PE20240099A1 - Nuevos derivados de indazol acetileno - Google Patents
Nuevos derivados de indazol acetilenoInfo
- Publication number
- PE20240099A1 PE20240099A1 PE2023001615A PE2023001615A PE20240099A1 PE 20240099 A1 PE20240099 A1 PE 20240099A1 PE 2023001615 A PE2023001615 A PE 2023001615A PE 2023001615 A PE2023001615 A PE 2023001615A PE 20240099 A1 PE20240099 A1 PE 20240099A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compounds
- halogen
- methyl
- indazole
- Prior art date
Links
- BCKAIZQTOOSCNL-UHFFFAOYSA-N C#C.N1N=CC2=CC=CC=C12 Chemical class C#C.N1N=CC2=CC=CC=C12 BCKAIZQTOOSCNL-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- WPAZPBFPWDTKBY-PSPFREQMSA-N CC(C1=NN(C(C(NC2=NC=CS2)=O)C2=C(C[C@H](C3)F)N3C=N2)C=C1C(C(F)F)=C1)=C1C#CC1=CC=C(CN2CCC(CO)CC2)C=C1 Chemical compound CC(C1=NN(C(C(NC2=NC=CS2)=O)C2=C(C[C@H](C3)F)N3C=N2)C=C1C(C(F)F)=C1)=C1C#CC1=CC=C(CN2CCC(CO)CC2)C=C1 WPAZPBFPWDTKBY-PSPFREQMSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 abstract 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 abstract 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 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
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Referido a compuestos derivados de indazol acetileno de formula I, en donde R1 es H o halogeno; R2 y R2' se seleccionan independientemente de H y alquilo; o R2 y R2', junto con el atomo de carbono al que estan unidos, forman cicloalquilo; R3 es H o halogeno; R4 es alquilo; y R5 es hidroxialquil(heterocicloalquil)alquilo; o una sal farmaceuticamente aceptable de este. Estos compuestos son inhibidores alostericos selectivos de T790M/L858R, T790M/L858R/C797S, L858R y/o L858R/C797S que contienen mutantes de EGFR. Un compuesto seleccionado es 2-[4-(difluorometil)-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-7-metil-indazol-2-il]-2-[(6R)-6-fluoro-6,7-dihidro-5H-pirrolo[1,2-c]imidazol-1-il]-N-tiazol-2-ilacetamida. Tambien se refiere procesos para preparar dichos compuestos, composiciones farmaceuticas que los contienen y su uso en el tratamiento o profilaxis de cancer, en particular cancer de pulmon no microcitico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20210859 | 2020-12-01 | ||
| PCT/EP2021/083279 WO2022117477A1 (en) | 2020-12-01 | 2021-11-29 | New indazole acetylene derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240099A1 true PE20240099A1 (es) | 2024-01-18 |
Family
ID=73654642
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001615A PE20240099A1 (es) | 2020-12-01 | 2021-11-29 | Nuevos derivados de indazol acetileno |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20240002390A1 (es) |
| EP (1) | EP4255908A1 (es) |
| JP (1) | JP2023550902A (es) |
| KR (1) | KR20230116799A (es) |
| CN (1) | CN116490182A (es) |
| AR (1) | AR124170A1 (es) |
| AU (1) | AU2021393722A1 (es) |
| CA (1) | CA3197659A1 (es) |
| CL (1) | CL2023001440A1 (es) |
| CO (1) | CO2023006912A2 (es) |
| CR (1) | CR20230218A (es) |
| IL (1) | IL303064A (es) |
| MX (1) | MX2023006176A (es) |
| PE (1) | PE20240099A1 (es) |
| TW (1) | TW202237611A (es) |
| WO (1) | WO2022117477A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113966335B (zh) | 2019-06-21 | 2024-08-02 | 豪夫迈·罗氏有限公司 | 用于治疗癌症的egfr抑制剂 |
| CN119173253A (zh) * | 2022-05-13 | 2024-12-20 | 豪夫迈·罗氏有限公司 | 用于治疗癌症的变构和正构egfr抑制剂的组合产品 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1252693A1 (zh) * | 2015-06-30 | 2019-05-31 | Dana Farber Cancer Institute, Inc. | Egfr抑制剂及其使用方法 |
| TW201834651A (zh) * | 2016-12-22 | 2018-10-01 | 瑞士商赫孚孟拉羅股份公司 | 化合物 |
| AR113299A1 (es) * | 2017-06-02 | 2020-04-08 | Hoffmann La Roche | Compuestos de isoindolina |
| PE20211388A1 (es) * | 2018-06-29 | 2021-07-27 | Hoffmann La Roche | Compuestos |
| MA56507A (fr) * | 2019-06-21 | 2022-04-27 | Hoffmann La Roche | Nouveaux inhibiteurs d'egfr |
-
2021
- 2021-11-29 US US18/255,083 patent/US20240002390A1/en active Pending
- 2021-11-29 MX MX2023006176A patent/MX2023006176A/es unknown
- 2021-11-29 KR KR1020237018340A patent/KR20230116799A/ko active Pending
- 2021-11-29 JP JP2023527318A patent/JP2023550902A/ja active Pending
- 2021-11-29 WO PCT/EP2021/083279 patent/WO2022117477A1/en not_active Ceased
- 2021-11-29 PE PE2023001615A patent/PE20240099A1/es unknown
- 2021-11-29 AR ARP210103288A patent/AR124170A1/es not_active Application Discontinuation
- 2021-11-29 IL IL303064A patent/IL303064A/en unknown
- 2021-11-29 CN CN202180079840.XA patent/CN116490182A/zh active Pending
- 2021-11-29 CA CA3197659A patent/CA3197659A1/en active Pending
- 2021-11-29 CR CR20230218A patent/CR20230218A/es unknown
- 2021-11-29 AU AU2021393722A patent/AU2021393722A1/en active Pending
- 2021-11-29 EP EP21816073.7A patent/EP4255908A1/en active Pending
- 2021-11-30 TW TW110144518A patent/TW202237611A/zh unknown
-
2023
- 2023-05-18 CL CL2023001440A patent/CL2023001440A1/es unknown
- 2023-05-26 CO CONC2023/0006912A patent/CO2023006912A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN116490182A (zh) | 2023-07-25 |
| AU2021393722A1 (en) | 2023-04-13 |
| CA3197659A1 (en) | 2022-06-09 |
| JP2023550902A (ja) | 2023-12-06 |
| KR20230116799A (ko) | 2023-08-04 |
| IL303064A (en) | 2023-07-01 |
| CR20230218A (es) | 2023-07-07 |
| TW202237611A (zh) | 2022-10-01 |
| CL2023001440A1 (es) | 2023-12-01 |
| EP4255908A1 (en) | 2023-10-11 |
| WO2022117477A1 (en) | 2022-06-09 |
| US20240002390A1 (en) | 2024-01-04 |
| MX2023006176A (es) | 2023-06-08 |
| CO2023006912A2 (es) | 2023-06-09 |
| AR124170A1 (es) | 2023-02-22 |
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