Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.

Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.

Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.

Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B-W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Indoline compounds having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.

Abstract: Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.

Abstract: The invention features a method of delivering a drug to a diseased cell by linking the drug to a rifamycin derivative, compositions that include drug-rifamycin conjugates of the invention, and methods for treating disease using those compositions.

Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.

Abstract: The present invention is directed to amides of antibiotic A82846B (also known as chloroorienticin A), and of N.sup.4 -derivatives of A82846B. The present amide compounds are useful as antibacterials, especially for the control of gram positive bacteria; the compounds are particularly useful for the control of resistant bacterial strains, such as vancomycin-resistant-enterococci ("VRE").

Abstract: An optical amplifier having an amplification medium which comprises a complex of a rare earth ion and a ligand, said complex being dissolved in a polymeric matrix, as well as an optical communications network comprising one or more optical amplifiers of the above-described polymeric type.

Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.

Abstract: The invention relates to macropolycyclic rare earth complexes, namely cryptates which are useful as fluorescent tracers.

Abstract: The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A.sub.1 --A.sub.2 --, --A.sub.3 --A.sub.4 -- and --A.sub.5 --A.sub.6 -- each denote ethylene or vinylene or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each denote ethylene and --A.sub.5 --A.sub.6 -- denotes vinylene; X represents >C(R.sub.6)-- or >N-- and R.sub.6 denotes hydrogen or alkyl; alk denotes an aliphatic hydrocarbon radical; R.sub.1 denotes hydrogen or acyl; R.sub.2 denotes acyl, or alkyl which is optionally substituted by an aromatic radical, and R.sub.3 and R.sub.3 ' represent a common bond, or R.sub.3 denotes hydrogen or acyl, and R.sub.3 ' is hydrogen; R.sub.4 denotes hydrogen, cycloalkyl or aryl; R.sub.5 denotes hydrogen or acetyl; R.sub.7 denotes hydrogen or alkyl, which can be used as active compounds in medicaments, the preparation and use thereof, and pharmaceutical products and the preparation thereof.

Abstract: Compounds of the general formula: ##STR1## in which R is a lower alkyl group, and R.sub.1 is a tri-lower alkylmethylcarbonyl group, the structure elements --A.sub.1 --A.sub.2 --, A.sub.3 --A.sub.4 -- or A.sub.5 --A.sub.6 -- each represent ethylene or vinylene, or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each represent ethylene and --A.sub.5 --A.sub.6 -- represents vinylene, their optical isomers and their salts exhibit valuable pharmaceutical properties.

Abstract: 3-W-Rifamycin SV and S compound, wherein W is a piperazin-1-yl radical of the formula ##STR1## wherein R.sup.1 and R.sup.2 are C.sub.1 -C.sub.4 alkyl and R.sup.3, R.sup.4 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl, or R.sup.2 together with R.sup.3 or R.sup.3 together with R.sup.4 are buta-1,3-dien-1,4-ylene, trimethylene or tetramethylene, each of which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, and R.sup.1, R.sup.4 and R.sup.5 or R.sup.1, R.sup.2 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl, and salts thereof, have long-term antituberculotic and antimicrobial activity.

Abstract: Compounds of the formula ##STR1## in which R represents lower alkyl, R.sub.1 represents tri-lower alkylmethylcarbonyl, and one of the radicals R.sub.2 and R.sub.3 represents tri-lower alkylmethylcarbonyl and the other represents hydrogen, and salts thereof, exhibit hypo-lipidaemic properties.

Abstract: The present invention concerns new 2'-substituted-4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives having antibacterial activity.These compounds are compounds obtained by chemical modification of thiazolo[5,4-c]rifamycin SV.

Abstract: The present invention provides expellants of phytopothogenic microbes comprising rifamycins, which have excellent in prevention of disease in plants with little adverse influence to human body and environments.