Abstract: Compounds of the formula I, ##STR1## and also their tautomeric forms of the formula Ia, ##STR2## in which the substituents R.sup.1 to R.sup.6 and X have said meanings, exhibit antiviral activity.

Abstract: Imidazopyridine derivatives and pharmacologically acceptable salts having antagonistic properties towards angiotensin II can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.

Abstract: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.

Abstract: The present invention provides a family of tropane analogs. More particularly, the present invention provides a family of 4' and 4',4"-substituted-3.alpha.-(diphenylmethoxy)tropane analogs having the formula ##STR1## in which R is a functional group including, but not limited to, hydrogen, alkyl, alkoxy, arylalkyl, aryloxyalkyl, cinnamyl and acyl; and R.sup.1 and R.sup.2 are independently selected and are functional groups including, but not limited to, hydrogen, alkyl, alkoxy, hydroxy, halogen, cyano, amino and nitro. The benztropine analogs of the present invention have a high affinity for the dopamine transporter and inhibit dopamine uptake, but they do not exhibit a cocaine-like behavioral profile. Moreover, the present invention provides methods of using such benztropine analogs to treat cocaine abuse, to image dopamine transporter/cocaine binding sites, and to diagnose and/or monitor neurodegenerative disorders (e.g., Parkinson's disease).

Abstract: Compounds of formula (I) are active antiviral compounds useful in the treatment of viral infections in mammals. The compounds of the invention are readily prepared by reaction of a suitable 2-thiothiazole derivative with an appropriate Het-(CH.sub.2).sub.n -halide.

Abstract: This invention relates to a 4-quinolinone derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 mean individually H, halogen, cyano, or lower alkyl, lower alkylsulfonyl, lower alkylsulfinyl, lower alkylthio or lower alkoxy which may be substituted by halogen, or phenylsulfonyl, phenylsulfinyl or phenylthio which may have a substituent; and R.sup.3 and R.sup.4 denote individually H, lower alkyl or cycloalkyl which may be substituted by halogen, or pyridyl, furanyl or phenyl which may have a substituent, or R.sup.3 and R.sup.4 may form a 4-, 5- or 6-membered heterocyclic ring, or a salt thereof, and an intermediate useful for the preparation thereof, and besides a medicinal composition comprising this compound as an active ingredient. The compound (1) or the salt thereof has an excellent potassium channel-activating effect and is useful as, for example, a prophylactic and therapeutic agent for diseases of circulatory and bronchial systems.

Abstract: Novel N-alkyl derivatives of deoxygalactonojirimycin are provided in which said alkyl contains from 3-6 carbon atoms. These novel compounds are useful for selectively inhibiting glycolipid synthesis.

Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.

Abstract: Antibacterial fluoroquinoline derivatives and salts thereof of the following formula are stable and have low toxicity and high photostability and low cytotoxicity under light irradiation: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl;R.sub.2 is hydrogen, optionally protected amino, optionally protected aminocarbonyl or optionally protected carboxyl;R.sub.5 is halogen, lower alkyl or optionally protected hydroxyl or is the same as R.sub.2 ;R.sub.6 is lower alkyl;A is CH.sub.2, optionally protected nitrogen or oxygen;andn and m are each an integer of from 0 to 4, provided that n +m is an integer of from 1 to 4.

Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: Impurities are separated from aqueous solutions of 1,6-hexanediol or 1,6-hexanediol precursors, such as adipic and 6-hydroxycaproic acid, by a process which comprises adding at least one carboxylic acid to a solution (a) of 1,6-hexanediol and subjecting this solution (a) or a solution (b) containing carboxylic acid(s) as precursor(s) of 1,6-hexanediol to a heat treatment at temperatures above room temperature in the absence of hydrogen.

Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.

Abstract: Compounds for treating cancer and other diseases involving telomerase activity are characterized by the following structure: ##STR1## Such compounds include those for which X.sub.1 is oxygen, sulfur, sulfone, or sulfinyl, and R.sub.1 is --Y.sub.n R.sub.6, where n is an integer between 0 and 10 and each Y.sub.n independently is methylene, methine, or quaternary carbon. R.sub.6, is alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, arninocarbonyl, alkylarninocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, carboxaldehyde, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, or arylsulfinyl. R.sub.6 can also be a linker selected from the group consisting of alkyl, aryl, and heterocycle. R.sub.

Abstract: Hydroxyquinolone monoazo dyestuffs of the formula I ##STR1## in which D is an organic radical such as one of the disclosed aromatic radicals, and R is substituted or unsubstituted alkyl, benzyl, phenyl, phenoxy, or alkoxy (most preferably C.sub.1 -C.sub.6 -alkyl) are especially well suited to dyeing and printing of hydrophobic materials and other dyeing or printing applications. The dyestuffs are prepared by diazotizing an amine (D--NH.sub.2) and coupling the diazotization product to a hydroxyquinolone compound.

Abstract: Photoconductive imaging members comprised of unsymmetrical dimeric perylene as a charge generator, wherein said perylene is of the following formula ##STR1## wherein R is hydrogen, alkyl, cycloalkyl, substituted alkyl, aryl, substituted aryl, aralkyl or substituted aralkyl group, and X--Y is an unsymmetrical bridging moiety of alkylene, substituted alkylene, arylene, substituted arylene, aralkylene or substituted aralkylene.

Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.

Abstract: This invention concerns a compound of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; optionally substituted by one or more substituents the same or different,R' represents one or more optional substituents the same or different, selected from the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6 )alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; andR" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.

Abstract: Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.

Abstract: The present invention is directed to methods for manufacturing 3-(aminomethyl)-6-chloropyridines represented by a general formula ?II!; ##STR1## wherein R.sup.2 represents hydrogen or a lower alkyl and R.sup.3 represents hydrogen, a lower alkyl or an halogen atom, characterized in that the compound represented by the general formula ?II! is manufactured by allowing 3-(substituted-aminomethyl)pyridine 1-oxide represented by a general formula ?I!; ##STR2## wherein R.sup.1 represents alkyl, aryl, aralkyl or alkoxy, R.sup.2 and R.sup.3 are as described above, to react with a base represented by a general formula ?a!;R'R"R'"N ?a!wherein R', R" and R'" may be the same or different one another and represent each independently a lower alkyl or an aromatic group, or R', R" , R'" and N may form together an optionally-substituted pyridine ring, in the presence of an electrophilic reagent having at least one chlorine atom, and subsequently treating the reaction product with hydrogen chloride and water.