Abstract: The invention concerns C-glycosylated derivatives of soft carbon nucleophile compounds, particularly compounds which contain acid-labile structural units. The invention further concerns a mild, cost-effective, non-hazardous and stereoselective method of general application employing a glycal as a glycosyulating agent and iodine as a catalyst for the preparation of C-glycosylated soft carbon nucleophile compounds.

Abstract: This invention is a water-soluble high molecular polymerized drug comprising a water-soluble clock copolymer having a hydrophilic segment and a hydrophobic pharmacological-functioning segment to side chain of which a drug is bonded. The hydrophilic first segments of the present invention include polyethylene glycol, polysaccharides, polyacrylamide, and so on. The hydrophobic segments being attached to a drug include polyaspartic acid, polyglutamic acid, polylysine, or derivatives thereof. Drugs to be attached to the hydrophobic segment include anti-cancer drugs, drugs for central nerve, drugs for circulatory organs, and so on.

Abstract: Anthracycline glycosides having the general formula 1 and 2: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, fluorine, hydroxy or amino; R.sub.2 and R.sub.3 represent hydroxy or one of R.sub.2 and R.sub.3 is a hydrogen atom, a nitro or an amino group and the other of R.sub.2 and R.sub.3 is a HYDROXY group, exhibit activity against LoVo and LoVo/Dx in vitro.

Abstract: The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.

Abstract: A novel composition of matter comprising a ligand-carbohydrate-cytotoxic drug conjugate is produced by the steps of (1) reacting a carbohydrate with a ligand, (2) reacting the product of step (1) with a cytotoxic drug, and (3) stabilizing the product of step (2) by reduction. The composition is used for treating a neoplastic disease by a process of administering a non-toxic, effective amount of a ligand-carbohydrate-cytotoxic drug conjugate to a human being or animal in need of such a treatment.

Abstract: Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.

Abstract: Cellulose esters of polycarboxylic acids, and their salts, such as the hydrogen cellulose ester of succinic acid, and the potassium salts thereof, are known to be useful in the preparation of conductive layers in composite such as photographic films. This invention comprises the discovery that such esters and salts provide improved conductive layers, if made from amorphous cellulose obtained by deacylating a material (such as cellulose acetate) using a lower alcohol as the deacylating agent, and an alkali metal alkoxide as the catalyst. Thus, the conductivity of potassium cellulose succinate (KCS) is improved, if made from a cellulose produced as described above. Furthermore, gelatin/KCS coating solutions made from improved KCS coating solutions of this invention have lower viscosities; this makes them much more suitable for roll coating, a support to be coated such as by a skim pan--air knife technique.

Abstract: Heterocyclic antitumor compounds are described, which are useful in the treatment of cancer and tumors in vitro, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, CNS cancer and melanoma. Pharmaceutical compositions and method of preparing the compounds are also described.

Abstract: Disclosed are novel pradimicin compounds which possess antifungal activity and, preferably, improved water solubility. The compounds of the invention are prepared by modifying the 4'-amino or 4'-alkylamino moieties of known pradimicin compounds.

Abstract: The present invention relates to intermediates, pradimic acids and pradimic acid amides of the formula (II) ##STR1## wherein R is OH or NH.sub.2 ; R.sup.1 is hydrogen or a group of the formula ##STR2## with the proviso that when R is OH, R.sup.1 is not hydrogen; Y is OH or NR.sup.2 R.sup.3 ; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen, C.sub.1-5 alkyl, or an amino protecting group; R.sup.4 is hydrogen, hydroxy protecting group, or .beta.-D-xylosyl. The invention relates also to novel processes for the preparation of pradimic acids and pradimic acid amides, as well as novel pradimicin derivatives prepared therefrom.

Abstract: This invention relates to the field of immune therapy of cancer, more specifically to immunoconjugates of a cytotoxic moiety with a targeting moiety, more specifically to immunoconjugates of antibodies or fragments or functional derivatives of antibodies coupled to a cytotoxic substance such as drugs, toxins or radioisotopes. It especially relates to the release of substances bound to a targeting moiety through the use of acid-cleavable linker molecules.

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: Disclosed are novel species of cellulose acetate butyrates and propionates that have significant surface activity. The cellulose acetate butyrate/propionate contains 9-16 wt. % butyryl or propionyl, 6-11 wt. % acetyl, and 12-15 wt. % hydroxyl.

Abstract: Benanomicin A and Benanomicin B are fermentatively produced by the cultivation of a new microorganism Actinomadura spadix, designated as MH193-16F4 strain.

Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.

