AR083091A1 - ((r)-(e)-2-(4-(2-(5-(1-(3,5-dicloropiridin-4-il)etoxi)-1h-indazol-3-il)vinil)-1h-pirazol-1-il)etanol cristalino - Google Patents
((r)-(e)-2-(4-(2-(5-(1-(3,5-dicloropiridin-4-il)etoxi)-1h-indazol-3-il)vinil)-1h-pirazol-1-il)etanol cristalinoInfo
- Publication number
- AR083091A1 AR083091A1 ARP110103482A ARP110103482A AR083091A1 AR 083091 A1 AR083091 A1 AR 083091A1 AR P110103482 A ARP110103482 A AR P110103482A AR P110103482 A ARP110103482 A AR P110103482A AR 083091 A1 AR083091 A1 AR 083091A1
- Authority
- AR
- Argentina
- Prior art keywords
- indazol
- vinyl
- dicloropiridin
- etoxi
- pirazol
- Prior art date
Links
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 title abstract 6
- 239000013078 crystal Substances 0.000 title 1
- 229920002554 vinyl polymer Polymers 0.000 title 1
- ORGHESHFQPYLAO-UHFFFAOYSA-N vinyl radical Chemical class C=[CH] ORGHESHFQPYLAO-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- -1 4- (2- (5- (1- (3,5-dichloropyridin-4-yl) ethoxy) -1H-indazol-3-yl) vinyl) -1H-pyrazol-1-yl Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000004682 monohydrates Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Composición farmacéutica para el tratamiento del cáncer.Reivindicación 1: Un compuesto caracterizado porque es ((R)-(E)-2-(4-(2-(5-(1-(3,5-dicloropiridin-4-il)etoxi)-1H-indazol-3-il)vinil)-1H-pirazol-1-il)etanol cristalino. Reivindicación 2: El compuesto de conformidad con la reivindicación 1, caracterizado porque es monohidrato de ((R)-(E)-2-(4-(2-(5-(1-(3,5-dicloropiridin-4-il)etoxi)-1H-indazol-3-il)vinil)-1H-pirazol-1-il)etanol cristalino. Reivindicación 4: El compuesto de conformidad con cualquiera de las reivindicaciones 1 a 3, caracterizado porque el compuesto es distinguido por el patrón de difracción en polvo de rayos-X (radiación Cu, l = 1.54059 Å) que comprende un pico a 14.65. Reivindicación 5: El compuesto de conformidad con la reivindicación 4, caracterizado porque además comprende un pico a 3.54 (2q ± 0.1º). Reivindicación 6: El compuesto de conformidad con la reivindicación 4 o reivindicación 5, caracterizado porque además comprende un pico a 12.51 (2q ± 0.1º).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38991110P | 2010-10-05 | 2010-10-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083091A1 true AR083091A1 (es) | 2013-01-30 |
Family
ID=44999860
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103482A AR083091A1 (es) | 2010-10-05 | 2011-09-23 | ((r)-(e)-2-(4-(2-(5-(1-(3,5-dicloropiridin-4-il)etoxi)-1h-indazol-3-il)vinil)-1h-pirazol-1-il)etanol cristalino |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US8530665B2 (es) |
| EP (1) | EP2625175B1 (es) |
| JP (1) | JP5940547B2 (es) |
| KR (1) | KR101527661B1 (es) |
| CN (1) | CN103153983B (es) |
| AR (1) | AR083091A1 (es) |
| AU (1) | AU2011312485B2 (es) |
| BR (1) | BR112013006336A2 (es) |
| CA (1) | CA2813329C (es) |
| CL (1) | CL2013000884A1 (es) |
| CO (1) | CO6710911A2 (es) |
| DK (1) | DK2625175T3 (es) |
| DO (1) | DOP2013000072A (es) |
| EA (1) | EA021817B1 (es) |
| EC (1) | ECSP13012539A (es) |
| ES (1) | ES2558777T3 (es) |
| HR (1) | HRP20151299T1 (es) |
| HU (1) | HUE026379T2 (es) |
| IL (1) | IL224850A (es) |
| JO (1) | JO3062B1 (es) |
| MA (1) | MA34552B1 (es) |
| ME (1) | ME02307B (es) |
| MX (1) | MX2013003907A (es) |
| NZ (1) | NZ608482A (es) |
| PE (1) | PE20140252A1 (es) |
| PH (1) | PH12013500649A1 (es) |
| PL (1) | PL2625175T3 (es) |
| PT (1) | PT2625175E (es) |
| RS (1) | RS54457B1 (es) |
| SG (1) | SG188286A1 (es) |
| SI (1) | SI2625175T1 (es) |
| TW (1) | TWI418554B (es) |
| UA (1) | UA111725C2 (es) |
| WO (1) | WO2012047699A1 (es) |
| ZA (1) | ZA201301560B (es) |
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| DE19945982A1 (de) * | 1999-09-24 | 2001-03-29 | Knoll Ag | Geschwindigkeitsbestimmte Partikel |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| CN103819396B (zh) * | 2014-02-26 | 2016-06-15 | 四川大学 | 一种手性的1-(3,5-二氯吡啶-4-基)-乙醇的合成方法 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| PE20171514A1 (es) | 2015-02-20 | 2017-10-20 | Incyte Corp | Heterociclos biciclicos como inhibidores de fgfr |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| SG11202010636VA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Solid forms of an fgfr inhibitor and processes for preparing the same |
| BR112020022373A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | sais de um inibidor de fgfr |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
