United States Patent 6,384,224
Greenlee , et al. May 7, 2002
Certain 1-(2-naphthyl) and 1-(2-azanaphthyl)-4-(1-phenylmethyl) piperazines; dopamine receptor subtype specific ligands
Abstract
Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen; R.sub.1 and R.sub.2 independently represent organic or inorganic substituents; R.sub.3 and R.sub.4 are variables independently representing inorganic or organic substituents; A represents C.sub.1 -C.sub.4 alkylene; and R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl, which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.
Inventors: Greenlee; William (Teaneck, NJ); Gangly; Ashit (U. Montclair, NJ); Wasley; Jan W. F. (Guilford, CT)
Assignee: Neurogen Corporation (Branford, CT)
Appl. No.: 897352
Filed: July 2, 2001
Current U.S. Class: 544/356; 514/249
Intern'l Class: C07D 403/04
Field of Search: 544/356
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United States Patent 6,380,210
DeSimone , et al. April 30, 2002
Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
Abstract
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6, are variables defined herein, 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, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
Inventors: DeSimone; Robert W. (Durham, CT); Hutchison; Alan (Madison, CT); Shaw; Kenneth (Weston, CT); Rosewater; Daniel L. (Golden, CO)
Assignee: Neurogen Corporation (Branford, CT)
Appl. No.: 540454
Filed: March 31, 2000
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United States Patent 6,380,209
Cai , et al. April 30, 2002
4-(4-piperidylmethylamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands
Abstract
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted alkyl, aryl, 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. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
Inventors: Cai; Guolin (Guilford, CT); Liu; Gang (Agoura, CA)
Assignee: Neurogen Corporation (Branford, CT)
Appl. No.: 583147
Filed: May 30, 2000 |
