ATE221887T1 - 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
ATE221887T1
ATE221887T1 AT98920635T AT98920635T ATE221887T1 AT E221887 T1 ATE221887 T1 AT E221887T1 AT 98920635 T AT98920635 T AT 98920635T AT 98920635 T AT98920635 T AT 98920635T AT E221887 T1 ATE221887 T1 AT E221887T1
Authority
AT
Austria
Prior art keywords
triazolo
ligands
substituted
gaba
alpha
Prior art date
Application number
AT98920635T
Other languages
English (en)
Inventor
William Robert Carling
Tamara Ladduwahetty
Angus Murray Macleod
Kevin John Merchant
Kevin William Moore
Francine Sternfeld
Leslie Joseph Street
Original Assignee
Merck Sharp & Dohme
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 & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE221887T1 publication Critical patent/ATE221887T1/de

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)
AT98920635T 1997-05-08 1998-05-06 Substituierte 1,2,4-triazolo(3,4,-a)phthalazin- derivate als gaba-alpha 5-liganden ATE221887T1 (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 (1)

Publication Number Publication Date
ATE221887T1 true ATE221887T1 (de) 2002-08-15

Family

ID=27451643

Family Applications (1)

Application Number Title Priority Date Filing Date
AT98920635T ATE221887T1 (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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WO1998050385A1 (en) 1997-05-08 1998-11-12 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
EP1047697A1 (de) * 1998-01-14 2000-11-02 MERCK SHARP & DOHME LTD. Triazolo-pyridazin-derivate als liganden für gaba-rezeptoren
CA2317416A1 (en) * 1998-02-25 1999-09-02 Merck Sharp & Dohme Limited Substituted 1,2,4-triazolo[3,4-a]pyridazine
KR20010041234A (ko) 1998-02-25 2001-05-15 더블유. 지. 콜 치환된 1,2,4-트리아졸로[3,4-a]피리다진
GB9805557D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
EP1131102A2 (de) * 1998-11-12 2001-09-12 Merck & Co., Inc. Kombination von inverse agonisten des gaba-a alpha-5 rezeptor subtyps und cox-2 inhibitoren, nsaid, östrogen oder vitamin e
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
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
GB9824897D0 (en) 1998-11-12 1999-01-06 Merck Sharp & Dohme Therapeutic compounds
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
JP4883862B2 (ja) * 1999-11-15 2012-02-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ファルネシルトランスフェラーゼ阻害剤としてのトリアゾール類
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
US7932272B2 (en) * 2003-09-30 2011-04-26 Eisai R&D Management Co., Ltd. Antifungal agent containing heterocyclic compound
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
JP5240899B2 (ja) 2005-01-05 2013-07-17 タケダ ゲゼルシャフト ミット ベシュレンクテル ハフツング トリアゾロフタラジン
US7671050B2 (en) 2005-01-05 2010-03-02 Nycomed Gmbh Triazolophthalazines
EP2275095A3 (de) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenese durch modulation des Muscarinrezeptors
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
EP2377530A3 (de) 2005-10-21 2012-06-20 Braincells, Inc. Modulation von Neurogenese durch PDE-Hemmung
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
EP2314289A1 (de) 2005-10-31 2011-04-27 Braincells, Inc. Gaba-rezeptor-vermittelte modulation von neurogenese
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007134077A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
CA2651813A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
AU2007292848A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US8183264B2 (en) 2006-09-21 2012-05-22 Eisai R&D Managment Co., Ltd. Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same
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
CA2709664A1 (en) * 2007-12-26 2009-07-02 Eisai R&D Management Co., Ltd. Method for manufacturing heterocycle substituted pyridine derivatives
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
CN104086528A (zh) 2010-07-15 2014-10-08 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
EP3766882B1 (de) * 2018-03-12 2023-08-23 Shanghai Simr Biotechnology Co., Ltd. Phthalazinisoxazol-alkoxyderivate, verfahren zu ihrer herstellung, pharmazeutische zusammensetzung und ihre verwendung
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
EP4334301A1 (de) 2021-05-05 2024-03-13 University College Cardiff Consultants Limited Heteroarylverbindungen zur behandlung von kognitiven störungen
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
DE69720732T2 (de) * 1996-07-25 2004-01-29 Merck Sharp & Dohme Substituierte Triazolo-Pyridazin-Derivate als Liganden von GABA-Rezeptoren
AU724076B2 (en) 1996-07-25 2000-09-14 Merck Sharp & Dohme Limited Substituted triazolo pyridazine derivatives as inverse agonists of the GABAAalpha5 receptor subtype
WO1998050385A1 (en) 1997-05-08 1998-11-12 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
JP2001525802A (ja) 2001-12-11
JP4672820B2 (ja) 2011-04-20
WO1998050385A1 (en) 1998-11-12
US6310203B1 (en) 2001-10-30
US6200975B1 (en) 2001-03-13
AU7342898A (en) 1998-11-27
CA2288789C (en) 2009-07-21
AU732455C (en) 2002-09-05
CA2288789A1 (en) 1998-11-12
EP0986562B1 (de) 2002-08-07
DE69807074D1 (de) 2002-09-12
AU732455B2 (en) 2001-04-26
EP0986562A1 (de) 2000-03-22
DE69807074T2 (de) 2003-04-03
ES2179490T3 (es) 2003-01-16

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