Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is ##STR1## n is 1-2; B is ##STR2## wherein R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro; ##STR3## R.sup.8 is lower alkyl; m is 0-3;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated nasobronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.

Abstract: A derivative of rapamycin in which the 27-position has the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl, or --CH.sub.2 Ar;Ar is ##STR2## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;X is N, O, or S;or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydroxy, lower alkoxy or lower alkoxyamino;R.sup.1 is hydrogen or A(CH.sub.2).sub.n O--;R.sup.2 is hydrogen or A(CH.sub.2).sub.n O--, with the proviso that one of R.sup.1 and R.sup.2 is A(CH.sub.2).sub.n O-- and the other is hydrogen;n is 1-2;A is phenoxyethyl, phenoxyphenyl or a group having the formula ##STR2## X is --N-- or ##STR3## Z is ##STR4## R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is hydrogen or lower alkyl; orR.sup.3 and R.sup.4 taken together form a benzene ring;R.sup.5 is hydrogen or lower alkyl;R.sup.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a trifluoromethoxy substituent in the 5-, 6-, 7-, or 8-position, and methods for their preparation and use, are disclosed. The derivatives are useful anti-inflammatory and analgesic agents.

Abstract: There is disclosed the compound 2-[4-[4-(2,7-naphthyridin-1-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3( 2H)-one 1,1-dioxide, and the method of producing said compound, and the pharmaceutically acceptable salts thereof, and the use of said compound as an anxiolytic agent having a low liability for extrapyramidal side effects.

Abstract: Process for the production of substituted 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid having useful analgesic and anti-inflammatory activity.

Abstract: N-[2-(dimethylamino)ethyl]-N'-[3-[3-[(1-piperidinyl)methyl]phenoxy]-propyl] -1,2,5-thiadiazole-3,4-diamine, 1-oxide is a long acting histamine H-2 receptor antagonist. The compound inhibits gastric acid secretion, and prevents and alleviates ulcers.

Abstract: The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

Abstract: The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucelus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

Abstract: The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or pheny(lower) alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

Abstract: The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano-[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

Abstract: Pyridylmethyl esters of N-(phenoxyalkanoyl)peptide derivatives are disclosed. The derivatives are characterized by having a phenoxyalkanoyl group and a pyridylmethyloxy group-joined together by a peptide group. They possess antihyperlipoproteinemic activity. In addition, methods for their preparation and use are disclosed.

Abstract: The tripeptide derivatives of formula 1H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

Abstract: .alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.

Abstract: Salts of phenoxyisobutyric acids with amino acid pyridylmethyl esters are disclosed. The salts possess antihyperlipoproteinemic activity. In addition, methods for their preparation and use, as well as pharmaceutical compositions thereof, are disclosed.

Abstract: There are disclosed herein derivatives of imidazolidin-2-ones and -2-thiones of the formula I ##SPC1##and their acid addition salts with pharmacologically acceptable acids, in which R.sup.1 is hydrogen or lower alkyl; R.sup.2 is lower alkyl, nitrothiazolyl, or nitrofuryl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached are a heterocyclic group containing 4-6 carbon atoms, or 4 carbon atoms and an additional nitrogen atom which may optionally be substituted with a lower alkyl group, or 4 carbon atoms and an oxygen atom, R.sup.3 is hydrogen or lower alkyl; R.sup.4 is lower alkyl or aralkyl, or R.sup.3 and R.sup.4 together with the carbon atom 5 of the imidazolidine ring to which they are attached are a carbocyclic ring containing 5-6 carbon atoms attached in spiro fashion to said imidazolidine ring; R.sup.5 is lower alkyl or cycloalkyl containing from 5-6 carbon atoms; and X is an oxygen or a sulfur atom.

Abstract: The tripeptide derivatives of formulaH--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R' is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, .Iadd.and with the further proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen or lower alkyl and Y is Gly then R.sup.3 is amino(lower)alkylamino, .Iaddend.and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.