Abstract: Piperidylidene derivatives of formula ##STR1## wherein n is 2 or 3, R.sub.1 comprises a tricyclic nucleus and R.sub.2 is hydrogen or an acid residue, useful in the treatment and prophylaxis of asthmatic conditions.

Abstract: The present invention provides an improved process for the production of a compound of formula I ##STR1## wherein R.sub.1 is carboxyl, alkoxy(C.sub.1-5)carbonyl, amido, alkyl(C.sub.1-5)amido, di(alkyl(C.sub.1-5)amido or an amido radical of formula II ##STR2## wherein R.sub.a is alkyl(C.sub.1-4),R.sub.b is alkyl(C.sub.1-4) or benzyl, andR.sub.2 is hydrogen or alkyl(C.sub.1-4), andeitherR.sub.3 is hydrogen and R.sub.4 is hydrogen or alkoxy(C.sub.1-4)orR.sub.3 and R.sub.4 together are a single bond,characterized in that a compound of formula III ##STR3## wherein R.sub.1 to R.sub.4 are as defined above,is brominated with a bromine complex of 3-bromo-6-chloro-2-methyl-imidazo[1,2-b]pyridazine.

Abstract: A 2-alkyl-9,10-dioxy-4,5,5a,6-tetrahydro-dibenz[cd,f]indole or an acid addition salt thereof is a useful anti-parkinson agent.

Abstract: This invention relates to a composition and method for potentiating the antidepressant effect of dibenzocycloheptadiene-type antidepressant agents, for example, nortriptyline, in the treatment of depression, especially geriatric depression, by administering them in combination with an approximately 1:1:1 by weight mixture of dihydroergocryptine (2:1 .alpha.:.beta.), dihydroergocornine and dihydroergocristine.

Abstract: This disclosure relates to substituted indolamines, which exhibit anti-diabetic activity, having the formula: ##STR1## where m is an integer from 1 to 4,x represents hydrogen or --OHR represents Ar or ##STR2## and Ar represents ##STR3## R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, R.sub.2 and R.sub.3 each, independently, represent lower alkyl, orR.sub.2 and R.sub.3 together with N represent ##STR4## wherein n is 1, 2 or 3,R.sub.4 represents hydrogen or lower alkyl, andR.sub.5 represents hydrogen or lower alkyl, unsubstituted phenyl or phenyl substituted with fluoro, chloro, lower alkyl or lower alkoxy, oror pharmaceutically acceptable acid addition salts thereof.

Abstract: Compounds of formula I ##STR1## wherein n=1 to 5 possessing analgesic activity with reduced hepatoxicity as compared with paracetamol.

Abstract: A 6- and/or 7-oxy-trans-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline in which the 3-position is substituted by an optionally amidated carboxy group, an optionally etherified hydroxymethyl group, a cyanomethyl group, an alkyl- or aryl-thiomethyl group or a sulfamoylamino or carbamoylamino group, or a physiologically-hydrolysable and -acceptable ester thereof. The subject compounds are useful as pharmaceuticals, in particular as prolactin secretion inhibitors, dopaminergic agents ad dopamine receptor stimulating agents.

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: A 2-methyl-8 (R) or (S) ergot peptide alkaloid in free base form or in pharmaceutically acceptable acid addition salt form is a useful anti-Parkinson agent, prolactin secretion inhibitor, anti-depressant, vigilance-increasing agent, and anti-migraine agent.

Abstract: This disclosure relates to the aspermatogenesis activity of(a) compounds of the formula: ##STR1## where m is an integer from 1 to 4X represents hydrogen or --OHR represents Ar, ##STR2## Ar represents ##STR3## R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, R.sub.2 and R.sub.3 each, independently, represent lower alkyl, orR.sub.2 and R.sub.3 together with N represent ##STR4## wherein n is 1, 2 or 3,R.sub.4 represents hydrogen or lower alkyl, andR.sub.5 represents hydrogen or lower alkyl, unsubstituted phenyl or phenyl mono- or di-substituted with fluoro, chloro, lower alkyl or lower alkoxy, or(b) compounds of the formula: ##STR5## where R' is Ar or ##STR6## Ar, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, or a pharmaceutically acceptable acid addition salt thereof.

