MX2016008110A - Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. - Google Patents
Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.Info
- Publication number
- MX2016008110A MX2016008110A MX2016008110A MX2016008110A MX2016008110A MX 2016008110 A MX2016008110 A MX 2016008110A MX 2016008110 A MX2016008110 A MX 2016008110A MX 2016008110 A MX2016008110 A MX 2016008110A MX 2016008110 A MX2016008110 A MX 2016008110A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- formula
- dlk
- inhibitors
- pyrazole derivatives
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- 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
-
- 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
- C07D471/04—Ortho-condensed 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
- C07D487/04—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
- C07D498/04—Ortho-condensed 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
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Abstract
La presente invención proporciona compuestos de fórmula 0 y varias modalidades de los mismos, y composiciones que comprenden compuestos de fórmula 0 y varias modalidades de los mismos. (ver Fórmula) En los compuestos de fórmula 0, los grupos R1A, R1B, R1C, R1D, R2, R3, R4, R5 y R6 tienen el significado, tal como se describe en la presente descripción. La presente invención también proporciona métodos para usar compuestos de fórmula 0 y composiciones que comprenden compuestos de fórmula 0 como inhibidores de DLK y para tratar enfermedades y afecciones neurodegenerativas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2013/090153 | 2013-12-20 | ||
| PCT/EP2014/078620 WO2015091889A1 (en) | 2013-12-20 | 2014-12-19 | Pyrazole derivatives and uses thereof as inhibitors of dlk |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2016008110A true MX2016008110A (es) | 2016-08-19 |
Family
ID=52278622
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016008110A MX2016008110A (es) | 2013-12-20 | 2014-05-28 | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9365583B2 (es) |
| EP (1) | EP3083599B1 (es) |
| JP (1) | JP6228310B2 (es) |
| CN (1) | CN105939997B (es) |
| AR (1) | AR098853A1 (es) |
| CA (1) | CA2934011A1 (es) |
| MX (1) | MX2016008110A (es) |
| RU (1) | RU2016128368A (es) |
| TW (1) | TW201609692A (es) |
| WO (1) | WO2015091889A1 (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6267193B2 (ja) * | 2012-05-22 | 2018-01-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 置換ジピリジルアミン類及びそれらの使用 |
| EP2945938B1 (en) | 2013-01-18 | 2018-03-07 | F. Hoffmann-La Roche AG | 3-substituted pyrazoles and use as dlk inhibitors |
| CA2907912A1 (en) | 2013-05-01 | 2014-11-06 | F. Hoffmann-La Roche Ag | C-linked heterocycloalkyl substituted pyrimidines and their uses |
| KR20190040068A (ko) * | 2016-08-29 | 2019-04-16 | 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 | 질환의 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 저해제 |
| EP3551610B1 (en) | 2016-12-08 | 2021-08-11 | Board of Regents, The University of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease |
| US11173145B2 (en) | 2017-01-17 | 2021-11-16 | Board Of Regents, The University Of Texas System | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
| EP3652178B1 (en) | 2017-07-14 | 2024-01-24 | F. Hoffmann-La Roche AG | Bicyclic ketone compounds and methods of use thereof |
| CN111601593B (zh) | 2017-10-05 | 2022-04-15 | 弗尔康医疗公司 | P38激酶抑制剂降低dux4和下游基因表达以用于治疗fshd |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| MA50356A (fr) | 2017-10-11 | 2021-04-21 | Hoffmann La Roche | Composés bicycliques destinés à être utilisés en tant qu'inhibiteurs de la kinase rip1 |
| WO2019086494A1 (en) | 2017-10-31 | 2019-05-09 | F. Hoffmann-La Roche Ag | Bicyclic sulfones and sulfoxides and methods of use thereof |
| WO2019204537A1 (en) | 2018-04-20 | 2019-10-24 | Genentech, Inc. | N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs) |
