Abstract: The current invention is based on the determination that a S1P receptor modulator compound of formula (I): decreases the heart rate of a subject to which it is administered by about 5 beats/min or less daily, or about 4 beats/min or less daily, or about 3 beats/min or less daily, or about 2 beats/min or less daily, wherein the S1P receptor modulator is administered at an initial daily dosage which is substantially the same as the standard daily therapeutic dosage.

Abstract: Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.

Abstract: Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.

Abstract: Compounds of the formulas ##STR1## wherein R.sup.1 is H and R.sup.2 is alkyl (3-8C) or wherein R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.n -- wherein n=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is a substituted or unsubstituted fused or conjugated bicycloaryl methylene;X is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amineare useful for treating or preventing ulceration of tissue, especially cornea.

Abstract: Compounds of the formulas ##STR1## wherein each R.sup.1 is independently H or alkyl (1-8C) and R.sup.2 is alkyl (1-8C) or wherein the proximal R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.p -- wherein p=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is fused or conjugated unsubstituted or substituted bicycloaryl methylene;n is 0, 1 or 2;m is 0 or 1; andx is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amine;Y is selected from the group consisting of R.sup.7 ONR.sup.6 CONR.sup.6 -, R.sup.6.sub.2 NCONOR.sup.7 -, and R.sup.6 CONOR.sup.7 -, wherein each R.sup.6 is independently H or lower alkyl (1-4C); R.sup.7 is lower alkyl (1-4C) or an acyl group; andwherein --CONR.sup.3 -- is optionally in modified isoteric form are inhibitors of matrix metalloproteases.

Abstract: Compounds of the formulas ##STR1## wherein each R.sup.1 is independently H or alkyl (1-8C) and R.sup.2 is alkyl (1-8C) or wherein the proximal R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.p -- wherein p=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is fused or conjugated unsubstituted or substituted bicycloaryl methylene;n is 0, 1 or 2;m is 0 or 1; andX is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amine;wherein R.sup.6 is H or lower alkyl (1-4C) and R.sup.7 is H, lower alkyl (1-4C) or an acyl group, and wherein --CONR.sup.3 -- is optionally in modified isosteric formare useful for treating conditions which are characterized by unwanted matrix metalloprotease activities.

Abstract: Compounds of the formulas ##STR1## wherein R.sup.1 is H and R.sup.2 is alkyl (3-8C) or wherein R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.n -- wherein n=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is a substituted or unsubstituted fused or conjugated bicycloaryl methylene;X is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amineare useful for treating conditions which are characterized by unwanted matrix metalloprotease activities.

Abstract: Compounds of the formulas ##STR1## wherein R.sup.1 is H and R.sup.2 is alkyl (3-8C) or wherein R.sup.1 and R.sup.2 taken together are --(CH.sub.2).sub.n -- wherein n=3-5;R.sup.3 is H or alkyl (1-4C);R.sup.4 is a substituted or unsubstituted fused or conjugated bicycloaryl methylene;X is OR.sup.5 or NHR.sup.5, wherein R.sup.5 is H or substituted or unsubstituted alkyl (1-12C), aryl (6-12C), aryl alkyl (6-16C); orX is an amino acid residue or amide thereof; orX is the residue of a cyclic amine or heterocyclic amineare useful for treating or preventing ulceration of tissue, especially cornea.

Abstract: This invention relates to amino acid derivatives that are useful as inhibitors of bacterial collagenase. The compounds of this invention have a general formula: ##STR1## wherein R is alkyl, aralkyl, aryl, alkoxy, aryloxy, hydroxy or pharmaceutically acceptable salts thereof; R.sub.1 is hydrogen, alkali metal, lower alkyl, phenyl lower alkyl, or phenyl, or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl or nitro or carboxy or cyano, and pharmaceutically acceptable salts thereof; R.sub.2, R.sub.3 and R.sub.4 is hydrogen or alkyl; R.sub.2 and R.sub.4 may be the side groups found on the 20 common .alpha.-amino acids; R.sub.3 and R.sub.4 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms; Y is alkoxy, aryloxy, primary amide, amino acid derivative or ##STR2## where R.sub.5 and R.sub.6 is hydrogen or alkyl; R.sub.5 and R.sub.

Abstract: The present invention relates to the compounds having the following general formula (1) ##STR1## where: X is a halogen atomQ is a formyl or nitrile (cyano) groupY is a hydroxyl, alkoxyl, alkyl or nitro group"m" is the number of Y substituents 0 or 1"n" equals 1-20U and T are methyl radicals or hydrogen atoms acting strongly towards pathogenic fungi, especially of the Alternaria and Botrytis genera.

Abstract: A parasiticide containing as an active ingredient the compound with the general formula 1, where:X is a halogen atom,Y is a hydroxyl, alkoxyl, alkyl or nitro group and "n" is the number of Y substituents and equals 0-4,R.sup.1 is an alkyl radical with 1-3 carbon atoms or hydrogen atom,R.sup.2 and R.sup.3 are alkyl or hydroxyalkyl radicals with 1-4 carbon atoms,R.sup.4 is an alkyl radical with 1-18 carbon atomsorR.sup.2 and R.sup.3 together with the nitrogen atom form a ring substituted as in formula 2, where:W is a methylene group or an oxygen atom,U and T are methyl radicals or hydrogen atoms,Z is a hydrogen atomorT and Z together are an oxygen atom.The agent containing an active compound with the general formula 1, where the substituents have the above meaning has strong fungicidal activity towards pathogenic fungi and bacteria, among which are fungi from the Alternaria genus.

Abstract: A parasiticide containing as an active ingredient the compound with the general formula ##STR1## where: X is a halogen atom,Y is a hydroxyl, alkoxyl, alkyl or nitro group and "n" is the number of Y substituents and equals 0-4,R.sup.1 is an alkyl radical with 1-3 carbon atoms or hydrogen atom,R.sup.2 and R.sup.3 are alkyl or hydroxyalkyl radicals with 1-4 carbon atoms,R.sup.4 is an alkyl radical with 1-18 carbon atomsorR.sup.2 and R.sup.3 together with the nitrogen atom form a ring substituted as in formula ##STR2## where: W is a methylene group or an oxygen atom,U and T are methyl radicals or hydrogen atoms,Z is a hydrogen atomorT and Z together are an oxygen atom.The agent containing an active compound with the general formula 1, where the substituents have the above meaning has strong fungicidal activity towards pathogenic fungi and bacteria, among which are fungi from the Alternaria genus.