Abstract: A method for the prophylaxis of inflammatory, degenerative or proliferative arterial disease which method comprises administering an effective amount of endralazine.

Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, orR.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.4 and R.sub.5 each independently represent hydrogen or lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.

Abstract: The present invention provides a nasal or pulmonary pharmaceutical composition comprising as active agent a compound of formula I, ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms,either (i)R.sub.3 is isopropyl, sec-butyl, or isobutyl,R.sub.4 methyl, ethyl or isopropyl andR.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxyor R.sub.5 and R.sub.6 are together a single bond,or (ii)R.sub.3 is benzyl, R.sub.4 is methyl, R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy, or (III) dihydroergocristine,in association with a pharmaceutically acceptable carrier or diluent, adapted for nasal or pulmonary administration.

Abstract: The invention provides polypeptides of formula I,A--B--Gly--D--E IwhereinA is Tyr or substituted Tyr,B is --Gly-- or --(D)Ala--,D is, for example, Phe or MePheand E is, for example, --Met--X, --Leu--X,--Nle--X, --Nva--X, --Ile--X, methioninesulphoxide--X, methioninesulphone--X wherein X is --NR'R" or --OR'" and each of R', R" and R'" independently signifies hydrogen or alkyl of 1 to 5 carbon atoms,which compounds possess pharmacological activity, for example, analgesic activity.

Abstract: N-Acyl-polypeptides comprising the basic sequence ##STR1## wherein "Acyl" is the acyl residue of an organic or inorganic acid; A is H or alkyl; >N--CH(Z)--CO-- and E are the residues of natural .alpha.-amino acids or corresponding (D)-amino acids; C is --Trp-- or --(D)Trp--; F is a terminal grouping; and Y.sub.1 and Y.sub.2 are each H or together are a direct bond; as well as their salt forms and complexes.

Abstract: Novel pleuromutilin derivatives of formula I, ##STR1## in which R.sub.1 is ethyl or vinyl,m is 0 or 1, andR.sub.2 is a heterocyclic radical, in which a 5- or 6-membered, unsaturated or saturated heterocyclic ring containing one or more hetero atoms selected from oxygen, sulphur and nitrogen, is attached to the --S(CH.sub.2).sub.m --group,provided that when m is 0, R.sub.2 is other than pyridyl,their production and use as antimicrobial agents are described.

Abstract: 6,7-Benzomorphan derivatives of formula I, ##STR1## wherein R.sub.1 is hydrogen; optionally hydroxy- and/or alkoxy-substituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkylalkyl; alkenyloxyalkyl, aralkyl, arylhydroxyalkyl, aralkenyl or tetrahydrofurylalkyl; or optionally alkyl-substituted furylalkyl or isoxazolylalkyl, R.sub.2 is hydrogen or methyl, R.sub.3 is hydrogen, alkyl, alkenyl, alkynyl, aralkyl, hydroxyalkyl of alkoxyalkyl and R.sub.4 is hydrogen, hydroxy, alkoxy or alkenyloxy, hydroxy groups in said compounds being each optionally acylated, having analgesic and luteinising hormone secretion inhibiting properties.

Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, orR.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.4 and R.sub.5 each independently represent hydrogen or lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.

Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 represents hydroxy, andR.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, orR.sub.3 and R.sub.4 together with N represent ##STR2## wherein n is 1, 2 or 3, andR.sub.5 and R.sub.6 each independently represent hydrogen or lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents, in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.

Abstract: This disclosure describes compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 represents lower alkyl or ##STR2## where R.sub.5 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, andR.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, andR.sub.3 and R.sub.4 together with N represent ##STR3## or pharmaceutically acceptable acid addition salts thereof, which are useful as anti-diabetic agents.

Abstract: Compounds of formula I ##STR1## wherein (i) m is O, n is 2 and p is 1 or(ii) m is 0 or 1, n is 1, and p is 1 or(iii) m is 1, n is 1 or 2 and p is 0,R.sub.1 is (i) alkyl of 3 to 7 carbon atoms or (ii) phenylalkyl, phenoxyalkyl or phenylthioalkyl of 8 to 11 carbon atoms in the aggregate thereof and wherein the phenyl ring is separated by at least 2 carbon atoms from the nitrogen atom to which R.sub.1 is bound and wherein the phenyl ring is unsubstituted, or mono-substituted by, or independently disubstituted by, alkyl or alkoxy of 1 to 4 carbon atoms, halogen of atomic number from 9 to 35, trifluoromethyl or cyano,R.sub.2 and R.sub.3 are either together straight chain alkylene of 4 to 6 carbon atoms, or, independently, hydrogen or alkyl of 1 to 4 carbon atoms, with the proviso that when m is 1, n is 1 and p is 0 then at least one of R.sub.2 and R.sub.3 is other than hydrogen, andR.sub.4 and R.sub.5 are, independently, hydrogen or alkyl of 1 to 4 carbon atoms, are useful in the treatment of coronary disorders.

