DE69807074T2 - 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
DE69807074T2
DE69807074T2 DE69807074T DE69807074T DE69807074T2 DE 69807074 T2 DE69807074 T2 DE 69807074T2 DE 69807074 T DE69807074 T DE 69807074T DE 69807074 T DE69807074 T DE 69807074T DE 69807074 T2 DE69807074 T2 DE 69807074T2
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
DE69807074D1 (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
Publication of DE69807074D1 publication Critical patent/DE69807074D1/de
Application granted granted Critical
Publication of DE69807074T2 publication Critical patent/DE69807074T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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 DE69807074D1 (de) 2002-09-12
DE69807074T2 true 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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CA2288789C (en) 1997-05-08 2009-07-21 Merck Sharp & Dohme Limited Substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives as gaba alpha 5 ligands
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
WO1999036423A1 (en) * 1998-01-14 1999-07-22 Merck Sharp & Dohme Limited Triazolo-pyridazine derivatives as ligands for gaba receptors
US6448249B1 (en) * 1998-02-25 2002-09-10 Merck Sharp & Dohme Ltd. Substituted 1,2,4-triazolo[3,4-A]phthalazine derivatives as GABAα5 ligands
CA2317416A1 (en) * 1998-02-25 1999-09-02 Merck Sharp & Dohme Limited 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
JP2002529468A (ja) * 1998-11-12 2002-09-10 メルク エンド カムパニー インコーポレーテッド GABA−Aα−5逆活性薬の治療性多形およびそのパモエート組成物
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
JP2002529406A (ja) * 1998-11-12 2002-09-10 メルク エンド カムパニー インコーポレーテッド GABAAα5逆活性薬と、COX−2阻害剤、NSAID、エストロゲン、又はビタミンEとの組合わせ
GB9824897D0 (en) * 1998-11-12 1999-01-06 Merck Sharp & Dohme Therapeutic compounds
GB9911804D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
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
ES2304996T3 (es) * 1999-11-15 2008-11-01 Janssen Pharmaceutica Nv Triazoles como inhibidores de farnesil transferasa.
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
US6653471B2 (en) 2000-08-07 2003-11-25 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
CA2578368C (en) 2004-09-02 2013-07-02 Altana Pharma Ag Triazolophthalazines
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
US7671050B2 (en) 2005-01-05 2010-03-02 Nycomed Gmbh Triazolophthalazines
BRPI0606379A2 (pt) 2005-01-05 2009-06-23 Nycomed Gmbh triazolftalazinas
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス,インコーポレイティド ムスカリン性受容体調節による神経発生
CA2625153A1 (en) 2005-10-21 2007-04-26 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
US7678808B2 (en) 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
EP2377531A2 (de) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenese mittels Angiotensin-Modulation
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
RU2474581C2 (ru) * 2007-12-26 2013-02-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Способ получения замещенных гетероциклом производных пиридина
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
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US8557815B2 (en) * 2009-08-14 2013-10-15 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
CN103140483B (zh) 2010-07-15 2015-06-24 拜耳知识产权有限责任公司 作为杀虫剂的新杂环化合物
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
CN110256440B (zh) * 2018-03-12 2023-05-23 上海赛默罗生物科技有限公司 酞嗪异噁唑烷氧基衍生物、其制备方法、药物组合物和用途
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
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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PH21834A (en) * 1982-01-18 1988-03-17 Lepetit Spa New 6-substituted-s-triazolo(3,4-a)phthalazine derivatives
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
CA2260900A1 (en) 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited Substituted triazolo pyridazine derivatives as inverse agonists of the gabaa.alpha.5 receptor subtype
WO1998004559A2 (en) * 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited Substituted triazolo-pyridazine derivatives as ligands for gaba receptors
CA2288789C (en) 1997-05-08 2009-07-21 Merck Sharp & Dohme Limited Substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives as gaba alpha 5 ligands

Also Published As

Publication number Publication date
DE69807074D1 (de) 2002-09-12
EP0986562B1 (de) 2002-08-07
US6310203B1 (en) 2001-10-30
AU732455B2 (en) 2001-04-26
AU732455C (en) 2002-09-05
AU7342898A (en) 1998-11-27
ES2179490T3 (es) 2003-01-16
CA2288789C (en) 2009-07-21
US6200975B1 (en) 2001-03-13
ATE221887T1 (de) 2002-08-15
EP0986562A1 (de) 2000-03-22
JP4672820B2 (ja) 2011-04-20
JP2001525802A (ja) 2001-12-11
CA2288789A1 (en) 1998-11-12
WO1998050385A1 (en) 1998-11-12

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Legal Events

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