Title:
SUBSTITUTED CYCLOALKYL-4-OXONICOTINIC CARBOXAMIDES; GABA BRAIN RECEPTOR LIGANDS
Document Type and Number:
WIPO Patent Application WO1999043661
Kind Code:
A3
Abstract:
Disclosed are compounds of Formula (a) or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
Inventors:
DESIMONE ROBERT W (US)
ROSEWATER DANIEL L (US)
ROSEWATER DANIEL L (US)
Application Number:
PCT/US1999/004310
Publication Date:
January 06, 2000
Filing Date:
February 26, 1999
Export Citation:
Assignee:
NEUROGEN CORP (US)
DESIMONE ROBERT W (US)
ROSEWATER DANIEL L (US)
DESIMONE ROBERT W (US)
ROSEWATER DANIEL L (US)
International Classes:
A61K31/435; A61K31/4427; A61K31/443; A61K31/4433; A61K31/444; A61K31/47; A61K31/4709; A61K31/473; A61P25/00; A61P25/08; A61P25/20; A61P25/22; A61P25/28; A61P43/00; C07D215/56; C07D221/04; C07D401/12; C07D405/12; C07D409/12; C07D417/12; (IPC1-7): C07D221/04; C07D215/54; C07D417/12; C07D407/12; C07D401/12; C07D409/12; A61K31/44; C07D215/56
Domestic Patent References:
| WO1998002420A1 | 1998-01-22 | |||
| WO1997034870A1 | 1997-09-25 |
Foreign References:
| DE2407744A1 | 1974-08-29 | |||
| EP0067772A1 | 1982-12-22 | |||
| EP0070767A1 | 1983-01-26 | |||
| EP0180318A1 | 1986-05-07 |
Other References:
BARNARD E A ET AL: "International Union of Pharmacology. XV. Subtypes of.gamma -aminobutyric acidA receptors: Classification on the basis of subunit structure and receptor function", PHARMACOLOGICAL REVIEWS, vol. 50, no. 2, June 1998 (1998-06-01), pages 291 - 313, XP002106519, ISSN: 0031-6997
MARYANOFF B E ET AL: "POTENTIAL ANXIOLYTIC AGENTS. PYRIDOL 1,2-ABENZIMIDAZOLES: A NEW STRUCTURAL CLASS OF LIGANDS FOR THE BENZODIAZEPINE BINDING SITE ON GABA-A RECEPTORS", JOURNAL OF MEDICINAL CHEMISTRY, vol. 38, 1 January 1995 (1995-01-01), pages 16 - 20, XP002053732, ISSN: 0022-2623
MARYANOFF B E ET AL: "POTENTIAL ANIOLYTIC AGENTS. 2. IMPROVEMENT OF ORAL EFFICACY FOR THEPYRIDO 1,2-ABENZIMIDAZOLE (PBI) CLASS OF GABA-A RECEPTOR MODULATORS", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 6, no. 3, 1 January 1996 (1996-01-01), pages 333 - 338, XP002054104, ISSN: 0960-894X
E.E. KILBOURN ET AL., JOURNAL OF ORGANIC CHEMISTRY, vol. 37, no. 8, 1972, EASTON US, pages 1145 - 1148, XP002118290, ISSN: 0002-6557
MARYANOFF B E ET AL: "POTENTIAL ANXIOLYTIC AGENTS. PYRIDOL 1,2-ABENZIMIDAZOLES: A NEW STRUCTURAL CLASS OF LIGANDS FOR THE BENZODIAZEPINE BINDING SITE ON GABA-A RECEPTORS", JOURNAL OF MEDICINAL CHEMISTRY, vol. 38, 1 January 1995 (1995-01-01), pages 16 - 20, XP002053732, ISSN: 0022-2623
MARYANOFF B E ET AL: "POTENTIAL ANIOLYTIC AGENTS. 2. IMPROVEMENT OF ORAL EFFICACY FOR THEPYRIDO 1,2-ABENZIMIDAZOLE (PBI) CLASS OF GABA-A RECEPTOR MODULATORS", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 6, no. 3, 1 January 1996 (1996-01-01), pages 333 - 338, XP002054104, ISSN: 0960-894X
E.E. KILBOURN ET AL., JOURNAL OF ORGANIC CHEMISTRY, vol. 37, no. 8, 1972, EASTON US, pages 1145 - 1148, XP002118290, ISSN: 0002-6557
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