Abstract: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Oligopeptide analogs are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivitals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: A chromogenic assay is described for the identification and isolation of drug-resistant HIV protease mutants. Coversely, the assay is useful to screen for new inhibitors of HIV protease, e.g., inhibitors not affected by drug-resistance of the HIV protease. This color screening assay contains a vector comprising a regulatable promoter which controls the transcription of two adjacent structural sequences, one sequence coding for HIV protease or mutant thereof, the other sequence coding for beta-galactosidase with an amino acid substrate insert cleavable by HIV protease. A library of HIV proteases is also described and is isolated in the form of a collection of such vectors, which is a color screen vector library.

Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.

Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation product the compound 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone . This product is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Abstract: Proteins which specifically inhibit coagulation Factor Xa. The inhibitors, which do not inhibit Factor VIIa, kallikrein, trypsin, chymotrypsin, thrombin, urokinase, tissue plasminogen activator, plasmin, elastase, Factor XIa or S. aureus V8 protease, are polypeptides of 60 amino acid residues. The inhibitors may be purified from Ornithodoros moubata extract, synthesized, or produced using a recombinant DNA yeast expression system.

Abstract: Described is a new process for producing the immunosuppressant, L-682,993, a C-31 demethylated derivative of L-679,934 (FK-506), produced under fermentation conditions utilizing the new mutant microorganism Streptomyces sp. (Merck Culture Collection MA 7017) ATCC No. 55334, being a blocked second generation mutant of Streptomyces sp. (MA 6858) ATCC No. 55098. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: Disclosed is a process utilizing yeast mutants for identifying active FK-506 type immunosuppressants. The process utilizes Saccharomyces cerevisiae mutants containing an fkr1, fkr2, fkr3 mutant gene or mixture thereof, which are resistant to FK-506 but sensitive to rapamycin. These mutants can be used in a diagnostic procedure for identifying FK-506 and FK-506 type immunosuppressants and in screening assays for compounds and fermentation broths which exhibit FK-506 type immunosuppressive activity. Specifically disclosed are the new yeast mutants, Saccharomyces cerevisiae YKF093, (Merck Culture Collection No. MY 2088) ATCC No. 74055, containing an fkr3 mutant gene, Saccharomyces cerevisiae YKF 012, (Merck Culture Collection No. MY 2096) ATCC No. 74061, which contains an fkr1 mutant gene, Saccharomyces cerevisiae YFK 014, (Merck Culture Collection No. MY 2097) ATCC No. 74062 and YFK-023-17A (Merck Culture Collection No. MY 2098) ATCC No.

Abstract: Disclosed are new Aspergillus niger mutants which can be used for identifying active FK-506/ rapamycin type, or cyclosporin A type inununosuppressants in a broth, natural product extract, or composition exhibiting inununosuppressant activity. Specifically disclosed are the new mutants, ATCC No. 74085 (MF 5659), which is sensitive to FK-506 and rapamycin but resistant to cyclosporin A; ATCC No. 74086 (MF 5659) which is resistant to FK-506, cyclosporin A and rapamycin; and ATCC No. 74087 (MF 5661) which is resistant to FK-506 and rapamycin, but sensitive to cyclosporin A.

Abstract: O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylrapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.

Abstract: Imidazolidyl rapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.

Abstract: Benzalkonium chloride and benzethorium chloride are each useful in radiopharmaceutical preparations (optionally in the presence of a polymyxin or a polymyxin derivative) as bacteriostatic agents which are compatible with anti-oxidants.

Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6969) ATCC No. 55280. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 represents phenyl or thienyl, either of which groups may be optionally substituted by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl;R.sup.2 represents benzyl which may be substituted in the benzyl ring by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, S0.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a C0.sub.2 R.sup.b, --C0.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.

Abstract: Alkyl and alkenyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and derivitization at C-17. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: Alkylidene macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6971) ATCC No. 55282. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: Described are new 17.beta.-aryl ester carboxylates of 4-aza-5.alpha.-androstan-3-ones and related compounds and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenetic related disorders.