Abstract: A method of inhibiting mammalian collagenase by using .alpha.-phenyl-2-(aza)benzothiazolylthioglycolic acids and derivatives thereof, and the pharmaceutically acceptable salts thereof.

Abstract: An improved process for the preparation of .alpha.-amino-penicillins from an aqueous solution of a derivative of 6-APA and amide-type Dane salts.

Abstract: A method of inhibiting mammalian collagenase by using 3-(p-substituted phenyl)-thiazolo[3,2-a]benzimidazole-2-alkanoic acids and esters thereof, and the pharmaceutically acceptable salts thereof.

Abstract: There are disclosed polypeptides having the formula:R.sub.1 --Lys--Lys--X--R.sub.2wherein R.sub.1 is hydrogen or p-Glu; X is Glu or Asp; and R.sub.2 is Val, NH.sub.2 or Val-NH.sub.2 ; the fully protected peptide-resin intermediates thereof and pharmaceutically acceptable salts thereof. These polypeptides have the capability of inducing the maturation of T-cell populations and thus are useful in a number of therapeutic areas.

Abstract: Novel compounds of formula I ##STR1## are described wherein R is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms, R.sup.1 is hydrogen, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, lower alkoxy, halogen, formyl, phenyl, phenylalkyl or acetal [CH(OR.sup.2).sub.2 where R.sup.2 is lower alkyl, or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, Z is an anion, A is an alkylene radical having from 1 to 3 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and X is a benzothiazole, benzimidazole, benzoxazole, or phenyl radical which may be substituted and acid addition or quaternary ammonium salts of compounds wherein X is a benzimidazole radical. The compounds are used for the treatment of ulcers or hypersecretion. Treatment methods are claimed as well as pharmaceutical compositions.

Abstract: 1-alkyl-4-amino-3-(3-aminotriazolo)-1,8-naphthyridine-2-ones are antihypertensive agents.

Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, eg where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.

Abstract: There are disclosed 2,6-bis-(pyrrolopyrazinyl)pyrazines which exhibit antihypertensive activity.

Abstract: The invention relates to a pharmaceutical composition comprising an anti-ulcer effective amount of a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl, or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or lower alkoxy, R.sup.2 represents hydrogen, chlorine or trifluoromethyl and n is 1 or 2, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier.A method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula I is also disclosed. Some compounds of formula I are novel and within the scope of the invention.

Abstract: 3-Aryl-3-aryloxyalkylamines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups, and Ar.sup.1 is methylsulphinyl, methylsulphonyl- or cyano-substituted phenyl, 2- or 4-pyridyl, 2-pyrazinyl, 2-quinolinyl, 2-thienyl or 2-thiazolyl exhibit activity on the central nervous system, e.g. as antidepressants.

Abstract: Novel 2-substituted-3-hydroxythiazolo[2,3-b]thiazolium salts, the mesoionic didehydro derivatives thereof and related compounds and their use as modulators of the immune response are disclosed.

Abstract: The invention provides a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or fluorine, R.sup.2 represents hydrogen, fluorine, chlorine or trifluoromethyl, n is 1 or 2 or pharmaceutically acceptable acid addition salt thereof.Pharmaceutical compositions containing the compounds are also covered as are methods of treating ulcers or hypersecretion using the compounds. Corresponding thiocompounds, useful as intermediates, are also disclosed.

Abstract: 4-Aryl-4-aryloxypiperidines of the general formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl, Ar is phenyl optionally substituted by one or more halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro or amino groups and Ar.sup.1 is a phenyl radical optionally substituted by one or more cyano, methylsulphinyl, methylsulphonyl, lower alkoxy, trifluoromethyl, lower alkyl, lower alkenyl, halogen, nitro, amino or acylamino groups or an aromatic heterocyclic mono- or di-cyclic radical, exhibit activity on the central nervous system, e.g. as antidepressants.

Abstract: 4-Amino-2-substituted-5-pyrimidinecarboxamidoximes and carbothioamides are immunomodulatory agents useful in the treatment of immune system diseases and disorders.

Abstract: Methods for the prevention of ulcer formation and for the depression of gastric secretions by the administration of guanabenz are disclosed.

Abstract: There are disclosed polypeptides having the following formula:R-X.sub.1 -Lys-X.sub.3 -Val-X.sub.5 -R.sub.1whereinR is hydrogen, alkanoyl of 1-4 carbon atoms or aroyl of 6-10 carbon atoms;X.sub.1 is L-Arg, D-Arg or D-homoarginine;X.sub.3 is Asn, Gln or the N-substituted carboxamides thereof;X.sub.5 is L- or D-Tyr, L- or D-Phe, L- or D-Trp, L- or D-Leu, L- or D-Met, D-Met-ol-oxide or D-Phe-ol;andR.sub.1 is amino, monoalkylamino of 1-4 carbon atoms, dialkylamino of 1-4 carbon atoms, hydroxy, alkoxy of 1-4 carbon atoms, ##STR1## the fully protected peptide-resin intermediates thereof, or pharmaceutically acceptable salts thereof. These polypeptides have the capability of inducing the differentiation of T-lymphocytes and thus are useful in a number of therapeutic areas.

Abstract: There are disclosed tetrapeptides having the formula:R.sub.1 -Ser-His-Leu-R.sub.2wherein R.sub.1 is N-lower alkanoyl or N-lower alkanoylGly; R.sub.2 is NH.sub.2 or Val-NH.sub.2 ; the fully protected peptide-resin intermediates thereof and pharmaceutically acceptable salts thereof. These tetrapeptides have the capability of inducing the proliferation of T-cell populations and thus are useful in a number of therapeutic areas.

Abstract: Bestatin and its analogues are compounds capable of inducing analgesia in mammals when administered peripherally.

Abstract: There are disclosed polypeptides having the formula:R-Arg-Lys-Asp-Val-D-Ala-R.sub.1whereinR is hydrogen, alkanoyl of 1-4 carbon atoms or aroyl of 6-10 carbon atoms; andR.sub.1 is amino, monoalkylamino of 1-4 carbon atoms, dialkylamino of 1-4 carbon atoms, hydroxy, alkoxy of 1-4 carbon atoms, ##STR1## the fully protected peptide-resin intermediates thereof, or pharmaceutically acceptable salts thereof. These polypeptides have the capability of inducing the differentiation of t-lymphocytes and thus are useful in a number of therapeutic areas.

Abstract: The invention concerns the treatment of ulcers and hypersecretion in a mammal using compounds of the formula IAr--A--S--Y Iwhere Ar is phenyl, which may be substituted or cycloalkyl of 5 to 7 carbon atoms, A is saturated or unsaturated lower alkylene which may be substituted by lower alkyl, oxo or hydroxy, S is sulphur and Y is an optionally substituted pyridine, pyridinium, tetrahydropyridine or tetrahydropyridinium radical. Certain novel compounds and pharmaceutical compositions are also disclosed.