PE20220141A1 - Inhibidores de la proteina tirosina fosfatasa - Google Patents
Inhibidores de la proteina tirosina fosfatasaInfo
- Publication number
- PE20220141A1 PE20220141A1 PE2021001646A PE2021001646A PE20220141A1 PE 20220141 A1 PE20220141 A1 PE 20220141A1 PE 2021001646 A PE2021001646 A PE 2021001646A PE 2021001646 A PE2021001646 A PE 2021001646A PE 20220141 A1 PE20220141 A1 PE 20220141A1
- Authority
- PE
- Peru
- Prior art keywords
- bicyclic
- membered
- heteroaryl
- heterocycle
- cyano
- Prior art date
Links
Classifications
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se refiere a compuestos de Formula I o una sal farmaceuticamente aceptable del mismo, donde: L1 se selecciona de un enlace directo, S, CH2, O, NH y Se; R1 se selecciona de hidrogeno y metilo; R2 se selecciona de fenilo, un heteroarilo de 5 a 6 miembros en donde el heteroarilo contiene 1 a 4 heteroatomos seleccionados del grupo que consiste en N, O y S, en donde un heteroatomo de N se puede sustituir con O para formar un oxido, un cicloalquilo biciclico de 8-10 miembros, un arilo biciclico de 10 miembros, un heterociclo biciclico de 9-10 miembros, en donde el heterociclo contiene 1 a 3 heteroatomos seleccionados del grupo que consiste en N, O y S, y un heteroarilo biciclico de 9-10 miembros, en donde el heteroarilo biciclico contiene 1 a 3 heteroatomos seleccionados del grupo que consiste en N, O y S, en donde el fenilo, heteroarilo, cicloalquilo biciclico, arilo biciclico, heterociclo biciclico y heteroarilo biciclico se sustituyen opcionalmente con halogeno, ciano, oxo, C1-C3 alquilo opcionalmente sustituido con 1 a 3 grupos seleccionados de halogeno, ciano y OH, C3-C6 cicloalquilo, C1-C3 alcoxi opcionalmente sustituido con 1 a 3 grupos seleccionados de halogeno, ciano y OH, NHRa, y un heterociclo de 3 a 6 miembros opcionalmente sustituido con 1 a 3 grupos seleccionados de halogeno, ciano y OH, en donde el heterociclo contiene 1 o 2 heteroatomos seleccionados de N, O y S. R2 se puede seleccionar del grupo de fenilo, 2-clorofenilo, 3-clorofenilo, 2,3-diclorofenilo, 2-amino-3-cloropiridin-4-ilo, 2,3-dicloropiridin-4-ilo, entre otros. Tambien se refiere a composiciones farmaceuticas. Dichos compuestos son utiles en el tratamiento de enfermedades hiperproliferativas y neoplasicas al inhibir la proteina SHP2 necesaria para la activacion completa de la via de Ras/ERK1/2, una cascada de senalizacion clave en la biologia del cancer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962828356P | 2019-04-02 | 2019-04-02 | |
| US202062992558P | 2020-03-20 | 2020-03-20 | |
| PCT/IB2020/053019 WO2020201991A1 (en) | 2019-04-02 | 2020-03-30 | Protein tyrosine phosphatase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220141A1 true PE20220141A1 (es) | 2022-01-27 |
Family
ID=70277430
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001646A PE20220141A1 (es) | 2019-04-02 | 2020-03-30 | Inhibidores de la proteina tirosina fosfatasa |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US11634417B2 (es) |
| EP (1) | EP3947367A1 (es) |
| JP (2) | JP7284830B2 (es) |
| KR (1) | KR102698608B1 (es) |
| CN (1) | CN113874363B (es) |
| AU (1) | AU2020251841B2 (es) |
| BR (1) | BR112021018664A2 (es) |
| CA (1) | CA3135555C (es) |
| CL (2) | CL2021002542A1 (es) |
| CO (1) | CO2021013030A2 (es) |
| CR (1) | CR20210501A (es) |
| CU (1) | CU20210080A7 (es) |
| DO (1) | DOP2021000206A (es) |
| EC (1) | ECSP21072994A (es) |
| GE (2) | GEP20237561B (es) |
| IL (2) | IL320682A (es) |
| MA (1) | MA55511A (es) |
| MX (1) | MX2021012122A (es) |
| PE (1) | PE20220141A1 (es) |
| PH (1) | PH12021552227A1 (es) |
| PY (1) | PY2018672A (es) |
| SG (1) | SG11202110502PA (es) |
| TW (1) | TWI766261B (es) |
| UY (1) | UY38628A (es) |
| WO (1) | WO2020201991A1 (es) |
| ZA (1) | ZA202108443B (es) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| JP7449282B2 (ja) | 2018-10-17 | 2024-03-13 | アレイ バイオファーマ インコーポレイテッド | タンパク質チロシンホスファターゼ阻害薬 |
| IL320682A (en) * | 2019-04-02 | 2025-07-01 | Array Biopharma Inc | Protein tyrosine phosphatase inhibitors |
| KR20230042600A (ko) | 2020-06-18 | 2023-03-28 | 레볼루션 메디슨즈, 인크. | Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법 |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| AU2021345111B2 (en) | 2020-09-15 | 2025-11-27 | Revolution Medicines, Inc. | Indole derivatives as Ras inhibitors in the treatment of cancer |
| US20240025924A1 (en) * | 2021-03-23 | 2024-01-25 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Heterocycle substituted ketone derivative, and composition and medicinal use thereof |
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| MX2023011664A (es) | 2021-04-01 | 2023-10-11 | Array Biopharma Inc | Forma cristalina de un inhibidor de shp2. |
| CN117460725A (zh) * | 2021-04-01 | 2024-01-26 | 阵列生物制药公司 | Shp2抑制剂的晶型 |
| AR125782A1 (es) | 2021-05-05 | 2023-08-16 | Revolution Medicines Inc | Inhibidores de ras |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
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| CN118684652A (zh) | 2017-09-11 | 2024-09-24 | 克鲁松制药公司 | SHP2的八氢环戊二烯并[c]吡咯别构抑制剂 |
| WO2019067843A1 (en) | 2017-09-29 | 2019-04-04 | Relay Therapeutics, Inc. | PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2 |
| SG11202002941WA (en) | 2017-10-12 | 2020-04-29 | Revolution Medicines Inc | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| CA3084058A1 (en) | 2017-12-15 | 2019-06-20 | Revolution Medicines, Inc. | Polycyclic compounds as allosteric shp2 inhibitors |
| US11426422B2 (en) | 2018-01-30 | 2022-08-30 | Research Development Foundation | SHP2 inhibitors and methods of use thereof |
| KR102724968B1 (ko) | 2018-03-21 | 2024-10-31 | 수조우 푸허 바이오파마 컴퍼니 리미티드 | Shp2 억제제 및 이의 용도 |
| CN117263942A (zh) | 2018-03-21 | 2023-12-22 | 传达治疗有限公司 | Shp2磷酸酶抑制剂及其使用方法 |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| WO2020033828A1 (en) | 2018-08-10 | 2020-02-13 | Board Of Regents, The University Of Texas System | 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer |
| CN112839935A (zh) * | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
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| IL320682A (en) * | 2019-04-02 | 2025-07-01 | Array Biopharma Inc | Protein tyrosine phosphatase inhibitors |
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