Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.

Abstract: The present invention relates to a group of compounds which are novel squalene derivatives containing the cyclopropyloxy functionality and which act to inhibit the synthesis of cholesterol in mammals and in fungi.

Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.

Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.

Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.

Abstract: The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.

Abstract: Novel nonaromatic fluoroallylamines are potent MAO inhibitors and at low dose selectively inhibit MAO-B. They are useful in the treatment of depression and co-administration with L-dopa and decarboxylase inhibitors, in the treatment of Parkinsonism.

Abstract: 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Methods of preparing the compounds and derivatives are also described.

Abstract: 1. A compound of the formula:H.sub.2 C.dbd.C.dbd.CHCH.sub.2 NHCH.sub.2 --Z--CH.sub.2 NHRwherein:Z is --CH.sub.2 CH.sub.2 -- or trans--CH.dbd.CH--,R is H, CH.sub.3 --, CH.sub.3 CH.sub.2, CH.sub.3 (CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 NH.sub.2, --(CH.sub.2).sub.3 NHCOCH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or --CH.sub.2 CH.dbd.C.dbd.CH.sub.2, or a pharmaceutically acceptable acid addition salt thereof are inhibitors of polyamine oxidase.

Abstract: 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Methods of preparing the compounds and derivatives are also described.

Abstract: Novel nonaromatic fluoroallylamines are potent MAO inhibitors and at low dose selectively inhibit MAO-B. They are useful in the treatment of depression and coadministered with L-dopa, in the treatment of Parkinsonism.

Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.

Abstract: 1. A compound of the formula:H.sub.2 C.dbd.C.dbd.CHCH.sub.2 NHCH.sub.2 --Z--CH.sub.2 NHRwherein:Z is --CH.sub.2 CH.sub.2 -- or trans-CH.dbd.CH--,R is H, CH.sub.3 --, CH.sub.3 CH.sub.2, CH.sub.3 (CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 NH.sub.2, --(CH.sub.2).sub.3 NHCOCH.sub.3, --CH.sub.2 CH.dbd.CH.sub.2, or --CH.sub.2 CH.dbd.C.dbd.CH.sub.2,or a pharmaceutically acceptable acid addition salt thereof are inhibitors of polyamine oxidase.

Abstract: A novel method of treating psoriasis which comprises administering a halomethyl derivative of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is FCH.sub.2 --, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .gamma.-guanidinopropyl or R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy; a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms, or ##STR3## wherein R.sub.

Abstract: Compounds of the formula ##STR1## wherein: R is phenyl, phenyl monosubstituted, disubstituted, or trisubstituted by (C.sub.1 -C.sub.8) alkyl, (C.sub.1 -C.sub.8)alkoxy, hydroxy, chlorine, bromine, iodine, fluorine, trifluoromethyl, nitro, (C.sub.1 -C.sub.6)alkylcarbonyl, benzoyl, or phenyl; 1-, or 2-naphthyl; 1-, 2-, or 3-indenyl; 1-, 2-, or 9-fluorenyl; 1-, 2-, or 3-piperidinyl; 2- or 3-pyrrolyl; 2- or 3-thienyl; 2- or 3-furanyl; 2- or 3- indolyl; 2- or 3-thianaphthenyl; or 2- or 3-benzofuranyl;R.sub.1 is hydrogen, (C.sub.1 -C.sub.8)alkyl, benzyl, or phenethyl;X and Y independently, are hydrogen, fluorine, chlorine, or bromine; andA is a divalent radical of the formula: ##STR2## wherein R.sub.2 is hydrogen, methyl, or ethyl, and m and n, independently, are an integer from 0 to 4, provided that m+n cannot be greater than 4; --(CH.sub.2).sub.p --D--(CH.sub.2).sub.

Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.

Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: wherein Y is ClCH.sub.2, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR1## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.

Abstract: Fluorinated diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl), or R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydrogen, or, except when R.sub.2 represents R.sub.4, R.sub.4, where R.sub.4 is as defined below;each R.sub.4, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from the carboxy moiety of an L-aminocarboxylic acid; andp represents 1 or 2,and pharmaceutically acceptable acid addition salts thereof.

Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.

Abstract: This invention relates to 2-(difluoromethyl)-2,5-diaminopentanoic acid, or a pharmaceutically acceptable acid addition salt thereof, and to the methods for the preparation and use thereof.