Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.

Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents; and the amount of viscosity modifying agents can optionally be reduced by at least an amount by weight that would have increased the viscosity of the carrier without the tetracycline antibiotic by at least 30%; wherein the tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline

Abstract: A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.

Abstract: The invention relates to tetracycline products produced by genetically engineered cells, and to therapeutic methods using such tetracyclines. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway.

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: The present invention provides compounds which exhibit an inhibitory effect on undecaprenyl diphosphate synthase of microbes and thereby they are expected to be used clinically as pharmaceutical agents for infectious diseases caused by bacteria. The process comprises culturing a microbe belonging to Penicillium and having ability of producing an FKI-3368 substance in or on a nutrient medium to accumulate the FKI-3368 substance in the nutrient medium and collecting the FKI-3368 substance from the culture.

Abstract: Provided herein are methods and compositions for the in vitro formation of tetracycline conjugates, for example, tetracycline conjugated to anti-coagulants. The present invention also provides methods for preventing or treating plaque-related diseases or disorders such as atherosclerosis using tetracycline alone, or the tetracycline conjugates of the present invention.

Abstract: The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II and Form III, of minocycline base are provided. These are characterised by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallisation from the mixture.

Abstract: The present invention pertains to novel 3, 10, and/or 12a-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: 13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines to 13-deoxyanthrcyclines wherein the reduction reaction is maintained at temperatures of about 55° C. to 64° C. without stirring or agitation. The reaction is completed with the addition of aqueous bicarbonate which forms the 13-deoxyanthracycline and precipitates. The precipitates are filtered and the precipitate and filtrate are extracted separately with organic solvents. The crude 13-deoxy anthracycline can be converted to 5-imino-13-deoxy anthracycline by reaction with methanolic ammonia. The reaction can also be performed with an acidic pyridinium salt instead of a strong acid so that neutralization of the reaction or extraction of the product is not necessary, thereby facilitating purification.

Abstract: The present invention discloses a process for the semi-synthesis of 4-demethoxydaunomycinone, (8s-cis)-acetyl-10-hydroxy-7,8,9,10-tetrahydro-6,8,11-trihydroxy-5,12-naphthacenedione, of formula (I).

Abstract: 7-phenyl-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-phenyl-substituted tetracycline compounds are described.

Abstract: The compound (W-Z-M) according to the invention comprises a component (M) chosen from the group consisting of markers and therapeutic agents possessing an intracellular active site (A.S.), linked to a ligand (W-Z) comprising an arm (Z) linked to a terminal group (W), characterized in that the linkage between the arm (Z) of the ligand (W-Z) and the component (M) prevents intracellular entry of the compound (W-Z-M) and/or inhibits expression of the marker (M), in that said linkage can be selectively cleaved by factors secreted by target cells so as to permit expression of the marker (M) or entry of the therapeutic agent (M) into said target cells, and in that the terminal group (W) provides for the stability of the compound (W-Z-M) in the serum and circulating blood.

Abstract: The present invention provides a lipid-modified insulin comprising an insulin molecule linked to an alkyl group by an amine linkage. Preferably, the alkyl group is a straight chain carbon comprising from about 14 to 20 carbon atoms. Preferably, the alkyl group is linked to the B1 phenylalanine or the B29 lysine. The present invention also provides a liposome comprising such lipid-modified insulin. Preferably, the liposomes are small unilamellar vesicles (SUVs) which have a particle size of less than 100 nm.The present invention also provides a method for making a lipid-modified insulin. The method comprises reacting the protein with a hydrophobic aldehyde in the presence a reducing agent to provide a lipid-modified insulin in which an amino acid of the insulin is linked to an alkyl group by an amine linkage.The present invention also relates to a method of killing hepatoma cells, particularly the hepatoma cells that are found in a hepatocellular carcinoma.

Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.

Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.

Abstract: Compounds of formula I or V or mixtures thereof ##STR1## wherein R is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.5, and R.sub.5 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, and at least one of the substituents R.sub.1 to R.sub.4 is --F, --Cl or --Br, or is independently the group RO--, and the other substituents R.sub.1 to R.sub.4 are H, --F, --Cl or --Br, are reversible photochromic systems which can be used for contrast formation, light absorption or for the reversible optical storage of information.

Abstract: Compounds of formula V, ##STR1## wherein R is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthiol, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.5, and R.sub.5 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, and at least one of the substituents R.sub.1 to R.sub.4 is an organic thiol, sulfoxyl or sulfonyl group, and the other members R.sub.1 to R.sub.4 are H, F, Cl or Br, are reversible photochromic systems which can be used for contrast formation or light absorption.

Abstract: This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.

Abstract: 4-substituted anthracyclinones of formula (I) ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

Abstract: To produce doxorubicin and its analogues methyl 3alpha, 5alpha-dihydroxy-5beta-(trimethylsilylethynyl)-2alpha-nitromethylcyclohexa ne-1beta-carboxylate acetonide is condensed with 1,4-dihydro-4,4,5-trimethoxy-1-oxonaphthalene in the presence of 1,8-diazabicyclo-[5.4.0]undec-7-ene in an aprotic solvent to produce 3-[ (2beta-carbomethoxy-4beta-ethynyl-4alpha, 6alpha-(di-O-isopropylidenyl)cyclohexanyl-1-yl]-nitromethyl-4,4,5-trimetho xy-1-oxo-1,2,3,4-tetrahydronaphthalene; which is cyclized to produce 9beta-ethynyl-12-hydroxy-7alpha,9alpha-(di-O-isopropylidenyl)-6-nitro-4,5, 5-trimethoxy-5,5a,6,6a,7,8,9,10,10a,11-decahydro -11-naphthacenone. The decahydro-11-naphthacenone is converted to 7alpha-9alpha,(di-O-isopropyl-idenyl)-4,5-dimethoxy-9beta-ethynyl-12-hydro xy-6-nitro-6,6a,7,8,9,10,10a,11-octahydro-11, -naphthacenone.

Abstract: Substituted naphthacenediones of the formula I ##STR1## in which R.sup.1 to R.sup.8 are H and at least one of R.sup.1 to R.sup.8, for example R.sup.2 and R.sup.3 or R.sup.2 and R.sup.6, are, for example, C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 alkenoxy, C.sub.1 -C.sub.20 -alkylsulfinyl, --CN, --CF.sub.3, --NO.sub.2, --Si(CH.sub.3).sub.3 or --COO(C.sub.1 -C.sub.12 alkyl), are suitable, when incorporated into polymers having hydroxyalkyl groups, for currentless deposition of metals onto the polymer surface. They are in some cases suitable as photoinitiators.

Abstract: Disclosed is novel compound UCT-1003 represented by the following formula: ##STR1## and having anti-tumor activity. UCT-1003 is produced by culturing a microorganism belonging to the genus Paecilomyces.

Abstract: Naphthacene-5,12-diones which are substituted by at least one organic thio radical are not only photoinitiators for the photopolymerization but also sensitizers for the photodimerization of ethylenically unsaturated compounds. Compositions made of these naphthacene-5,12-diones and ethylenically unsaturated compounds are suitable for the preparation of printing inks, paints, printing plates, resist materials or as image recording material.