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MX2010005753A - Derivados de isoxazolo-pirazina. - Google Patents

Derivados de isoxazolo-pirazina.

Info

Publication number
MX2010005753A
MX2010005753A MX2010005753A MX2010005753A MX2010005753A MX 2010005753 A MX2010005753 A MX 2010005753A MX 2010005753 A MX2010005753 A MX 2010005753A MX 2010005753 A MX2010005753 A MX 2010005753A MX 2010005753 A MX2010005753 A MX 2010005753A
Authority
MX
Mexico
Prior art keywords
optionally substituted
isoxazolo
halo
pyrazine derivatives
present
Prior art date
Application number
MX2010005753A
Other languages
English (en)
Inventor
Bernd Buettelmann
Roland Jakob-Roetne
Andrew Thomas
Henner Knust
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 MX2010005753A publication Critical patent/MX2010005753A/es

Links

Classifications

    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente invención se refiere a derivados de isoxazolo- pirazina de fórmula (I) en donde X es O ó NH, R1 es fenilo o piridina-2-il, en donde los anillos pueden ser opcionalmente sustituidos con uno, dos o tres halo; R2 es H ó alquilo de 1 a 4 átomos de carbono; R3 y R4 cada uno independientemente H, opcionalmente sustituido por alquilo de 1 a 7 átomos de carbono, opcionalmente sustituido por alcoxi de 1 a 7 átomos de carbono, CN, halo, NO2, -C (0) Ra-C (0) -NRbRC o R y R4 juntos forman un anillo de venzo-anelado opcionalmente sustituido, o una sal farmacéuticamente aceptable de lo mismo, después de haber afinidad y selectividad del receptor GABA A a5 sitio de unión, su fabricación, composiciones farmacéuticas que los contienen y su uso como medicamento. Los compuestos activos de la presente invención son útiles como potenciador cognitivo 6 para el tratamiento de trastornos cognitivos como la enfermedad de Alzheimer.
MX2010005753A 2007-12-04 2008-11-25 Derivados de isoxazolo-pirazina. MX2010005753A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07122271 2007-12-04
PCT/EP2008/066127 WO2009071464A1 (en) 2007-12-04 2008-11-25 Isoxazolo-pyrazine derivatives

Publications (1)

Publication Number Publication Date
MX2010005753A true MX2010005753A (es) 2010-06-15

Family

ID=40256991

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2010005753A MX2010005753A (es) 2007-12-04 2008-11-25 Derivados de isoxazolo-pirazina.

Country Status (15)

Country Link
US (2) US7618973B2 (es)
EP (1) EP2229383B1 (es)
JP (1) JP5301556B2 (es)
KR (1) KR101175859B1 (es)
CN (1) CN101883769B (es)
AR (1) AR069524A1 (es)
AU (1) AU2008333320B2 (es)
BR (1) BRPI0820649A2 (es)
CA (1) CA2706990C (es)
CL (1) CL2008003592A1 (es)
IL (1) IL205755A0 (es)
MX (1) MX2010005753A (es)
PE (1) PE20091444A1 (es)
TW (1) TW200924769A (es)
WO (1) WO2009071464A1 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008333326B2 (en) 2007-12-04 2013-05-30 F. Hoffmann-La Roche Ag Isoxazolo-pyridine derivatives
CN102186825A (zh) * 2008-10-21 2011-09-14 麦它波莱克斯股份有限公司 芳基gpr120受体激动剂和其用途
US8227461B2 (en) * 2009-04-30 2012-07-24 Hoffmann-La Roche Inc. Isoxazoles
ES2601181T3 (es) * 2009-05-05 2017-02-14 F. Hoffmann-La Roche Ag Derivados de isoxazol-tiazol como agonistas inversos del receptor GABA A para su uso en el tratamiento de trastornos cognitivos
AU2010244553A1 (en) * 2009-05-05 2011-12-01 F. Hoffmann-La Roche Ag Isoxazole-pyridine derivatives
JP5460858B2 (ja) * 2009-05-05 2014-04-02 エフ．ホフマン−ラ ロシュ アーゲー イソオキサゾール−ピラゾール誘導体
US8466181B2 (en) * 2010-12-10 2013-06-18 Hoffmann-La Roche Inc. 1,2,3-triazole-imidazole compounds
US8604062B2 (en) 2011-10-20 2013-12-10 Hoffman-La Roche Inc. Process for the preparation of isoxazolyl-methoxy nicotinic acids
US8785435B2 (en) 2011-10-20 2014-07-22 Hoffmann-La Roche Inc. Solid forms
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
WO2014001279A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
JP6223443B2 (ja) 2012-06-26 2017-11-01 サニオナ・エイピイエス フェニルトリアゾール誘導体及びｇａｂａａ受容体複合体を調節するための該フェニルトリアゾール誘導体の使用
WO2014001278A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
KR20150033678A (ko) 2012-06-26 2015-04-01 사니오나 에이피에스 페닐 트리아졸 유도체 및 이의 gabaa 수용체 복합체 조절용 용도
WO2014001280A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
BR102019014802A2 (pt) 2018-07-20 2020-02-04 Boehringer Ingelheim Int difluorometil-fenil triazóis
HU231223B1 (hu) * 2018-09-28 2022-01-28 Richter Gedeon Nyrt. GABAA A5 receptor modulátor hatású biciklusos vegyületek
US20240043418A1 (en) 2020-03-26 2024-02-08 Richter Gedeon Nyrt. 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators
KR20240005848A (ko) 2021-05-05 2024-01-12 유니버시티 칼리지 카디프 컨설턴츠 리미티드 인지 장애의 치료에 유용한 헤테로아릴 화합물
CN116854680A (zh) * 2022-03-28 2023-10-10 上海赛默罗生物科技有限公司 异噁唑-杂环类衍生物、药物组合物和用途

