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.

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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
Application number
MX2016008110A
Other languages
English (en)
Inventor
P Lyssikatos Joseph
Huestis Malcolm
Siu Michael
Patel Snahel
Liu Wen
Estrada Anthony
LIANG Guibai
Chen Kevin
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2016008110A publication Critical patent/MX2016008110A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/10Spiro-condensed systems

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.
MX2016008110A 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. MX2016008110A (es)

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

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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 (11)

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)
HK (1) HK1226053A1 (es)
MX (1) MX2016008110A (es)
RU (1) RU2016128368A (es)
TW (1) TW201609692A (es)
WO (1) WO2015091889A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2852584B1 (en) * 2012-05-22 2018-02-28 F. Hoffmann-La Roche AG Substituted dipyridylamines and uses thereof
BR112015016395A2 (pt) * 2013-01-18 2017-07-11 Hoffmann La Roche pirazóis 3-substituídos e uso como inibidores de dlk
KR20160002850A (ko) 2013-05-01 2016-01-08 에프. 호프만-라 로슈 아게 C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도
EP3503889A1 (en) * 2016-08-29 2019-07-03 Board Of Regents, The University Of Texas System Inhibitors of dual leucine ziper (dlk) kinase for the treatment of disease
US10093664B2 (en) * 2016-12-08 2018-10-09 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
WO2018136437A2 (en) 2017-01-17 2018-07-26 Tesaro, Inc. Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
KR20200030558A (ko) 2017-07-14 2020-03-20 에프. 호프만-라 로슈 아게 이환형 케톤 화합물 및 이의 사용 방법
CA3128468A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of 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
CA3078653A1 (en) 2017-10-11 2019-04-18 F. Hoffmann-La Roche Ag Bicyclic compounds for use as rip1 kinase inhibitors
CR20200168A (es) 2017-10-31 2020-07-12 Hoffmann La Roche Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos
CN112074519A (zh) 2018-04-20 2020-12-11 豪夫迈·罗氏有限公司 作为rip1激酶抑制剂用于治疗e.g.肠易激综合征(ibs)的n-[4-氧代-2,3-二氢-1,5-苯并氧氮杂-3-基]-5,6-二氢-4h-吡咯并[1,2-b]吡唑-2-甲酰胺衍生物和有关化合物
WO2020018670A1 (en) 2018-07-17 2020-01-23 Board Of Regents, The University Of Texas System Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
JP2022516651A (ja) 2019-01-11 2022-03-01 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 二環式ピロロトリアゾールケトン化合物及びその使用方法
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
CA3229861A1 (en) * 2021-09-01 2023-03-09 John F. BROGNARD Mixed lineage kinase inhibitors and methods of use
WO2023097230A1 (en) * 2021-11-23 2023-06-01 Genentech, Inc. Spirocyclic bicyclic modulators of cholesterol biosynthesis and their use for promoting remyelination
WO2024073662A1 (en) * 2022-09-30 2024-04-04 Genentech, Inc. Azole modulators of cholesterol biosynthesis and their use for promoting remyelination

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
ATE191853T1 (de) 1992-07-27 2000-05-15 Us Health Zielgerichte liposome zur blut-hirne schranke
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
US20020065259A1 (en) 2000-08-30 2002-05-30 Schatzberg Alan F. 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
WO2003009815A2 (en) 2001-07-25 2003-02-06 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
CA2507762C (en) 2002-12-03 2013-02-05 Blanchette Rockefeller Neurosciences Institute Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier
WO2005025511A2 (en) 2003-09-10 2005-03-24 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
BR112012009257A2 (pt) 2009-10-22 2016-11-22 Genentech Inc modulação de degeneração de axônio.
US8846909B2 (en) 2010-05-24 2014-09-30 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
EP2852584B1 (en) * 2012-05-22 2018-02-28 F. Hoffmann-La Roche AG Substituted dipyridylamines and uses thereof
CA2875080C (en) * 2012-06-01 2020-03-24 Taisho Pharmaceutical Co., Ltd. Prodrug of fluorine-containing amino acid
BR112015016395A2 (pt) * 2013-01-18 2017-07-11 Hoffmann La Roche pirazóis 3-substituídos e uso como inibidores de dlk
PE20200447A1 (es) * 2013-05-01 2020-02-28 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos

Also Published As

Publication number Publication date
WO2015091889A1 (en) 2015-06-25
EP3083599A1 (en) 2016-10-26
RU2016128368A (ru) 2018-01-23
HK1226053A1 (zh) 2017-09-22
JP6228310B2 (ja) 2017-11-08
JP2017504605A (ja) 2017-02-09
CN105939997B (zh) 2020-01-21
US20150175619A1 (en) 2015-06-25
TW201609692A (zh) 2016-03-16
CA2934011A1 (en) 2015-06-25
AR098853A1 (es) 2016-06-15
US9365583B2 (en) 2016-06-14
EP3083599B1 (en) 2020-07-01
CN105939997A (zh) 2016-09-14

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