RU2019134679A - Соединения на основе ингибиторов ask1 и их применение - Google Patents
Соединения на основе ингибиторов ask1 и их применение Download PDFInfo
- Publication number
- RU2019134679A RU2019134679A RU2019134679A RU2019134679A RU2019134679A RU 2019134679 A RU2019134679 A RU 2019134679A RU 2019134679 A RU2019134679 A RU 2019134679A RU 2019134679 A RU2019134679 A RU 2019134679A RU 2019134679 A RU2019134679 A RU 2019134679A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- group
- heterocycle
- solvate
- pharmaceutically acceptable
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims 59
- 101001018196 Homo sapiens Mitogen-activated protein kinase kinase kinase 5 Proteins 0.000 title 1
- 102100033127 Mitogen-activated protein kinase kinase kinase 5 Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 78
- 150000003839 salts Chemical class 0.000 claims 77
- 239000012453 solvate Substances 0.000 claims 77
- 125000001072 heteroaryl group Chemical group 0.000 claims 71
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 61
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 60
- 125000000217 alkyl group Chemical group 0.000 claims 54
- 229910052736 halogen Inorganic materials 0.000 claims 49
- 150000002367 halogens Chemical class 0.000 claims 49
- 125000003118 aryl group Chemical group 0.000 claims 40
- 229910052799 carbon Inorganic materials 0.000 claims 39
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 32
- 125000001424 substituent group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 28
- 239000001257 hydrogen Substances 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 27
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 22
- -1 —C 1-6 alkyl-OH Chemical group 0.000 claims 22
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 19
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 18
- 125000005842 heteroatom Chemical group 0.000 claims 17
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 14
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 4
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 4
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 4
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 4
- 150000003222 pyridines Chemical class 0.000 claims 4
- 150000003536 tetrazoles Chemical class 0.000 claims 4
- 150000003852 triazoles Chemical class 0.000 claims 4
- 150000002460 imidazoles Chemical class 0.000 claims 3
- 150000003217 pyrazoles Chemical class 0.000 claims 3
- 150000003557 thiazoles Chemical class 0.000 claims 3
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 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
- A61K31/435—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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- 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
- 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
- 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
- C07D487/04—Ortho-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
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cosmetics (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762482085P | 2017-04-05 | 2017-04-05 | |
| US62/482,085 | 2017-04-05 | ||
| PCT/US2018/026134 WO2018187506A1 (en) | 2017-04-05 | 2018-04-04 | Ask1 inhibitor compounds and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2019134679A true RU2019134679A (ru) | 2021-05-05 |
Family
ID=63712299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019134679A RU2019134679A (ru) | 2017-04-05 | 2018-04-04 | Соединения на основе ингибиторов ask1 и их применение |
