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DE69807074D1 - Substituierte 1,2,4-triazolo[3,4,-a]phthalazin-derivate als gaba-alpha 5-liganden - Google Patents

Substituierte 1,2,4-triazolo[3,4,-a]phthalazin-derivate als gaba-alpha 5-liganden

Info

Publication number
DE69807074D1
DE69807074D1 DE69807074T DE69807074T DE69807074D1 DE 69807074 D1 DE69807074 D1 DE 69807074D1 DE 69807074 T DE69807074 T DE 69807074T DE 69807074 T DE69807074 T DE 69807074T DE 69807074 D1 DE69807074 D1 DE 69807074D1
Authority
DE
Germany
Prior art keywords
triazolo
ligands
substituted
phthalazine derivatives
gaba alpha
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
DE69807074T
Other languages
English (en)
Other versions
DE69807074T2 (de
Inventor
Robert Carling
Tamara Ladduwahetty
Murray Macleod
John Merchant
William Moore
Francine Sternfeld
Joseph Street
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 DE69807074D1 publication Critical patent/DE69807074D1/de
Publication of DE69807074T2 publication Critical patent/DE69807074T2/de
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)
DE69807074T 1997-05-08 1998-05-06 Substituierte 1,2,4-triazolo[3,4,-a]phthalazin-derivate als gaba-alpha 5-liganden Expired - Lifetime DE69807074T2 (de)

Applications Claiming Priority (5)

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
PCT/GB1998/001307 WO1998050385A1 (en) 1997-05-08 1998-05-06 SUBSTITUTED 1,2,4-TRIAZOLO[3,4-a]PHTHALAZINE DERIVATIVES AS GABA ALPHA 5 LIGANDS

Publications (2)

Publication Number Publication Date
DE69807074D1 true DE69807074D1 (de) 2002-09-12
DE69807074T2 DE69807074T2 (de) 2003-04-03

Family

ID=27451643

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69807074T Expired - Lifetime DE69807074T2 (de) 1997-05-08 1998-05-06 Substituierte 1,2,4-triazolo[3,4,-a]phthalazin-derivate als gaba-alpha 5-liganden

Country Status (9)

