PE20200009A1 - Compuestos inhibidores de ask1 y usos de los mismos - Google Patents
Compuestos inhibidores de ask1 y usos de los mismosInfo
- Publication number
- PE20200009A1 PE20200009A1 PE2019001990A PE2019001990A PE20200009A1 PE 20200009 A1 PE20200009 A1 PE 20200009A1 PE 2019001990 A PE2019001990 A PE 2019001990A PE 2019001990 A PE2019001990 A PE 2019001990A PE 20200009 A1 PE20200009 A1 PE 20200009A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- same
- ask1
- inhibiting compounds
- triazol
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 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
- 230000002401 inhibitory effect Effects 0.000 title 1
- OBYPIQGEFWHGBZ-UHFFFAOYSA-N 2-[6-(4-cyclopropyl-1,2,4-triazol-3-yl)pyridin-2-yl]-3H-isoindol-1-one Chemical compound O=C1N(CC2=C1C=CC=C2)C1=NC(=CC=C1)C1=NN=CN1C1CC1 OBYPIQGEFWHGBZ-UHFFFAOYSA-N 0.000 abstract 1
- WFSMLFYAIYBAIR-UHFFFAOYSA-N 2-[6-(4-cyclopropyl-1,2,4-triazol-3-yl)pyridin-2-yl]-N,N-dimethyl-1-oxo-3H-isoindole-5-carboxamide Chemical compound CN(C)C(=O)C1=CC2=C(C=C1)C(=O)N(C2)C1=NC(=CC=C1)C1=NN=CN1C1CC1 WFSMLFYAIYBAIR-UHFFFAOYSA-N 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 230000006907 apoptotic process Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 abstract 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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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
- A61K31/435—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)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Cosmetics (AREA)
Abstract
La presente invencion se refiere a un compuesto de Formula III, o sales o solvatos farmaceuticamente aceptables del mismo, donde: A es una de las formulas que se indica a continuacion; Z es O, S, C (=O), N(R8) o C(R9)2; n es 0, 1, 2, 3 o 4; y R25 es halogeno, CN, OH, OR6, SR6, entre otros. Entre los compuestos preferidos tenemos los siguientes: 2-(6-(4-ciclopropil-4H-1,2,4-triazol-3-il)piridin-2-il)isoindolin-1-ona; 2-(6-(4-ciclopropil-4H-1,2,4-triazol-3-il)piridin-2-il)-N,N-dimetil-1-oxoisoindolina-5-carboxamida; entre otros. Dichos compuestos son inhibidores de ASK1 (apoptosis que regula la senal de la quinasa 1), siendo utiles para el tratamiento de esteatohepatitis no alcoholica. Tambien se refiere a una composicion farmaceutica que contiene dichos compuestos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762482085P | 2017-04-05 | 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 |
|---|---|
| PE20200009A1 true PE20200009A1 (es) | 2020-01-06 |
Family
ID=63712299
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001990A PE20200009A1 (es) | 2017-04-05 | 2018-04-04 | Compuestos inhibidores de ask1 y usos de los mismos |
Country Status (34)
| Country | Link |
|---|---|
| US (3) | US20210087167A1 (es) |
| EP (1) | EP3606519B1 (es) |
| JP (1) | JP7196093B2 (es) |
| KR (1) | KR102665145B1 (es) |
| CN (1) | CN110730661B (es) |
| AR (1) | AR111407A1 (es) |
| AU (1) | AU2018250217B2 (es) |
| CA (1) | CA3059107A1 (es) |
| CL (1) | CL2019002810A1 (es) |
| CO (1) | CO2019011708A2 (es) |
| CR (1) | CR20190503A (es) |
| CU (1) | CU20190080A7 (es) |
| DK (1) | DK3606519T3 (es) |
| DO (1) | DOP2019000255A (es) |
| EA (1) | EA201992299A1 (es) |
| EC (1) | ECSP19078393A (es) |
| ES (1) | ES2992084T3 (es) |
| FI (1) | FI3606519T3 (es) |
| HU (1) | HUE068103T2 (es) |
| IL (1) | IL269711B (es) |
| JO (1) | JOP20190221A1 (es) |
| MA (1) | MA49047A (es) |
| MX (1) | MX394098B (es) |
| NI (1) | NI201900102A (es) |
| NZ (1) | NZ758345A (es) |
| PE (1) | PE20200009A1 (es) |
| PH (1) | PH12019502288A1 (es) |
| PL (1) | PL3606519T3 (es) |
| PT (1) | PT3606519T (es) |
| RU (1) | RU2019134679A (es) |
| SG (1) | SG11201909155VA (es) |
| SI (1) | SI3606519T1 (es) |
| TW (1) | TWI779022B (es) |
| WO (1) | WO2018187506A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109071448B (zh) * | 2017-01-22 | 2020-03-17 | 福建广生堂药业股份有限公司 | Ask1抑制剂及其制备方法和应用 |
| ES2971098T3 (es) | 2017-05-12 | 2024-06-03 | Enanta Pharm Inc | Inhibidores de la quinasa 1 que regula la señal de apoptosis y métodos de uso de los mismos |
| CN111801314B (zh) | 2018-01-02 | 2023-10-31 | 西尔洛克治疗公司 | Ask1抑制剂化合物及其用途 |
| 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 |
