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7244829 Compositions and processes for preparing 13-deoxy-anthracyclines  
13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines...
7067504 Di-steroidal prodrugs of ethinyl estradiol  
The present invention is a di-steroidal prodrug of ethinyl estradiol according to formula I:
7067505 Di-steroidal prodrugs of estradiol  
The present invention is a di-steroidal prodrug of estradiol having the following formula:
6159931 Lipid-modified insulin incorporated liposomes for selectively delivering cytotoxic agents to hepatoma cells  
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...
6028207 Bone resorption inhibition/osteogenesis promotion compound  
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...
5998615 Anthracyclinone derivatives  
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...
5945518 Process for the preparation of anthracycline antibiotics  
A process for the preparation of antibiotics of the anthracycline class of formula (A), wherein R 1 is hydrogen, OH, or OCOR 2 , wherein R 2 is a C 1 -C 4 -alkyl group; which comprises the...
5877158 Pro-prodrugs, their production and use  
Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.
5874412 Bis-anthracyclines with high activity against doxorubicin resistant tumors  
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....
5814608 S-fluoro-anthracyclines, processes for their preparation and pharmaceutical compositions containing them  
8-fluoro-anthracyclines of formula (I) have anti-tumor activity. ##STR1## wherein: R is chosen in the group consisting of H, OH, OR 4 wherein R 4 is chosen in the group consisting of CHO, COCH 3...
5646177 Glutathione derivatives of anthracyclines  
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...
5606037 Processes antineoplastic heteronaphthoquinones  
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...
5594158 Processes for producing doxorubicin, daunomycinone, and derivatives of doxorubicin  
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...
5510501 Saintopin derivatives  
The present invention relates to Saintopin derivatives represented by the following formula (I): ##STR1## wherein R 1 is hydrogen and R 2 is SO 2 OH (UCE 1022), or R 1 is acetyl and R 2 is H...
5488119 Polymerisable photochromic naphthacenediones, polymers of these monomers, process for their preparation and the use thereof  
Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R 1 to R 4 are H or a substituent such as phenylthio, and one of the substituents R 1 , R 2 , R 3 and R 4 ...
5407885 Photochromic naphthacenequinones, process for their preparation and the use thereof  
Compounds of formula I or V or mixtures thereof ##STR1## wherein R is unsubstituted C 6 -C 14 aryl or C 6 -C 14 aryl which is substituted by C 1 -C 12 alkyl, C 1 -C 12 alkoxy, C 1 -C 12 ...
5391749 Substituted naphthacene-5,12-diones and their use  
Substituted naphthacenediones of the formula I ##STR1## in which R 1 to R 8 are H and at least one of R 1 to R 8 , for example R 2 and R 3 or R 2 and R 6 , are, for example, C 1 -C 20 ...
5366966 Compound UCE6  
A compound represented by formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is provided, which has an excellent antitumor activity.
5294701 Anthracycline compounds and intermediates  
This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R 1 and R 2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally...
5218130 4-substituted anthracyclinones and their preparation  
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...
5206390 Substituted bisacyloxynaphthacenes  
Compounds of the formula I ##STR1## in which R 1 to R 8 independently of one another are H and at least one of R 1 to R 8 is a substituent belonging to the group --F, --Si(C 1 -C 4 alkyl) 3 ...
5180758 Process for preparing anthracyclinones  
4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR 1 group in which R 1 may be a hydrogen atom or an optionally substituted C 1 -C 10 ...
5110960 Antifungal antibiotics  
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...
5103029 Process for preparing 4-demethoxydaunomycinone  
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,...
5091418 Novel alpha-glucosidase inhibitor, pradimicin Q  
The present invention relates to a novel α-glucosidase inhibitor, pradimicin Q, having the following formula ##STR1## and its pharmaceutically acceptable base salts.
5079349 Trimethylsilyl acetylene compounds, their preparation and their use in the preparation of daunomycinone derivatives  
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...
5015745 Process for the preparation of 4-demethoxydaunomycinone, the aglycone of 4-demethoxy-daunorubicin  
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,...
5001243 Substituted naphthacene-5, 12-diones  
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...
4962125 Novel substance KS-619-1, preparation process and pharmaceutical composition  
A novel physiologically active substance KS-619-1 having a vasodilative activity is produced by culturing Streptomyces californicus ATCC 3312.
4954438 Process for preparing antibiotics D788-7  
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...
4877870 Process for producing 10-hydroxyanthracyclines  
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...
4822873 Carminomycinone precurses and analogues  
A compound of formula II and tautomeric forms thereof wherein: R 1 -R 4 are H, alkyl, aryl, alkaryl, halogen, hydroxy, alkoxy, aryloxy, aralkoxy, acyloxy, amino or alkylamino: R 8 has the...