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3525205A1 (de) * 1984-09-11 1986-03-20 Hoechst Ag, 6230 Frankfurt Pflanzenschuetzende mittel auf basis von 1,2,4-triazolderivaten sowie neue derivate des 1,2,4-triazols
GB9808663D0 (en) 1998-04-23 1998-06-24 Merck Sharp & Dohme Therapeutic agents
ES2255294T3 (es) * 1998-08-07 2006-06-16 Chiron Corporation Derivados de isoxazol sustituidos como moduladores del receptor de estrogenos.
US6660753B2 (en) * 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
IT1314191B1 (it) 1999-10-18 2002-12-06 Recordati Chem Pharm Derivati isossazolcarbossamidici
WO2001034603A2 (en) 1999-11-12 2001-05-17 Neurogen Corporation Bicyclic and tricyclic heteroaromatic compounds
PA8535601A1 (es) 2000-12-21 2002-11-28 Pfizer Derivados benzimidazol y piridilimidazol como ligandos para gabaa
GB0108475D0 (en) 2001-04-04 2001-05-23 Merck Sharp & Dohme New compounds
EA005934B1 (ru) 2001-07-05 2005-08-25 Х. Лундбекк А/С Замещённые анилиновые пиперидины в качестве селективных антагонистов мсн
DE60131967D1 (de) 2001-08-13 2008-01-31 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
EP1448561B1 (en) 2001-11-20 2008-02-20 Eli Lilly And Company Beta 3 adrenergic agonists
GB0128160D0 (en) * 2001-11-23 2002-01-16 Merck Sharp & Dohme Novel compounds
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
WO2005113519A1 (en) * 2004-05-14 2005-12-01 Irm Llc Compounds and compositions as ppar modulators
EP1756086B1 (en) 2004-06-01 2008-06-04 F.Hoffmann-La Roche Ag Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists
EP1773807A2 (en) 2004-06-14 2007-04-18 Takeda San Diego, Inc. Kinase inhibitors
CA2581945C (en) * 2004-10-01 2011-01-18 Henrietta Dehmlow Hexafluoroisopropanol substituted ether derivatives
US7351724B2 (en) 2004-10-15 2008-04-01 The Scripps Research Institute Oxadiazole ketone inhibitors of fatty acid amide hydrolase
US20070060589A1 (en) 2004-12-21 2007-03-15 Purandare Ashok V Inhibitors of protein arginine methyl transferases
WO2007002635A2 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
EP1904337B1 (de) 2005-07-20 2010-10-13 Prospective Concepts AG Pneumatisch verstellbare seitenwangen für fahrzeugsitze
DE602006003777D1 (de) * 2005-09-19 2009-01-02 Hoffmann La Roche Isoxazolderivate als inverse gaba a alpha5 agonisten
WO2007052843A1 (ja) 2005-11-04 2007-05-10 Takeda Pharmaceutical Company Limited 複素環アミド化合物およびその用途
JP5081161B2 (ja) 2005-12-19 2012-11-21 スミスクライン ビーチャム コーポレーション ファルネソイドｘ受容体アゴニスト
US7863302B2 (en) 2006-02-03 2011-01-04 Eli Lilly And Company Compounds and methods for modulating FX-receptors
JP2007230909A (ja) 2006-03-01 2007-09-13 Univ Of Tokyo 置換イソキサゾール誘導体
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds

Also Published As

Publication number Publication date
KR20100075674A (ko) 2010-07-02
AU2008333320A1 (en) 2009-06-11
BRPI0820649A2 (pt) 2015-06-16
PE20091444A1 (es) 2009-09-24
JP5301556B2 (ja) 2013-09-25
CA2706990C (en) 2016-05-10
CA2706990A1 (en) 2009-06-11
CN101883769B (zh) 2012-08-08
WO2009071464A1 (en) 2009-06-11
JP2011505399A (ja) 2011-02-24
US20090143407A1 (en) 2009-06-04
US20100041886A1 (en) 2010-02-18
IL205755A0 (en) 2010-11-30
US7618973B2 (en) 2009-11-17
KR101175859B1 (ko) 2012-08-24
CL2008003592A1 (es) 2010-01-04
TW200924769A (en) 2009-06-16
CN101883769A (zh) 2010-11-10
EP2229383B1 (en) 2017-01-18
EP2229383A1 (en) 2010-09-22
AU2008333320B2 (en) 2012-12-20
AR069524A1 (es) 2010-01-27

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