PE20211053A1 - Inhibicion de la proteasa 30 especifica de la ubiquitina (usp30) - Google Patents
Inhibicion de la proteasa 30 especifica de la ubiquitina (usp30)Info
- Publication number
- PE20211053A1 PE20211053A1 PE2021000398A PE2021000398A PE20211053A1 PE 20211053 A1 PE20211053 A1 PE 20211053A1 PE 2021000398 A PE2021000398 A PE 2021000398A PE 2021000398 A PE2021000398 A PE 2021000398A PE 20211053 A1 PE20211053 A1 PE 20211053A1
- Authority
- PE
- Peru
- Prior art keywords
- usp30
- ubiquitin
- specific protease
- substituted
- inhibition
- Prior art date
Links
Classifications
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- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- A61K31/435—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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- 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
-
- 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
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D471/08—Bridged systems
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/18—Bridged 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
La presente invencion se refiere a un compuesto de formula (I) o una sal farmaceuticamente aceptable de este, donde: Ar1 y Ar2 son fenileno o heteroarileno de 5-6 miembros, donde Ar1 y Ar2 estan sustituido con m y n grupos R1 y R2, respectivamente; L es -O-, -S-, S(O)2-, -S(O)-, entre otros; M es cicloalquilo de 3-6 miembros, fenilo o heteroarilo de 5-6 miembros, sustituido con p grupos R5; R1, R2 y R5 son halo, ciano, NO2, oxo, hidroxilo, entre otros; m, n y p son 0 a 4; Ra, Rb, Rc, Rd, Re, Rf, Rg y Rh se definen de la siguiente manera: i) Ra y Rb forman un grupo alquileno C1-C4 opcionalmente sustituido y Rc, Rd, Re, Rf, Rg y Rh son hidrogeno, halogeno, entre otros; o ii) Ra y Re forman un grupo alquileno C1-C2 opcionalmente sustituido y Rb, Rc, Rd, Rf, Rg y Rh son hidrogeno, halogeno, entre otros; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son inhibidores de la proteasa 30 especifica de la ubiquitina (USP30), siendo utiles en el tratamiento de la enfermedad de Parkinson.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862741945P | 2018-10-05 | 2018-10-05 | |
PCT/US2019/054803 WO2020072964A1 (en) | 2018-10-05 | 2019-10-04 | Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20211053A1 true PE20211053A1 (es) | 2021-06-07 |
Family
ID=68296856
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2021000398A PE20211053A1 (es) | 2018-10-05 | 2019-10-04 | Inhibicion de la proteasa 30 especifica de la ubiquitina (usp30) |
Country Status (28)
Country | Link |
---|---|
US (2) | US11535618B2 (es) |
EP (2) | EP3860989B1 (es) |
JP (1) | JP2022504211A (es) |
KR (1) | KR20210072791A (es) |
CN (1) | CN113166108A (es) |
AU (1) | AU2019356011A1 (es) |
BR (1) | BR112021003620A2 (es) |
CA (1) | CA3110113A1 (es) |
CL (1) | CL2021000793A1 (es) |
CO (1) | CO2021005070A2 (es) |
CY (1) | CY1126067T1 (es) |
DK (1) | DK3860989T3 (es) |
EA (1) | EA202190960A1 (es) |
ES (1) | ES2945834T3 (es) |
FI (1) | FI3860989T3 (es) |
HR (1) | HRP20230409T1 (es) |
HU (1) | HUE062240T2 (es) |
IL (1) | IL281980A (es) |
LT (1) | LT3860989T (es) |
MA (1) | MA53816A (es) |
MX (1) | MX2021002981A (es) |
PE (1) | PE20211053A1 (es) |
PL (1) | PL3860989T3 (es) |
PT (1) | PT3860989T (es) |
RS (1) | RS64321B1 (es) |
SG (1) | SG11202102815SA (es) |
SI (1) | SI3860989T1 (es) |
WO (1) | WO2020072964A1 (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2018346597B2 (en) | 2017-10-06 | 2023-07-13 | Forma Therapeutics, Inc. | Inhibiting Ubiquitin Specific Peptidase 30 |
EP3860989B1 (en) | 2018-10-05 | 2023-04-05 | Forma Therapeutics, Inc. | Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors |
GB201912674D0 (en) | 2019-09-04 | 2019-10-16 | Mission Therapeutics Ltd | Novel compounds |
JP2023520727A (ja) | 2020-04-08 | 2023-05-18 | ミッション セラピューティクス リミティド | Usp30阻害剤として活性を有するn-シアノピロリジン |
EP4157834A1 (en) | 2020-05-28 | 2023-04-05 | Mission Therapeutics Limited | N-(1-cyano-pyrrolidin-3-yl)-5-(3-(trifluoromethyl)phenyl)oxazole-2-carboxamide derivatives and the corresponding oxadiazole derivatives as usp30 inhibitors for the treatment of mitochondrial dysfunction |
CN115698001A (zh) | 2020-06-04 | 2023-02-03 | 特殊治疗有限公司 | 具有作为usp30抑制剂活性的n-氰基吡咯烷类化合物 |
WO2021249909A1 (en) | 2020-06-08 | 2021-12-16 | Mission Therapeutics Limited | 1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyr role-5(1h)-carbonitrile as usp30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis |
GB202016800D0 (en) | 2020-10-22 | 2020-12-09 | Mission Therapeutics Ltd | Novel compounds |
WO2023099561A1 (en) | 2021-12-01 | 2023-06-08 | Mission Therapeutics Limited | Substituted n-cyanopyrrolidines with activity as usp30 inhibitors |
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MA53816A (fr) | 2022-04-06 |
ES2945834T3 (es) | 2023-07-07 |
EP3860989A1 (en) | 2021-08-11 |
HRP20230409T1 (hr) | 2023-07-07 |
MX2021002981A (es) | 2021-05-14 |
SG11202102815SA (en) | 2021-04-29 |
RS64321B1 (sr) | 2023-08-31 |
CO2021005070A2 (es) | 2021-04-30 |
US20210355126A1 (en) | 2021-11-18 |
CY1126067T1 (el) | 2023-11-15 |
US11814386B2 (en) | 2023-11-14 |
LT3860989T (lt) | 2023-06-12 |
HUE062240T2 (hu) | 2023-10-28 |
WO2020072964A1 (en) | 2020-04-09 |
DK3860989T3 (da) | 2023-05-01 |
FI3860989T3 (fi) | 2023-05-25 |
EP3860989B1 (en) | 2023-04-05 |
EA202190960A1 (ru) | 2021-06-28 |
KR20210072791A (ko) | 2021-06-17 |
AU2019356011A1 (en) | 2021-04-01 |
CL2021000793A1 (es) | 2021-08-20 |
SI3860989T1 (sl) | 2023-06-30 |
US20230126252A1 (en) | 2023-04-27 |
CN113166108A (zh) | 2021-07-23 |
EP4218934A1 (en) | 2023-08-02 |
US11535618B2 (en) | 2022-12-27 |
PL3860989T3 (pl) | 2023-07-10 |
IL281980A (en) | 2021-05-31 |
BR112021003620A2 (pt) | 2021-05-18 |
CA3110113A1 (en) | 2020-04-09 |
PT3860989T (pt) | 2023-06-30 |
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