MX2017012926A - Inhibidores y sus usos. - Google Patents
Inhibidores y sus usos.Info
- Publication number
- MX2017012926A MX2017012926A MX2017012926A MX2017012926A MX2017012926A MX 2017012926 A MX2017012926 A MX 2017012926A MX 2017012926 A MX2017012926 A MX 2017012926A MX 2017012926 A MX2017012926 A MX 2017012926A MX 2017012926 A MX2017012926 A MX 2017012926A
- Authority
- MX
- Mexico
- Prior art keywords
- inhibitors
- ppp1r15b
- ppp1r15a
- compounds
- disorder
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
- C12Q1/42—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving phosphatase
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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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C281/00—Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
- C07C281/16—Compounds containing any of the groups, e.g. aminoguanidine
- C07C281/18—Compounds containing any of the groups, e.g. aminoguanidine the other nitrogen atom being further doubly-bound to a carbon atom, e.g. guanylhydrazones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/61—Halogen atoms or nitro radicals
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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
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/30—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N11/00—Carrier-bound or immobilised enzymes; Carrier-bound or immobilised microbial cells; Preparation thereof
- C12N11/14—Enzymes or microbial cells immobilised on or in an inorganic carrier
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N21/00—Investigating or analysing materials by the use of optical means, i.e. using sub-millimetre waves, infrared, visible or ultraviolet light
- G01N21/17—Systems in which incident light is modified in accordance with the properties of the material investigated
- G01N21/25—Colour; Spectral properties, i.e. comparison of effect of material on the light at two or more different wavelengths or wavelength bands
- G01N21/31—Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/914—Hydrolases (3)
- G01N2333/916—Hydrolases (3) acting on ester bonds (3.1), e.g. phosphatases (3.1.3), phospholipases C or phospholipases D (3.1.4)
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Physics & Mathematics (AREA)
- Neurosurgery (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biotechnology (AREA)
- Analytical Chemistry (AREA)
- Microbiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- General Engineering & Computer Science (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Biophysics (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Food Science & Technology (AREA)
- Cell Biology (AREA)
- Spectroscopy & Molecular Physics (AREA)
Abstract
La presente invención se refiere a inhibidores de PPP1R15A y PPP1R15B, así como su uso en terapia, particularmente en el tratamiento de un estado de la enfermedad aliviado por la inhibición de PPP1R15A y PPP1R15B, por ejemplo un trastorno asociado con la acumulación de proteínas mal plegadas o trastorno de proteostasis. Los compuestos de la invención incluyen compuestos que tienen la fórmula IA o una sal farmacéuticamente aceptable de la misma, en donde R1a, R3a, R5a, Xa y Ya son como se define en la presente.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1505975.1A GB201505975D0 (en) | 2015-04-08 | 2015-04-08 | Inhibitors and their uses |
| GBGB1505971.0A GB201505971D0 (en) | 2015-04-08 | 2015-04-08 | Inhibitors and their uses |