Country Status (34)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018209573B2 (en) * | 2017-01-22 | 2020-08-13 | Fujian Akeylink Biotechnology Co., Ltd. | ASK1 inhibitor and preparation method and use thereof |
| EP3621615B1 (en) | 2017-05-12 | 2023-11-15 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US11434249B1 (en) | 2018-01-02 | 2022-09-06 | Seal Rock Therapeutics, Inc. | ASK1 inhibitor compounds and uses thereof |
| CN110407806B (zh) * | 2018-04-28 | 2021-08-17 | 深圳微芯生物科技股份有限公司 | 甲酰胺类化合物、其制备方法及其应用 |
| US11008304B2 (en) | 2018-05-02 | 2021-05-18 | Enanta Pharmaceuticals, Inc. | Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US10654833B2 (en) | 2018-06-28 | 2020-05-19 | Hepatikos Therapeutics, Llc | ASK1 isoindolin-1-one inhibitors and methods of use thereof |
| US10968199B2 (en) | 2018-08-22 | 2021-04-06 | Enanta Pharmaceuticals, Inc. | Cycloalkyl-containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| WO2020106707A1 (en) | 2018-11-19 | 2020-05-28 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| US11466033B2 (en) | 2019-03-25 | 2022-10-11 | Enanta Pharmaceuticals, Inc. | Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors |
| CN112409332B (zh) * | 2019-08-23 | 2023-12-08 | 广东东阳光药业股份有限公司 | 三氮唑衍生物及其在药物中的应用 |
| PH12022551585A1 (en) | 2019-12-27 | 2023-11-29 | Lupin Ltd | Substituted tricyclic compounds |
| KR20230003128A (ko) | 2020-05-01 | 2023-01-05 | 화이자 인코포레이티드 | Hpk1 억제제로서의 아잘락탐 화합물 |
| WO2021224818A1 (en) * | 2020-05-08 | 2021-11-11 | Pfizer Inc. | Isoindolone compounds as hpk1 inhibitors |
| CN116134027B (zh) * | 2020-08-03 | 2025-01-24 | 诺华股份有限公司 | 杂芳基取代的3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途 |
| AU2023311333A1 (en) * | 2022-07-20 | 2025-02-27 | Seal Rock Therapeutics, Inc. | Method of treating organ diseases or disorders with ask1 inhibitors |
| WO2025233319A1 (en) | 2024-05-06 | 2025-11-13 | Genfit | (1,2,4-triazol-3-yl)-2-pyridyl-1-isoindolinone for use in the treatment of sepsis |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4229447A (en) | 1979-06-04 | 1980-10-21 | American Home Products Corporation | Intraoral methods of using benzodiazepines |
| US4596795A (en) | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
| US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| US5739136A (en) | 1989-10-17 | 1998-04-14 | Ellinwood, Jr.; Everett H. | Intraoral dosing method of administering medicaments |
| TWI491606B (zh) | 2009-07-13 | 2015-07-11 | Gilead Sciences Inc | 調節細胞凋亡信號之激酶的抑制劑 |
| EP2531501B1 (en) * | 2010-02-03 | 2013-11-20 | Takeda Pharmaceutical Company Limited | Apoptosis signal-regulating kinase 1 inhibitors |
| WO2012079022A1 (en) * | 2010-12-10 | 2012-06-14 | Concert Pharmaceuticals, Inc. | Substituted dioxopiperidinyl phthalimide derivatives |
| EP2651417B1 (en) | 2010-12-16 | 2016-11-30 | Calchan Limited | Ask1 inhibiting pyrrolopyrimidine derivatives |
| ES2731602T3 (es) * | 2014-09-24 | 2019-11-18 | Gilead Sciences Inc | Métodos para tratar la enfermedad hepática |
| WO2017214359A1 (en) * | 2016-06-10 | 2017-12-14 | Venenum Biodesign Llc | Novel clostridium difficile toxin inhibitors |
| MY174821A (en) | 2017-01-22 | 2020-05-18 | Fujian Cosunter Pharmaceutical Co Ltd | Pyridine derivative as ask1 inhibitor and preparation method and use thereof |
| AU2018209573B2 (en) * | 2017-01-22 | 2020-08-13 | Fujian Akeylink Biotechnology Co., Ltd. | ASK1 inhibitor and preparation method and use thereof |