Abstract: 9-Thia ergot cyclic peptide alkaloids produced by fermentation or synthetic methods have interesting anti-parkinson and other pharmacological activities.

Abstract: This disclosure describes novel compounds of the formula ##STR1## where m is 2, 3 or 4X is hydrogen or hydroxyR.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 represents hydrogen or lower alkyl as defined above, andR.sub.5 represents hydrogen, lower alkyl, phenyl or phenyl substituted with fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, with the proviso that when X is hydroxy, m is 3 or 4,or a pharmaceutically acceptable acid addition salt thereof, which are useful in the treatment of diabetes by inhibiting or impeding post-prandial hyperglycemia.

Abstract: This disclosure relates to the aspermatogenesis activity of compounds of the following formula: ##STR1## where R.sub.1 and R.sub.2 each independently represent hydrogen, halo having an atomic weight of about 19 to 36, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms, trifluoromethyl, orR.sub.1 is ##STR2## and R.sub.2 is hydrogen, whereinR.sub.7 and R.sub.8 are each independently hydrogen or lower alkyl having 1 to 2 carbon atoms,n is 0 or 1, andR.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent lower alkyl having 1 to 2 carbon atoms ora pharmaceutically acceptable salt thereof.

Abstract: The invention concerns a process for the isomerization of ergoline derivatives substituted in the 8.beta. position by an electron withdrawing radical to the corresponding 8.alpha. compounds by removal of the proton in the 8.alpha. position and by a following, separately effected, protonation.

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: Straight-chain or mono-cyclicpolypeptides comprising a heptapeptide moiety, said moiety having in the 1-position (N-terminal) an .alpha.-N-phenylalkylated, optionally ring-substituted phenylalanine residue, in the 2-position a cysteine residue, in the 3-position an optionally ring-substituted phenylalanine residue, in the 4-position an optionally benzene-ring-substituted tryptophan residue, in the 5-position an optionally .epsilon.-N-alkylated lysine residue and in the 7-position (C-terminal) a cysteine or cysteinol residue the S-atoms of the cysteine residue at the 2-position and the cysteine or cysteinol residue at the 7-position being linked together in the case of the mono-cyclic polypeptides to form an -S-S-bridge, whereby the residues at the 1-, 2-, 4-, 6-, and 7-positions of said heptapeptide moiety may each be in the (L)- or (D)-configuration and the residues at the 4-, 5- and 6-positions of said heptapeptide moiety may each be optionally .alpha.

Abstract: A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.

Abstract: The antibiotics S 54832/A-I, S 54832/A-II, S 54832/A-III and S 54832/A-IV are obtained from a new Micromonospora globosa strain.

Abstract: Pharmaceutical compositions comprising as the active ingredient thereof an aminopyridazine derivative of the formula: ##STR1## wherein R.sub.1 is amino, or ##STR2## wherein each of R.sub.3 and R.sub.4 is alkyl of 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the carbon atom to which they are bound, form a cycloalkylidene radical of 5 to 12 carbon atoms,R.sub.2 is hydrogen or methyl,A is --(CH.sub.2).sub.n --, wherein n is 0 or an integer from 1 to 7, or >N--CO--R.sub.5, wherein R.sub.5 is alkyl of 1 to 16 carbon atoms, alkenyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, 1-adamantyl, or --(CH.sub.2).sub.m --R.sub.6, whereinm is 0 or an integer from 1 to 4, andR.sub.

Abstract: 9,9-Dimethyl-6,7-benzomorphan derivatives having an oxygen-containing substituent on the nitrogen atom, optionally an alkyl or phenyl 5-substituent and optionally a hydroxy, alkoxy or acyloxy 2'-substituent have analgetic and/or morphine-antagonist properties.