PE20212331A1 - Derivados de pirrolotriazina para tratar enfermedades mediadas por kit y pdgfra - Google Patents
Derivados de pirrolotriazina para tratar enfermedades mediadas por kit y pdgfraInfo
- Publication number
- PE20212331A1 PE20212331A1 PE2021001699A PE2021001699A PE20212331A1 PE 20212331 A1 PE20212331 A1 PE 20212331A1 PE 2021001699 A PE2021001699 A PE 2021001699A PE 2021001699 A PE2021001699 A PE 2021001699A PE 20212331 A1 PE20212331 A1 PE 20212331A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- taken together
- cyclopropyl
- together form
- pyrrolotriazine derivatives
- Prior art date
Links
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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Referido a un compuesto de formula I, en donde R1 es H y metilo; R2 es H y metilo; o R1 y R2 tomados juntos forman un ciclopropilo; R3 se selecciona de H y metilo; R4 se selecciona de H y metilo; o R3 y R4 tomados juntos forman un ciclopropilo; R5 se selecciona de H y metilo; R6 se selecciona de H y metilo; o R5 y R6 tomados juntos forman un ciclopropilo, o uno o R2 o R4 tomado junto con R6 forma un ciclobutilo; R7 es hidrogeno, o uno de R2, R4, o R6 tomado junto con R7 forma un anillo seleccionado de oxetano, tetrahidrofurano, entre otros; m es 0 o 1; y n es 0 o 1; una sal farmaceuticamente aceptable y/o un solvato del mismo. Estos compuestos son derivados de pirrolotriazina y son inhibidores selectivos de proteinas cinasas mutantes de PDGFR alfa y KIT activado. Tambien se refiere a la preparacion de esto compuestos, una composicion farmaceutica que comprende dicho compuesto y su uso para tratar tumores del estroma gastrointestinal y mastocitosis sistemica y para el tratamiento de trastornos cronicos.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962833529P | 2019-04-12 | 2019-04-12 | |
| US201962911016P | 2019-10-04 | 2019-10-04 | |
| US201962930240P | 2019-11-04 | 2019-11-04 | |
| PCT/US2020/027177 WO2020210293A1 (en) | 2019-04-12 | 2020-04-08 | Pyrrolotriazine derivatives for treating kit- and pdgfra-mediated diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20212331A1 true PE20212331A1 (es) | 2021-12-14 |
Family
ID=70416596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001699A PE20212331A1 (es) | 2019-04-12 | 2020-04-08 | Derivados de pirrolotriazina para tratar enfermedades mediadas por kit y pdgfra |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US10829493B2 (es) |
| EP (2) | EP3953357B1 (es) |
| JP (1) | JP2022526850A (es) |
| KR (1) | KR20220025704A (es) |
| CN (1) | CN113939515B (es) |
| AU (1) | AU2020272743A1 (es) |
| BR (1) | BR112021020441A2 (es) |
| CA (1) | CA3136802A1 (es) |
| CL (1) | CL2021002656A1 (es) |
| CO (1) | CO2021015113A2 (es) |
| DK (1) | DK3953357T3 (es) |
| EC (1) | ECSP21080096A (es) |
| FI (1) | FI3953357T3 (es) |
| HR (1) | HRP20240702T1 (es) |
| IL (1) | IL287168A (es) |
| LT (1) | LT3953357T (es) |
| MA (1) | MA55604A (es) |
| MX (1) | MX2021012469A (es) |
| PE (1) | PE20212331A1 (es) |
| PL (1) | PL3953357T3 (es) |
| PT (1) | PT3953357T (es) |
| RS (1) | RS65644B1 (es) |
| SG (1) | SG11202111244XA (es) |
| SI (1) | SI3953357T1 (es) |
| TW (1) | TW202104231A (es) |
| WO (1) | WO2020210293A1 (es) |
| ZA (1) | ZA202108104B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109970745B (zh) * | 2018-04-16 | 2020-12-08 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡咯并三嗪类化合物及其药物组合物及其用途 |
| JP2023546109A (ja) * | 2020-10-14 | 2023-11-01 | ブループリント メディシンズ コーポレイション | Ｋｉｔおよびｐｄｇｆｒａ媒介疾患を処置するための組成物および方法 |
