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
Authority: AT; Austria
Prior art keywords: triazolo; ligands; substituted; gaba; alpha
Prior art date: 1997-05-08

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.)

1997-05-08

Filing date

1998-05-06

Publication date

2002-08-15

1997-05-08 Priority claimed from GBGB9709368.6A external-priority patent/GB9709368D0/en

1997-07-10 Priority claimed from GBGB9714508.0A external-priority patent/GB9714508D0/en

1997-11-11 Priority claimed from GBGB9723741.6A external-priority patent/GB9723741D0/en

1998-02-25 Priority claimed from GBGB9803992.8A external-priority patent/GB9803992D0/en

1998-05-06 Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme

2002-08-15 Application granted granted Critical

2002-08-15 Publication of ATE221887T1 publication Critical patent/ATE221887T1/de

Links

239000003446 ligand Substances 0.000 title abstract 2
LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical class C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 title 1
JVJPJKLSGUJUJK-UHFFFAOYSA-N [1,2,4]triazolo[3,4-a]phthalazine Chemical class C1=CC=C2C=NN3C=NN=C3C2=C1 JVJPJKLSGUJUJK-UHFFFAOYSA-N 0.000 abstract 1
229960003692 gamma aminobutyric acid Drugs 0.000 abstract 1
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract 1

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)

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)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
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
CA2315219A1 (en) *	1998-01-14	1999-07-22	Merck Sharp & Dohme Limited	Triazolo-pyridazine derivatives as ligands for gaba receptors
IL137117A0 (en) *	1998-02-25	2001-06-14	Merck Sharp & Dohme	Substituted 1,2,4-triazolo [3,4-a] pyridazine
TR200002469T2 (tr) *	1998-02-25	2000-12-21	Merck Sharp & Dohme Limited	İkameli 1,2,4-triazol [3,4-a]piridazin.
GB9805557D0 (en)	1998-03-16	1998-05-13	Merck Sharp & Dohme	A combination of therapeutic agents
GB9824897D0 (en) *	1998-11-12	1999-01-06	Merck Sharp & Dohme	Therapeutic compounds
WO2000027849A2 (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
AU764875B2 (en) *	1998-11-12	2003-09-04	Merck & Co., Inc.	Combination of a GABA-A alpha 5 inverse agonist and COX-2 inhibitor, NSAID, estrogen or vitamin
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
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
GB0000564D0 (en) *	2000-01-11	2000-03-01	Merck Sharp & Dohme	Therapeutic agents
AU2001275014A1 (en) *	2000-05-30	2001-12-11	Neurogen Corporation	Imidazoloisoquinolines
PY0119496A (es)	2000-08-07	2003-11-03	Neurogen Corp	Compuestos heterociclicos como ligandos de receptores gabaa
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
WO2005033079A1 (ja) *	2003-09-30	2005-04-14	Eisai Co., Ltd.	ヘテロ環化合物を含有する新規な抗真菌剤
KR101368093B1 (ko)	2004-09-02	2014-03-14	다케다 게엠베하	트리아졸로프탈라진
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
CA2591991C (en)	2005-01-05	2013-11-19	Altana Pharma Ag	Triazolophthalazines
CN101103033B (zh)	2005-01-05	2010-08-04	尼科梅德有限责任公司	作为pde2抑制剂的三唑并酞嗪
EP2275095A3 (de)	2005-08-26	2011-08-17	Braincells, Inc.	Neurogenese durch modulation des Muscarinrezeptors
EP2258358A3 (de)	2005-08-26	2011-09-07	Braincells, Inc.	Neurogenese mit Acetylcholinesterasehemmer
EP1940389A2 (de)	2005-10-21	2008-07-09	Braincells, Inc.	Modulation von neurogenese durch pde-hemmung
AU2006308889A1 (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
JP2009536667A (ja)	2006-05-09	2009-10-15	ブレインセルス，インコーポレイティド	５ｈｔ受容体介在性の神経新生
EP2382975A3 (de)	2006-05-09	2012-02-29	Braincells, Inc.	Neurogenese mittels Angiotensin-Modulation
AU2007292848A1 (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
CN101910159B (zh) *	2007-12-26	2013-06-19	卫材R&D管理有限公司	杂环取代吡啶衍生物的制备方法
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
EP2464355A4 (de) *	2009-08-14	2013-01-02	Concert Pharmaceuticals Inc	Substituierte triazolphthalazinderivate
AR079451A1 (es)	2009-12-18	2012-01-25	Nycomed Gmbh	Compuestos 3,4,4a,10b-tetrahidro-1h-tiopirano[4,3-c]isoquinolina
JP5996532B2 (ja)	2010-07-15	2016-09-21	バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒＩｎｔｅｌｌｅｃｔｕａｌＰｒｏｐｅｒｔｙＧｍｂＨ	有害生物防除剤としての新規複素環式化合物
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
US11512089B2 (en)	2018-03-12	2022-11-29	Shanghai SIMR Biotechnology Co., Ltd	Substituted [1,2,4]triazolo[3,4-a]phthalazines as modulators of GABAA receptor activity
HU231223B1 (hu)	2018-09-28	2022-01-28	Richter Gedeon Nyrt.	GABAA A5 receptor modulátor hatású biciklusos vegyületek
EP4126858B1 (de)	2020-03-26	2026-03-18	Richter Gedeon Nyrt.	Dihydro-2-pyrrolo[3,4-c pyridin-derivate als gabaa a5 rezeptormodulatoren
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
US20240425491A1 (en)	2021-05-05	2024-12-26	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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
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
WO1998004560A1 (en)	1996-07-25	1998-02-05	Merck Sharp & Dohme Limited	SUBSTITUTED TRIAZOLO PYRIDAZINE DERIVATIVES AS INVERSE AGONISTS OF THE GABAAα5 RECEPTOR SUBTYPE
KR20000029548A (ko) *	1996-07-25	2000-05-25	더블유. 지. 콜	가바수용체에대한리간드로서의치환된트리아졸로-피리다진유도체
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

