Abstract: A novel, overall process for the preparation of a compound of the formula I: ##STR1## where R.sup.1 and R.sup.2 are each independently hydrogen, an alkyl group, a cycloalkyl group, an aryl group or, taken together with the carbon atom to which they are attached, form a cycloalkyl group; andR.sup.3 is hydrogen, an alkyl group, or an aryl group, or salts thereof, useful as intermediates in the preparation of HMG-CoA reductase inhibitors; novel methods within the overall process; and novel intermediates produced by those methods.

Abstract: There are disclosed compounds having the formula ##STR1## wherein the variables are defined in the specification, and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.

Abstract: Novel tetrazole derivatives represented by the formula ##STR1## wherein n denotes an integer of 1 to 3; A is an optionally substituted heterocyclic residue; Y is a divalent hydrocarbon residue; and X is CH or N, or pharmaceutically acceptable salts thereof have excellent hypoglycemic and hypolipidemic activities.

Abstract: Diketopyrrolopyrrole of the formula ##STR1## in its .beta.-modification. The new .beta.-modification is suitable as a pigment for coloring high-molecular weight organic material and shows, in comparison to the .alpha.-modification, a shift in shade towards yellowish-red.

Abstract: The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: This invention relates to a compound (a quinoline derivative) represented by the formula (I): ##STR1## The quinoline derivative of this invention has a strong leukotriene antagonistic action and is extremely useful as an antiallergic medicine and an anti-inflammatory medicine.

Abstract: The present invention is concerned with novel quinoline derivatives having anti-Helicobacter activity of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the stereochemically isomeric forms thereof, the quaternized forms thereof and the N-oxides thereof, wherein --A-- represents a bivalent radical of formula--N.dbd.CH--CH.dbd.CH-- (a),--CH.dbd.N--CH.dbd.CH-- (b),--N.dbd.N--CH.dbd.CH-- (c),--N.dbd.CH--N.dbd.CH-- (d),--N.dbd.CH--CH.dbd.N-- (e),--CH.dbd.N--N.dbd.CH-- (f),--N.dbd.N--N.dbd.CH-- (g),--N.dbd.N--CH.dbd.N-- (h),or--CH.dbd.CH--CH.dbd.CH-- (i);R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent hydrogen, halo, hydroxy, C.sub.1-4 alkyloxy, C.sub.1-4 alkyl, trifluoromethyl, amino, mono- or di(C.sub.

Abstract: A process for preparing substituted benzopyran derivatives which comprises a final step cyclisation of the corresponding open-chain intermediates.

Abstract: There have been discovered new bicyclic pyrrolidone compounds such as: ##STR1## which are useful as insecticides, ascaricides and herbicides.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: A method of producing optically active pyrrolidines of the general formula ##STR1## in which R.sup.1 is hydrogen or OH,R.sup.2 is a benzyl group which can have one or more alkyl-, alkoxy- and/or halogen substituents on the aromatic, and* is and/or can be an asymmetric center,by reducing the corresponding, enantiomerically pure pyrrolidinediones using activated alkali boron hydride.

Abstract: The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.

Abstract: This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.

Abstract: The subject invention relates to compounds having the structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl;(b) R' is selected from unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; and halo; and(c) R" is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; methyl monosubstituted with hydroxy, thiol or amino; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; amino; unsubstituted amide; unsubstituted or C.sub.1 -C.sub.3 substituted amido; halo; unsubstituted sulfoxide; unsubstituted sulfonyl; and cyano;pharmaceutical compositions containing such compounds, and the use of such compounds for preventing or treating respiratory, ocular, and/or gastrointestinal disorders.

Abstract: Disclosed is a method for removing a protective group of an N-protected tetrazolyl compound which comprises reacting said N-protected tetrazolyl compound with a mineral acid under substantially anhydrous conditions in the presence of an alcohol, insuring a high reaction yield of the object tetrazolyl compound.

Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.

Abstract: The invention relates to novel derivatives of quinolone-carboxylic acid and naphthyridonecarboxylic acid which are substituted in the 7 position by a 1- (or 5-)amino-methyl-2- (or 3-)oxa-7-aza-bicyclo[3.3.0]oct-7-yl residue, their salts, processes for their preparation and antibacterial agents containing these compounds.

Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.