CA2301599C - 4-oxo-naphtyridine-3-carboxamides substitues comme ligands de recepteur de gaba du cerveau - Google Patents

4-oxo-naphtyridine-3-carboxamides substitues comme ligands de recepteur de gaba du cerveau Download PDF

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Publication number
CA2301599C
CA2301599C CA002301599A CA2301599A CA2301599C CA 2301599 C CA2301599 C CA 2301599C CA 002301599 A CA002301599 A CA 002301599A CA 2301599 A CA2301599 A CA 2301599A CA 2301599 C CA2301599 C CA 2301599C
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CA
Canada
Prior art keywords
dihydro
oxo
naphthyridine
carboxamide
compound according
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 - Fee Related
Application number
CA002301599A
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English (en)
Other versions
CA2301599A1 (fr
Inventor
Pamela Albaugh
Robert W. Desimone
Gang Liu
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.)
Neurogen Corp
Original Assignee
Neurogen Corp
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
Application filed by Neurogen Corp filed Critical Neurogen Corp
Publication of CA2301599A1 publication Critical patent/CA2301599A1/fr
Application granted granted Critical
Publication of CA2301599C publication Critical patent/CA2301599C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des structures de la formule (I) ou leurs sels non toxiques et acceptables du point de vue pharmaceutique; dans la formule (I): X est hydrogène, halogène, alkyle (non) substitué, alcoxy ou amine (non) substitué; et Y est alkyle (non) substitué, aryle ou hétéroaryle; ces composés sont des agonistes, antagonistes ou agonistes inverses de récepteurs de GABAa du cerveau ou des promédicaments d'agonistes, d'antagonistes ou d'agonistes inverses de récepteurs de GABAa du cerveau. Ces composés s'utilisent dans le diagnostic et le traitement de l'anxiété, du syndrome de Down, du sommeil, de troubles cognitifs et épileptiques et de l'overdose de médicaments au benzodiazépine et pour l'activation de la vigilance.
CA002301599A 1997-08-25 1998-08-24 4-oxo-naphtyridine-3-carboxamides substitues comme ligands de recepteur de gaba du cerveau Expired - Fee Related CA2301599C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91818097A 1997-08-25 1997-08-25
US08/918,180 1997-08-25
PCT/US1998/017513 WO1999010347A1 (fr) 1997-08-25 1998-08-24 4-oxo-naphtyridine-3-carboxamides substitues comme ligands de recepteur de gaba du cerveau

Publications (2)

Publication Number Publication Date
CA2301599A1 CA2301599A1 (fr) 1999-03-04
CA2301599C true CA2301599C (fr) 2003-03-25

Family

ID=25439933

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002301599A Expired - Fee Related CA2301599C (fr) 1997-08-25 1998-08-24 4-oxo-naphtyridine-3-carboxamides substitues comme ligands de recepteur de gaba du cerveau

Country Status (24)

