Abstract: The present invention is directed to the use of compounds of Formula (I), as active principals for treating skin conditions and compositions containing these compounds wherein R4 is (CR5R6-CR7R81-X1)n-CR9R10R11; n is an integer from 1 to 18; R1, R2, R3, R5, R6, R7, R8, R9, R10 and R11, are independently, herein defined and X, X1, Y and Z are independently, 0, NH or S.

Abstract: The present invention relates to new pyranoside derivatives of general formula I, processes for preparing them as well as their use as medicaments:

Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).

Abstract: Polymeric prodrugs of the formula: 1

Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.

Abstract: This invention relates to a biocidal composition resistant to the formation of a gel and to the method for stabilizing a concentrate containing, in addition to the biocide, a carbodiimide in monomeric or polymeric form or a mixture thereof and a lipophilic/hydrophilic emulsifier mixture having a HLB of at least 7 comprising an oil and an alkoxylated ester of a polyhydroxylated compound, by adding to the concentrate between about 0.5 and about 15 wt. % of a saturated, aliphatic compound having a molecular weight of less than 400, selected from the group consisting of a polyhydroxyated alkanol and/or a polyhydroxylated ketone.

Abstract: Compounds that prolong thrombin time. Exemplary are: (a) rac-4-{3-[5-ethoxycarbonylmethyl-2-methyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, (b) rac-4-{3-[2,5-dimethyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, and (c) 4-[3-(2,5-dimethyl-4-isopropylcarbonyl-phenyl)propargyl-amino]benzamidine.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Abstract: Novel compounds of the formula I in which X, R1, R2, R3, R4 and R5 have the meaning indicated in Patent Claim 1, are inhibitors of the coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: The present invention is a biphenylamidine derivative represented by the formula (1) or a pharmaceutically acceptable derivative thereof: and the biphenylamidine derivative or the pharmaceutically acceptable derivative thereof is a novel compound which can be used as a clinically applicable FXa inhibitor.

Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.

Abstract: The present invention is directed to the use of compounds of Formula (I), as active principals for treating skin conditions and compositions containing these compounds; wherein R4 is (CR5R6—CR7R8—X1)n—CR9R10R11, n is an integer from 1 to 18; R1, R2, R3, R5, R6, R7, R8, R9, R10 and R11, are independently, hydrogen or non-hydrogen substituents; and X, X1, Y and Z are independently NH.

Abstract: Compounds represented by formula I: or a pharmaceutically acceptable salt or hydrate thereof, are disclosed. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.

Abstract: The present invention relates to a new LTB4 antagonist, processes for the preparation thereof and its use as a pharmaceutical composition.

Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the indexes have the meanings given in the specification, their salts, their preparation and their use.

Abstract: The compound of the above formula wherein R1-R5 are independently selected from hydrogen, alkyl and aryl and prodrugs thereof; and pharmaceutically acceptable salts thereof; and use of the compounds in therapy, particularly for treatment of a condition generally associated with abnormalities in glutamtergic transmission.

Abstract: Novel benzamidines, having LTB4-antagonistic activity, of the formula methods for their preparation, their and their use as medicaments.

Abstract: The present invention relates to a method for inhibiting the etiology of disease in patients having a disease state caused by an excess of 12-lipoxygenase or its products. In particular, the invention provides for administration of a human leukocyte 12-lipoxygenase pathway inhibitor to inhibit disease etiology, to inhibit the proliferation of breast cancer and to increase insulin receptor phosphorylation in a patient having Type II diabetics.

Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: A method for controlling ectoparasites systemically through host animal blood which comprises administering at least one neonocotinoid compound among those defined in the specification to the host animal.

Abstract: Provided is a pharmaceutical composition comprising a tablet or capsule containing a pharmacologically effective amount of a pharmaceutical compound, or a pharmaceutically acceptable salt thereof, having an amidine-based group and an optional ester group, a pharmaceutically acceptable solid carrier, and a pharmaceutically acceptable acid in an amount to modify the pH of the composition to substantially that of the compound at pH of maximum stability.Such a composition is prepared by adding water during formulation manufacture and contacting the compound during formulation manufacture with a pharmaceutically acceptable acid having a pH in a saturated aqueous solution substantially that of the compound at pH of maximum stability.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions.

Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: This invention relates to compounds having serotonin receptor binding activity and to their medical use, particularly in the treatment of CNS conditions such as migraine. Described herein are compounds which have the general formula: ##STR1## wherein R.sup.1 is selected from a group of Formula i and ii: ##STR2## n is 1-3; R.sup.2 is selected from H and C.sub.1-6 alkyl;R.sup.3 is selected from H and C.sub.1-6 alkyl;R.sup.4 is selected from C.sub.1-6 alkyl, halo, phenyl, amino and nitro;R.sup.5 is selected from H, C.sub.1-6 alkyl and arylalkyl;R.sup.6 is selected from H or a alkylene group which is bonded to R.sup.4 to form the naphthalene ring skeleton; and salts, hydrates and solvates thereof.

Abstract: The present invention relates to methods and compositions useful for treating and preventing conditions in which inhibition of nitric oxide synthetase is beneficial. These conditions include stroke, schizophrenia, anxiety, and pain.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: This invention provides a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.3 independently are hydrogen, --CHO, --COCH.sub.3, --COR.sup.7, --A--Ar--(Q).sub.z, etc.; wherein D is a C.sub.1-6 linear, C.sub.3-8 branched or cyclic group having from 4 to about 15 atoms, consisting of C, etc.; wherein D is unsubstituted or substituted with one or more groups independently selected from the group consisting of --OH, NH.sub.2, --NHR.sub.7, etc.; wherein each Q is independently --CNH(NHY), --NHCNH(NHY), --SO.sub.2 W, --SOW, etc.; wherein Y is hydrogen, alkyl, alkenyl, --B--NH.sub.2, --B--NHR.sup.8, etc.; wherein W is alkyl, alkenyl, --B--NH.sub.2, etc.; wherein A nd B independently are a bond, or a C.sub.1-6 linear, C.sub.3-8 branched or cyclic linking group having from 1 to about 15 atoms, consisting of C, optionally interrupted by N, S, P and O; wherein A and B independently are unsubstituted or substituted with --OH, NH.sub.2, etc.; wherein R.sup.7 is an alkyl, a branched alkyl, etc.; wherein R.sup.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.

Abstract: A compound which inhibits human thrombin and which has the general structure ##STR1##

Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.

Abstract: A class of acetamidine derivatives of general formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR.sup.3 wherein X is oxygen, C(O).sub.m wherein m is 1 or 2, S(O).sub.n wherein n is 0, 1 or 2, or a group NR.sup.4 wherein R.sup.4 is hydrogen or C.sub.1-6 alkyl; and R.sup.3 is hydrogen, C.sub.1-6 alkyl, or a group NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl, provided that R.sup.3 is not NR.sup.5 R.sup.6 when X is oxygen or S(O).sub.n; R.sup.1a and R.sup.1b are independently selected from hydrogen and halo; R.sup.2 is a C.sub.1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R.sup.2 being optionally substituted by one or more groups independently selected from halo; N.sub.3 ; nitro; CF.sub.3 ; ZR.sup.7 wherein Z is oxygen, C(O).sub.m' wherein m' is 1 or 2, S(O).sub.n' wherein n' is 0, 1 or 2, or a group NR.sup.8 wherein R.sup.

Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The current invention discloses amidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: Amidine derivative compounds of formula I as defined in the Specification having nitric oxide synthetase inhibitory activity as well as processes for the preparation of and compositions containing said compounds are described.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: Bi-aromatic compounds are provided along with methods for their preparation and use.

Abstract: The invention comprises a composition of matter containing a matrix, a plasticizer and pyriproxifen for controlling fleas.

Abstract: Compounds of formula ##STR1## and their therapeutic use, inter alia, as LTB.sub.4 -antagonists. Exemplary compounds are:(Methoxycarbonyl-imino-{4'-?2-(2-propylphenoxy)-ethoxy!-biphenyl-4-yl}-meth yl)-amine;(Benzyloxycarbonyl-imino-{4'-?2-(2-propylphenoxy)-ethoxy!-biphenyl-4-yl}-me thyl-amine;?Hydroxy-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!-benzoyloxy} phenyl)-methyl!-amine;?Ethoxycarbonyl-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!-benz oyloxy}phenyl)-methyl!-amine; and,?3'-Pyridylcarbonyl-imino-(4-{3-?4-(1-methyl-1-phenylethyl)-phenoxymethyl!- benzyloxy}phenyl)-methyl!-amine.

Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.

Abstract: There are provided novel compounds of formula I ##STR1## wherein D, R.sup.1, R.sup.2, R.sup.3, X and p are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy.Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

Abstract: A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or R