Abstract: An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.

Abstract: A belt extender for installation on a belt with a removable buckle comprising a main body with a first end and a second end, a metal tab fixedly attached to and extending from a first end of the main body of the belt extender, and a longitudinal slot roughly centrally disposed on the main body of the belt extender. The main body folds over itself at a fold line that extends through the center of the longitudinal slot and is secured in place with snap fasteners to create a folded end. A belt buckle comprising a tongue and a frame is installed on the folded end of the belt extender by sliding the frame of the belt buckle over the second end of the belt extender and inserting the tongue through the longitudinal slot prior to folding. The metal tab is inserted into a longitudinal slot on the buckle end of the belt strap and rotated so that the main body of the belt extender is aligned with the belt strap on the buckle end of the belt.

Abstract: A belt extender for installation on a belt with a removable buckle comprising a main body with a first end and a second end, a metal tab fixedly attached to and extending from a first end of the main body of the belt extender, and a longitudinal slot roughly centrally disposed on the main body of the belt extender. The main body folds over itself at a fold line that extends through the center of the longitudinal slot and is secured in place with snap fasteners to create a folded end. A belt buckle comprising a tongue and a frame is installed on the folded end of the belt extender by sliding the frame of the belt buckle over the second end of the belt extender and inserting the tongue through the longitudinal slot prior to folding. The metal tab is inserted into a longitudinal slot on the buckle end of the belt strap and rotated so that the main body of the belt extender is aligned with the belt strap on the buckle end of the belt.

Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

Abstract: Animals with mutations in COL4a4 present with autosomal recessive Alport Syndrome (ARAS). Through sequencing of COL4a4, the mutation causative for ARAS in the English Cocker Spaniel (ECS) has been identified. The resulting protein is severely truncated due to a premature stop codon in exon 3. This nonsense mutation occurs in the 7S domain and also causes the loss of the entire collagenous and NC1 domains of the protein. Methods for the identification of animals that harbor a mutation in the COL4a4 gene are described. Mutations in the COL4a4 gene can be identified from any biological sample such as a cell or tissue that contains genomic DNA. Methods for identifying single nucleotide polymorphisms (SNPs) that are inherited with the disease are also described. A microsatellite marker that segregates with ARAS is also described that was identified using linkage disequilibrium mapping.

Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

Abstract: The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

Abstract: This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are as defined within, which process comprises preparing treating a compound such as physostigmine to form eseroline which is then treated with an appropriate compound or its equivalent. Acetic acid is added to the reaction mixture after the formation of eseroline.

Abstract: A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to fore compound II. Hydrolysis of compound(II) yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.

Abstract: A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II) yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.

Abstract: A process for preparing N-ethylhydroxylamine hydrochloride which comprises reacting hydroxylamine hydrochloride with di-t-butyl dicarbonate in the presence of a base thus producing N,O-bis-[(1,1-dimethylethoxy)carbonyl]-hydroxylamine, alkylating said reaction product and then cleaving with acid the tert-butyloxy carbonyl (BOC) portion of the alkylated product.

Abstract: A process for preparing N-ethylhydroxylamine hydrochloride which comprises reacting hydroxylamine hydrochloride with di-t-butyl dicarbonate in the presence of a base selected from sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, sodium or potassium hydroxide or triethylamine, in a non-reactive solvent, alkylating said reaction product with an alkyl halide and then cleaving with a strong acid the tert-butyloxycarbonyl (BOC) portion of the alkylated product.

Abstract: A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.

Abstract: There is described an improved method for synthesizing N-aminophthalimide from phthalimide and hydrazine wherein the reaction is conducted in a medium consisting essentially of water and alcohol at a volume ratio within the range of from 80:20 to 20:80 at a temperature within the range of from -5.degree. C. to 35.degree. C., said alcohol being methanol, ethanol, n-propanol, iso-propanol or a mixture thereof.

Abstract: A compound of the formula ##STR1## is prepared by reacting an N-acylated-o-toluidine of the formula ##STR2## with n-alkyllithium to form a dilithio intermediate of the formula ##STR3## which can then be quenched with N-benzylidenemethylamine to form compound II. Hydrolysis of compound(II)yields the free base ##STR4## or its salt, which can be cyclized to form 4,5-dihydro-2,3-dimethyl-4-phenyl-3H-1,3-benzodiazepine or its physiologically acceptable salts, which are useful as pharmacological agents.

Abstract: A stereoselective reduction of 2- or 3-substituted 4-piperidones of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or benzyl and R.sub.2 is methyl or ethyl, to the di-equatorial isomer of the corresponding 4-piperidinol is described. Said reduction is conducted by use of sodium borohydride in a protic solvent medium at a temperature substantially lower than ambient temperature in the presence of an effective amount of an inorganic acid. Under favorable reaction conditions, the stereoselectivity of the reduction is so high that simple crystallization of the reaction product affords the pure isomer in a commercially acceptable and advantageous process.

Abstract: The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.

Abstract: A method for the preparation of 6,11-dihydro-11-oxodibenz[b,e]oxepin-acetic acids having pharmaceutical activity is disclosed. Compounds represented by the formula: ##STR1## wherein R is OH or Cl are provided as intermediates. An aldehyde of the formula: ##STR2## wherein R.sub.1 is a lower alkyl, e.g., 1 to 4 carbon atoms, is reacted with chloroform and aqueous base to form an .alpha.-hydroxy dicarboxylic acid. Alternatively, the aldehyde can be converted to the corresponding cyanohydrin, which is then converted to the corresponding .alpha.-hydroxy dicarboxylic acid. The .alpha.-hydroxy dicarboxylic acid can also be prepared from reaction of a halogenated toluate of the formula: ##STR3## wherein X is Cl or Br with mandelic acid or a derivative thereof of the formula: ##STR4## wherein R.sub.3 and R.sub.4 are independently selected from hydrogen and alkyl of 1 to 4 carbon atoms. The .alpha.-hydroxy dicarboxylic acid is cyclized and then converted to the oxepin acetic acid by reduction. Alternatively, the .

Abstract: The invention relates to compounds of the formula ##STR1## where Y is --OH; halogen; ##STR2## R.sub.1 SO.sub.3 --, where R.sub.1 is a straight chain or branched chain alkyl group having 1 to 5 carbon atoms, or aryl; and R.sub.2 is --C(CH.sub.3).sub.3 or --O--C(CH.sub.3).sub.3. Processes for preparing the compounds are provided. The compounds are useful as intermediates in the preparation of 4-phenyl-1,3-benzodiazepins, which exhibit activity as antidepressants, analgetics and anticonvulsants.