4749693 Nitro anthracyclines, process for their preparation and use thereof  
Anthracycline glycosides of the general formula (A'): ##STR1## wherein R 1 represents a hydrogen atom, a hydroxy group or a methoxy group; one of R 2 and R 3 represents a hydroxy group and the...
4739062 Method of producing paraquinones  
A new widely-applicable method has been found for synthesis of 9,10-anthraquinones and similar chemical compounds of wide use in industry and pharmacology, by reacting suitable aromatic substrates...
4697005 1-fluoro, 4-fluoro, and 1,4-difluoro anthracycline anticancer antibiotics  
Compounds represented by the formula (I) ##STR1## wherein R is hydrogen or hydroxyl, one of X and Y is fluorine and the other is hydrogen or both X and Y are fluorine, and Su is a hydrogen atom or...
4613464 Process for the preparation of anthracyclinones  
The present invention relates to a new process for the preparation of anthracyclinones of the formula ##STR1## in which R denotes C 1 -C 4 -alkyl, R 1 denotes H or OH, and R 2 and R 3 are...
4610986 Aminonaphthacene derivatives and their production  
A (7S,9S) isomer or its racemic modification of the aminonaphthacene derivative of the formula: ##STR1## wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a...
4600537 Preparation of (±) 4-demethoxy-6 (and-11-)-deoxydaunomycinone  
(±)4-demethoxy-6(and-11-)-deoxydaunomycinone which are starting materials for anthracycline antitumor antibiotics are prepared by reacting 1,2,3,6-tetrahydrophthalic anhydride with an alcohol of...
4591636 Anthracycline glycosides  
The invention relates to compounds of the formula ##STR1## wherein R is lower alkyl or a carboxy group or a group of the formula --(CH 2 ) n --OY a in...
4564674 Process for an anthracycline derivative, and an anthracyclinone derivative useful for the process  
A process for producing an anthracycline derivative represented by the general formula: ##STR1## where R 1 is an acyl group, each of X 1 and X 2 is a hydrogen atom, a methoxy group, a hydroxyl...
4545936 Novel aminonaphthacene derivatives and process for preparation thereof  
An aminonaphthacene derivative of the formula: ##STR1## wherein R 1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R 2 is a hydrogen atom or a hydroxyl group, R 3 is a hydrogen...
4537882 4-Demethoxy-3'-desamino-2'-halo-anthracycline and pharmaceutical composition containing same  
Compounds of the formula (I), acid addition salts thereof, and pharmaceutical preparations containing the same are disclosed ##STR1## wherein R 1 is hydroxy; one of X and X' is hydrogen and the...
4536336 New anthracyclinones and their production  
A new compound of the formula ##STR1## wherein R 1 is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R 2 is an ethyl group or acetyl group is now provided, which is...
4522815 Anthracycline glycosides  
Disclosed is a process for preparing the glycoside antitumor anthracyclines 7-0-(2,6-dideoxy-α-L-arabino-hexopyranosyl)-daunomycinone (Ia);...
4518784 Cyclic compounds  
There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R 1 and R 2 represents a hydrogen atom and the other represents...
4515720 Method of synthesizing a late-stage intermediate to 11-deoxydaunorubicin and 11-deoxyadriamycin, and two precursors to the object intermediate  
Preparation of 9-acetyl-6-hydroxy-4-methoxy-7,8,9,10-tetrahydronaphthacene- 5,12-dione (the object intermediate), and precursor compounds to the object intermediate. Preparation of the object...
4501699 Maggiemycin, anhydromaggiemycin and processes for making  
New anthracyclinones, including maggiemycin, anhydromaggiemycin and 7-oxidodaunorubicinone, have been prepared. Maggiemycin, anhydromaggiemycin, and 7-oxidodaunorubicinone all exhibit biological...
4501700 Preparation of optically active 4-demethoxydaunomycinone  
A process for preparing racemic 4-demethoxy-7-deoxydaunomycinone which comprises methylating an optically active α-hydroxyketone to give the corresponding methylated product of either one of the...
4496485 Asymmetric 7-O-(substituted acetyl)-4-demethoxydaunomycinones  
This invention relates to novel diastereomeric 7-O-(substituted acetyl)-4-demethoxydaunomycinones that are useful in the preparation of optically pure 4-demethoxydaunorubicin, a drug used in the...
4489206 Synthesis of (+)-4-demethoxydaunomycinone  
It has been found that stereospecific R(-)-4-demethoxy-7-deoxydaunomycinone can be synthesized from the known compound 4-demethoxy-7,9-dideoxydaunomycinone. R(-)-4-Demethoxy-7-deoxy-daunomycinone...
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