Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl;. . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.0 or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.

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: 1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system.

Abstract: A class of spirocyclic piperidine derivatives are selective ligands at sigma recognition sites and are therefore useful in the treatment and/or prevention of psychiatric disorders. The claimed compounds are of the formula ##STR1## wherein, A and B are hydrogen, Q is a bond, R.sup.11, R.sup.12, and R.sup.13 are as defined in the specification.

Abstract: A class of indole-substituted five-membered heteroaromatic compounds are specific agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: Impinging fluid jet streams are used in a continuous crystallization process to achieve high intensity micromixing of fluids so as to form a homogeneous composition prior to the start of nucleation. This process permits direct crystallization of high surface area particles of high purity and stability.

Abstract: A process for preparing a single enantiomer of a 4-aryloxyazetidin-2-one derivative in optically pure form comprises reacting a hindered vinyl ester with chlorosulphonyl isocyanate; displacing the hindered acyloxy group with a phenolic derivative containing a protected carboxy group; deprotecting the carboxylate moiety; resolving with a chiral amine; filtering; and regenerating the desired enantiomer by acidification. A method for enriching the product obtained from the acyloxy displacement step in favour of the desired enantiomeric form, by treating with an asymmetric catalyst such as a chiral alkaloid derivative, is provided; as also is a method for racemising the unwanted antipode of the desired 4-aryloxyazetidin-2-one enantiomer. The invention further provides novel enantiomers based on the 4-aryloxyazetidin-2-one ring structure.

Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## R.sup.1 is H, certain optionally substituted alkyl or C.sub.3-7 cycloalkyl;R.sup.2 represents (CH.sub.2).sub.m -tetrazolyl, (CH.sub.2).sub.m -imidazolyl, CONR.sup.6 R.sup.7, CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9, SOC.sub.1-4 alkyl, SO.sub.2 NHR.sup.10, 5-hydroxy-4-pyrone, (CH.sub.2).sub.n CO.sub.2 H, ##STR2## or a group ##STR3## wherein X is O, S or NR.sup.11 ; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.12 ;R.sup.3 represents H or C.sub.1-6 alkyl;R.sup.4 represents 2-, 3- or 4-pyridyl;R.sup.5 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists useful in therapy.

Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: A class of 1,2,3,4,4a,5,6,10b-octahydrobenz[f]isoquinoline compounds and pharmaceutically acceptable salts of formula I: ##STR1## wherein, R.sup.1 represents hydrocarbon;R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, halogen, cyano, trifluoromethyl, nitro, --OR.sup.x, --SR.sup.x, --NR.sup.x R.sup.y, --CO.sub.2 R.sup.x or together represent methylenedioxy; andR.sup.x and R.sup.y independently represent hydrogen or hydrocarbon.The compounds disclosed herein are selective ligands at sigma recognition sites and are therefore useful in the treatment of psychiatric disorders.

Abstract: Macrocyclic compounds of general Structure I: ##STR1## Wherein M is C or N are angiotensin II receptor (A-II) antagonists useful in the treatment of certain cardiovascular dysfunctions and ocular hypertension.

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: Described is a process for producing an immunosuppressant, "demethimmunomycin" (L-683,7411) a C-31 demethylated analog of L-683,590 under fermentation conditions utilizing the microorganism, Actinoplanacete sp, (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow 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: 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.

Abstract: Described is a new process for producing the immunosuppressant, L-683,742, a C-31 demethylated, derivative of L-683,590 (FK-520), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: Described is a process for producing a new immunosuppressant, L-682,992, a C-13, C-31 demethylated ring-rearranged analog of L-679,934, under novel fermentation conditions utilizing the microorganism, Actinoplanacete Sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: 4-Oxo-1,4-dihydroquinoline compounds having a 2-acidic group or a group convertible thereto in vivo, and their pharmaceutically acceptable salts, are potent specific antagonists of N-methyl-D-aspartate (NMDA) receptors and are therefore useful in the treatment of neurodegenerative disorders. 4-Oxo-1,4-dihydroquinoline compounds having a 2-acidic group or a group convertible thereto in vivo, other than carboxy or C.sub.1-6 alkoxycarbonyl, are novel compounds, as also are compounds of formula II ##STR1## wherein R.sup.2 represents carboxy or a group convertible thereto in vivo, R.sup.6 is hydrogen and R.sup.5 and R.sup.7 represent C.sub.1-6 alkyl or halogen, provided that R.sup.5 and R.sup.7 are not simultaneously chlorine or simultaneously bromine; a process for preparing the novel compounds is described, as also are pharmaceutical compositions containing the novel compounds.

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 MA6968) ATCC No. 55279. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.