| EP3580224B1 (en) | 2017-02-07 | 2022-07-13 | Biogen MA Inc. | Ask1 inhibiting agents |
| WO2018149284A1 (zh) | 2017-02-16 | 2018-08-23 | 四川科伦博泰生物医药股份有限公司 | 激酶抑制剂及其制备方法和用途 |
| WO2018151830A1 (en) | 2017-02-17 | 2018-08-23 | Fronthera U.S. Pharmaceuticals Llc | Pyridinyl based apoptosis signal-regulation kinase inhibitors |
| WO2018157277A1 (en) | 2017-02-28 | 2018-09-07 | Eli Lilly And Company | Isoquinolin and naphthydrin compounds |
| JP7211959B2 (ja) | 2017-03-03 | 2023-01-24 | 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 | アミド類誘導体阻害剤及びその製造方法と使用 |
| US11345676B2 (en) | 2017-03-27 | 2022-05-31 | Pharmakea, Inc. | Apoptosis signal-regulating kinase 1 (ASK 1) inhibitor compounds |
| US20200308165A1 (en) * | 2017-09-13 | 2020-10-01 | D.E. Shaw Research, Llc | Compounds as Ras Inhibitors and Use Thereof |
| US10654833B2 (en) * | 2018-06-28 | 2020-05-19 | Hepatikos Therapeutics, Llc | ASK1 isoindolin-1-one inhibitors and methods of use thereof |
-
2017
- 2017-06-16 JO JOP/2019/0221A patent/JOP20190221A1/ar unknown
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2018
- 2018-04-03 TW TW107111742A patent/TWI779022B/zh active
- 2018-04-04 CN CN201880037304.1A patent/CN110730661B/zh active Active
- 2018-04-04 CR CR20190503A patent/CR20190503A/es unknown
- 2018-04-04 FI FIEP18780760.7T patent/FI3606519T3/fi active
- 2018-04-04 RU RU2019134679A patent/RU2019134679A/ru not_active Application Discontinuation
- 2018-04-04 MX MX2019012013A patent/MX394098B/es unknown
- 2018-04-04 EA EA201992299A patent/EA201992299A1/ru unknown
- 2018-04-04 US US16/499,075 patent/US20210087167A1/en not_active Abandoned
- 2018-04-04 CA CA3059107A patent/CA3059107A1/en active Pending
- 2018-04-04 NZ NZ758345A patent/NZ758345A/en unknown
- 2018-04-04 ES ES18780760T patent/ES2992084T3/es active Active
- 2018-04-04 HU HUE18780760A patent/HUE068103T2/hu unknown
- 2018-04-04 EP EP18780760.7A patent/EP3606519B1/en active Active
- 2018-04-04 JP JP2019553366A patent/JP7196093B2/ja active Active
- 2018-04-04 AU AU2018250217A patent/AU2018250217B2/en active Active
- 2018-04-04 SI SI201831140T patent/SI3606519T1/sl unknown
- 2018-04-04 MA MA049047A patent/MA49047A/fr unknown
- 2018-04-04 PL PL18780760.7T patent/PL3606519T3/pl unknown
- 2018-04-04 WO PCT/US2018/026134 patent/WO2018187506A1/en not_active Ceased
- 2018-04-04 PE PE2019001990A patent/PE20200009A1/es unknown
- 2018-04-04 CU CU2019000080A patent/CU20190080A7/es unknown
- 2018-04-04 PT PT187807607T patent/PT3606519T/pt unknown
- 2018-04-04 DK DK18780760.7T patent/DK3606519T3/da active
- 2018-04-04 KR KR1020197032180A patent/KR102665145B1/ko active Active
- 2018-04-04 SG SG11201909155V patent/SG11201909155VA/en unknown
- 2018-04-05 AR ARP180100846A patent/AR111407A1/es active IP Right Grant
- 2018-05-03 US US15/970,587 patent/US10150755B2/en active Active
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2019
- 2019-09-26 IL IL269711A patent/IL269711B/en unknown
- 2019-10-02 CL CL2019002810A patent/CL2019002810A1/es unknown
- 2019-10-03 PH PH12019502288A patent/PH12019502288A1/en unknown
- 2019-10-03 NI NI201900102A patent/NI201900102A/es unknown
- 2019-10-04 DO DO2019000255A patent/DOP2019000255A/es unknown
- 2019-10-23 CO CONC2019/0011708A patent/CO2019011708A2/es unknown
- 2019-10-31 EC ECSENADI201978393A patent/ECSP19078393A/es unknown
-
2024
- 2024-09-26 US US18/897,798 patent/US20250304552A1/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA93 | Acknowledgement of application withdrawn (no request for examination) |
Effective date: 20210405 |