Abstract: The present invention is directed to a process for preparing the following compound ##STR1## which is prepared starting from ##STR2## which is reacted succesively with 4-iodobenzyl or 4-bromobenzyl bromide, hydrazine and 1,4-dimethyl-1,3-cyclohexadiene, reduced and reacted with phenyltetrazole or suitably protected phenyltetrazole followed by removal

Abstract: Antibiotic 10381a.sub.1, wherein R is hydrogen, is a cytosine-containing antibiotic producible by culturing the novel microorganism Streptomyces arginensis in an aqueous medium and isolation thereof. Derivatives wherein R is a C.sub.1 to C.sub.3 alkyl ester of antibiotic 10381a.sub.1, are also disclosed along with the pharmaceutically acceptable salts of both the native and esterified forms. Antibiotic 10381a.sub.1 inhibits the growth of selected species of yeast, fungi and bacteria. This invention also relates to a novel process for the preparation of the antibiotics 10381b and to a method of using antibiotics 10381b to promote growth in meat-producing animals. These antibiotics are also obtained by the fermentation of a nutrient medium with the novel microorganism Streptomyces arginensis and are active against selected species of bacteria.

Abstract: Antibiotic 10381a.sub.1, wherein R is hydrogen, is a cytosine-containing antibiotic producible by culturing the novel microorganism Streptomyces arginensis in an aqueous medium and isolation thereof. Derivatives wherein R is a C.sub.1 to C.sub.3 alkyl ester of antibiotic 10381a.sub.1, are also disclosed along with the pharmaceutically acceptable salts of both the native and esterified forms. Antibiotic 10381a.sub.1 inhibits the growth of selected species of yeast, fungi and bacteria. This invention also relates to a novel process for the preparation of the antibiotics 10381b and to a method of using antibiotics 10381b to promote growth in meat-producing animals. These antibiotics are also obtained by the fermentation of a nutrient medium with the novel microorganism Streptomyces arginensis and are active against selected species of bacteria.

Abstract: The present invention provides a method for treatin hypertension in insulin resistant patients comprising the administration of an insulin sensitizing agent, particularly ciglitazone or pioglitazone.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The invention concerns novel pharmaceutical compositions containing as an active ingredient a 2-benzoyl-1,3-cyclohexanedione which is an inhibitor of the enzyme 4-hydroxyphenylpyruvate dioxygenase (HPPD). The compositions are valuable in the treating those disorders and diseases in which it is desirable to intervene in the metabolic sequences catalysed by HPPD, such as in treating tyrosinemia type I.

Abstract: Compounds of formula I ##STR1## wherein X and Y are H or halo; R.sup.2 is: [structures Ia, Ib or Ic;] ##STR2## R.sup.3 is selected from unsubstituted or substituted alkyl, aryl or heteroaryl groups;R.sup.4 is selected from H or (C1-6)alkyl,and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disoders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective mount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

Abstract: A method for the treatment of neurological disorders, comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I or of formula II (formulae set out on pages following the Examples), whereinR.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from:hydrogen,(1-3C)perfluoroalkyl,halo, nitro and cyano;R.sup.5 is a (1-5C)alkyl group;or a pharmaceutically acceptable salt thereof.Also provided are compounds and pharmaceutical compositions suitable for the treatment of neurological disorders.

Abstract: The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.

Abstract: The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

Abstract: Compounds of formula I or I', ##STR1## wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R.sup.1 is selected from(A) (1-6C)alkyl;(B) phenyl and naphthyl or substituted versions thereof;(C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five- and six-membered heteroaryl rings;(E) heteroaryl (1-3C)alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.

Abstract: Antagonists at the NMDA receptor complex which are benz b!azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.

Abstract: Benz[b]azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.

Abstract: Compounds of formula I ##STR1## wherein X.sup.a, X.sup.b, R, R.sup.1 and R.sup.2 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention relates to certain novel heterocyclic ketones which are 1-pyridylacetamide ketones of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic ketones, processes for preparing the heterocyclic ketones, pharmaceutical compositions containing such heterocyclic ketones and methods for their use.

Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.

Abstract: Compounds of formula I, Ia or Ib and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

Abstract: A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.

Abstract: A compound of the following general formula which is useful in treating hypocholesterolemia and atherosclerosis: ##STR1## wherein X is oxygen or sulfur; R is hydrogen, alkyl having from 1 to 8 carbon atoms, or benzyl; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a heterocyclic group, or a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds and each of R.sub.2 and R.sub.3 is selected from hydrogen, provided both are not hydrogen, an aralkyl group, a hydrocarbon chain of from 1 to 20 carbon atoms which is saturated or contains 1 to 3 double bonds, an w-substituted alkylC.sub.1-6, a heterocyclic group, phenyl, substituted phenyl or NR.sub.2 R.sub.3 taken together form a monocyclic heterocyclic group.

Abstract: The present invention provides pharmaceutically useful compounds which are aminosulfonyl urea compounds which are ACAT inhibitors rendering them useful in controlling blood cholesterol levels, pharmaceutical compositions and methods of using the ACAT inhibitors and closely related compounds which are also aminosulfonyl urea compounds.