PE20220961A1 - Moduladores de la via de respuesta integrada al estres - Google Patents
Moduladores de la via de respuesta integrada al estresInfo
- Publication number
- PE20220961A1 PE20220961A1 PE2021001762A PE2021001762A PE20220961A1 PE 20220961 A1 PE20220961 A1 PE 20220961A1 PE 2021001762 A PE2021001762 A PE 2021001762A PE 2021001762 A PE2021001762 A PE 2021001762A PE 20220961 A1 PE20220961 A1 PE 20220961A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- optionally substituted
- modulators
- stress response
- fluorophenoxy
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invencion se refiere a los compuestos de la formula (I), en donde X1 es N(Ra1); X1a es un enlace covalente simple, CH(Ra3) o CH(Ra3)CH2; R1 es H o C1-4 alquilo opcionalmente sustituido con uno o mas halogenos, que son iguales o diferentes; R2 es H, F, o C1-4 alquilo, en donde C1-4 alquilo esta opcionalmente sustituido con uno o mas halogenos; R3 es A3, C1-6 alquilo, C2-6 alquenilo o C2-6 alquinilo, opcionalmente sustituidos; Ra2, Ra3 se seleccionan independientemente de H, OH, OC1-4 alquilo, halogeno, C1-4 alquilo y A2a; A1 es C5 cicloalquileno, C5 cicloalquenileno o un anillo heterocicleno de 5 miembros que contiene de nitrogeno, opcionalmente sustituidos; A2 es R6a o A2a; Ra4, Ra5, Ra6, Ra7 se seleccionan independientemente de H, halogeno, C1-4 alquilo y A2a. Un compuesto seleccionado es (2R,5S)-5-[2-(4-cloro-3-fluorofenoxi)acetamido]-2-{5-[4- (trifluorometil)fenil]-1,3,4-oxadiazol-2-il}piperidina-1-carboxilato de terc butilo 2-(4-cloro-3-fluorofenoxi)-N-[(3S,6R)-6-{5-[4-(trifluorometil)fenil]-1,3,4- oxadiazol-2-il}piperidin-3-il]acetamida. Dichos compuestos son moduladores de la via de respuesta integrada al estres (ISR). Tambien provee una composicion farmaceutica que los contiene para el tratamiento de enfermedades o trastornos asociados con la respuesta integrada al estres.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19170504 | 2019-04-23 | ||
| EP19216875 | 2019-12-17 | ||
| PCT/EP2020/061150 WO2020216766A1 (en) | 2019-04-23 | 2020-04-22 | Modulators of the integrated stress response pathway |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220961A1 true PE20220961A1 (es) | 2022-06-10 |
Family
ID=70289816
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001762A PE20220961A1 (es) | 2019-04-23 | 2020-04-22 | Moduladores de la via de respuesta integrada al estres |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20220227747A1 (es) |
| EP (1) | EP3959198A1 (es) |
| JP (1) | JP2022530049A (es) |
| KR (1) | KR20220004105A (es) |
| CN (1) | CN113993850B (es) |
| AU (1) | AU2020261234A1 (es) |
| BR (1) | BR112021020402A2 (es) |
| CA (1) | CA3137213A1 (es) |
| CL (1) | CL2021002772A1 (es) |
| CO (1) | CO2021014292A2 (es) |
| IL (1) | IL287379A (es) |
| MX (1) | MX2021012903A (es) |
| PE (1) | PE20220961A1 (es) |
| SG (1) | SG11202111119PA (es) |
| WO (1) | WO2020216766A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018383675A1 (en) | 2017-12-13 | 2020-07-09 | Altos Labs, Inc. | Inhibitors of integrated stress response pathway |
| SG11202011014VA (en) | 2018-06-05 | 2020-12-30 | Praxis Biotech LLC | Inhibitors of integrated stress response pathway |
