Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

Abstract: The present invention relates to triazolylmethyloxiranes of the formula I in which the variables A, B and D have the meanings described in the claims and the description.

Abstract: The present invention relates to triazolylmethyloxiranes of the formula I in which the variables D and B have the meanings as defined in the description and the claims.

Abstract: A urea-urethane compound having one or more urea groups and one or more urethane groups in the molecular structure, the number of said urea groups (A) and the number of said urethane groups (B) satisfying the following numerical formula: 10?(A+B)?3 wherein each of A and B is an integer of 1 or more.

Abstract: The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.

Abstract: The invention provides compounds of formula 1,

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group.

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme.

Abstract: Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

Abstract: Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

Abstract: A process for the attachment of aromatic or heteroaromatic rings to a polymeric support via a silyl ether linkage is described. Such process involves the synthesis of a chlorodialkyl aryl or heteroarylsilane which is then coupled to a polymeric support via a hydroxyl functionality to form a polymer-bound silyl ether. Further modification provides a polymer-bound small organic molecule that is cleaved from the polymeric support under mild conditions to give an aryl or heteroaryl silanol or a compound in which the aryl or heteroaryl carbon-silicon bond is replaced with a carbon-hydrogen, carbon-halogen, carbon-hydroxyl, carbon-sulfur, or carbon—carbon bond. Such methods are useful for the preparation of a library of diverse aromatic and heteroaromatic compounds by both manual and automated synthesis.

Abstract: The present invention relates to novel compounds useful for the treatment and prophylaxis of degenerative bone disorders and to the preparation thereof. These compounds are particularly characterized by two active moieties, the first of which possesses "bone-seeking" affinity and the second which is an inhibition of the enzyme carbonic anhydrase and/or an inhibitor of bone resorption. The novel compounds of this invention can be administered as pharmaceutically acceptable compositions and in convenient dosage unit form in a method for the treatment and prophylaxis of degenerative bone disorders.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.

Abstract: CCK modulators, e.g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.

Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.

Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinR.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, fluoroC.sub.1-6 alkyl, C.sub.1-6 alkoxy, --CHO, --CO.sub.2 H or --COR.sup.2 ;Ar represents the group ##STR2## Het represents an N-linked imidazolyl group optionally substituted by one, two or three substituents.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Abstract: A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.

Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.

Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.

Abstract: This invention provides novel tetrazole intermediates of the formula ##STR1## wherein R.sup.1 and R.sup.4 each are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl;R.sup.2,R.sup.3,R.sup.5 and R.sup.6 each are independently hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;B is hydrogen, C.sub.1-4 alkoxycarbonyl, CH.sub.2 Y or CH.sub.2 Z;Y is hydrogen, hydroxyl or X;Z is ##STR2## X is bromo, chloro or iodo; R.sup.10 is C.sub.1-4 alkyl; andR.sup.11 is phenyl which is unsubstituted or substituted by one or two C.sub.1-4 alkyl or chloro substituents.and processes thereof which are useful for the preparation of antihypercholesterolemic agents.

Abstract: This invention provides novel intermediates of the formula ##STR1## in substantially the cis or cis-(4R,6S) form wherein R.sup.9 and R.sup.10 each are C.sub.1-4 alkyl or R.sup.9 and R.sup.10, taken together with the carbon atom to which they are attached, is cyclopentyl, cyclohexyl or cycloheptyl; andR.sup.12 is hydrogen, C.sub.1-4 alkyl or a metal cationand processes thereof which are useful for the preparation of antihypercholesterolemic agents.

Abstract: New reaction products, useful as additives for functional fluids, are obtained by reacting, at elevated temperature,(A) a triazole having the formula IA or IB: ##STR1## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.20 alkyl residue;R.sub.8 and R.sub.9 are the same or different and each is C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.20 alkenyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.7 -C.sub.13 aralkyl, C.sub.6 -C.sub.10 aryl or R.sub.8 and R.sub.9, together with the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic residue or R.sub.8 and R.sub.9 is each a residue of formula:R.sub.12 X[(alkylene)O].sub.n (alkylene)-- IIwherein X is O, S or N(R.sub.12), R.sub.12 is hydrogen or C.sub.1 -C.sub.20 alkyl, "alkylene" is a C.sub.1 -C.sub.12 alkylene residue and n is 0 or an integer from 1 to 6;R.sub.10 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.18 alkyl phenyl; and R.sub.11 is hydrogen, C.sub.1 -C.sub.20 alkyl or a residue --CH.sub.2 NR.sub.8 R.sub.

Abstract: In the preparation of a (thiono)phosphoric ester of the formula ##STR1## in which X represents oxygen or sulphur,R and R.sup.1 are identical or different and represent alkyl, andR.sup.2 represents optionally substituted aryl or represents optionally substituted hetaryl having at least one nitrogen atom,wherein a hydroxyl derivative of the formulaR.sup.2 --OHor an ammonium, alkali metal or alkaline earth metal salt thereof is reacted with a (thiono)phosphoric halide of the formula ##STR2## in which Hal represents halogen,the improvement which comprises effecting the reaction in the presence of a bicyclic organic amine as catalyst. Advantageously the reaction is effected in a diluent in the presence of potassium carbonate as an acid acceptor at 20.degree. to 100.degree. C., and 0.8 to 1.5 mols of the halide and 0.005 to 0.5 mol of 1,4-diazabicayclo-(2,2,2)-octane are used as bicyclic organic amine per mol of the hydroxyl compound.

Abstract: Resins are obtained by Diels-Alder polymerization of a monomer of the formula ##STR1## where R is a hydrogen atom or an aryl group; andL is an aromatic linking group.