| US11046649B2 (en) | 2018-07-17 | 2021-06-29 | Board Of Regents, The University Of Texas System | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
| JP7212781B2 (ja) | 2018-12-19 | 2023-01-25 | ディスアーム セラピューティクス, インコーポレイテッド | 神経保護剤と組み合わせたsarm1の阻害剤 |
| EP3908586B1 (en) | 2019-01-11 | 2022-12-21 | F. Hoffmann-La Roche AG | Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof |
| US11560366B2 (en) | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
| WO2023034808A1 (en) * | 2021-09-01 | 2023-03-09 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Mixed lineage kinase inhibitors and methods of use |
| CN118696049A (zh) * | 2021-11-23 | 2024-09-24 | 基因泰克公司 | 胆固醇生物合成的螺环双环调节剂及其用于促进髓鞘再生的用途 |
| AU2023354158A1 (en) * | 2022-09-30 | 2025-04-03 | Convelo Therapeutics, Inc. | Azole modulators of cholesterol biosynthesis and their use for promoting remyelination |
| WO2024123967A1 (en) * | 2022-12-08 | 2024-06-13 | Senya Pharmaceuticals, Inc. | Sarm1 inhibitors, pharmaceutical compositions, and therapeutic applications |
| WO2025021997A1 (en) | 2023-07-27 | 2025-01-30 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | New map4k1 inhibitors |
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| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| DE69328430T2 (de) | 1992-07-27 | 2001-01-25 | The Government Of The United States Of America As Represented By The Secretary Of National Institute Of Health, Office Of Technology Transfer | Zielgerichte liposome zur blut-hirne schranke |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| WO2002017930A2 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| CA2450073C (en) | 2001-07-25 | 2017-08-29 | Biomarin Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| JP4995423B2 (ja) | 2002-12-03 | 2012-08-08 | ブランシェット・ロックフェラー・ニューロサイエンスィズ・インスティテュート | 物質を血液−脳関門を渡って輸送するための人工低密度リポタンパク質キャリア |
| US20050089473A1 (en) | 2003-09-10 | 2005-04-28 | Cedars-Sinai Medical Center | Potassium channel mediated delivery of agents through the blood-brain barrier |
| CN102047061A (zh) * | 2008-05-30 | 2011-05-04 | 福斯特韦勒能源股份公司 | 通过氧化燃料燃烧发电的方法和系统 |
| SG10201406763WA (en) * | 2009-10-22 | 2014-11-27 | Genentech Inc | Modulation of axon degeneration |
| US8846909B2 (en) | 2010-05-24 | 2014-09-30 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| JP6267193B2 (ja) * | 2012-05-22 | 2018-01-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 置換ジピリジルアミン類及びそれらの使用 |
| TWI602801B (zh) * | 2012-06-01 | 2017-10-21 | Taisho Pharmaceutical Co Ltd | Fluorinated amino acid prior to drug |
| EP2945938B1 (en) * | 2013-01-18 | 2018-03-07 | F. Hoffmann-La Roche AG | 3-substituted pyrazoles and use as dlk inhibitors |
| MY182082A (en) * | 2013-05-01 | 2021-01-18 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
-
2014
- 2014-05-28 MX MX2016008110A patent/MX2016008110A/es unknown
- 2014-12-19 TW TW103144678A patent/TW201609692A/zh unknown
- 2014-12-19 US US14/576,890 patent/US9365583B2/en active Active
- 2014-12-19 CN CN201480069220.8A patent/CN105939997B/zh active Active
- 2014-12-19 CA CA2934011A patent/CA2934011A1/en not_active Abandoned
- 2014-12-19 RU RU2016128368A patent/RU2016128368A/ru unknown
- 2014-12-19 WO PCT/EP2014/078620 patent/WO2015091889A1/en not_active Ceased
- 2014-12-19 EP EP14821614.6A patent/EP3083599B1/en active Active
- 2014-12-19 JP JP2016541483A patent/JP6228310B2/ja active Active
- 2014-12-19 AR ARP140104786A patent/AR098853A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3083599A1 (en) | 2016-10-26 |
| CA2934011A1 (en) | 2015-06-25 |
| RU2016128368A (ru) | 2018-01-23 |
| AR098853A1 (es) | 2016-06-15 |
| EP3083599B1 (en) | 2020-07-01 |
| CN105939997B (zh) | 2020-01-21 |
| TW201609692A (zh) | 2016-03-16 |
| CN105939997A (zh) | 2016-09-14 |
| JP2017504605A (ja) | 2017-02-09 |
| US20150175619A1 (en) | 2015-06-25 |
| US9365583B2 (en) | 2016-06-14 |
| WO2015091889A1 (en) | 2015-06-25 |
| JP6228310B2 (ja) | 2017-11-08 |
| HK1226053A1 (zh) | 2017-09-22 |
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