Country Link
EP (1) EP1007526A1 (fr)
JP (1) JP2001514181A (fr)
KR (1) KR20010023313A (fr)
CN (1) CN1268136A (fr)
AP (1) AP2000001742A0 (fr)
AU (1) AU753800B2 (fr)
BG (1) BG104192A (fr)
BR (1) BR9811362A (fr)
CA (1) CA2301599C (fr)
EG (1) EG21717A (fr)
HU (1) HUP0003258A3 (fr)
IL (1) IL134291A0 (fr)
IS (1) IS5382A (fr)
LV (1) LV12539B (fr)
NO (1) NO20000822L (fr)
NZ (1) NZ502548A (fr)
OA (1) OA11293A (fr)
PE (1) PE130999A1 (fr)
PL (1) PL338783A1 (fr)
SI (1) SI20270A (fr)
SK (1) SK2162000A3 (fr)
TW (1) TW574221B (fr)
WO (1) WO1999010347A1 (fr)
YU (1) YU10500A (fr)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01011173A (es) * 1999-05-06 2002-04-24 Neurogen Corp 4-0x0-quinolin-3-carboxamidas sustituidas: ligandos del receptor cerebro de gaba.
US6448246B1 (en) 1999-05-25 2002-09-10 Neurogen Corporation Substituted 4H-1,4-benzothiazine-2-carboxamide: GABA brain receptor ligands
US6730682B2 (en) 2000-07-12 2004-05-04 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
US6559145B2 (en) 2000-07-12 2003-05-06 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
US6562822B2 (en) 2000-07-12 2003-05-13 Pharmacia & Upjohn Company Heterocyle carboxamides as antiviral agents
JP2004517860A (ja) 2000-10-12 2004-06-17 メルク　エンド　カムパニー　インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
AU1532802A (en) 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
EP1326865B1 (fr) 2000-10-12 2009-05-06 Merck & Co., Inc. Aza- et polyaza-naphthalenyl carboxamides utiles comme inhibiteurs de l'integrase du vih
US20020151591A1 (en) * 2000-10-17 2002-10-17 Anabella Villalobos Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders
IL157465A0 (en) * 2001-03-01 2004-03-28 Pfizer Products Inc Pfizer Pro Use of gabaa inverse agonists in combination with nicotine receptor partial agonists, estrogen, selective estrogen modulators, or vitamin e for the treatment of cognitive disorders
AR036256A1 (es) 2001-08-17 2004-08-25 Merck & Co Inc Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento
EP1467970B1 (fr) 2002-01-17 2007-08-22 Merck & Co., Inc. Carboxamides hydroxynaphthyridinone utiles comme inhibiteurs de l'integrase du vih
WO2003077857A2 (fr) 2002-03-15 2003-09-25 Merck & Co., Inc. N-(benzyl substitue)-8-hydroxy-1,6-naphtyridine-7-carboxamides utiles comme inhibiteurs de l'integrase du vih
WO2004106336A1 (fr) * 2003-05-27 2004-12-09 Pfizer Products Inc. Procede de preparation et de purification de 1,5-naphtyridine-3-carboxyamides
WO2004106334A2 (fr) * 2003-05-28 2004-12-09 Pfizer Products Inc. Procede de preparation de 1,5-naphtyridine-3-carboxyamides par amidation directe d'esters
SI2074123T1 (sl) * 2006-10-16 2013-03-29 Bionomics Limited Nove anksiolitične spojine
DK2083811T3 (en) * 2006-11-22 2017-01-30 Clinical Res Ass Llc PROCEDURES FOR TREATING DOWNS SYNDROME, FRAGILT X SYNDROME AND AUTISM

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR204813A1 (es) * 1972-05-08 1976-03-05 Yamanouchi Pharma Co Ltd Proceso para la preparacion de derivados de ampilicina
GB1433774A (en) * 1973-02-26 1976-04-28 Allen & Hanburys Ltd Heterocyclic compounds apparatus for conveying articles
US4374138A (en) * 1981-11-13 1983-02-15 Warner-Lambert Company Antibacterial amide compounds, compositions, and methods of use
DD279887A1 (de) * 1987-07-03 1990-06-20 Inst Pharmakologische Forschun Verfahren zur herstellung von d-alpha-(4(1h)-1,5-naphthyridon-3-carboxamido)-benzylpenicillin und anderen beta-lactamantibiotika
DD279875A1 (de) * 1987-07-03 1990-06-20 Inst Pharmakologische Forschun Verfahren zur herstellung von aktivierten carbonsaeureestern
DD295360A5 (de) * 1987-07-03 1991-10-31 Akad Wissenschaften Verfahren zur Herstellung von aktivierten Carbonsäureestern
JPS6461461A (en) * 1987-09-01 1989-03-08 Otsuka Pharma Co Ltd Benzohetero ring derivative

Also Published As

Publication number Publication date
AU9117398A (en) 1999-03-16
OA11293A (en) 2002-11-19
IL134291A0 (en) 2001-04-30
CA2301599A1 (fr) 1999-03-04
HUP0003258A3 (en) 2001-05-28
NO20000822D0 (no) 2000-02-18
TW574221B (en) 2004-02-01
WO1999010347A1 (fr) 1999-03-04
IS5382A (is) 2000-02-22
BR9811362A (pt) 2000-08-22
CN1268136A (zh) 2000-09-27
PL338783A1 (en) 2000-11-20
BG104192A (en) 2001-05-31
AU753800B2 (en) 2002-10-31
LV12539A (en) 2000-10-20
EP1007526A1 (fr) 2000-06-14
AP2000001742A0 (en) 2000-02-24
JP2001514181A (ja) 2001-09-11
NO20000822L (no) 2000-04-13
EG21717A (en) 2002-02-27
NZ502548A (en) 2002-06-28
LV12539B (en) 2001-01-20
PE130999A1 (es) 1999-12-16
SI20270A (sl) 2000-12-31
HUP0003258A2 (en) 2001-03-28
SK2162000A3 (en) 2001-03-12
KR20010023313A (ko) 2001-03-26
YU10500A (sh) 2002-10-18

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