CA2805494A1 - 6-(1-methyl-1h-pyrazol-4-yl)-3-(2-methyl-2h-indazol-5-ylthio)-[1,2,4] triazolo [4,3-b] pyridazine as a c-met inhibitor - Google Patents
6-(1-methyl-1h-pyrazol-4-yl)-3-(2-methyl-2h-indazol-5-ylthio)-[1,2,4] triazolo [4,3-b] pyridazine as a c-met inhibitor Download PDFInfo
- Publication number
- CA2805494A1 CA2805494A1 CA2805494A CA2805494A CA2805494A1 CA 2805494 A1 CA2805494 A1 CA 2805494A1 CA 2805494 A CA2805494 A CA 2805494A CA 2805494 A CA2805494 A CA 2805494A CA 2805494 A1 CA2805494 A1 CA 2805494A1
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- Prior art keywords
- compound
- met
- cancer
- salt
- methyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- OGPBJKLSAFTDLK-UHFFFAOYSA-N europium atom Chemical compound [Eu] OGPBJKLSAFTDLK-UHFFFAOYSA-N 0.000 description 1
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- 230000035772 mutation Effects 0.000 description 1
- RZSCFTDHFNHMOR-UHFFFAOYSA-N n-(2,4-difluorophenyl)-2-[3-(trifluoromethyl)phenoxy]pyridine-3-carboxamide;1,1-dimethyl-3-(4-propan-2-ylphenyl)urea Chemical compound CC(C)C1=CC=C(NC(=O)N(C)C)C=C1.FC1=CC(F)=CC=C1NC(=O)C1=CC=CN=C1OC1=CC=CC(C(F)(F)F)=C1 RZSCFTDHFNHMOR-UHFFFAOYSA-N 0.000 description 1
- 238000004848 nephelometry Methods 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
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- 201000002689 pediatric hepatocellular carcinoma Diseases 0.000 description 1
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- DCWXELXMIBXGTH-UHFFFAOYSA-N phosphotyrosine Chemical compound OC(=O)C(N)CC1=CC=C(OP(O)(O)=O)C=C1 DCWXELXMIBXGTH-UHFFFAOYSA-N 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 235000015320 potassium carbonate Nutrition 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
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- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 235000010288 sodium nitrite Nutrition 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
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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
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36933510P | 2010-07-30 | 2010-07-30 | |
| US61/369,335 | 2010-07-30 | ||
| PCT/US2011/044926 WO2012015677A1 (en) | 2010-07-30 | 2011-07-22 | 6- (1-methyl-1h-pyrazol-4-yl)-3-(2-methyl-2h-indazol-5- |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2805494A1 true CA2805494A1 (en) | 2012-02-02 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2805494A Abandoned CA2805494A1 (en) | 2010-07-30 | 2011-07-22 | 6-(1-methyl-1h-pyrazol-4-yl)-3-(2-methyl-2h-indazol-5-ylthio)-[1,2,4] triazolo [4,3-b] pyridazine as a c-met inhibitor |
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| EP (1) | EP2598144B1 (enExample) |
| JP (1) | JP5738412B2 (enExample) |
| KR (1) | KR20130052740A (enExample) |
| CN (1) | CN103002898A (enExample) |
| AR (1) | AR085183A1 (enExample) |
| AU (1) | AU2011282973B2 (enExample) |
| BR (1) | BR112013002211A2 (enExample) |
| CA (1) | CA2805494A1 (enExample) |
| EA (1) | EA201270818A1 (enExample) |
| ES (1) | ES2516940T3 (enExample) |
| IN (1) | IN2012MN02924A (enExample) |
| MX (1) | MX2013001247A (enExample) |
| TW (1) | TWI431008B (enExample) |
| WO (1) | WO2012015677A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2869316C (en) * | 2012-05-09 | 2016-12-20 | Eli Lilly And Company | Anti-c-met antibodies |
