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 MA6970) ATCC No. 55281. 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: A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.

Abstract: Described is a new immunosuppressant, L-683,519, a monodemethylated rearranged derivative of L-679,934, (FK-506) produced under fermentation conditions utilizing the microorganism, unidentified Actinomycete (Merck Culture Collection MA 6474) ATCC No. 53828. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: A human urinary metabolite of Losartan has been isolated and identified as structure I. ##STR1## This compound is an active angiotensin II receptor antagonist useful in the treatment of hypertension and congestive heart failure.

Abstract: A human urinary metabolite of Losartan has been isolated and identified as Structure I: ##STR1## This compound is an active angiotensin II receptor antagonist useful in the treatment of hypertension and congestive heart failure.

Abstract: A pharmaceutical composition comprising a non-peptide type angiotension II receptor antagonist is useful for the treatment of hyperuricemia.

Abstract: The present invention provides pyrazines, pyridazines or pyrimidines, or salts or prodrugs thereof, substituted on one of the ring carbon atoms thereof with a non-aromatic azacyclic or azabicyclic ring system; and independently substituted on each of the other ring carbon atoms with a substituent of low lipophilicity or a hydrocarbon substituent; which compounds stimulate central muscarinic acetylcholine receptors and therefore are useful in the treatment of neurological and mental illnesses.

Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.

Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;the dotted line represents an optional double bond;X represents H, --OH, .dbd.O or halo;R.sup.1 represents H, phenyl or thienyl, which phenyl or thienyl groups may be optionally substituted by halo or trifluoromethyl;R.sup.2 represents phenyl, thienyl or benzyl, any of which groups may be optionally substituted by halo or trifluoromethyl; 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, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.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: A class of 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridine and 2,3,4,4a,5,6,7,11b-octahydro-1H-benzo[3,4]cyclohepta[1,2-c]pyridine derivatives are selective ligands at sigma recognition sites and are therefore useful in the treatment and/or prevention of psychiatric and/or gastrointestinal disorders.

Abstract: A class of 4-hydroxy-2(1H)-quinolone derivatives, substituted at the 3-position by an N-linked heteroaromatic ring system, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and or AMPA receptor antagonist.

Abstract: Described is a new immunosuppressant, L-683,756, a bisdemethylated, ring rearranged derivative of L-683,590, produced 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: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.

Abstract: Derivatives of synthetic fragments of mammalian atrial natriuretic factor (ANF) in which a chelate molecule is attached to the N-terminal of the peptide are described. The chelate component allows the facile labelling of these peptides with metallic isotopes such as Tc-99m, Ga-67, In-111 and others. These radioactive chelates are useful in determining the in vivo behavior and fate of derivatives of ANF.

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 and R.sup.2 independently represent phenyl or thienyl, either of which groups may be optionally substituted by halo or trifluoromethyl;R.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, SO.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;R.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl,are tachykinin antagonists. They and compositions thereof are therefore useful in therapy.

Abstract: A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring and on the other ring carbon atom with a substituent which is convertible in vivo to an amino group, are potent muscarinic agonists, and exhibit improved CNS penetrability and duration of action compared with the corresponding amino compounds. The compounds are therefore useful in the treatment of neurological and mental illnesses.

Abstract: Novel substituted quinazolinones of the formula (I), which are useful as angiotensin II antagonists, are disclosed.

Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors.

Abstract: An intermediate, useful in the conversion of FK-506 to FK-525 and analogous 23-membered ring macrolides, of the structure: ##STR1##

Abstract: A class of 1,2,3,4-tetrahydroquinolines possessing at least one substituent, or a spirocyclic moiety, at the 4-position, and an acidic group or a group convertible thereto in vivo at the 2-position, are specific antagonists of N-methyl-D-aspartate (NMDA) receptors and are therefore useful in the treatment and/or prevention of neurodegenerative disorders.