| CR20210426A (es) * | 2019-02-13 | 2021-09-30 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| EP3924341A4 (en) | 2019-02-13 | 2022-11-02 | Denali Therapeutics Inc. | COMPOUNDS, COMPOSITIONS AND METHODS |
| EP3982965A4 (en) | 2019-06-12 | 2023-01-25 | Praxis Biotech LLC | INTEGRATED STRESS RESPONSE PATHWAY MODULATORS |
| WO2021165927A1 (en) * | 2020-02-21 | 2021-08-26 | Wockhardt Bio Ag | 2-cyanopyrroldines, -piperidines or -dazepines as hyperglycemic agents |
| EP4117780A1 (en) | 2020-03-11 | 2023-01-18 | Evotec International GmbH | Modulators of the integrated stress response pathway |
| AU2021366303A1 (en) | 2020-10-22 | 2023-06-22 | Evotec International Gmbh | Modulators of the integrated stress response pathway |
| US20230391725A1 (en) | 2020-10-22 | 2023-12-07 | Evotec International Gmbh | Modulators of the integrated stress response pathway |
| AU2021363616A1 (en) | 2020-10-22 | 2023-06-22 | Evotec International Gmbh | Modulators of the integrated stress response pathway |
| US20230083885A1 (en) * | 2021-04-02 | 2023-03-16 | Praxis Biotech LLC | Modulators of integrated stress response pathway |
| WO2024109736A1 (zh) * | 2022-11-21 | 2024-05-30 | 深圳众格生物科技有限公司 | 一种化合物、包含其的药物组合物及其合成方法和用途 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2904794C (en) | 2013-03-15 | 2021-11-23 | Peter Walter | Modulators of the eif2alpha pathway |
| SG11201610770PA (en) * | 2014-07-04 | 2017-01-27 | Lupin Ltd | Quinolizinone derivatives as pi3k inhibitors |
| TW201722957A (zh) * | 2015-09-15 | 2017-07-01 | 葛蘭素史克智慧財產（第二）有限公司 | 化學化合物 |
| WO2017046739A1 (en) * | 2015-09-15 | 2017-03-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Imidazolidinone derivatives as inhibitors of perk |
| TWI844006B (zh) | 2016-05-05 | 2024-06-01 | 美商嘉來克生命科學有限責任公司 | 整合應激途徑之調節劑 |
| TW201808888A (zh) | 2016-05-05 | 2018-03-16 | 嘉來克生命科學有限責任公司 | 整合應激途徑之調節劑 |
| TW201808914A (zh) | 2016-05-05 | 2018-03-16 | 嘉來克生命科學有限責任公司 | 整合應激途徑之調節劑 |
| TW201808903A (zh) | 2016-05-05 | 2018-03-16 | 嘉來克生命科學有限責任公司 | 整合應激途徑之調節劑 |
| EP3468960B1 (en) | 2016-06-08 | 2022-03-23 | GlaxoSmithKline Intellectual Property Development Limited | Chemical compounds as atf4 pathway inhibitors |
| WO2017212423A1 (en) | 2016-06-08 | 2017-12-14 | Glaxosmithkline Intellectual Property Development Limited | Chemcical compounds |
| WO2018225093A1 (en) | 2017-06-07 | 2018-12-13 | Glaxosmithkline Intellectual Property Development Limited | Chemical compounds as atf4 pathway inhibitors |
| US20200140383A1 (en) | 2017-07-03 | 2020-05-07 | Glaxosmithkline Intellectual Property Development Limited | 2-(4-chlorophenoxy)-n-((1 -(2-(4-chlorophenoxy)ethynazetidin-3-yl)methyl)acetamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases |
| US20210145771A1 (en) | 2017-07-03 | 2021-05-20 | Glaxosmithkline Intellectual Property Development Limited | N-(3-(2-(4-chlorophenoxy)acetamido)bicyclo[1.1.1] pentan-1-yl)-2-cyclobutane-1- carboxamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases |
| EP3665156A4 (en) | 2017-08-09 | 2021-04-28 | Denali Therapeutics Inc. | COMPOUNDS, COMPOSITIONS, AND PROCEDURES |