| CN103122000B (zh) * | 2012-09-03 | 2013-12-25 | 中美冠科生物技术（太仓）有限公司 | 用作抗肿瘤药物的高选择性的c-Met激酶抑制剂 |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| US10386376B2 (en) | 2015-11-09 | 2019-08-20 | Jeimei, Llc | Sample container with integrated test strip |
| CN108853108A (zh) * | 2015-12-31 | 2018-11-23 | 北京浦润奥生物科技有限责任公司 | 化合物在制备用于治疗脑胶质瘤的药物中的用途 |
| CA3129665A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7728017B2 (en) * | 2005-11-30 | 2010-06-01 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Met and uses thereof |
| PE20121506A1 (es) * | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| CN101553490A (zh) * | 2006-10-23 | 2009-10-07 | Sgx药品公司 | 用作蛋白激酶调节剂的二环三唑类化合物 |
| BRPI0717320A2 (pt) | 2006-10-23 | 2013-10-22 | Sgx Pharmaceuticals Inc | Triazóis bicíclicos como moduladores de proteína cinase |
| EA016527B1 (ru) | 2006-10-23 | 2012-05-30 | ЭсДжиЭкс ФАРМАСЬЮТИКАЛЗ, ИНК. | Триазолопиридазиновые модуляторы протеинкиназ |
| PA8792501A1 (es) * | 2007-08-09 | 2009-04-23 | Sanofi Aventis | Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met. |
| PE20091468A1 (es) | 2008-02-28 | 2009-10-22 | Novartis Ag | DERIVADOS DE 3-METIL-IMIDAZO-[1,2-b]-PIRIDAZINA |
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2011
- 2011-07-20 AR ARP110102632A patent/AR085183A1/es unknown
- 2011-07-22 CN CN2011800371928A patent/CN103002898A/zh active Pending
- 2011-07-22 EP EP11741372.4A patent/EP2598144B1/en not_active Not-in-force
- 2011-07-22 ES ES11741372.4T patent/ES2516940T3/es active Active
- 2011-07-22 AU AU2011282973A patent/AU2011282973B2/en not_active Expired - Fee Related
- 2011-07-22 JP JP2013521838A patent/JP5738412B2/ja not_active Expired - Fee Related
- 2011-07-22 KR KR1020137002382A patent/KR20130052740A/ko not_active Ceased
- 2011-07-22 CA CA2805494A patent/CA2805494A1/en not_active Abandoned
- 2011-07-22 US US13/188,496 patent/US8268836B2/en not_active Expired - Fee Related
- 2011-07-22 TW TW100126076A patent/TWI431008B/zh not_active IP Right Cessation
- 2011-07-22 MX MX2013001247A patent/MX2013001247A/es not_active Application Discontinuation
- 2011-07-22 WO PCT/US2011/044926 patent/WO2012015677A1/en not_active Ceased
- 2011-07-22 BR BR112013002211A patent/BR112013002211A2/pt not_active IP Right Cessation
- 2011-07-22 EA EA201270818A patent/EA201270818A1/ru unknown
-
2012
- 2012-12-31 IN IN2924MUN2012 patent/IN2012MN02924A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2516940T3 (es) | 2014-10-31 |
| TWI431008B (zh) | 2014-03-21 |
| EA201270818A1 (ru) | 2013-05-30 |
| US8268836B2 (en) | 2012-09-18 |
| JP2013532687A (ja) | 2013-08-19 |
| BR112013002211A2 (pt) | 2016-05-24 |
| AR085183A1 (es) | 2013-09-18 |
| WO2012015677A9 (en) | 2012-12-13 |
| EP2598144A1 (en) | 2013-06-05 |
| MX2013001247A (es) | 2013-03-18 |
| WO2012015677A1 (en) | 2012-02-02 |
| IN2012MN02924A (enExample) | 2015-06-12 |
| KR20130052740A (ko) | 2013-05-23 |
| AU2011282973B2 (en) | 2014-03-20 |
| AU2011282973A1 (en) | 2013-01-10 |
| CN103002898A (zh) | 2013-03-27 |
| EP2598144B1 (en) | 2014-08-13 |
| JP5738412B2 (ja) | 2015-06-24 |
| US20120028984A1 (en) | 2012-02-02 |
| TW201219393A (en) | 2012-05-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20130114 |
|
| FZDE | Discontinued |
Effective date: 20150722 |