Abstract: Insecticidally and nematicidally active novel triazol-3-yl thionophosphates of the formula ##STR1## in which R represents i-propyl or sec.-butyl,R.sup.1 represents alkyl or aryl andR.sup.2 represents halogen.

Abstract: 1,2,4-triazol-(5)-yl-[thio] phosphates are disclosed having the formula ##STR1## wherein R.sup.1 =alkyl with from 1 to 5 carbon atoms;R.sup.2 =OR.sup.1, R.sup.1, C.sub.6 H.sub.5, NHR.sup.1, N(R.sup.1).sub.2 ;X=O, SR.sup.3 =H, alkyl with from 1 to 5 carbon atoms, C.sub.6 H.sub.5, benzyl, alkenyl with from 2 to 6 carbon atoms, alkynyl with from 2 to 6 carbon atoms; andR.sup.4 =vinyl, halovinyl, polyhalovinyl, vinyl substituted with aryl groups, alkyl groups with from 1 to 4 carbon atoms, O-alkyl groups with from 1 to 4 carbon atoms, S-alkyl groups with from 1 to 4 carbon atoms; haloalkyl, acetyl, cyclohexenyl, benzoyl ##STR2## Also disclosed are 1,2,4-triazole intermediates having the formula ##STR3## wherein: X, R.sup.3 and R.sup.4 have the same meanings as indicated above. The phosphate esters are useful in combatting infestations of pests such as orthoptera, aphides, diptera, lepidoptera, coleoptera, acari, nematodes.

Abstract: Organophosphorus esters, useful in increasing the resistance of keratinous materials to attack by keratin-eating insects, have the general formula: ##STR1## wherein: X and Y are independently O or S;R.sub.1 is an alkyl, alkoxy, alkylamino, dialkylamino or alkylmercapto radical having 1 to 6 carbon atoms;an amino or aryl radical;R.sub.2 is an alkyl radical having 1 to 6 carbon atoms;R.sub.3 is a radical of the general formula:-J-(K-L).sub.n (2)wherein:J is an aliphatic radical, or radical containing an aromatic or heterocyclic ring;K is one of the following radicals: ##STR2## linked to J through the oxygen atom in the case of (3), (5) or (6), and through the nitrogen atom in the case of (4), and in which the carbonyl oxygen atom of (3), (4) or (5), or one or both carbonyl oxygen atoms of (6) may be replaced by sulphur; R.sub.

Abstract: O-Alkyl-O-[1-(2-cyanoalkyl)-5-halo-1,2,4-triazol(3)yl]-(thiono)(thiol)-phos phoric(phosphonic) acid esters and ester-amides of the formula ##STR1## in which R is alkyl with 1 to 6 carbon atoms,R.sub.1 is phenyl or alkyl, alkoxy, alkylthio, monoalkylamino or dialkylamino with 1 to 6 carbon atoms per alkyl or alkoxy,R.sub.2 is hydrogen or alkyl with 1 to 4 carbon atoms,Hal is halogen, andX is oxygen or sulfur,which possess insecticidal and acaricidal properties.

Abstract: O-alkyl-O-[1,5-disubstituted-1,2,4-triazolyl-(3)]-thiono-phosphoric (phosphonic) acid esters and ester-amides of the formula ##STR1## in which R is alkyl of 1 to 6 carbon atoms,R' is alkyl, alkoxy or alkylamino of 1 to 6 carbon atoms or phenyl,R" is alkyl or cyanoalkyl of 1 to 4 carbon atoms or alkenyl of 3 or 4 carbon atoms,R'" is alkyl or cyanoalkyl with 1 to 6 carbon atoms in the alkyl radical, andX is oxygen or sulfur,which possess insecticidal and acaricidal properties.

Abstract: 1,2,4-triazol-(5)-yl-[thio] phosphates are disclosed having the formula ##STR1## wherein R.sup.1 =alkyl with from 1 to 5 carbon atoms;R.sup.2 =OR.sup.1, R.sup.1, C.sub.6 H.sub.5, NHR.sup.1, N(R.sup.1);X=O, S;R.sup.3 =H, alkyl with from 1 to 5 carbon atoms, C.sub.6 H.sub.5, benzyl, alkenyl with from 2 to 6 carbon atoms, alkynyl with from 2 to 6 carbon atoms; andR.sup.4 =vinyl, halovinyl, polyhalovinyl, vinyl substituted with aryl groups, alkyl groups with from 1 to 4 carbon atoms, O-alkyl groups with from 1 to 4 carbon atoms, S-alkyl groups with from 1 to 4 carbon atoms; haloalkyl, acetyl, cyclohexenyl, benzoyl, ##STR2## [wherein R.sup.5 =OH, ##STR3## Cl, SR.sup.1, OR.sup.1, N(R.sup.1).sub.2, NHR.sup.1 ], --CO--CH.sub.2 --SR.sup.1, ##STR4## Also disclosed are 1,2,4-triazole intermediates having the formula: ##STR5## wherein: X, R.sup.3 and R.sup.4 have the same meanings as indicated above.

Abstract: New 1,2,4-triazoles, their manufacture and use as active ingredient on pest control is disclosed. The triazoles correspond to the formula ##STR1## wherein R.sub.1 represents C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -alkylthio,R.sub.2 represents C.sub.1 -C.sub.6 -alkyl,R.sub.3 represents hydrogen, chlorine, bromine, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.5 -alkenylthio or C.sub.3 -C.sub.5 -alkynylthio, andX represents oxygen or sulphur.