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

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ES2179490T3 (es) 1997-05-08 2003-01-16 Merck Sharp & Dohme Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5.
GB9715977D0 (en) * 1997-07-29 1997-10-01 Merck Sharp & Dohme Therapeutic agents
GB9718254D0 (en) * 1997-08-28 1997-11-05 Merck Sharp & Dohme Therapeutic agents
EP1047697A1 (de) * 1998-01-14 2000-11-02 MERCK SHARP & DOHME LTD. Triazolo-pyridazin-derivate als liganden für gaba-rezeptoren
YU46500A (sh) * 1998-02-25 2002-11-15 Merck Charp & Dohme Limited Substituisani 1,2,4-triazolo /3,4-a/piridazin
SK12772000A3 (sk) * 1998-02-25 2001-03-12 Merck Sharp & Dohme Limited 3-(5-metylizoxazol-3-yl)-6-(1-metyl-1,2,3-triazol-4-yl)metyloxy- -1,2,4-triazolo[3,4-a]ftalazín, farmaceutický prostriedok s jeho obsahom a jeho požitie
GB9805557D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
EP1129094A2 (de) 1998-11-12 2001-09-05 Merck & Co., Inc. Therapeutische polymorphe von inverse agonisten des gaba-a alpha-5 rezeptor und pamoat-formulierungen
CA2351057A1 (en) * 1998-11-12 2000-05-18 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
US6440967B1 (en) * 1998-11-12 2002-08-27 Merck & Co., Inc. Combination of a GABAA alpha 5 inverse agonist and COX-2 inhibitor, NSAID, estrogen or vitamin E
GB9911802D0 (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
GB9911803D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
AU779426B2 (en) * 1999-11-15 2005-01-27 Janssen Pharmaceutica N.V. Triazoles as farnesyl transferase inhibitors
GB9929569D0 (en) 1999-12-14 2000-02-09 Merck Sharp & Dohme Therapeutic agents
GB0000564D0 (en) 2000-01-11 2000-03-01 Merck Sharp & Dohme Therapeutic agents
US6528649B2 (en) 2000-05-30 2003-03-04 Neurogen Corporation Imidazoloisoquinolines
CA2420967A1 (en) 2000-08-07 2002-02-14 Neurogen Corporation Heterocyclic compounds as ligands of the gabaa receptor
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
EP1669348A4 (de) * 2003-09-30 2009-03-11 Eisai R&D Man Co Ltd Neues antipilzmittel, das eine heterocyclische verbindung enthält
ES2347337T3 (es) 2004-09-02 2010-10-28 Nycomed Gmbh Triazoloftalazinas.
CA2491067A1 (en) * 2004-12-24 2006-06-24 Stichting Katholieke Universiteit Mrna rations in urinary sediments and/or urine as a prognostic marker for prostate cancer
EA012505B1 (ru) 2005-01-05 2009-10-30 Никомед Гмбх Триазолофталазины в качестве ингибиторов pde-2
WO2006072612A2 (en) 2005-01-05 2006-07-13 Nycomed Gmbh Triazolophthalazines as pde2- inhibitors
EP1928437A2 (de) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenese mittels muscarinrezeptormodulation
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス，インコーポレイティド Ｐｄｅ阻害による神経新生の調節
WO2007053596A1 (en) * 2005-10-31 2007-05-10 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
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2026813A2 (de) 2006-05-09 2009-02-25 Braincells, Inc. 5-ht-rezeptor-vermittelte neurogenese
WO2008030651A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
EP2065377B1 (de) * 2006-09-21 2011-11-23 Eisai R&D Management Co., Ltd. Durch einen heteroarylring substituiertes pyridinderivat und antipilzmittel, das dieses enthält
TW200841879A (en) * 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
JPWO2009081970A1 (ja) * 2007-12-26 2011-05-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環置換ピリジン誘導体の製造方法
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
US8188119B2 (en) 2008-10-24 2012-05-29 Eisai R&D Management Co., Ltd Pyridine derivatives substituted with heterocyclic ring and γ-glutamylamino group, and antifungal agents containing same
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2011020044A1 (en) * 2009-08-14 2011-02-17 Concert Pharmaceuticals, Inc. Substituted triazolophthalazine derivatives
AR079451A1 (es) 2009-12-18 2012-01-25 Nycomed Gmbh Compuestos 3,4,4a,10b-tetrahidro-1h-tiopirano[4,3-c]isoquinolina
BR112013000925A2 (pt) 2010-07-15 2020-12-01 Bayer Intellectual Property Gmbh compostos heterocíclicos como pesticidas
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
CN106854207B (zh) * 2015-12-08 2019-10-29 上海赛默罗生物科技有限公司 呔嗪类衍生物、其制备方法、药物组合物和用途
ES2964534T3 (es) * 2018-03-12 2024-04-08 Shanghai Simr Biotechnology Co Ltd Derivados de ftalazina isoxazol alcoxi, método de preparación de los mismos, composición farmacéutica y uso de la misma
HU231223B1 (hu) 2018-09-28 2022-01-28 Richter Gedeon Nyrt. GABAA A5 receptor modulátor hatású biciklusos vegyületek
WO2021191837A1 (en) 2020-03-26 2021-09-30 Richter Gedeon Nyrt. 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa α5 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
WO2022234271A1 (en) 2021-05-05 2022-11-10 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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FI81350C (fi) * 1982-01-18 1990-10-10 Lepetit Spa Analogfoerfarande foer framstaellning av nya, farmakologiskt aktiva 6-substituerade s-triatsolo/3,4-a/ ftalazinderivat.
IT1194310B (it) * 1983-07-12 1988-09-14 Lepetit Spa Derivati triazolo (3,4-a) ftalazinici 3,6-disostituiti
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
US5182290A (en) 1991-08-27 1993-01-26 Neurogen Corporation Certain oxazoloquinolinones; a new class of GABA brain receptor ligands
US5212310A (en) 1991-12-19 1993-05-18 Neurogen Corporation Certain aryl fused imidazopyrimidines; a new class of GABA brain receptor ligands
JPH05229946A (ja) * 1992-02-20 1993-09-07 Sapporo Breweries Ltd トリアゾロフタラジン誘導体を含有する抗潰瘍剤
US5306819A (en) * 1992-08-27 1994-04-26 Neurogen Corporation Certain aryl a cycloalkyl fused imidazopyrazinols; and new class of GABA brain receptor ligands
GB9503601D0 (en) 1995-02-23 1995-04-12 Merck Sharp & Dohme Method of treatment and method of manufacture of medicament
DE19617862A1 (de) * 1996-04-23 1997-10-30 Schering Ag Phthalazinderivate, deren Herstellung und Verwendung als Arzneimittel
JP2000515851A (ja) 1996-07-25 2000-11-28 メルク シヤープ エンド ドーム リミテツド ＧＡＢＡ▲下Ａα５▼レセプターサブタイプの逆アゴニストとしての置換のあるトリアゾロピリダジン誘導体
WO1998004559A2 (en) * 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
ES2179490T3 (es) 1997-05-08 2003-01-16 Merck Sharp & Dohme Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5.

Also Published As

Publication number Publication date
AU732455C (en) 2002-09-05
AU732455B2 (en) 2001-04-26
AU7342898A (en) 1998-11-27
JP4672820B2 (ja) 2011-04-20
WO1998050385A1 (en) 1998-11-12
DE69807074T2 (de) 2003-04-03
EP0986562B1 (de) 2002-08-07
US6310203B1 (en) 2001-10-30
ES2179490T3 (es) 2003-01-16
US6200975B1 (en) 2001-03-13
CA2288789A1 (en) 1998-11-12
ATE221887T1 (de) 2002-08-15
CA2288789C (en) 2009-07-21
JP2001525802A (ja) 2001-12-11
EP0986562A1 (de) 2000-03-22

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Legal Events

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8364 No opposition during term of opposition