020-01-16 | Loxo Oncology Inc | Methods of treating pediatric cancers |
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| FI3800189T3 (en) | 2016-05-18 | 2023-07-31 | Loxo Oncology Inc | (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDIN-1- PREPARATION OF CARBOXAMIDE |
| CN107400082A (en) * | 2016-05-19 | 2017-11-28 | 湖南华腾制药有限公司 | A kind of preparation method of substituted piperidine derivative |
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| TWI704148B (en) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
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| TWI876442B (en) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile |
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| WO2019107671A1 (en) | 2017-11-29 | 2019-06-06 | 서울대학교 산학협력단 | Anti-ros1 antibody and use thereof |
| CN108129288B (en) * | 2017-12-27 | 2021-01-22 | 上海毕得医药科技股份有限公司 | Synthesis method of trans-3-hydroxycyclobutylformic acid |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| TW201932464A (en) | 2018-01-18 | 2019-08-16 | 美商亞雷生物製藥股份有限公司 | Substituted pyrazolyl[4,3-C]pyridine compounds as RET kinase inhibitors |
| US20210023086A1 (en) | 2018-03-29 | 2021-01-28 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| JP7174143B2 (en) | 2018-07-24 | 2022-11-17 | 大鵬薬品工業株式会社 | Heterobicyclic compounds that inhibit SHP2 activity |
| US12109193B2 (en) | 2018-07-31 | 2024-10-08 | Loxo Oncology Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide |
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| WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
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| AR122159A1 (en) | 2020-05-28 | 2022-08-17 | Novartis Ag | MLL1 INHIBITORS AND ANTINEOPLASTIC AGENTS |
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2013
- 2013-05-31 TW TW102119261A patent/TWI585088B/en active
- 2013-06-03 MY MYPI2014003346A patent/MY170326A/en unknown
- 2013-06-03 MX MX2014014803A patent/MX357021B/en active IP Right Grant
- 2013-06-03 EP EP13801320.6A patent/EP2857404B1/en active Active
- 2013-06-03 CN CN201380041498.XA patent/CN104520300B/en active Active
- 2013-06-03 KR KR1020147033351A patent/KR101781255B1/en active Active
- 2013-06-03 NO NO13801320A patent/NO2857404T3/no unknown
- 2013-06-03 CA CA2874819A patent/CA2874819C/en active Active
- 2013-06-03 US US14/378,318 patent/US9187489B2/en active Active
- 2013-06-03 WO PCT/JP2013/065328 patent/WO2013183578A1/en active Application Filing
- 2013-06-03 NZ NZ702574A patent/NZ702574A/en unknown
- 2013-06-03 ES ES13801320.6T patent/ES2648228T3/en active Active
- 2013-06-03 DK DK13801320.6T patent/DK2857404T3/en active
- 2013-06-03 SI SI201330798T patent/SI2857404T1/en unknown
- 2013-06-03 JP JP2014519977A patent/JP5814467B2/en active Active
- 2013-06-03 PL PL13801320T patent/PL2857404T3/en unknown
- 2013-06-03 HU HUE13801320A patent/HUE037221T2/en unknown
- 2013-06-03 BR BR112014029851-3A patent/BR112014029851B1/en active IP Right Grant
- 2013-06-03 HR HRP20171724TT patent/HRP20171724T1/en unknown
- 2013-06-03 RS RS20171198A patent/RS56625B1/en unknown
- 2013-06-03 SG SG11201408052WA patent/SG11201408052WA/en unknown
- 2013-06-03 AU AU2013272701A patent/AU2013272701B2/en active Active
- 2013-06-03 SM SM20170539T patent/SMT201700539T1/en unknown
- 2013-06-03 PT PT138013206T patent/PT2857404T/en unknown
- 2013-06-03 LT LTEP13801320.6T patent/LT2857404T/en unknown
- 2013-06-03 RU RU2014153627A patent/RU2635917C2/en active
- 2013-06-03 IN IN2497MUN2014 patent/IN2014MN02497A/en unknown
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2014
- 2014-12-02 ZA ZA2014/08843A patent/ZA201408843B/en unknown
- 2014-12-04 PH PH12014502721A patent/PH12014502721A1/en unknown
- 2014-12-04 IL IL236075A patent/IL236075A/en active IP Right Grant
- 2014-12-30 CO CO14286593A patent/CO7160119A2/en unknown
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2015
- 2015-10-29 US US14/926,973 patent/US9751887B2/en active Active
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2017
- 2017-11-15 CY CY20171101204T patent/CY1119607T1/en unknown
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