Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention is directed to analogs of paromomycin having a variety of chemical functional groups attached at the 2?-O-position as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention is directed to analogs of paromomycin having a variety of chemical functional groups attached at the 2?-O-position as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: There is provided a compound of formula I wherein the dashed line, R1, R2, R3a, R3b, A, D, E, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of thrombin is required or desired, and/or conditions where anticoagulant therapy is indicated).

Abstract: There is provided a compound of formula (I) wherein R1, R2a, R2b, R3a, R3b, R4, R5, R6, A, G and L have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as trombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is beneficial (e.g. conditions, such as thrombo-embolisms, where inhibition of trombin is required or desired, and/or conditions whereas anticoagulant therapy is indicated).

Abstract: A process is provided for the preparation of a compound of the general formula (I): wherein R is H or C1-4 alkyl, which comprises treating a compound of the general formula (II): where R? is R or R8CO, R is as defined above, R8 is C1-8 alkyl or optionally substituted phenyl and R9 is optionally substituted C1-8 alkyl or optionally substituted aryl, with an amine R??NH2 wherein R?? is H or C1-4 alkyl. Also provided are the trans isomers of the compound (I) where R is CH3 (6-epi-malayamycin A) and H (6-epi-desmethylmalayamycin A), the cis and trans isomers of the compound (I) where R is C2-4alkyl and various intermediate compounds.

Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

Abstract: Disclosed are compounds of the formula: 1

Abstract: The present invention provides compounds of formula Ia and Ib or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.

Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y,or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.

Abstract: A process for the preparation of a compound (I) ##STR1## wherein R is a hydroxyl protecting group which comprises isomerising a compound of formula (I) wherein R is a hydroxyl protecting group by reacting the compound of formula (I) with a sterically hindered organic base in the presence of a Lewis acid and a compound of forumula (III) ##STR2## wherein R.sub.1 and R.sub.2 each independently represent cyano, COR.sub.5 or COR.sub.2 R.sub.6 or R.sub.1 andR.sub.2 together with the carbon atom to which they are attached from a C.dbd.O group;R.sub.5 represents alkyl, cycloalkyl, amino, alkylamino, dialkyl amino or optionally substituted phenyl or phenylalkyl group;R.sub.6 represents alkyl, cycloalkyl or optionally substituted phenyl or phenylalkyl group;R.sub.3 and R.sub.4 represent each independently hydrogen, alkyl, alkoxy or optionally substituted phenyl group.

Abstract: Novel glycosides containing novel leaving groups, pyridyloxy, pyrimidyloxy, methoxypyridyloxy, pyridyl carbonate and pyridyl thiocarbonate are utilized in many fertile syntheses of glycosides, disaccharides, trisaccharides, oligosaccharides, nucleosides and the like. These synthetic schemes are superior in stereospecificity, yield and speed of preparation of numerous novel compounds. Polymer supported syntheses may be utilized within the general scheme to provided enhanced product purity.

Abstract: This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R.sub.2 are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, R.sub.3 is a halogen atom or a hydroxy radical, R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.

Abstract: This invention relates to derivatives of perhydroisoindol of formula: ##STR1## in which the radicals R are hydrogen atoms or together form a bond, the symbols R' are phenyl radicals which can be substituted by a halogen atom or a methyl radical in position 2 or 3, X is an oxygen atom or an NH radical, R.sub.1 is optionally substituted phenyl, or cyclohexadienyl, naphthyl, or heterocyclyl, R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R.sub.3 is halogen or OH and R.sub.4 is H or halogen if R.sub.3 is halogen, in their isomer forms, or mixture thereof, and possibly also their salts when they exist, and preparation thereof. The derivatives of the invention are particularly interesting as P substance antagonist.

Abstract: Compounds of the formula I ##STR1## wherein R' is a free or esterified carboxy group or a carboxylate anion and R.sup.2 is an organic group have beta-lactamase inhibition activity. A process for the preparation of the same and pharmaceutical compositions containing these compounds are provided.

Abstract: A process for selectively deacetylating an acetyl derivative of a saccharide is described, comprising treating an acetyl derivative of a monosaccharide or oligosaccharide using a mixture of an aqueous solution of alkali metal hydroxide/aqueous hydrogen peroxide/organic solvent to selectively hydrolyze acetate bonds at specific positions in the molecule, and thereby obtain a partially hydrolyzed acetyl derivative of a saccharide.