Abstract: An optically active or racemic 2-amino-5-hydroxy-1,2,3,4-tetrahydronaphthalene wherein the nitrogen atom of the amino group carrier two alkyl groups, one of which is unsubstituted and the other is substituted by at least one functional group, or a physiologically hydrolysable ester thereof in free base form or in the form of an acid addition salt thereof is provided which is active against heart circulatory disorders and Morbus Parkinson and inhibits prolactin secretion inhibition.

Abstract: 6,7-Benzomorphan derivatives of formula I, ##STR1## wherein R.sub.1 is hydrogen; optionally hydroxy- and/or alkoxy-substituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkylalkyl; alkenyloxyalkyl, aralkyl, arylhydroxyalkyl, aralkenyl or tetrahydrofurylalkyl; or optionally alkyl-substituted furylalkyl or isoxazolylalkyl, R.sub.2 is hydrogen or methyl, R.sub.3 is hydrogen, alkyl, alkenyl, alkynyl, aralkyl, hydroxyalkyl of alkoxyalkyl and R.sub.4 is hydrogen, hydroxy, alkoxy or alkenyloxy, hydroxy groups in said compounds being each optionally acylated, having analgesic and luteinising hormone secretion inhibiting properties.

Abstract: Pentapeptides of formula I, ##STR1## wherein Z.sup.1 =H, CH.sub.3 or amidino; R.sub.1 =H or alkyl and R.sub.2 =H or R.sub.1 +R.sub.2 =--CH.sub.2 --CH.sub.2 --; R.sub.3 =m- or p--OH or -alkoxy; B=residue of a (D)-.alpha.-amino acid; R.sub.4 =H or alkyl; Z.sup.2 =optionally substituted phenyl; and E=.beta.-amino alcohol residue (whereby when Z.sup.1 =H or CH.sub.3, R.sub.4 =C.sub.3-4 -alkyl) as well as their esters and the acid addition salts and complexes of such peptides and esters. Compounds according to the invention have valuable pharmacological, in particular LH-secretion inhibiting activity.

Abstract: This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, andR.sub.2 represents hydroxy, andR.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, orR.sub.3 and R.sub.4 together with N represent ##STR2## wherein n is 1, 2, or 3, andR.sub.5 and R.sub.6 each independently represent hydrogen or lower alkyl as defined above, andR.sub.7 represents lower alkyl as defined above,or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents, in particular as hypoglycemic agents and inhibiting or impeding postprandial hyperglycemia.

Abstract: A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.

Abstract: Straight-chain and mono-cyclic polypeptides containing the basic sequence ##STR1## wherein X is an amino acid residue, the residues in the 1- and 6-positions being linked by an --S--S-- bridge when the polypeptide is monocyclic, have pharmacological, in particular GH--, gastric- and pancreatic-secretion inhibiting activity.

Abstract: Novel cyclosporins having an -Allylgly- residue in the 2-position and/or a -(D)-Ser- residue in the 8-position and process for their production. The novel cyclosporins are useful as pharmaceuticals, e.g. as immunosuppressive and anti-inflammatory agents.

Abstract: A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition salt thereof is a useful cardiotonic agent and vasodilator in heart insufficiency and a blood platelet aggregation inhibitor.

Abstract: A stable ergot alkaloid soft gelatin capsule consisting essentially of a soft gelatin capsule shell and encapsulated therein a liquid center fill solution consisting essentially of a therapeutically effective amount of an ergot alkaloid of the formula ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydrogen or C.sub.1-4 alkyl,R.sub.3 is isopropyl, sec.-butyl, isobutyl or benzyl,R.sub.4 is methyl, ethyl or isopropyl, and eitherR.sub.5 is hydrogen andR.sub.6 is hydrogen or methoxy orR.sub.5 and R.sub.6 together is an additional bond,or mixtures thereof, dissolved in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent.