Abstract: Heterocyclic compounds of Formula I: ##STR1## in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R.sup.4); Y and Z are independently C(O), C(S) or CH.sub.2 (provided that Y and Z are not both CH.sub.2); R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis.

Abstract: The invention is directed to an improved process for the preparation of spirocyclic lactams which utilizes diiodides in the spiro alkylation of lactams N-substituted with a tertiary amine group. The resultant spirocyclic lactams are useful in the production of various substituted azaspiranes which are useful as immunomodulatory agents.

Abstract: Purified preparations of PMPA are provided, together with analytical methods for the detection of undesired contaminants in PMPA preparations. The PMPA compositions of the invention are of particular utility in therapeutics intended for the treatment or prophylaxis of viral infections.

Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 represents a phenyl, C.sub.3-7 cycloalkyl, C.sub.7-11 bridgedcycloalkyl or C.sub.1-6 alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C.sub.1-6 alkoxycarbonyl, C.sub.3-7 cycloalkyl, or C.sub.3-7 bridgedcycloalkyl group;R.sup.2 represents phenyl substituted by a group (CH.sub.2).sub.n NR.sup.4 R.sup.5, O(CH.sub.2).sub.p R.sup.6, or (CH.sub.2).sub.n CO.sub.2 R.sup.11 ;R.sup.3 represents phenyl optionally substituted by one or 2 halogen atoms;R.sup.4 represents hydrogen or C.sub.1-4 alkyl;R.sup.5 represents acyl, or C.sub.2-4 alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C.sub.1-4 alkyl or hydroxy groups.R.sup.6 represents hydroxy, C.sub.1-4 alkoxy, CO.sub.2 R.sup.7 or NR.

Abstract: Immunomodulatory macrocyclic compounds having the formula: ##STR1## and pharmaceutically-acceptable salts, esters, amides and prodrugs thereof, as well as pharmaceutical compositions containing the same, which possess immunosuppressive, antimicrobial, antifungal, antiviral, antiinflammatory and antiproliferative activity, as well as the ability to reverse chemotherapeutic drug resistance.

Abstract: A process for preparing triethylenediamine by passing an ethanolamine, ethyleneamine, piperaziHe or morpholine over a pentasil-type zeolite at elevated temperature characterized by employing a ZSM-5 zeolite in the hydrogen or ammonium form which has been pretreated with an aqueous caustic solution.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Compounds of formula (I) ##STR1## wherein the substituents are defined in the specification are antagonists of gastrin and CCK.

Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Process for the preparation of .epsilon.-caprolactam starting from an aldehyde compound comprising at least one member from among 5-formylvaleric acid, ester or amide in which the aldehyde compound is allowed to react in the presence of ammonia and hydrogen and a subsequent cyclization of the reaction products thus formed (.epsilon.-caprolactam-precursors) to .epsilon.-caprolactam is performed in the presence of water, involved the combination of steps(a) contacting the 5-formylvaleric acid, ester or amide with ammonia and water under non-hydrogenation conditions,(b) contacting the resulting mixture of step (a) with hydrogen in the presence of ammonia under hydrogenation conditions, wherein the water content is greater than 10 wt. %,(c) heating the resulting mixture of step (b) at a temperature between 200.degree. and 350.degree. C. in order to convert the reaction products of step (b) to .epsilon.-caprolactam.

Abstract: Caprolactam and hexamethylenediamine are prepared simultaneously starting from adiponitrile by a process in which(a) adiponitrile is partially hydrogenated to give a mixture containing essentially 6-aminocapronitrile, hexamethylenediamine, ammonia, adiponitrile and hexamethyleneimine,(b) the mixture obtained in (a) is subjected to a distillation to give ammonia as the top product and a bottom product I,(c) the bottom product I containing essentially 6-aminocapronitrile, hexamethylenediamine, adiponitrile, hexamethyleneimine, inert compound A and ammonia, the ammonia content being lower than that of the mixture used in stage (b), is subjected to a second distillation to give a mixture comprising the inert compound A and ammonia as the top product and a bottom product II,(d) the bottom product II is subjected, in a third column, to a distillation to give the inert compound A as the top product and a bottom product III,(e) the bottom product III is subjected, in a fourth column, to a distillation to give a top p

Abstract: Muscarinic M.sub.2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.

Abstract: A compound of formula (I) is obtainable by the cultivation of a genus Streptomyces, such as Streptomyces NCIMB 40515. in the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent as an anticancer agent, or in the treatment of microbial infections in animals including humans.

Abstract: Benz?b!azepine compounds, pharmaceutical compositions containing them and methods for the treatment of neurological disorders utilizing them.

Abstract: Compounds of the formula I, ##STR1## are NMDA antagonists and useful in the treatment and prevention of nervous system related pathological conditions resulting from overstimulation by excitatory amino acids. Methods for their preparation and pharmaceutical compositions containing them are also comprised according to the invention.

Abstract: Immunomodulatory macrocyclic compounds having the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is selected from one of the formulae ##STR2## as well as pharmaceutical compositions containing the same.

Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.

Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.

Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Disclosed are novel 8-arylalkyl-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines. These are useful in the treatment of HIV-1 infection.