| US20230391780A1 (en) * | 2020-10-14 | 2023-12-07 | Blueprint Medicines Corporation | Compositions and methods for treating kit- and pdgfra-mediated diseases |
| WO2022187477A1 (en) | 2021-03-03 | 2022-09-09 | Blueprint Medicines Corporation | Synthetic methods and intermediates for producing compounds for treating kit- and pdgfra-mediated diseases |
| MX2023010606A (es) | 2021-03-10 | 2023-10-19 | Blueprint Medicines Corp | Formas de sales y sólidas de un inhibidor de cinasas. |
| CN113278023B (zh) * | 2021-07-22 | 2021-10-15 | 上海睿跃生物科技有限公司 | 含氮杂环化合物及其制备方法和应用 |
| IL312506A (en) * | 2021-11-08 | 2024-07-01 | Progentos Therapeutics Inc | Platelet-based alpha inhibitors and their uses |
| WO2024171143A1 (en) * | 2023-02-17 | 2024-08-22 | Assia Chemical Industries Ltd. | Salts and solid forms of elenestinib |
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| JPS61238784A (ja) | 1985-04-17 | 1986-10-24 | Sumitomo Seiyaku Kk | コハク酸イミド誘導体及びその酸付加塩 |
| US6982265B1 (en) | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| DK1183033T3 (da) | 1999-05-21 | 2006-06-06 | Bristol Myers Squibb Co | Pyrrolotriazininhibitorer af kinaser |
| ES2306671T3 (es) | 1999-10-07 | 2008-11-16 | Amgen Inc. | Inhibidores de triazina quinasa. |
| SE0102616D0 (sv) | 2001-07-25 | 2001-07-25 | Astrazeneca Ab | Novel compounds |
| RS92004A (en) | 2002-04-23 | 2006-12-15 | Bristol-Myers Squibb Company | Pyrrolo-triazine aniline compounds useful as kinase inhibitors |
| TW200508224A (en) | 2003-02-12 | 2005-03-01 | Bristol Myers Squibb Co | Cyclic derivatives as modulators of chemokine receptor activity |
| UA81453C2 (en) | 2003-02-27 | 2008-01-10 | Pyrazolopyridine derivates | |
| CA2563699C (en) | 2004-04-23 | 2014-03-25 | Exelixis, Inc. | Kinase modulators and method of use |
| WO2005115397A2 (en) | 2004-04-29 | 2005-12-08 | Pharmix Corporation | Compositions and treatments for modulating kinase and/or hmg-coa reductase |
| US7173031B2 (en) | 2004-06-28 | 2007-02-06 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| JP5116687B2 (ja) | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ［２，１−ｆ］［１，２，４］トリアジン−４−イルアミンＩＧＦ−１Ｒキナーゼ阻害剤 |
| US7348325B2 (en) | 2005-11-30 | 2008-03-25 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| PT1973910E (pt) | 2006-01-27 | 2013-09-06 | Shanghai Hengrui Pharm Co Ltd | Inibidores de pirrolo [3,2-c] piridina-4-ona 2-indolinona proteína cinase |
| JP5185930B2 (ja) | 2006-07-07 | 2013-04-17 | ブリストル−マイヤーズ スクイブ カンパニー | ピロロトリアジンキナーゼ阻害剤 |
| WO2009015254A1 (en) | 2007-07-25 | 2009-01-29 | Bristol-Myers Squibb Company | Triazine kinase inhibitors |
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| EP2440051A4 (en) | 2009-06-08 | 2012-12-19 | California Capital Equity Llc | TRIAZINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS |
| WO2011005119A1 (en) | 2009-07-07 | 2011-01-13 | Pathway Therapeutics Limited | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
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| US8609672B2 (en) | 2010-08-27 | 2013-12-17 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| CN102040494A (zh) | 2010-11-12 | 2011-05-04 | 西北师范大学 | 对氟苯甲醛的制备方法 |
| JP6318156B2 (ja) | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
| US9676748B2 (en) | 2012-12-21 | 2017-06-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EP2970231A1 (en) | 2013-03-15 | 2016-01-20 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| CN105658652B (zh) | 2013-10-17 | 2019-04-12 | 蓝图药品公司 | 可用于治疗与kit相关的病症的组合物 |
| US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| KR20180048635A (ko) | 2015-07-24 | 2018-05-10 | 블루프린트 메디신즈 코포레이션 | Kit 및 pdgfr에 관련된 장애를 치료하는데 유용한 조성물 |