| EP3787621B1 (en) | 2018-05-02 | 2024-12-18 | 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 |
| US11345699B2 (en) | 2018-11-19 | 2022-05-31 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| WO2020198214A1 (en) * | 2019-03-25 | 2020-10-01 | Enanta Pharmaceuticals, Inc. | Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
| 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 |
| MX2022008066A (es) | 2019-12-27 | 2022-08-15 | Lupin Ltd | Compuestos triciclicos sustituidos. |
| JP7303948B2 (ja) | 2020-05-01 | 2023-07-05 | ファイザー・インク | Ｈｐｋ１阻害薬としてのアザラクタム化合物 |
| WO2021224818A1 (en) * | 2020-05-08 | 2021-11-11 | Pfizer Inc. | Isoindolone compounds as hpk1 inhibitors |
| US20230271940A1 (en) * | 2020-08-03 | 2023-08-31 | Novartis Ag | Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US20260021084A1 (en) * | 2022-07-20 | 2026-01-22 | 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 |
| WO2026057806A1 (en) | 2024-09-13 | 2026-03-19 | Genfit | Injectable dosage form of 2-[6-(4-cyclopropyl-4h-1,2,4-triazol-3-yl)-2-pyridyl]-5-morpholinocarbonyl-1-isoindolinone |
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 |
| WO2011097079A1 (en) * | 2010-02-03 | 2011-08-11 | 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 |
| JP5927201B2 (ja) * | 2010-12-16 | 2016-06-01 | カルチャン リミテッド | Ａｓｋ１阻害ピロロピリミジン誘導体 |
| SG11201701723XA (en) * | 2014-09-24 | 2017-04-27 | Gilead Sciences Inc | Methods of treating liver disease |
| US10669242B2 (en) * | 2016-06-10 | 2020-06-02 | Venenum Biodesign, LLC | Clostridium difficile toxin inhibitors |
| PH12019501688B1 (en) | 2017-01-22 | 2023-08-04 | Fujian Akeylink Biotechnology Co Ltd | Pyridine derivative as ask1 inhibitor and preparation method and use thereof |
| CN109071448B (zh) | 2017-01-22 | 2020-03-17 | 福建广生堂药业股份有限公司 | Ask1抑制剂及其制备方法和应用 |
| EP3580224B1 (en) | 2017-02-07 | 2022-07-13 | Biogen MA Inc. | Ask1 inhibiting agents |
| CN109071498B (zh) | 2017-02-16 | 2021-03-30 | 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 |
| WO2018157856A1 (zh) | 2017-03-03 | 2018-09-07 | 江苏豪森药业集团有限公司 | 酰胺类衍生物抑制剂及其制备方法和应用 |
| US11345676B2 (en) | 2017-03-27 | 2022-05-31 | Pharmakea, Inc. | Apoptosis signal-regulating kinase 1 (ASK 1) inhibitor compounds |
| WO2019055540A1 (en) * | 2017-09-13 | 2019-03-21 | D.E. Shaw Research, Llc | COMPOUNDS AS INHIBITORS OF RAS AND THEIR USE |
| 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
-
2018
- 2018-04-03 TW TW107111742A patent/TWI779022B/zh active
- 2018-04-04 AU AU2018250217A patent/AU2018250217B2/en active Active
- 2018-04-04 CN CN201880037304.1A patent/CN110730661B/zh active Active
- 2018-04-04 CR CR20190503A patent/CR20190503A/es unknown
- 2018-04-04 US US16/499,075 patent/US20210087167A1/en not_active Abandoned
- 2018-04-04 SI SI201831140T patent/SI3606519T1/sl unknown
- 2018-04-04 NZ NZ758345A patent/NZ758345A/en unknown
- 2018-04-04 RU RU2019134679A patent/RU2019134679A/ru not_active Application Discontinuation
- 2018-04-04 FI FIEP18780760.7T patent/FI3606519T3/fi active
- 2018-04-04 CA CA3059107A patent/CA3059107A1/en active Pending
- 2018-04-04 WO PCT/US2018/026134 patent/WO2018187506A1/en not_active Ceased
- 2018-04-04 EA EA201992299A patent/EA201992299A1/ru unknown
- 2018-04-04 PT PT187807607T patent/PT3606519T/pt unknown
- 2018-04-04 CU CU2019000080A patent/CU20190080A7/es unknown
- 2018-04-04 PE PE2019001990A patent/PE20200009A1/es unknown
- 2018-04-04 DK DK18780760.7T patent/DK3606519T3/da active
- 2018-04-04 MA MA049047A patent/MA49047A/fr unknown
- 2018-04-04 ES ES18780760T patent/ES2992084T3/es active Active
- 2018-04-04 HU HUE18780760A patent/HUE068103T2/hu unknown
- 2018-04-04 PL PL18780760.7T patent/PL3606519T3/pl 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 SG SG11201909155V patent/SG11201909155VA/en unknown
- 2018-04-04 KR KR1020197032180A patent/KR102665145B1/ko active Active
- 2018-04-04 MX MX2019012013A patent/MX394098B/es 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
-
2019
- 2019-09-26 IL IL269711A patent/IL269711B/en unknown
- 2019-10-02 CL CL2019002810A patent/CL2019002810A1/es unknown
- 2019-10-03 NI NI201900102A patent/NI201900102A/es unknown
- 2019-10-03 PH PH12019502288A patent/PH12019502288A1/en 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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