Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R and R represent substituted or unsubstituted organic residues. These 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.
Pamela A. Albaugh - Clinton CT Robert W. DeSimone - Durham CT Gang Liu - Agoura CA
Assignee:
Neurogen Corporation - Branford CT
International Classification:
A61K 31535
US Classification:
5142352, 514300, 544128, 546123
Abstract:
The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y 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. These compounds 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.
Fused Pyrrolecarboxamides; A New Class Of Gaba Brain Receptor Ligands
Pamela Albaugh - Clinton CT Gang Liu - Agoura CA Kenneth Shaw - Weston CT Alan Hutchison - Madison CT
Assignee:
Neurogen Corporation - Branford CT
International Classification:
C07D40312
US Classification:
548455, 548454, 544105
Abstract:
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R -R are as 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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
Pamela A. Albaugh - Clinton CT Robert W. DeSimone - Durham CT Gang Liu - Agoura CA
Assignee:
Neurogen Corporation - Branford CT
International Classification:
A61K 3144 C07D47102
US Classification:
514300
Abstract:
The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y 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. These compounds 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.
Fused Pyrrolecarboxamides; A New Class Of Gaba Brain Receptor Ligands
Pamela Albaugh - Clinton CT Gang Liu - Branford CT Kenneth Shaw - Weston CT Alan Hutchison - Madison CT
Assignee:
Neurogen Corporation - Branford CT
International Classification:
C07D20914 C07D20934 C07D20940
US Classification:
548516
Abstract:
The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: G represents ##STR2## where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with subtituents on Q; ##STR3## independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3 R. sub. 3, R. sub. 4, R. sub. 5, and R. sub. 6 are the same or different and represent organic or inorganic substituents. These 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.
Fused Pyrrolecarboxamides; A New Class Of Gaba Brain Receptor Ligands
Pamela Albaugh - Clinton CT Gang Liu - Branford CT Kenneth Shaw - Weston CT Alan Hutchison - Madison CT
Assignee:
Neurogen Corporation - Brandford CT
International Classification:
C07D20914
US Classification:
548516
Abstract:
The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: G represents ##STR2## where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with subtituents on Q; ##STR3## independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3 R. sub. 3, R. sub. 4, R. sub. 5, and R. sub. 6 are the same or different and represent organic or inorganic substituents. These 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.
Fused Pyrrolecarboxamides; A New Class Of Gaba Brain Receptor Ligands
Pamela Albaugh - Clinton CT Gang Liu - Agoura CA Kenneth Shaw - Weston CT Alan Hutchison - Madison CT
Assignee:
Neurogen Corporation - Branford CT
International Classification:
C07D41312
US Classification:
544144
Abstract:
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R. sub. 3 -R. sub. 6 are as 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. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
Certain Fused Pyrrolecarboxamides A New Class Of Gaba Brain Receptor Ligands
Pamela Albaugh - Clinton CT Gang Liu - Branford CT Alan Hutchison - Madison CT
Assignee:
Neurogen Corporation - Branford CT
International Classification:
C07D23970 C07D20918 C07D27502 A61K 31425
US Classification:
514249
Abstract:
Disclosed are compounds of formula I: ##STR1## wherein R. sub. 8 and R. sub. 9 independently represent hydrogen or organic substituents; W represents optionally substituted thiazolyl or quinoxalinyl; X is hydrogen, hydroxy or lower alkyl; and T is hydrogen, halogen, hydroxy, nitro, amino or alkyl, 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 receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.