1998
- 1998-05-06 CA CA002288789A patent/CA2288789C/en not_active Expired - Fee Related
- 1998-05-06 WO PCT/GB1998/001307 patent/WO1998050385A1/en not_active Ceased
- 1998-05-06 US US09/180,623 patent/US6200975B1/en not_active Expired - Lifetime
- 1998-05-06 JP JP54784398A patent/JP4672820B2/ja not_active Expired - Fee Related
- 1998-05-06 DE DE69807074T patent/DE69807074T2/de not_active Expired - Lifetime
- 1998-05-06 ES ES98920635T patent/ES2179490T3/es not_active Expired - Lifetime
- 1998-05-06 AU AU73428/98A patent/AU732455C/en not_active Ceased
- 1998-05-06 AT AT98920635T patent/ATE221887T1/de not_active IP Right Cessation
- 1998-05-06 EP EP98920635A patent/EP0986562B1/de not_active Expired - Lifetime
2000
- 2000-04-11 US US09/547,216 patent/US6310203B1/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
EP0986562B1 (de)	2002-08-07
US6310203B1 (en)	2001-10-30
ES2179490T3 (es)	2003-01-16
CA2288789A1 (en)	1998-11-12
AU732455C (en)	2002-09-05
AU732455B2 (en)	2001-04-26
AU7342898A (en)	1998-11-27
DE69807074D1 (de)	2002-09-12
EP0986562A1 (de)	2000-03-22
DE69807074T2 (de)	2003-04-03
JP2001525802A (ja)	2001-12-11
WO1998050385A1 (en)	1998-11-12
JP4672820B2 (ja)	2011-04-20
CA2288789C (en)	2009-07-21
US6200975B1 (en)	2001-03-13

Legal Events

Date	Code	Title	Description
2003-02-15	RER	Ceased as to paragraph 5 lit. 3 law introducing patent treaties

Publication	Publication Date	Title
ATE221887T1 (de)	2002-08-15	Substituierte 1,2,4-triazolo(3,4,-a)phthalazin- derivate als gaba-alpha 5-liganden
TR199902516T2 (xx)	2000-02-21	Kalsilitik bile�imleri.
TR199901653T2 (xx)	1999-10-21	Fitalazinonlar.
TR199902400T2 (xx)	2000-01-21	Fungusit etkinlik g�steren terkiplerin birle�imleri.
ES2184077T3 (es)	2003-04-01	Nuevas fenantridinas sustituidas en la posicion 6.
ATE233735T1 (de)	2003-03-15	Neue phenanthridine
BG102616A (en)	1999-04-30	Substituted aza- and diazacycloheptane and cyclooctane derivatives and their application
DE69805643D1 (de)	2002-07-04	Membrane-elektroden-anordnung
ATE293618T1 (de)	2005-05-15	4, 5, 6, 7-tetrahydroindazolderivate als antitumormittel
IT1285770B1 (it)	1998-06-18	Composti corticoidei
ID21413A (id)	1999-06-10	Turunan-turunan 1,3,8,-triaza-spiro (4,5) dekan-4-on
RU95101375A (ru)	1996-11-20	Производные n-(3-аминопропил)-n-фенил-5,6,7,8-тетрагидронафталин-2-карбоксамида, их получение и применение в терапии
TR199800988A3 (tr)	1998-12-21	5' Deoksi-Sitidin türevleri.
GB2324091A (en)	1998-10-14	Metalloproteinase inhibitors
TR199701202T1 (xx)	1998-03-21	Yeni hidroksimik asit t�revleri.
TR199701298T1 (xx)	1998-02-21	Tetralinler.
ATE192428T1 (de)	2000-05-15	Nitro-benzamides verwendbar als antiarrythmica
HRP20000866B1 (en)	2009-02-28	A reference compound for use in the analysis of levosimendan batches
ATE213236T1 (de)	2002-02-15	Substituierte benzyloxyimino-verbindungen
DE60003560D1 (de)	2003-07-31	1,2-dihydro-1-oxo-pyrazino[1,2-]indolederivate
PT1104419E (pt)	2002-09-30	Derivados de azabicicloheptano substituidos no azoto sua preparacao e utilizacao
TR199701011A2 (xx)	1998-04-21	1-karba-(detia)-sefalosforin t�revleri.
YU48719B (sh)	1999-07-28	Lizin so 6-hloro-5-fluoro-3-(2-tenoil)-2-oksindol-1-karboksamida
FI950101A7 (fi)	1995-03-07	4-oksa-1-atsabisyklo 3,2,0 -7heptanoni-johdannaiset kasvainten vastaisina aineina
ATE223380T1 (de)	2002-09-15	Heteroaryloxyethylaminen als 5-ht1a rezeptor liganden