PE20211504A1 - Compuestos de anillo fusionado - Google Patents
Compuestos de anillo fusionadoInfo
- Publication number
- PE20211504A1 PE20211504A1 PE2021000682A PE2021000682A PE20211504A1 PE 20211504 A1 PE20211504 A1 PE 20211504A1 PE 2021000682 A PE2021000682 A PE 2021000682A PE 2021000682 A PE2021000682 A PE 2021000682A PE 20211504 A1 PE20211504 A1 PE 20211504A1
- Authority
- PE
- Peru
- Prior art keywords
- ras
- halo
- fused ring
- ring compounds
- bond
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 101710113436 GTPase KRas Proteins 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 102100039788 GTPase NRas Human genes 0.000 abstract 1
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 102000008300 Mutant Proteins Human genes 0.000 abstract 1
- 108010021466 Mutant Proteins Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 102000016914 ras Proteins Human genes 0.000 abstract 1
- 108010014186 ras Proteins Proteins 0.000 abstract 1
- 102200124918 rs121913250 Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Oncology (AREA)
- Hematology (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente invencion se refiere un compuesto de formula (I) o una sal aceptable de los mismos; donde R1 es una porcion electrofila capaz de formar un enlace covalente con un residuo de cisteina en la posicion 12 de una proteina mutante en G12C K-Ras; R2 es H, OH, NH2, halo, entre otros; R3 y R4 son H, NH2, halo, entre otros; R5 es H, NH2, halo, entre otros, en donde al menos uno de R2, R3, R4 y R5 es diferente de H; o R2 y R3, R3 y R4, o R4 y R5, junto con los atomos a los que cada uno esta unido, forman un C3-7 cicloalquilo, heterocicloalquilo de 3 a 7 miembros, entre otros; X es NH2, C1-6 alcoxi, C1-6 alquilo, entre otros; Y es -L-Y1 o Y1; U es C(R6a); V es C(R6b); W es C(R6c) o N; n se selecciona del grupo que consiste en 0 a 2; L es un enlace, O, S, entre otros; R6a, R6b y R6c son independientemente H, OH, NH2, entre otros; Y1 es H, NH2, halo, entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son anillos fusionados que inhiben las proteinas Ras, tales como K-Ras, H-Ras y N-Ras, siendo utiles en la inhibicion de la metastasis tumoral.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018114788 | 2018-11-09 | ||
| PCT/US2019/060578 WO2020097537A2 (en) | 2018-11-09 | 2019-11-08 | Fused ring compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211504A1 true PE20211504A1 (es) | 2021-08-11 |
Family
ID=69232886
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000682A PE20211504A1 (es) | 2018-11-09 | 2019-11-08 | Compuestos de anillo fusionado |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US11236068B2 (es) |
| EP (1) | EP3735299B1 (es) |
| JP (3) | JP6941241B2 (es) |
| KR (2) | KR20230147742A (es) |
| CN (5) | CN118084868A (es) |
| AR (1) | AR117194A1 (es) |
| AU (3) | AU2019377130B2 (es) |
| BR (1) | BR112021008986A2 (es) |
| CA (1) | CA3087089C (es) |
| CL (2) | CL2021001171A1 (es) |
| CO (1) | CO2021005987A2 (es) |
| CR (1) | CR20210229A (es) |
| IL (2) | IL311187A (es) |
| MA (1) | MA51530A (es) |
| MX (2) | MX2021005428A (es) |
| MY (1) | MY196726A (es) |
| NZ (1) | NZ775003A (es) |
| PE (1) | PE20211504A1 (es) |
| PH (1) | PH12021551065A1 (es) |
| SG (1) | SG11202103298QA (es) |
| TW (2) | TWI784209B (es) |
| UA (1) | UA127930C2 (es) |
