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.

Abstract: Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 whereR.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.

Abstract: The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl;X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxy, nitro, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4,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.

Abstract: This invention encompasses compounds of formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groups.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

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; andT 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.

Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.9 and Y are substituents as defined herein; andR.sub.a and R.sub.b independently represent halogen, hydroxy, amino, mono or dialkylamino where each alkyl is straight or branched chain alkyl having 1-6 carbon atoms, straight or branched chain lower alkyl having 1-6 chain atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms, where R.sub.a and R.sub.b each appear at most only once on the phenyl ringwhich compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein: X is hydrogen or lower alkyl having 1-6 carbon atoms; andW is an optionally substituted aryl group as defined herein.

Abstract: Disclosed are methods for screening compounds for potential therapeutic activity based on selective binding to GABAa receptors, and where the methods employ compounds of formulas I and II shown herein.

Abstract: This invention encompasses compounds of the formulas: ##STR1## where R.sub.1 R.sub.3, R.sub.4, R.sub.6, X, Y, and Z are T are variables; andM is ##STR2## where R.sub.2 is a variable; or R.sub.1 and R.sub.2 together may represent --(CH.sub.2).sub.n.sbsb.1 where .sub.n.sbsb.1 is 1, 2, or 3.These compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects asssociated with the use of conventional neuroleptic agents.

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groupsThese compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: Disclosed are compounds and the pharmaceutically acceptable salts thereof useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism and useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents, which compounds have the formula: ##STR1## where R.sub.1 and R.sub.2 are independently represent hydrogen or inorganic groups.

Abstract: Disclosed are compounds and the pharmaceutically acceptable salts thereof useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism and useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents, which compounds have the formula: ##STR1## where R.sub.1, X, Y and T indepedently represent inorganic or organic groups such as hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or sulfonyl;R.sub.3 is hydrogen or lower alkyl or R.sub.3 and R.sub.4 together may form a ring structure; andR.sub.4 and R.sub.5 are the same or different and represent organic or inorganic groups where the groups may form a ring optionally substituted with various organic or inorganic substituents.

Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: This invention encompasses compounds of the formulas: ##STR1## where R.sub.1 R.sub.3, R.sub.4, R.sub.6, X, Y, and Z are T are variables; andM is ##STR2## where R.sub.2 is a variable; or R.sub.1 and R.sub.2 together may represent --(CH.sub.2).sub.n1 where n.sub.1 is 1, 2, or 3.These compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents.

Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and W, X, A, B, C, D, E, R.sub.3, R.sub.4 are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, over-dose with benzodiaziepine drugs, and enhancement of memory.

Abstract: This invention encompasses compounds of formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## represents: ##STR3## where n is 0, 1, or 2; R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups;Y represents various organic and inorganic substituents;W represents an aromatic group substituted with various organic and inorganic substituents;A is CH or N;B is a substituted or unsubstituted carbon or N; andE is hydrogen or straight or branched alkyl groups.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: The present invention encompasses structures of the formula I: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted aryl groups;X is hydrogen, hydroxy or lower alkyl;T is hydrogen, halogen, hydroxyl, amino or alkyl;R.sub.3 is hydrogen or an organic group;R.sub.4 is hydrogen or substituted or unsubstituted organic substituent;R.sub.5 and R.sub.6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4.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 recpetors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: This invention encompasses compounds of formula (I) and pharmaceutically acceptable non-toxic salts thereof wherein (Ia) represents (i) or (ii) where n is 0, 1, or 2: R.sub.1 and R.sub.2 are hydrogen or straight or branched chain alkyl groups; Y various organic and inorganic substituents; W represents an aromatic group substituted with various organic and inorganic substituents; A is CH or N; B is a substituted or unsubstituted carbon or N; and E is hydrogen or straight or branched alkyl groups. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ is hydrogen or fluorine.The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas I and II radiolabeled with tritium or isotopes of iodine.The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas I or II.The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula I or II.The compounds provided herein bind selectively to a novel subtype of the GABAa binding site.