| CN115151539A (zh) | 2019-12-04 | 2022-10-04 | 因赛特公司 | Fgfr抑制剂的衍生物 |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN111705099B (zh) * | 2020-07-01 | 2022-03-08 | 天津药明康德新药开发有限公司 | 一种(s)-1-(3,5-二氯吡啶-4-取代)乙醇的制备方法 |
| CN116635076A (zh) * | 2020-12-17 | 2023-08-22 | 荣山医药股份有限公司 | 大环化合物及其用途 |
| MX2023007162A (es) * | 2020-12-17 | 2023-06-29 | Blossomhill Therapeutics Inc | Macrociclos y sus usos. |
| CA3205986A1 (en) * | 2020-12-30 | 2022-07-07 | Tyra Biosciences, Inc. | Indazole compounds as kinase inhibitors |
| US12065494B2 (en) | 2021-04-12 | 2024-08-20 | Incyte Corporation | Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent |
| AR126102A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | 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 |
| WO2025255438A1 (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 |
| 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 |
| 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| AP1666A (en) * | 2000-09-11 | 2006-09-29 | Chiron Corp | Quinolinone derivatives as tyrosine kinase inhibitors. |
| IL164209A0 (en) | 2002-05-31 | 2005-12-18 | Eisai Co Ltd | Pyrazole derivatives and pharmaceutical compositions containing the same |
| AU2005223486A1 (en) * | 2004-03-17 | 2005-09-29 | Pfizer Inc. | Polymorphic and amorphous forms of 2,5-Dimethyl-2H-pyrazole-3-carboxylic acid {2-fluoro-5-[3-((e)-2-pyridin-2-yl-vinyl)-1H-indasol-6-ylamino]-phenyl}-amide |
| JP4746299B2 (ja) * | 2004-07-16 | 2011-08-10 | ジュズ インターナショナル ピーティーイー エルティーディー | 金属酸化物粉末の製造方法 |
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| WO2007058626A1 (en) | 2005-11-16 | 2007-05-24 | S*Bio Pte Ltd | Indazole compounds |
| EP2134702B2 (en) * | 2007-04-05 | 2023-08-30 | Pfizer Products Inc. | Crystalline forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-e-[2-(pyridin-2-yl)ethenyl]indazole suitable for the treatment of abnormal cell growth in mammals |
| JO2860B1 (en) * | 2009-05-07 | 2015-03-15 | ايلي ليلي اند كومباني | Phenylendazolyl compounds |
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2011
- 2011-09-22 JO JOP/2011/0294A patent/JO3062B1/ar active
- 2011-09-23 TW TW100134428A patent/TWI418554B/zh not_active IP Right Cessation
- 2011-09-23 AR ARP110103482A patent/AR083091A1/es unknown
- 2011-09-29 PT PT117713123T patent/PT2625175E/pt unknown
- 2011-09-29 UA UAA201303378A patent/UA111725C2/uk unknown
- 2011-09-29 HR HRP20151299TT patent/HRP20151299T1/hr unknown
- 2011-09-29 KR KR1020137008655A patent/KR101527661B1/ko not_active Expired - Fee Related
- 2011-09-29 ES ES11771312.3T patent/ES2558777T3/es active Active
- 2011-09-29 US US13/248,055 patent/US8530665B2/en not_active Expired - Fee Related
- 2011-09-29 CA CA2813329A patent/CA2813329C/en not_active Expired - Fee Related
- 2011-09-29 MA MA35780A patent/MA34552B1/fr unknown
- 2011-09-29 AU AU2011312485A patent/AU2011312485B2/en not_active Ceased
- 2011-09-29 HU HUE11771312A patent/HUE026379T2/en unknown
- 2011-09-29 PH PH1/2013/500649A patent/PH12013500649A1/en unknown
- 2011-09-29 BR BR112013006336A patent/BR112013006336A2/pt not_active IP Right Cessation
- 2011-09-29 DK DK11771312.3T patent/DK2625175T3/en active
- 2011-09-29 WO PCT/US2011/053798 patent/WO2012047699A1/en not_active Ceased
- 2011-09-29 SI SI201130673T patent/SI2625175T1/sl unknown
- 2011-09-29 JP JP2013532838A patent/JP5940547B2/ja not_active Expired - Fee Related
- 2011-09-29 EA EA201390275A patent/EA021817B1/ru not_active IP Right Cessation
- 2011-09-29 RS RS20150828A patent/RS54457B1/sr unknown
- 2011-09-29 CN CN201180048148.7A patent/CN103153983B/zh not_active Expired - Fee Related
- 2011-09-29 NZ NZ608482A patent/NZ608482A/en not_active IP Right Cessation
- 2011-09-29 SG SG2013013743A patent/SG188286A1/en unknown
- 2011-09-29 ME MEP-2015-198A patent/ME02307B/me unknown
- 2011-09-29 MX MX2013003907A patent/MX2013003907A/es active IP Right Grant
- 2011-09-29 PL PL11771312T patent/PL2625175T3/pl unknown
- 2011-09-29 PE PE2013000789A patent/PE20140252A1/es not_active Application Discontinuation
- 2011-09-29 EP EP11771312.3A patent/EP2625175B1/en active Active
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- 2013-02-21 IL IL224850A patent/IL224850A/en not_active IP Right Cessation
- 2013-02-28 ZA ZA2013/01560A patent/ZA201301560B/en unknown
- 2013-04-02 DO DO2013000072A patent/DOP2013000072A/es unknown
- 2013-04-02 CL CL2013000884A patent/CL2013000884A1/es unknown
- 2013-04-03 EC ECSP13012539 patent/ECSP13012539A/es unknown
- 2013-04-08 CO CO13090555A patent/CO6710911A2/es unknown
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