MA48577A1 - Composes biheteroaryle et leurs utilisations - Google Patents

Composes biheteroaryle et leurs utilisations

Info

Publication number
MA48577A1
MA48577A1 MA48577A MA48577A MA48577A1 MA 48577 A1 MA48577 A1 MA 48577A1 MA 48577 A MA48577 A MA 48577A MA 48577 A MA48577 A MA 48577A MA 48577 A1 MA48577 A1 MA 48577A1
Authority
MA
Morocco
Prior art keywords
biheteroaryl compounds
formula
compounds
biheteroaryl
diseases
Prior art date
Application number
MA48577A
Other languages
English (en)
Inventor
Kevin X Chen
Luigi Franchi
Liting Dong
Anthony Estrada
Paul Gibbons
Malcolm Huestis
Terry Kellar
Wen Liu
Joseph P Lyssikatos
Changyou Ma
Alan Olivero
Snahel Patel
Daniel Shore
Michael Siu
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 MA48577A1 publication Critical patent/MA48577A1/fr

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/30—Nerves; Brain; Eyes; Corneal cells; Cerebrospinal fluid; Neuronal stem cells; Neuronal precursor cells; Glial cells; Oligodendrocytes; Schwann cells; Astroglia; Astrocytes; Choroid plexus; Spinal cord tissue
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    • 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
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    • 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
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    • 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
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    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
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    • 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
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    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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Abstract

La présente invention concerne des composés représentés par la formule i-i ainsi que des modes de réalisation et des sels correspondants qui sont destinés au traitement de maladies (notamment, de maladies neurodégénératives). R 1, r 2, r 3, x 1, x 2, a et la variable cy de la formule i-i possèdent tous la signification telle que définie dans la description.
MA48577A 2013-05-01 2014-04-30 Composes biheteroaryle et leurs utilisations MA48577A1 (fr)

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Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2844652B1 (fr) * 2012-05-03 2019-03-13 Genentech, Inc. Dérivés de pyrazole aminopyrimidine en tant que modulateurs de lrrk2
MX2015009270A (es) * 2013-01-18 2015-10-30 Hoffmann La Roche Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk).
CA2907912A1 (fr) * 2013-05-01 2014-11-06 F. Hoffmann-La Roche Ag Pyrimidines a substitution heterocycloalkyle liees a c et leurs utilisations
EP2991978A4 (fr) 2013-05-01 2016-09-14 Hoffmann La Roche Composés bihétéroaryle et leurs utilisations
MX2016008110A (es) * 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
CN104926716A (zh) * 2015-06-10 2015-09-23 哈尔滨工业大学 吡啶衍生物2,6-二[(6-甲氧基吡啶-2-基)甲基]吡啶及其合成方法
WO2018044808A1 (fr) * 2016-08-29 2018-03-08 Board Of Regents, University Of Texas System Inhibiteurs de la kinase à double motif de type glissière à leucines (dlk) destinés au traitement de maladie
CA3045947A1 (fr) 2016-12-08 2018-06-14 Michael J. Soth Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture a glissiere de leucine kinase (dlk) destines au traitement de maladie
AR112274A1 (es) 2017-07-14 2019-10-09 Hoffmann La Roche Compuestos bicíclicos de cetona y sus métodos de uso
AU2018348930A1 (en) 2017-10-11 2020-03-26 F. Hoffmann-La Roche Ag Bicyclic compounds for use as RIP 1 kinase inhibitors
ES2946551T3 (es) * 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina
MX2020003451A (es) 2017-10-31 2020-08-03 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de uso de los mismos.
EP3781571B1 (fr) 2018-04-20 2024-01-17 F. Hoffmann-La Roche AG Dérivés de n-[4-oxo-2,3-dihydro-pyrido[3,2-b][1,4]oxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole-2-carboxamide et composés similaires en tant qu'inhibiteurs de la kinase rip1 pour le traitement p.e. du syndrome de l'intestin irritable (sii)
AR119673A1 (es) 2019-01-11 2022-01-05 Hoffmann La Roche Compuestos bicíclicos de cetona y métodos para utilizarlos
WO2020156241A1 (fr) * 2019-01-31 2020-08-06 中国医药研究开发中心有限公司 Composés cycliques aromatiques ou cycliques hétéroaromatiques, procédé de préparation correspondant et utilisation médicale associée
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
EP4222154A1 (fr) * 2020-10-02 2023-08-09 Genentech, Inc. Procédé de préparation de composés bihétéroaryle et leurs formes cristallines
CA3229861A1 (fr) * 2021-09-01 2023-03-09 John F. BROGNARD Inhibiteurs de kinase de lignee mixte et procedes d'utilisation
CA3235739A1 (fr) * 2021-10-20 2023-04-27 Yousef Najajreh Composes inhibiteurs allosteriques pour surmonter la resistance d'un cancer