| PCT/GB2016/050991 WO2016162689A1 (en) | 2015-04-08 | 2016-04-08 | Inhibitors and their uses |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017012926A true MX2017012926A (es) | 2017-12-20 |
| MX379437B MX379437B (es) | 2025-03-10 |
Family
ID=55759894
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017012926A MX379437B (es) | 2015-04-08 | 2016-04-08 | Derivados de hidrazina-bencilo sustituidos, como inhibidores de ppp1r15a y ppp1r15b, y el uso de los mismos para el tratamiento de trastorno de proteostasis. |
| MX2017012924A MX382385B (es) | 2015-04-08 | 2016-04-08 | Métodos para seleccionar inhibidores selectivos de fosfatasa e inhibidores no selectivos de fosfatasa. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017012924A MX382385B (es) | 2015-04-08 | 2016-04-08 | Métodos para seleccionar inhibidores selectivos de fosfatasa e inhibidores no selectivos de fosfatasa. |
Country Status (14)
| Country | Link |
|---|---|
| US (5) | US11364211B2 (es) |
| EP (2) | EP3280404B1 (es) |
| JP (2) | JP6868568B2 (es) |
| KR (2) | KR102572217B1 (es) |
| CN (2) | CN107709291B (es) |
| AU (2) | AU2016246098B2 (es) |
| BR (2) | BR112017021522B1 (es) |
| CA (2) | CA2982040C (es) |
| DK (2) | DK3280404T3 (es) |
| ES (2) | ES2897712T3 (es) |
| IL (2) | IL254928B (es) |
| MX (2) | MX379437B (es) |
| SG (2) | SG11201708249SA (es) |
| WO (2) | WO2016162689A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6868568B2 (ja) | 2015-04-08 | 2021-05-12 | メディカル リサーチ カウンシルＭｅｄｉｃａｌ Ｒｅｓｅａｒｃｈ Ｃｏｕｎｃｉｌ | ホスファターゼ選択的および非選択的なホスファターゼ阻害剤を選択するための方法 |
| US20180230105A1 (en) | 2017-01-13 | 2018-08-16 | Regents Of The University Of Minnesota | Therapeutic compounds |
| GB201709927D0 (en) * | 2017-06-21 | 2017-08-02 | Medical Res Council | Biochemically defined functional and selective activity and methods for selecting selective inhibitors of holophosphatases targeting their regulatory subunits |
| WO2024009280A1 (en) * | 2022-07-08 | 2024-01-11 | Baylor College Of Medicine | Integrated stress response inhibitors and methods of using the same |
| US20240293343A1 (en) * | 2023-02-13 | 2024-09-05 | Inflectis Bioscience | Benzylideneaminoguanidine derivatives as NR2B-selective NMDA receptor antagonists and their therapeutic applications |
| KR20250157531A (ko) * | 2023-03-16 | 2025-11-04 | 교토후고리츠다이가쿠호진 | Ampk 활성화 및/또는 chop 억제에 의한 치료가 가능한 질환 및 장애의 치료를 위한 sephin1 및 관련 화합물 |
| CN116735892A (zh) * | 2023-05-24 | 2023-09-12 | 中南大学湘雅医院 | 一种阿尔茨海默病早期诊断标志物及其应用 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1223491A (en) | 1967-10-13 | 1971-02-24 | American Home Prod | Guanidines |
| US3592935A (en) * | 1969-12-11 | 1971-07-13 | Sandoz Ag | Substituted benzylidene hydrazines as anti-inflammatory agents |
| US3982020A (en) * | 1970-03-17 | 1976-09-21 | Sandoz, Inc. | Substituted benzylidene hydrazines for treating hyperglycemia, obesity and inflammation |
| GB1550401A (en) * | 1976-01-07 | 1979-08-15 | Hexachimie | Hydrazine derivatives their preparation and their use |
| WO2001025192A1 (en) * | 1999-10-06 | 2001-04-12 | Melacure Therapeutics Ab | Guanidine derivatives and their use in the production of a medicament for blocking xanthine oxidase/dehydrogenase |
| GB0019357D0 (en) * | 2000-08-07 | 2000-09-27 | Melacure Therapeutics Ab | Novel phenyl guanidines |
| AU2004276812A1 (en) * | 2003-09-25 | 2005-04-07 | Acadia Pharmaceuticals Inc. | Treating neuropathic pain with neuropeptide FF receptor 2 agonists |
| FR2893844B1 (fr) | 2005-11-28 | 2008-02-01 | Centre Nat Rech Scient | Utilisation du guanabenz et de ses derives pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules |
