Abstract: Compounds of formula IIA and IIB are novel guanidine compounds 1

Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.

Abstract: Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided.

Abstract: Process for the coupling of

Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.

Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: Compounds of the formula I: 1

Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.

Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: Compounds of the formula I: 1

Abstract: This invention provides compounds of formula I having the structure Wherein substitutions at X, G, R1, R2, R3, R4, R5 are set forth in the specification.

Abstract: A compound of the formula is disclosed, the compound being suited for therapeutical uses. The invention also discloses compositions comprising said compound, methods of treatment involving administering said compound to a patient, and the use of said compound in the manufacture of medicaments.

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.

Abstract: The invention relates to compounds of the formula I 1

Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Abstract: The present invention relates to compounds according to the structure: Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3 , CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80° C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.

Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.

Abstract: The present invention relates to compounds of the general formula 1

Abstract: The present invention relates to a class of compounds represented by the Formula I.

Abstract: Compounds of the formula Useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, humanherpesviruses-6 and -7, and Kaposi herpesvirus.

Abstract: Compounds of the formula I  in which A is ═N— or R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1-C4alkyl, C1-C4haloalkyl, halogen, R6O—, nitro, amino or cyano; W is a group  or  and R3, R6, R14 to R24 and X3 to X9 have the meanings given in claim 1 and the agrochemically tolerated salts and stereoisomers of these compounds of the formula I are suitable for use as herbicides.

Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.

Abstract: This invention is directed to benzamidine 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 relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, ca

Abstract: Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.

Abstract: 4-Aminopicolinic acids, having halogen, alkoxy, alkylthio, aryloxy, heteroaryloxy or trifluoromethyl substituents in the 3-, 5- and 6-positions, and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.

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

Abstract: A cyanoguanidine compound of the following formula: is disclosed. A cyanoguanidine compound of the present invention possess a high specificity for tumor cells. Also disclosed are methods for preparing a cyanoguanidine compound.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Pyridine derivatives of the formula I and their salts, their preparation, and their use for controlling animal pests and harmful fungi.

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: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl nitro, amino, cyano, carboxy, or alkyl, alkoxy, or alkoxycarbonyl, the C-content of which can be from 1 to 4; X stands for a straight or branched C9-C20 carbon chain, saturated or unsaturated or Q—Ar—R; in which formula Ar stands for phenyl, Q stands for a C5-C20 divalent hydrocarbon radical which can be straight, branched, saturated or unsaturated and R stands for hydrogen or for one or more substituents which can be the same or different and are selected from the group consisting of: hydroxy, amino, halogen, trifluoromethyl, cyano, nitro, carboxy, carbamoyl, or alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 4; and p

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: 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: 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: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R.sub.1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C.sub.1 -C.sub.4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C.sub.9 -C.sub.20 divalent hydrocarbon radical which can be saturated, straight or branched or Q stands for C.sub.4 -C.sub.20 divalent hydrocarbon radical which can be cyclic or unsaturated and X stands for oxygen, sulfur or nitrogen the latter optionally being substituted by hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C.sub.1 -C.sub.

Abstract: This invention relates to a compound of the formula: ##STR1## wherein A.sup.1 is lower alkylene,R.sup.1 is substituted quinolyl, etc.,R.sup.2 is hydrogen, halogen or lower alkyl,R.sup.3 is halogen or lower alkyl, andR.sup.4 is a group of the formula:--Q--A.sup.2 --R.sup.5, etc.,in whichR.sup.5 is amino, acylamino, etc.,A.sup.2 is lower alkylene or a single bond, andQ is a group of the formula: ##STR2## etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group; n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.

Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.17, R.sup.18 and R.sup.1 are as defined below. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

Abstract: The invention provides novel sulphonylurea, sulphonylthiourea and sulphonylguanidine compounds which have the ability to block potassium ion channels regulated by intracellular concentrations of ATP. Methods of synthesis, pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes, cardiac arrhythmias, ischaemic and hypoxic cardiovascular incidents, and cancers are also claimed.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.

Abstract: Substituted 2-acylaminopyridine compounds and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.