Family Cites Families (35)

* 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 (fr) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipides et composés tensio-actifs en phase aqueuse
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
DE60234057D1 (de) 2001-07-25 2009-11-26 Raptor Pharmaceutical Inc Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
EP1549652B1 (fr) 2002-09-30 2008-10-22 Bayer HealthCare AG Derives d'azole-pyrimidines fondues
KR101186210B1 (ko) 2002-12-03 2012-10-08 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 혈뇌장벽을 통과하는 물질 수송용 인공 저밀도 지단백질 운반체
EP1663239A4 (fr) 2003-09-10 2008-07-23 Cedars Sinai Medical Center Administration assistee par les canaux potassiques d'agents a travers la barriere hemato-encephalique
GB0508471D0 (en) 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008064244A2 (fr) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Modulation des phosphoinositides pour le traitement de maladies neurodégénératives
WO2008098058A1 (fr) * 2007-02-06 2008-08-14 Novartis Ag Inhibiteurs de la pi3-kinase et procédés de leur utilisation
KR101552742B1 (ko) 2007-07-19 2015-09-11 머크 샤프 앤드 돔 코포레이션 단백질 키나제 억제제로서의 헤테로사이클릭 아미드 화합물
WO2009066084A1 (fr) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2-morpholinopyrimidines et leur utilisation en tant qu'inhibiteurs de kinase pi3
US20100056609A1 (en) 2008-08-26 2010-03-04 Washington University Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway
AU2009309616B2 (en) * 2008-10-31 2014-02-13 Novartis Ag Combination of a phosphatidylinositol-3-kinase (PI3K) inhibitor and a mTOR inhibitor
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
SG179085A1 (en) * 2009-09-09 2012-04-27 Avila Therapeutics Inc Pi3 kinase inhibitors and uses thereof
MX2012004638A (es) 2009-10-22 2012-07-04 Genentech Inc Modulacion de degeneracion de axones.
GB201004200D0 (en) * 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
CN103153994B (zh) 2010-05-24 2016-02-10 罗切斯特大学 双环杂芳基激酶抑制剂及使用方法
CA2829558A1 (fr) * 2011-03-09 2012-09-13 Celgene Avilomics Research, Inc. Inhibiteurs de pi3 kinase et leurs utilisations
EP2991978A4 (fr) * 2013-05-01 2016-09-14 Hoffmann La Roche Composés bihétéroaryle et leurs utilisations
CN103483345B (zh) 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
JP5920747B1 (ja) 2015-04-07 2016-05-18 エイピーエス．エスエイ アプリケーションプログラムおよびカード

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US10028954B2 (en) 2018-07-24
USRE47848E1 (en) 2020-02-11
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US20160052940A1 (en) 2016-02-25
US20160158234A1 (en) 2016-06-09
AU2014261894B2 (en) 2018-10-18
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JP2023011775A (ja) 2023-01-24
US20170239246A9 (en) 2017-08-24
PE20161063A1 (es) 2016-10-22
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US20200171029A1 (en) 2020-06-04
IL296526A (en) 2022-11-01
TW201841907A (zh) 2018-12-01
WO2014177060A1 (fr) 2014-11-06
US10010549B2 (en) 2018-07-03
BR112015027055B1 (pt) 2023-09-26
EP2991978A4 (fr) 2016-09-14
JP2020079264A (ja) 2020-05-28
JP6655052B2 (ja) 2020-02-26
PH12015502410A1 (en) 2016-02-22
EP2991978A1 (fr) 2016-03-09
KR20160003241A (ko) 2016-01-08
BR112015027055A2 (pt) 2017-07-25
IL242164B (en) 2021-04-29
MA42164A1 (fr) 2019-01-31
CA2911051C (fr) 2021-08-17
CL2015003147A1 (es) 2016-06-17
CA2911051A1 (fr) 2014-11-06
EA201592060A1 (ru) 2016-02-29
US9266862B2 (en) 2016-02-23
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US20140328805A1 (en) 2014-11-06
EA029568B1 (ru) 2018-04-30
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UA121016C2 (uk) 2020-03-25
MA38624A1 (fr) 2017-02-28
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