Abstract: A reversible thermochromic system comprising a) a compound of the formula (IA) or a tautomer thereof or a compound of the formula (IB) or a tautomer thereof (IA) (IB) wherein R1 is C1-C18alkyl, C2-C18alkenyl, C3-C12cycloalkyl, C3-C12cycloalkyl substituted by 1, 2 or 3 C1-C4alkyl; phenyl, phenyl substituted by 1, 2 or 3 C1-C4alkyl; or C7-C12phenylalkyl; R2 is hydrogen or a group —SO2—R; R3 and R4 independently of one another are hydrogen, C1-C18alkyl, C2-C18alkenyl, C3-C12cycloalkyl, C3-C12cycloalkyl substituted by 1, 2 or 3 C1-C4alkyl; phenyl, phenyl substituted by 1, 2 or 3 C1-C4alkyl; or C7-C12phenylalkyl; and R is C1-C18alkyl, C2-C18alkenyl, C3-C12cycloalkyl, C3-C12cycloalkyl substituted by 1, 2 or 3 C1-C4alkyl; phenyl, phenyl substituted by 1, 2 or 3 C1-C4alkyl; or C7-C12phenylalkyl; and b) a compound containing a group of the formula (III).

Abstract: Devices for detecting an analyte comprising a redox active analyte sensitive material on a working electrode and computer assisted signal acquisition and processing.

Abstract: Described herein are substrates composed of a base coated with a fluorophore-labeled calcium phosphate coating. The substrates are useful in culturing and studying the activity of a variety of cells. The substrates described herein can be used for both solution- and image-based analysis of cultured cells. New methods for producing and using such coated substrates are also disclosed.

Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.

Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.

Abstract: The present invention pertains to a reversibly thermochromic system comprising a substituted or an unsubstituted 6,11-dihydroxy-naphthacene-5,12-dione and a base and to a reversibly thermochromic composition comprising the reversibly thermochromic system and a carrier material and to novel substituted 6,11-dihydroxy-naphthacene-5,12-diones.

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 is a di-steroidal prodrug of ethinyl estradiol according to formula I:

Abstract: The present invention is a di-steroidal prodrug of estradiol having the following formula:

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: A compound represented by the following formula (I):X--Y--Z (I)where Y is represented by the following formulae: ##STR1## X is a monovalent group of a tetracycline type compounds and Z is a monoent group of a steroid type compound such as estrogen.The compound can concentrate on the bone tissue and has bone resorption inhibition/ossification promotion functions.

Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.

Abstract: A process for the preparation of antibiotics of the anthracycline class of formula (A), wherein R.sup.1 is hydrogen, OH, or OCOR.sup.2, wherein R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group; which comprises the epimerization of the 4' hydroxy group of the daunosamine residue by nucleophilic substitution of a triflate group with a carboxylate, which epimerization is carried out on the whole molecule with the hydroxy groups being protected, and subsequent transformation into the final product.

Abstract: Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.

Abstract: The present invention discloses new and novel bisanthracyclines linked through the saccharide portions. These compounds show high activity against two clinically relevant mechanisms of resistance. A novel approach of the invention produces compounds that are as active or more so than the parent compounds. Furthermore, the inventor's discovery is also for the design of effective DNA-binding bisanthracyclines as well as anthracyclines mixed with other intercalators and groove binders.

Abstract: 8-fluoro-anthracyclines of formula (I) have anti-tumor activity. ##STR1## wherein: R is chosen in the group consisting of H, OH, OR.sub.4 wherein R.sub.4 is chosen in the group consisting of CHO, COCH.sub.3, acyl derivative of a carboxylic acid containing up to 6 carbon atoms;R.sub.1 is chosen in the group consisting of: H, OH, OCH.sub.3 ;R.sub.2 is chosen in the group consisting of: H, OH, NH.sub.2R.sub.3 is chosen in the group consisting of: H, OH, NH.sub.2, residue of formula (A) ##STR2## The compounds are characterized by having cis-stereochemistry between the groups 8--F and 9--OH. Their preparation and pharmaceutical compositions containing them are also described.

Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.

Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group.

Abstract: Disclosed herein are new anthracyclines which are derived from conjugation with glutathione, for example from conjugation of adriamycin, daunomycin and menogaril with glutathione: compounds 7 I, 7 II, 8 I, 8 II, 9 I and 9II, are obtained by reduction of the anthracycline followed by reaction of the reduced product with glutathione in aqueous (H.sub.2 O or D.sub.2 O) or organic solvent. The invention also provides salts of these glutathione derivatives, particularly salts formed from anthracycline glutathione anions with anthracycline cations. These anthracycline derivatives are useful as antibiotics, as antitumor agents, and in the treatment of AIDS. These derivatives are particularly useful in the treatment of cancer when multiple drug resistance is present.

Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.

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: Daunomycinone is a known precursor of the well known antibiotic and antineoplastic, doxorubicin. Daunomycinone may be synthesized by preparing mono ketal of a 1,4-naphthoquinone as the precursor of the CD rings of daunomycinone followed by preparing a precursor for ring A with C.sub.6 and C.sub.11 attached and the stereochemistry at C.sub.7 and C.sub.9 established and coupling it to CD and then completing ring B.

Abstract: The present invention relates to Saintopin derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is hydrogen and R.sup.2 is SO.sub.2 OH (UCE 1022), or R.sup.1 is acetyl and R.sup.2 is H (Saintopin E), which are useful as antibacterial and anti-tumor agents.

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: 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: A compound represented by formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is provided, which has an excellent antitumor activity.

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: Compounds of formula I or V or mixtures thereof ##STR1## whereinR 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 the 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.16 l-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 thio, 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: Compounds of the formula I ##STR1## in which R.sup.1 to R.sup.8 independently of one another are H and at least one of R.sup.1 to R.sup.8 is a substituent belonging to the group --F, --Si(C.sub.1 -C.sub.4 alkyl).sub.3 or --COOR.sup.10 ; or each pair of adjacent radicals of R.sup.1 to R.sup.8 is --CO--O--CO--; or at least one of R.sup.1 to R.sup.8 is C.sub.1 -C.sub.20 alkyl--(X).sub.p --, C.sub.2 -C.sub.20 alkenyl--(X).sub.p --, C.sub.2 -C.sub.20 -alkynyl--(X).sub.p --, C.sub.3 -C.sub.8 cycloalkyl--(X).sub.p --, (C.sub.1 -C.sub.12 alkyl--C.sub.3 -C.sub.8 cycloalkyl--(X).sub.p --, C.sub.3 -C.sub.8 -cycloalkyl--CH.sub.2 --(X).sub.p --, C.sub.1 -C.sub.12 alkyl--C.sub.3 -C.sub.8 cycloalkyl--CH.sub.2 --(X).sub.p --, C.sub.6 -C.sub.10 aryl--X--, C.sub.7 -C.sub.20 alkaryl--X--, C.sub.7 -C.sub.12 aralkyl--(X).sub.p -- or C.sub.8 -C.sub.20 --alkaralkyl--(X).sub.p -- or --Y--(C.sub.m H.sub.2m --O)--.sub.n R.sup.10 each of which is unsubstituted or substituted by --F, --OH, --CN, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.

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: 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.

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 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: 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: Novel antibiotic herein designated as BU-3608, BU-3608 B, and BU-3608 C are produced by fermentation of Actinomadura hibisca Strain No. P157-2, ATCC 53557, and Strain No. Q278-4, ATCC 53646. The antibiotics possess antifungal and antiviral activities.

Abstract: 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.

Abstract: The present invention relates to a novel .alpha.-glucosidase inhibitor, pradimicin Q, having the following formula ##STR1## and its pharmaceutically acceptable base salts.

Abstract: The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof.Daunomycinone can be used for the preparation of daunomycin and adriamycin.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolysis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.

Abstract: 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyl-daunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound with an amine, removing the amino protecting group from the resultant 4-demethyl-4-(protected amino)-13-dioxolanyl-daunomycinone, diazotizing the thus-freed 4-amino group and reducing under mild conditions the resulting diazonium compound.

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.

Abstract: A novel physiologically active substance KS-619-1 having a vasodilative activity is produced by culturing Streptomyces californicus ATCC 3312.

Abstract: This invention relates to a process for preparing an antibiotic D788-7 wherein, after culturing carborubicin-producing bacteria, the obtained culture liquid is extracted in acidic conditions while stirring to be absorbed to synthetic resin, followed by desorption from the resin and elution with acetone and the resulting acetone solution containing carborubicin is converted into an antibiotic D788-7 by photo radiation, for obtaining D788-7 in the purified form from the reaction solution. The production yield for D788-7 is extremely high and its use as an antitumor agent can be made possible.

Abstract: Disclosed is a process for producing a 10-hydroxyanthracycline of the following formula (II) which comprises reacting a compound of the following formula (I) or an acid addition salt thereof with an N-oxide of a tertiary amine ##STR1## wherein: R.sup.1 through R.sup.6 each designate any of H, OH and OCH.sub.3 ; R.sup.7 designates any of H, OH and a sugar residue; and R.sup.8 designates any of C.sub.2 H.sub.5, COCH.sub.3, CH(OH)CH.sub.3, CH(OH)CH.sub.2 (OH) and COCH.sub.2 OH. In accordance with this process, it is possible to efficiently introduce a hydroxyl group into the 10-position of an anthracycline having no substitutent at the same position thereof.