Abstract: Disclosed is a method for preventing cardiotoxicity in a human in need of such preventive treatment, the method including administering an effective amount of a bisdioxopiperazine. Also disclosed is a method for preventing cardiotoxicity induced by the administration of an anthracycline. Further, a tumoricidal, cardioprotective combination of agents is disclosed.

Abstract: The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.

Abstract: A compound of the following formula (I) exhibits an excellent antitumor activity ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atom, respectively, or include both straight or branch chain alkylidene group of 1-10 carbon atoms; R.sub.3 represents hydrogen atoms, straight and branch chain alkyl group of 1-10 carbon atoms, straight or branch chain alkyloxycarbonyl group of 1-10 carbon atoms or 3-membered to 6-membered heterocycle containing one nitrogen atom with adjacent alkylene group such as pyrrolidine and N-butoxycarbonyl-pyrrolidine; R.sub.4 and R.sub.5 represent hydrogen atom or alkyl group of 1-5 carbon atoms, respectively; and n represents 0 or an integer of 1-10, or pharmaceutically acceptable salt thereof.

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: 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: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.

Abstract: The present invention relates to antitumor compounds of the formula I: ##STR1## wherein M is selected from the group consisting of an hydrogen atom, a peptide residue, and a protein residue linked to the carbon atom via the amino residue of .epsilon.-lysine present therein which can be an antibody used to target the anti-tumor agent to the malignant cells, and R can be an antitumor agent such as daunorubicin, doxorubicin, or an epirublicin derivative.

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: The present invention is a compound having the structure ##STR1##Work relating to the development of the present invention was supported by Grant CA 42708 from the National Institutes of Health, DHHS. This support gives the United States Government certain rights in the present invention .

Abstract: An aromatic derivative of butyric acid has the formula ##STR1## These aromatic derivatives of butyric acid are useful in human and veterinary medicines as well as in cosmetic compositions.

Abstract: The present invention relates to a fermentation process for producing BMY-28960 and desxylosyl BMY-28960, and to a novel BMY-28960-producing organism belonging to the genus Actinomadura and designated as strain AB 1236 (ATCC 55208).

Abstract: A compound having the structure: ##STR1## wherein R is CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, t-C.sub.4 H.sub.9 or C.sub.6 H.sub.5 ; R.sup.1 is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7).sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OC.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.2 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 CH.sub.2 Cl).sub.2.These compounds may be used to eliminate occult leukemic clonogenic cells from bone marrow by contacting the bone marrow with a solution comprising levels of said compound sufficient to eliminate occult leukemic clonogenic cells.

Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.

Abstract: The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)--C.sub.r H.sub.2r --wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.

Abstract: An improved process for the production of cellulose ester fibrets wherein a thickened slurry of the fibrets in a liquid mixture of a solvent for the fibrets and a fibret non-solvent is contacted with saturated steam in the separation of the solvent from the fibrets.

Abstract: Novel antineoplastic amine-containing derivatives and methods for synthesizing such derivatives of anthracycline antibiotics are disclosed. The derivatives are useful to anthracycline antibiotic conjugates which retain substantial immunospecificity of the unconjugated antibody molecule. Using the conjugates, targeted delivery of the attached antibiotics is achieved in vivo. Such conjugates are thus therapeutically effective against a variety of neoplastic cellular disorders when administered in vivo. Methods for preparing the antibody conjugates and for use of the conjugates in vivo are also disclosed.

Abstract: Disclosed is a novel tobacco smoke filter material comprising a filter element such as cellulose acetate crimped tow having at least about 1 weight percent of micro acicular crystals of a compound such as sodium carbonate present on the surfaces of the filter element. Also disclosed is a process for preparation of such tobacco smoke filter material comprising immersing the filter element in a solution of the compound capable of forming the micro acicular crystals, followed by removing the filter element from the solution and removing residual liquid, thereby forming the novel tobacco smoke filter material.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein X is hydroxyl group or hydrogenatom, or a salt thereof. The compound (I) has an acitivity to inhibit angiogenesis, which is useful for prophylaxis and therapy of various diseases accompanying abnormally increased angiogenesis, especially of tumors.

Abstract: Process for reducing the degree of substitution of cellulose esters employing Lewis acids as solvolysis promoters is disclosed. Novel low degree of substitution cellulose esters produced by the invention process are also described.

Abstract: The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-subhstituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the perferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.

Abstract: Anthracycline glycosides useful as antitumor agents of formula XV: ##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.

Abstract: Three'-deaminodoxorubicin esters have been found to have excellent encapsulization efficiency in liposomes and to display high antineoplastic activity. The liposomal formulations have also been found to be quite stable.