| WO2018183712A1 (en) * | 2017-03-31 | 2018-10-04 | Blueprint Medicines Corporation | Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr |
| CN109400610A (zh) | 2017-08-18 | 2019-03-01 | 浙江海正药业股份有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途 |
| CN108191874B (zh) | 2018-01-16 | 2019-11-29 | 成都施贝康生物医药科技有限公司 | 一种C-Kit抑制剂及其应用 |
| TW202039862A (zh) | 2018-11-12 | 2020-11-01 | 美商藍印藥品公司 | 受體酪氨酸激酶(kit)基因突變 |
| CN110938077B (zh) | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
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-
2020
- 2020-04-08 LT LTEPPCT/US2020/027177T patent/LT3953357T/lt unknown
- 2020-04-08 PT PT207210832T patent/PT3953357T/pt unknown
- 2020-04-08 EP EP20721083.2A patent/EP3953357B1/en active Active
- 2020-04-08 FI FIEP20721083.2T patent/FI3953357T3/fi active
- 2020-04-08 CA CA3136802A patent/CA3136802A1/en active Pending
- 2020-04-08 EP EP24170331.3A patent/EP4424312A2/en active Pending
- 2020-04-08 JP JP2021560255A patent/JP2022526850A/ja active Pending
- 2020-04-08 SI SI202030454T patent/SI3953357T1/sl unknown
- 2020-04-08 AU AU2020272743A patent/AU2020272743A1/en active Pending
- 2020-04-08 BR BR112021020441A patent/BR112021020441A2/pt unknown
- 2020-04-08 SG SG11202111244XA patent/SG11202111244XA/en unknown
- 2020-04-08 RS RS20240664A patent/RS65644B1/sr unknown
- 2020-04-08 PL PL20721083.2T patent/PL3953357T3/pl unknown
- 2020-04-08 PE PE2021001699A patent/PE20212331A1/es unknown
- 2020-04-08 WO PCT/US2020/027177 patent/WO2020210293A1/en active Application Filing
- 2020-04-08 KR KR1020217036868A patent/KR20220025704A/ko unknown
- 2020-04-08 TW TW109111858A patent/TW202104231A/zh unknown
- 2020-04-08 MX MX2021012469A patent/MX2021012469A/es unknown
- 2020-04-08 HR HRP20240702TT patent/HRP20240702T1/hr unknown
- 2020-04-08 CN CN202080042732.0A patent/CN113939515B/zh active Active
- 2020-04-08 MA MA055604A patent/MA55604A/fr unknown
- 2020-04-08 DK DK20721083.2T patent/DK3953357T3/da active
- 2020-04-08 US US16/842,969 patent/US10829493B2/en active Active
- 2020-04-08 US US17/602,770 patent/US20220153748A1/en active Pending
-
2021
- 2021-10-11 IL IL287168A patent/IL287168A/en unknown
- 2021-10-12 CL CL2021002656A patent/CL2021002656A1/es unknown
- 2021-10-21 ZA ZA2021/08104A patent/ZA202108104B/en unknown
- 2021-11-09 CO CONC2021/0015113A patent/CO2021015113A2/es unknown
- 2021-11-12 EC ECSENADI202180096A patent/ECSP21080096A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3136802A1 (en) | 2020-10-15 |
| CN113939515B (zh) | 2024-06-18 |
| US10829493B2 (en) | 2020-11-10 |
| MX2021012469A (es) | 2022-01-18 |
| LT3953357T (lt) | 2024-07-25 |
| JP2022526850A (ja) | 2022-05-26 |
| FI3953357T3 (fi) | 2024-07-15 |
| CO2021015113A2 (es) | 2022-02-28 |
| DK3953357T3 (en) | 2024-06-10 |
| TW202104231A (zh) | 2021-02-01 |
| MA55604A (fr) | 2022-02-16 |
| EP3953357B1 (en) | 2024-04-17 |
| EP3953357A1 (en) | 2022-02-16 |
| BR112021020441A2 (pt) | 2021-12-14 |
| RS65644B1 (sr) | 2024-07-31 |
| PT3953357T (pt) | 2024-07-24 |
| WO2020210293A1 (en) | 2020-10-15 |
| PL3953357T3 (pl) | 2024-09-02 |
| US20200325141A1 (en) | 2020-10-15 |
| SG11202111244XA (en) | 2021-11-29 |
| EP4424312A2 (en) | 2024-09-04 |
| HRP20240702T1 (hr) | 2024-08-16 |
| ECSP21080096A (es) | 2022-02-25 |
| SI3953357T1 (sl) | 2024-08-30 |
| CL2021002656A1 (es) | 2022-08-26 |
| AU2020272743A1 (en) | 2021-11-11 |
| ZA202108104B (en) | 2024-02-28 |
| US20220153748A1 (en) | 2022-05-19 |
| KR20220025704A (ko) | 2022-03-03 |
| CN113939515A (zh) | 2022-01-14 |
| IL287168A (en) | 2021-12-01 |
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