ES2179490T3 - Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5. - Google Patents

Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5.

Info

Publication number
ES2179490T3
ES2179490T3 ES98920635T ES98920635T ES2179490T3 ES 2179490 T3 ES2179490 T3 ES 2179490T3 ES 98920635 T ES98920635 T ES 98920635T ES 98920635 T ES98920635 T ES 98920635T ES 2179490 T3 ES2179490 T3 ES 2179490T3
Authority
ES
Spain
Prior art keywords
triazolo
substituted
gaba
derivatives
ftalazina
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES98920635T
Other languages
English (en)
Inventor
William Robert Carling
Tamara Ladduwahetty
Angus Murray Macleod
Kevin John Merchant
Kevin William Moore
Francine Sternfeld
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Original Assignee
Merck Sharp and Dohme Ltd
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
Priority claimed from GBGB9709368.6A external-priority patent/GB9709368D0/en
Priority claimed from GBGB9714508.0A external-priority patent/GB9714508D0/en
Priority claimed from GBGB9723741.6A external-priority patent/GB9723741D0/en
Priority claimed from GBGB9803992.8A external-priority patent/GB9803992D0/en
Application filed by Merck Sharp and Dohme Ltd filed Critical Merck Sharp and Dohme Ltd
Application granted granted Critical
Publication of ES2179490T3 publication Critical patent/ES2179490T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La invención se refiere a un compuesto de la fórmula (I) en la que R{sub,1} es hidrógeno, halógeno o CN o un grupo CF{sub,3}, OCF{sub,3}, alquilo en C{sub,1-4}, alquenilo en C{sub,2-4}, alquinilo en C{sub,2-4}, alcoxi en C{sub,1-4}, alqueniloxi en C{sub,2-4}, alquiniloxi en C{sub,2-4}, estando cada uno de estos grupos no sustituido o sustituido con uno o dos átomos de halógeno o con un núcleo de piridilo o de fenilo, puediendo cada uno de estos núcleos estar no sustituido o sustituido independientemente por uno o dos átomos de halógeno o grupos nitro, ciano, amina, metilo o CF{sub,3}; R{sup,2} es hidrógeno, halógeno o CN o un grupo CF{sub,3}, OCF{sub,3}, un alquilo en C{sub,1-4}, un alquenilo C{sub,2-4},, un alquinilo en C{sub,2-4}, , un alcoxi en C{sub,1-4}, , unalqueniloxi en C{sub,2-4}, o un alquiniloxi en C{sub,2-4},, estando cada uno de estos grupos no sustituido o sustituido con uno o dos átomos de halógno; L es O, S o NR{sup,n}, siendo R{sup,n} H, alquilo en C{sub,1-6}, o cicloalquilo en C{sub,3-6}, X es un heterociclo de cinco a seis elementos eventualmente sutituidos; Y es un alcidileno eventualmente ramificado eventualmente sustituido por un grupo oxo o Y es un grupo (CH{sub,2}){sub,j}O en el que el átomo de oxígeno es el más cercano al grupo X y j representa 2,3 o 4; Z es un heterociclo de cinco o seis elementos eventualmente sustituido; o una sal de este último farmacéuticamente aceptable; la invención se refiere también a una composición farmacéutica que comprende este compuesto, a su utilización en un tratamiento médico, y a sus procedimientos de producción y a los intermedios utilizados en estos procedimientos
ES98920635T 1997-05-08 1998-05-06 Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5. Expired - Lifetime ES2179490T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB9709368.6A GB9709368D0 (en) 1997-05-08 1997-05-08 GABA-A Alpha 5 selective inverse agonists for cognition enhancement
GBGB9714508.0A GB9714508D0 (en) 1997-07-10 1997-07-10 Therapeutic agents
GBGB9723741.6A GB9723741D0 (en) 1997-11-11 1997-11-11 Therapeutic agents
GBGB9803992.8A GB9803992D0 (en) 1998-02-25 1998-02-25 Therapeutic agents

Publications (1)

Publication Number Publication Date
ES2179490T3 true ES2179490T3 (es) 2003-01-16

Family

ID=27451643

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98920635T Expired - Lifetime ES2179490T3 (es) 1997-05-08 1998-05-06 Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5.

