Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.

Abstract: The novel antitumor antibiotics designated stephacidin A and stephacidin B are produced by fermentation of Aspergillus ochraceus ATCC-74432. The antibiotics inhibit the growth of mammalian tumors, including particularly prostate carcinoma.

Abstract: Provided by the present invention are cephem derivatives represented by the general formula wherein Ar is an optionally substituted lipophilic phenyl, naphthyl or pyridyl group; L1 and L2 are (C1-C6)alkylene optionally substituted with hydroxy or oxo and/or optionally interrupted with a vinylene group, S, O, aryl, heteroaryl, in which R1 is H or (C1-C6)alkyl; A is CO2H, PO3H, SO3H, tetrazolyl or x′{circle around (−)} is a pharmaceutically acceptable anion; and Q is an quaternized nitrogen group. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.

Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

Abstract: A high drug load enteric coated pharmaceutical composition is provided which includes a core comprised of a medicament which is sensitive to a low pH environment of less than 3, such as ddl, which composition is preferably in the form of beadlets having an enteric coating formed of methacrylic acid copolymer, plasticizer and an additional coat comprising an anti-adherent. The so-called beadlets have excellent resistance to disintegration at pH less than 3 but have excellent drug release properties at pH greater than 4.5. A novel method of making said pharmaceutical composition is also disclosed.

Abstract: Provided are very highly water soluble, stable, crystalline salts of 2′,3′-dideoxy-2′,3′-didehydrothymidine (“d4T”), 2′,3′-dideoxyinosine (“ddI”), and 2′,3′-dideoxy-2′-fluoroinosine (“F-ddI”). Such salts are useful as intermediates or as antiviral agents.

Abstract: The 5,6-dihydronaphthalenyl derivatives of the formulae possess potent retinoid-like activity against dermatological diseases with a substantially reduced irritancy profile when administered topically.

Abstract: Disclosed is a process for the synthesis of .beta.-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process.

Abstract: Novel suppository pharmaceutical formulations of the platinum antitumor agent, JM216, are provided. Such dosage forms provide an alternative to the oral form currently available and offer improved bioavailability of this promising drug.

Abstract: The present invention provides the crystalline bisulfate salt of the formula ##STR1## which is found to have unexpectedly high solubility/dissolution rate and oral bioavailability relative to the free base form of this azapeptide HIV protease inhibitor compound.

Abstract: The present invention relates to a compound of the formula ##STR1## wherein X is --CONH-- or --NHCO--, or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.The compounds of the present invention exhibit retinoid-like properties and are thus useful as antiinflammatory agents for chronic skin inflammatory diseases such as psoriasis and atopic dermatitis, as agents for the treatment of rheumatic diseases such as rheumatoid arthritis, as antitumor agents for the treatment of various tumors, and as agents for the treatment of non-malignant proliferative skin conditions.

Abstract: A novel class of antibiotics, designated bravomicins, is obtained by fermentation of a strain of Micromonospora polytrota. Six bioactive compounds, designated bravomicins A, B, C, D, E and F, are obtained and found to be useful in the treatment of a wide variety of bacterial diseases.

Abstract: Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.

Abstract: The present invention relates to the novel antitumor antibiotic designated BMS-199687 and to its preparation. The compound is obtained by culturing a new strain of Actinomadura ferruginea. BMS-199687 demonstrates antitumor activity in standard antitumor animal model systems.

Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH=CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.C is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl.

Abstract: This invention provides a novel series of taxane derivatives which are characterized by the C3' nitrogen bearing one or two sulfur substituents. The new derivatives are antitumor agents useful in the treatment of such cancers as ovarian, breast, lung, gastric, colon, head and neck, melanoma and leukemia.

Abstract: The present invention relates to the novel antitumor antibiotic designated BMS-199687 and to its preparation. The compound is obtained by culturing a new strain of Actinomadura ferruginea. BMS-199687 demonstrates antitumor activity in standard antitumor animal model systems.

Abstract: The cephalosporin intermediates, desacetyl 7-glutaryl ACA and desacetyl cephalosporin D, are obtained in the form of a concentrated aqueous solution from an aqueous solution containing said intermediates in less concentrated form by solvent extraction using cyclohexanone followed by back-extraction into water. The concentrated aqueous solution of intermediate is in a form which can be used for economical production of 7-ACA using known procedures.