AR128761A1 - Compuesto heterocíclico para inducir la degradación de la proteína kras mutante en g12d - Google Patents
Compuesto heterocíclico para inducir la degradación de la proteína kras mutante en g12dInfo
- Publication number
- AR128761A1 AR128761A1 ARP230100604A ARP230100604A AR128761A1 AR 128761 A1 AR128761 A1 AR 128761A1 AR P230100604 A ARP230100604 A AR P230100604A AR P230100604 A ARP230100604 A AR P230100604A AR 128761 A1 AR128761 A1 AR 128761A1
- Authority
- AR
- Argentina
- Prior art keywords
- pancreatic cancer
- mutant kras
- degradation
- heterocyclic compound
- induce
- Prior art date
Links
- 102100030708 GTPase KRas Human genes 0.000 title abstract 3
- 150000002391 heterocyclic compounds Chemical class 0.000 title abstract 3
- 102200006539 rs121913529 Human genes 0.000 title abstract 3
- 230000015556 catabolic process Effects 0.000 title abstract 2
- 238000006731 degradation reaction Methods 0.000 title abstract 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 4
- 201000002528 pancreatic cancer Diseases 0.000 abstract 4
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 4
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 229940124597 therapeutic agent Drugs 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
[Problema] Proporcionar un compuesto de utilidad como ingrediente activo de una composición farmacéutica para tratar el cáncer de páncreas. [Medio de solución] Los inventores de la presente han estudiado un compuesto que resulta de utilidad como ingrediente activo de una composición farmacéutica para tratar el cáncer de páncreas y han establecido que los compuestos heterocíclicos representados por la fórmula (1) y la fórmula (1A) tienen una excelente acción inductora de la degradación sobre una proteína KRAS mutante en G12D y actividad de inhibición de KRAS mutante en G12D y que pueden usarse como agentes terapéuticos para el cáncer de páncreas, habiendo de esta forma concebido la presente invención. El compuesto heterocíclico o una sal del mismo de la presente invención se puede usar como agente terapéutico para el cáncer de páncreas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022038252 | 2022-03-11 | ||
| JP2022126816 | 2022-08-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR128761A1 true AR128761A1 (es) | 2024-06-12 |
Family
ID=87935451
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP230100604A AR128761A1 (es) | 2022-03-11 | 2023-03-10 | Compuesto heterocíclico para inducir la degradación de la proteína kras mutante en g12d |
Country Status (4)
| Country | Link |
|---|---|
| AR (1) | AR128761A1 (es) |
| AU (1) | AU2023231912A1 (es) |
| TW (1) | TW202346270A (es) |
| WO (1) | WO2023171781A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024188281A1 (zh) * | 2023-03-13 | 2024-09-19 | 南京明德新药研发有限公司 | 含喹唑啉结构的化合物及其应用 |
| WO2024199266A1 (en) * | 2023-03-27 | 2024-10-03 | Shenzhen Ionova Life Science Co., Ltd. | Compounds for degradation and inhibition of kras (g12d) protein |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017172979A1 (en) * | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| WO2021041671A1 (en) * | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| CN116848120A (zh) * | 2021-02-15 | 2023-10-03 | 安斯泰来制药株式会社 | 用于诱导g12d突变kras蛋白分解的喹唑啉化合物 |
| AU2022219651A1 (en) * | 2021-02-15 | 2023-09-07 | Astellas Pharma Inc. | 4-aminoquinazoline compound |
-
2023
- 2023-03-10 AU AU2023231912A patent/AU2023231912A1/en active Pending
- 2023-03-10 WO PCT/JP2023/009205 patent/WO2023171781A1/ja active Application Filing
- 2023-03-10 AR ARP230100604A patent/AR128761A1/es unknown
- 2023-03-10 TW TW112108905A patent/TW202346270A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2023231912A1 (en) | 2024-08-15 |
| WO2023171781A1 (ja) | 2023-09-14 |
| TW202346270A (zh) | 2023-12-01 |
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