Country Status (9)

Country Link
US (2) US6200975B1 (es)
EP (1) EP0986562B1 (es)
JP (1) JP4672820B2 (es)
AT (1) ATE221887T1 (es)
AU (1) AU732455C (es)
CA (1) CA2288789C (es)
DE (1) DE69807074T2 (es)
ES (1) ES2179490T3 (es)
WO (1) WO1998050385A1 (es)

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GB9715977D0 (en) * 1997-07-29 1997-10-01 Merck Sharp & Dohme Therapeutic agents
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PL341975A1 (en) * 1998-02-25 2001-05-07 Merck Sharp & Dohme Substituted 1,2,4-triazole[3,4-a]phtalazine
IL137117A0 (en) 1998-02-25 2001-06-14 Merck Sharp & Dohme Substituted 1,2,4-triazolo [3,4-a] pyridazine
GB9805557D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
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EP1131102A2 (en) * 1998-11-12 2001-09-12 Merck & Co., Inc. Combination of a gaba-a alpha 5 inverse agonist and cox-2 inhibitor, nsaid, estrogen or vitamin e
GB9824897D0 (en) * 1998-11-12 1999-01-06 Merck Sharp & Dohme Therapeutic compounds
CA2349700A1 (en) * 1998-11-12 2000-05-18 Merck & Co., Inc. Therapeutic polymorphs of a gaba-a alpha-5 inverse agonist and pamoate formulations of the same
GB9911802D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
GB9911803D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
GB9911804D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
ATE391123T1 (de) * 1999-11-15 2008-04-15 Janssen Pharmaceutica Nv Triazole als farnesyl-transferase-hemmer
GB9929569D0 (en) * 1999-12-14 2000-02-09 Merck Sharp & Dohme Therapeutic agents
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GB0028583D0 (en) * 2000-11-23 2001-01-10 Merck Sharp & Dohme Therapeutic compounds
GB0108475D0 (en) * 2001-04-04 2001-05-23 Merck Sharp & Dohme New compounds
GB0128499D0 (en) * 2001-11-28 2002-01-23 Merck Sharp & Dohme Therapeutic agents
JP4795022B2 (ja) * 2003-09-30 2011-10-19 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環化合物を含有する新規な抗真菌剤
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AU2006204451C1 (en) 2005-01-05 2012-05-24 Takeda Gmbh Triazolophthalazines as PDE2-inhibitors
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) * 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
TWI385169B (zh) * 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
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US8513287B2 (en) * 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
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AU2019233183B2 (en) * 2018-03-12 2024-02-01 Shanghai SIMR Biotechnology Co., Ltd Phthalazine isoxazole alkoxy derivatives, preparation method thereof, pharmaceutical composition and use thereof
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
CN112279802B (zh) * 2020-10-12 2022-03-08 江苏美迪克化学品有限公司 一种2-氯甲基-3-三氟甲基吡啶的制备方法
AU2022270411A1 (en) 2021-05-05 2023-11-23 University College Cardiff Consultants Limited Heteroaryl compounds useful in the treatment of cognitive disorders
CN114591352B (zh) * 2022-05-11 2022-09-09 上海赛默罗生物科技有限公司 一种三唑并哒嗪类化合物及其应用
CN114773352B (zh) * 2022-06-20 2023-03-17 上海赛默罗生物科技有限公司 制备取代的烟酰胺的方法

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Also Published As

Publication number Publication date
CA2288789C (en) 2009-07-21
AU7342898A (en) 1998-11-27
CA2288789A1 (en) 1998-11-12
EP0986562B1 (en) 2002-08-07
DE69807074T2 (de) 2003-04-03
US6200975B1 (en) 2001-03-13
DE69807074D1 (de) 2002-09-12
AU732455B2 (en) 2001-04-26
JP2001525802A (ja) 2001-12-11
AU732455C (en) 2002-09-05
WO1998050385A1 (en) 1998-11-12
JP4672820B2 (ja) 2011-04-20
ATE221887T1 (de) 2002-08-15
EP0986562A1 (en) 2000-03-22
US6310203B1 (en) 2001-10-30

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