| WO (1) | WO2020097537A2 (es) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7451419B2 (ja) | 2018-10-26 | 2024-03-18 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| CA3139348A1 (en) | 2019-05-21 | 2020-11-26 | InventisBio Co., Ltd. | Heterocyclic compounds for inhibiting ras and uses thereof |
| IL292438A (en) | 2019-10-28 | 2022-06-01 | Merck Sharp & Dohme | Small molecules that inhibit the g12c mutant of kras |
| WO2021108683A1 (en) | 2019-11-27 | 2021-06-03 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2021120045A1 (en) | 2019-12-18 | 2021-06-24 | InventisBio Co., Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| CN115916194A (zh) | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
| AU2021325869C1 (en) * | 2020-08-12 | 2024-05-30 | F. Hoffmann-La Roche Ag | Synthesis of quinazoline compounds |
| CA3189912A1 (en) * | 2020-08-17 | 2022-02-24 | Xiaofeng Xu | Bicyclic compounds, compositions and use thereof |
| WO2022060583A1 (en) | 2020-09-03 | 2022-03-24 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| EP4223761A1 (en) * | 2020-09-30 | 2023-08-09 | Shanghai Pharmaceuticals Holding Co., Ltd. | Quinazoline compound and application thereof |
| EP4240489A4 (en) * | 2020-11-03 | 2024-09-25 | Mirati Therapeutics Inc | KRAS G12D INHIBITORS |
| MX2023005529A (es) * | 2020-11-13 | 2023-05-25 | Genentech Inc | Metodos y composiciones que comprenden un inhibidor de krasg12c y un inhibidor de vegf para tratar tumores solidos. |
| US20220152029A1 (en) * | 2020-11-13 | 2022-05-19 | Genentech, Inc. | Methods and compositions comprising a krasg12c inhibitor and a pd-l1 binding antagonist for treating lung cancer |
| TW202229285A (zh) * | 2020-11-20 | 2022-08-01 | 大陸商北京加科思新藥研發有限公司 | Kras g12d抑制劑 |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| TW202423446A (zh) * | 2020-12-08 | 2024-06-16 | 美商建南德克公司 | 用於治療實性瘤之包含 krasg12c 抑制劑及 egfr 抑制劑之組成物及方法 |
| CN113999226B (zh) * | 2020-12-22 | 2023-01-06 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| TW202241869A (zh) * | 2020-12-22 | 2022-11-01 | 大陸商上海科州藥物研發有限公司 | 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法 |
| WO2022171013A1 (zh) * | 2021-02-09 | 2022-08-18 | 南京明德新药研发有限公司 | 四氢喹唑啉类化合物 |
| WO2022171018A1 (zh) * | 2021-02-09 | 2022-08-18 | 苏州泽璟生物制药股份有限公司 | 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用 |
| MX2023009135A (es) * | 2021-02-09 | 2023-08-16 | Genentech Inc | Compuestos de oxazepina tetraciclica y usos de estos. |
| JP2024506329A (ja) * | 2021-02-09 | 2024-02-13 | カムクワット バイオサイエンシーズ インコーポレイテッド | 複素環式化合物およびその使用 |
| MX2023008463A (es) * | 2021-02-16 | 2023-12-07 | Leidos Biomedical Res Inc | Composiciones y métodos para la inhibición del gen del virus de sarcoma de rata kirsten (kras). |
| WO2022214102A1 (zh) * | 2021-04-09 | 2022-10-13 | 杭州英创医药科技有限公司 | 作为kras g12d抑制剂的杂环化合物 |
| WO2022221386A1 (en) * | 2021-04-14 | 2022-10-20 | Erasca, Inc. | Selective kras inhibitors |
| US20240239788A1 (en) * | 2021-04-16 | 2024-07-18 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12d mutant |
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| CN115043729B (zh) * | 2022-07-04 | 2024-09-27 | 青岛大学 | 一种2,2’-二氟联芳基化合物的不对称合成方法 |
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2019
- 2019-11-08 TW TW108140719A patent/TWI784209B/zh active
- 2019-11-08 SG SG11202103298QA patent/SG11202103298QA/en unknown
- 2019-11-08 AR ARP190103302A patent/AR117194A1/es unknown
- 2019-11-08 CR CR20210229A patent/CR20210229A/es unknown
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