PE20231311A1 - Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos - Google Patents
Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismosInfo
- Publication number
- PE20231311A1 PE20231311A1 PE2023001652A PE2023001652A PE20231311A1 PE 20231311 A1 PE20231311 A1 PE 20231311A1 PE 2023001652 A PE2023001652 A PE 2023001652A PE 2023001652 A PE2023001652 A PE 2023001652A PE 20231311 A1 PE20231311 A1 PE 20231311A1
- Authority
- PE
- Peru
- Prior art keywords
- group
- alkyl
- gcn2
- methods
- halogen
- Prior art date
Links
- 101000926525 Homo sapiens eIF-2-alpha kinase GCN2 Proteins 0.000 title abstract 2
- 102100034175 eIF-2-alpha kinase GCN2 Human genes 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- -1 (C=O)R13 Chemical group 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010027406 Mesothelioma Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108010089429 PERK kinase Proteins 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical group O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- 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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable, enantiomero, estereoisomero, o tautomero del mismo, donde: X1 se selecciona del grupo que consiste en CH y N; X2 y X3 se seleccionan en forma independiente entre si entre el grupo que consiste en N, CH, C-O-L2-E2, C-L2-E2, y C-N(R2)-L2-E2; X4 se selecciona del grupo que consiste en CR3 y N; X10 se selecciona del grupo que consiste en CR5 y N; X11 se selecciona del grupo que consiste en CR7 y N; R1 se selecciona del grupo que consiste en H, alquilo, (C=O)R13, cicloalquilo, entre otros; R2 se selecciona del grupo que consiste en H y alquilo; R3 se selecciona del grupo que consiste en H, alquilo, y halogeno; R4 y R5 se seleccionan en forma independiente entre si entre el grupo que consiste en halogeno, H, alcoxi, alquilamino, entre otros; R6 y R7 se seleccionan en forma independiente entre si entre el grupo que consiste en halogeno, H, y alquilo; R13 se selecciona del grupo que consiste en H, alquilo, cicloalquilo, entre otros; A se selecciona del grupo que consiste en un heteroarilo de 5 miembros sustituido, un heteroarilo de 6 miembros sustituido, una piridona, y un anillo arilo sustituido. Estos compuestos son inhibidores de GCN2 Y PERK quinasas. Tambien se refiere a metodos de preparacion de dichos compuestos, compuestos intermediarios, una composicion farmaceutica, y su uso en el tratamiento del cancer, tales como cancer colorrectal, cancer de pulmon, mesotelioma, entre otros.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063115496P | 2020-11-18 | 2020-11-18 | |
US202163185846P | 2021-05-07 | 2021-05-07 | |
PCT/US2021/059678 WO2022109001A1 (en) | 2020-11-18 | 2021-11-17 | Gcn2 and perk kinase inhibitors and methods of use thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20231311A1 true PE20231311A1 (es) | 2023-08-24 |
Family
ID=78844846
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2023001652A PE20231311A1 (es) | 2020-11-18 | 2021-11-17 | Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos |
Country Status (14)
Country | Link |
---|---|
US (1) | US11912668B2 (es) |
EP (1) | EP4247795A1 (es) |
JP (1) | JP2023549540A (es) |
KR (1) | KR20230121758A (es) |
AU (1) | AU2021381949A1 (es) |
BR (1) | BR112023009531A2 (es) |
CA (1) | CA3198943A1 (es) |
CL (1) | CL2023001399A1 (es) |
CO (1) | CO2023006705A2 (es) |
IL (1) | IL302807A (es) |
MX (1) | MX2023005747A (es) |
PE (1) | PE20231311A1 (es) |
TW (1) | TW202237568A (es) |
WO (1) | WO2022109001A1 (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB202008749D0 (en) | 2020-06-09 | 2020-07-22 | Ip2Ipo Innovations Ltd | Novel compounds |
US11912668B2 (en) | 2020-11-18 | 2024-02-27 | Deciphera Pharmaceuticals, Llc | GCN2 and perk kinase inhibitors and methods of use thereof |
MX2024003028A (es) * | 2021-09-10 | 2024-03-26 | Black Diamond Therapeutics Inc | Derivados de 6 aza quinolina y usos relacionados. |
TW202339730A (zh) * | 2021-12-03 | 2023-10-16 | 美商迪賽孚爾製藥有限公司 | Gcn2及perk激酶抑制劑及其使用方法 |
WO2023159322A1 (en) * | 2022-02-25 | 2023-08-31 | Ontario Institute For Cancer Research (Oicr) | Quinazoline derivatives as inhibitors of the gcn2 kinase, compositions and uses thereof |
WO2023196659A1 (en) * | 2022-04-08 | 2023-10-12 | Alesta Therapeutics BV | Gcn2 modulator compounds |
WO2023218195A1 (en) * | 2022-05-11 | 2023-11-16 | Ip2Ipo Innovations Limited | Gcn2 inhibitorr |
WO2023239165A1 (ko) * | 2022-06-08 | 2023-12-14 | 한국화학연구원 | 페닐설폰아마이드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
WO2024081916A1 (en) * | 2022-10-14 | 2024-04-18 | Black Diamond Therapeutics, Inc. | Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives |
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