Abstract: A sealed glass container containing therein a stable, injectable, sterile, pyrogen-free doxorubicin anti-tumor composition in a solution which consists essentially of a physiologically acceptable salt of doxorubicin dissolved in a physiologically acceptable solvent therefor, wherein said solution has not been reconstructed from a lyophilizate, and wherein said solution has a pH of from 2.5-3.5 and a concentration of said doxorubicin of from 0.1 to 100 mg/ml.

Abstract: Therapeutically active organic compound exhibiting at least one group comprising a structure --S'--S"--R, wherein the group --S"--R is defined by R being an organic group comprised in a physiologically acceptable compound H--S"--R obtainable by the splitting of the disulfide bridge --S'--S"-- in said structure, in which compound H--S"--R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H--S"--R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure --S'--S"--R, consisting of a residue of a therapeutically active organic base compound of non-polypeptide structure bound to S'.

Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs, e.g. doxorubicin, in the treatment of both human and animal tumors.

Abstract: The invention relates to anthracycline conjugates comprising at least one anthracycline molecule linked to a molecule that is reactive with a cell population to be eliminated such as antibody, bombesin, EGF and transferrin. Each anthracycline molecule, having a keto group at the C-13 position, is conjugated to the antibody via a linker arm and is bound to that linker arm via an acid-sensitive acylhydrazone bond at the 13-keto position of the anthracycline. The linker additionally contains a disulfide or thioether linkage as part of the antibody or ligand attachment to the immunoconjugate. The novel anthracycline acylhydrazone derivatives are useful in the preparation of the conjugates of this invention. The acid-sensitive hydrazone bond of the conjugates of this invention allows the release of free anthracycline from the conjugates in the acidic external or internal environment of the target cell.

Abstract: Pharmaceutical compositions containing at least one of benanomicins A and B and their salts are now provided, which are useful to inhibit the infection of human T-cells with HIV, namely a virus causative of acquired human immunodeficiency syndrome (AIDS). Thus, benanomicins A and B as well as their salts are useful as antiviral agent against HIV.

Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.

Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.

Abstract: Two new antibiotics which are now nominated as benanomicin A and benanomicin B, respectively, are fermentatively produced by the cultivation of a new microorganism, designated as MH193-16F4 strain, of Actinomycetes. Benanomicins A and B each show antifungal activity and are useful as a therapeutic antifungal agent. A new compound, dexylosylbenanomicin B is now produced by chemical conversion of benanomicin B, and this semi-synthetic antibiotic also shows antifungal activity and is useful as a therapeutic antifungal agent.

Abstract: As a new compound is now provided N-acetylbenanomicin B which is useful as an antifungal agent and also as antiviral agent for inhibiting infection of human T-cell with HIV, namely a virus causative of acquired human immunodeficiency syndrome. N-acetylbenanomicin B may be prepared by acetylation of 4"-amino group of benanomicin B which is fermentatively produced by a new microorganism, MH193-16F4 strain of actinomycetes.

Abstract: A modified cellulose and/or chitin for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein cell is unmodified cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, m=0.75 to 2.85, and x=0.005 to 2.10. A process for preparation of the cellulose and/or chitin derivatives is also disclosed.

Abstract: A modified cellulose and/or chitin for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein Cell is cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, R" is H or R, Z corresponds to the following groups of atoms: SR", SO.sub.3 H and salts thereof, SO-R, SONR".sub.2, SO.sub.2 -R, SO.sub.2 NR".sub.2, SO.sub.2 H and salts thereof, F, Cl, Br, I, NR".sub.2, PR".sub.2, PO.sub.3 H.sub.2 and salts thereof, PO.sub.2 H(OR), PO(OR).sub.2, PO.sub.2 HR" and salts thereof, POR"(OR) and POR".sub.2, x+t=0.75 to 2.85, t=0 to 2.85, x=0 to 2.85, and z=0.01 to 0.45. A process for preparation of the cellulose and/or chitin derivatives is also disclosed.

Abstract: A modified cellulose and/or chitin for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein cell is cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, R" is H or R, R"' denotes R, x+t=0.75 to 2.85, t=0 to 2.85, x=0 to 2.85, and r=0 to 1. A process for preparation of the cellulose and/or chitin derivatives is also disclosed.

Abstract: A mixture of chemical substances such as optical isomers, geometrical isomers and polymers having different molecular weight ranges is separated to each ingredient by use of a cellulose derivative having an aromatic ring in the chromatographic method.