| EP1908465B1 (en) | 2006-10-04 | 2009-04-29 | Centre National De La Recherche Scientifique (Cnrs) | Use of chlorine guanabenz derivatives for treating prion-based diseases |
| EP1908464A1 (en) | 2006-10-04 | 2008-04-09 | Centre National De La Recherche Scientifique (Cnrs) | Use of chlorine guanabenz derivatives for treating polyglutamine expansion associated diseases |
| GB201300435D0 (en) | 2013-01-10 | 2013-02-27 | Medical Res Council | Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases |
| US10905663B2 (en) | 2013-03-05 | 2021-02-02 | The University Of Chicago | Treatment of demyelinating disorders |
| US20150246140A1 (en) | 2014-02-10 | 2015-09-03 | California Institute Of Technology | Compositions and methods for modulating sleep and wakefulness |
| AU2015282900B2 (en) | 2014-07-02 | 2020-06-18 | Inflectis Bioscience | Novel therapeutic uses of benzylideneguanidine derivatives for the treatment of proteopathies |
| SI3164391T1 (sl) | 2014-07-02 | 2019-12-31 | InFlectis BioScience, | O-alkil-benzilidengvanidinski derivati in terapevtska uporaba za zdravljenje motenj, povezanih z nabiranjem napačno zvitih proteinov |
| JP6868568B2 (ja) | 2015-04-08 | 2021-05-12 | メディカル リサーチ カウンシルＭｅｄｉｃａｌ Ｒｅｓｅａｒｃｈ Ｃｏｕｎｃｉｌ | ホスファターゼ選択的および非選択的なホスファターゼ阻害剤を選択するための方法 |
| US20180230105A1 (en) * | 2017-01-13 | 2018-08-16 | Regents Of The University Of Minnesota | Therapeutic compounds |
-
2016
- 2016-04-08 JP JP2017553071A patent/JP6868568B2/ja not_active Expired - Fee Related
- 2016-04-08 CA CA2982040A patent/CA2982040C/en active Active
- 2016-04-08 WO PCT/GB2016/050991 patent/WO2016162689A1/en not_active Ceased
- 2016-04-08 US US15/564,863 patent/US11364211B2/en active Active
- 2016-04-08 JP JP2017553070A patent/JP6882189B2/ja active Active
- 2016-04-08 SG SG11201708249SA patent/SG11201708249SA/en unknown
- 2016-04-08 CA CA2982033A patent/CA2982033C/en active Active
- 2016-04-08 US US15/564,834 patent/US11154519B2/en active Active
- 2016-04-08 DK DK16717193.3T patent/DK3280404T3/da active
- 2016-04-08 EP EP16717193.3A patent/EP3280404B1/en active Active
- 2016-04-08 CN CN201680033508.9A patent/CN107709291B/zh active Active
- 2016-04-08 EP EP16717688.2A patent/EP3280405B1/en active Active
- 2016-04-08 CN CN201680033501.7A patent/CN107820518B/zh active Active
- 2016-04-08 KR KR1020177032389A patent/KR102572217B1/ko active Active
- 2016-04-08 DK DK16717688.2T patent/DK3280405T3/da active
- 2016-04-08 MX MX2017012926A patent/MX379437B/es unknown
- 2016-04-08 KR KR1020177032404A patent/KR102602998B1/ko active Active
- 2016-04-08 SG SG11201708246TA patent/SG11201708246TA/en unknown
- 2016-04-08 BR BR112017021522-5A patent/BR112017021522B1/pt active IP Right Grant
- 2016-04-08 AU AU2016246098A patent/AU2016246098B2/en not_active Ceased
- 2016-04-08 WO PCT/GB2016/050990 patent/WO2016162688A1/en not_active Ceased
- 2016-04-08 MX MX2017012924A patent/MX382385B/es unknown
- 2016-04-08 BR BR112017021507-1A patent/BR112017021507B1/pt not_active IP Right Cessation
- 2016-04-08 ES ES16717193T patent/ES2897712T3/es active Active
- 2016-04-08 AU AU2016246099A patent/AU2016246099B2/en active Active
- 2016-04-08 ES ES16717688T patent/ES2886571T3/es active Active
-
2017
- 2017-10-08 IL IL254928A patent/IL254928B/en unknown
- 2017-10-08 IL IL254916A patent/IL254916B/en unknown
-
2020
- 2020-02-28 US US16/804,353 patent/US11337941B2/en active Active
- 2020-02-28 US US16/804,402 patent/US11331286B2/en active Active
-
2022
- 2022-05-24 US US17/664,759 patent/US20220313628A1/en not_active Abandoned
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