| EP4248965A3 (en) | 2017-09-01 | 2023-11-22 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| UY37956A (es) | 2017-11-02 | 2019-05-31 | Abbvie Inc | Moduladores de la vía de estrés integrada |
| AU2018358160B2 (en) | 2017-11-02 | 2023-03-16 | Abbvie Inc. | Modulators of the integrated stress pathway |
| UY37957A (es) | 2017-11-02 | 2019-05-31 | Abbvie Inc | Moduladores de la vía de estrés integrada |
| CN112154142B (zh) | 2017-11-02 | 2023-11-21 | 卡里科生命科学有限责任公司 | 整合应激通路的调节剂 |
| MX2020004534A (es) | 2017-11-02 | 2020-10-19 | Calico Life Sciences Llc | Moduladores de la vía integrada del estrés. |
| AU2018360855B2 (en) | 2017-11-02 | 2023-04-06 | Abbvie Inc. | Modulators of the integrated stress pathway |
| AU2018358157B2 (en) | 2017-11-02 | 2023-03-09 | Abbvie Inc. | Modulators of the integrated stress pathway |
| UY37958A (es) | 2017-11-02 | 2019-05-31 | Abbvie Inc | Moduladores de la vía de estrés integrada |
| CA3080948A1 (en) | 2017-11-02 | 2019-05-09 | Calico Life Sciences Llc | Modulators of the integrated stress pathway |
| AU2018383675A1 (en) | 2017-12-13 | 2020-07-09 | Altos Labs, Inc. | Inhibitors of integrated stress response pathway |
| WO2019183589A1 (en) | 2018-03-23 | 2019-09-26 | Denali Therapeutics Inc. | Modulators of eukaryotic initiation factor 2 |
| WO2019193540A1 (en) | 2018-04-06 | 2019-10-10 | Glaxosmithkline Intellectual Property Development Limited | Heteroaryl derivatives of formula (i) as atf4 inhibitors |
| WO2019193541A1 (en) | 2018-04-06 | 2019-10-10 | Glaxosmithkline Intellectual Property Development Limited | Bicyclic aromatic ring derivatives of formula (i) as atf4 inhibitors |
-
2020
- 2020-04-22 JP JP2021562988A patent/JP2022530049A/ja active Pending
- 2020-04-22 MX MX2021012903A patent/MX2021012903A/es unknown
- 2020-04-22 PE PE2021001762A patent/PE20220961A1/es unknown
- 2020-04-22 CA CA3137213A patent/CA3137213A1/en active Pending
- 2020-04-22 SG SG11202111119PA patent/SG11202111119PA/en unknown
- 2020-04-22 US US17/605,037 patent/US20220227747A1/en active Pending
- 2020-04-22 WO PCT/EP2020/061150 patent/WO2020216766A1/en unknown
- 2020-04-22 CN CN202080045788.1A patent/CN113993850B/zh active Active
- 2020-04-22 EP EP20719452.3A patent/EP3959198A1/en active Pending
- 2020-04-22 AU AU2020261234A patent/AU2020261234A1/en active Pending
- 2020-04-22 KR KR1020217037824A patent/KR20220004105A/ko unknown
- 2020-04-22 BR BR112021020402A patent/BR112021020402A2/pt unknown
-
2021
- 2021-10-19 IL IL287379A patent/IL287379A/en unknown
- 2021-10-22 CL CL2021002772A patent/CL2021002772A1/es unknown
- 2021-10-26 CO CONC2021/0014292A patent/CO2021014292A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN113993850A (zh) | 2022-01-28 |
| IL287379A (en) | 2021-12-01 |
| CA3137213A1 (en) | 2020-10-29 |
| JP2022530049A (ja) | 2022-06-27 |
| KR20220004105A (ko) | 2022-01-11 |
| MX2021012903A (es) | 2022-01-18 |
| BR112021020402A2 (pt) | 2021-12-07 |
| US20220227747A1 (en) | 2022-07-21 |
| WO2020216766A1 (en) | 2020-10-29 |
| CL2021002772A1 (es) | 2022-07-29 |
| EP3959198A1 (en) | 2022-03-02 |
| SG11202111119PA (en) | 2021-11-29 |
| CO2021014292A2 (es) | 2022-04-29 |
| AU2020261234A1 (en) | 2021-11-11 |
| CN113993850B (zh) | 2024-03-29 |
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