Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or ◯subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which comprises a

Abstract: N-(Triazoloazinyl)thiophenesulfonamide compounds were prepared from appropriately substituted 2-amino[1,2,4]triazolo[1,5-c]pyrimidine, 2-amino[1,2,4]triazolo[1,5-a]pyrimidine and 2-amino[1,2,4]triazolo[1,5-a]pyridine compounds and appropriately substituted thiophenesulfonyl chloride compounds. The compounds were found to be useful as herbicides.

Abstract: Fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of (a) at least one azolopyrimidine of formula I  in which R1, R2, L1, L2 and L3 have the meaning given in claim 1; and (b) at least one fungicidal active ingredient selected from benomyl, carboxin, captan, chlorothalonil, copper oxychloride, cyprodinil, dimethomorph, dithianon, dodine, famoxadone, fenhexamid, fenpiclonil, fenpropimorph, fluazinam, mancozeb, metalaxyl, pyrimethanil, quinoxifen, sulfur, triforine, vinclozolin, a fungicidal triazole derivative, and a synthetic strobilurine derivative. The invention also provides a method of controlling the growth of phytopathogenic fungi at a locus by applying synergistically effective amounts of at least one azolopyrimidine of formula I and at least one fungicidal active ingredient (b) to the locus.

Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).

Abstract: This invention relates to compounds of the formula 1

Abstract: The present invention relates to pyrazolotriazines according to formula (I) 1

Abstract: N-(5,7-dimethoxy[1,2,4]triazolo[1,5-a]pyrimidin-2-yl) arylsulfonamide compounds were prepared from 2-amino-5,7-dimethoxy[1,2,4]triazolopyrimidine and appropriately substituted benzenesulfonyl chloride and pyridinesulfonyl chloride compounds. The compounds were found to be useful as herbicides.

Abstract: 2-Alkoxy-6-trifluoromethyl-N-([1,2,4]triazolo[1,5-c]pyrimidin-2-yl)benzenesulfonamides are prepared by introducing the 2-alkoxy substituent of the benzenesulfonamide ring in the last step by contacting the corresponding 2-fluoro substituted material with the appropriate alkoxide.

Abstract: N-(Triazoloazinyl)thiophenesulfonamide compounds were prepared from appropriately substituted 2-amino[1,2,4]triazolo[1,5-c]pyrimidine, 2-amino[1,2,4]triazolo[1,5-a]pyrimidine and 2-amino[1,2,4]triazolo[1,5-a]pyridine compounds and appropriately substituted thiophenesulfonyl chloride compounds. The compounds were found to be useful as herbicides.

Abstract: The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity and high systemicity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract: 2-Alkoxy-6-trifluoromethyl-N-([1,2,4]triazolo[1,5-c]pyrimidin-2-yl)benzenesulfonamides are prepared by introducing the 2-alkoxy substituent of the benzenesulfonamide ring in the last step by contacting the corresponding 2-fluoro substituted material with the appropriate alkoxide.

Abstract: 2-Amino-5, 8-dimethoxy[1,2,4]triazolo[1,5-c]-pyrimidine is prepared from a 5-chloro or 5-methoxy substituted 3-amino-8-methoxy[1,2,4]triazolo[4,3-c]-pyrimidine by reaction with methoxide in an alcohol solvent. Both rearrangement and, when the 5-substituent is chloro, methoxy substitution can be accomplished directly.

Abstract: 2-Amino-5,8-dimethoxy[1,2,4]triazolo[1,5-c]-pyrimidine is prepared from a 5-chloro or 5-methoxy substituted 3-amino-8-methoxy[1,2,4]triazolo[4,3-c]-pyrimidine by reaction with methoxide in an alcohol solvent. Both rearrangement and, when the 5-substituent is chloro, methoxy substitution can be accomplished directly.

Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-&agr;]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions.

Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: The novel compounds of formula I: (R1, R2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: The invention concerns novel substituted triazoloazine sulphonamides of formula (I) in which Q1 stands for nitrogen or a CH group: Q2 stands for nitrogen or a CH group; R1 stands for hydrogen or halogen, or for C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylamino or di(C1-C4 alkyl)amino, in each case optionally substituted by hydroxy, halogen or C1-C4 alkoxy; R2 stands for hydrogen or halogen, or for C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylamino or di(C1-C4 alkyl)amino, in each case optionally substituted by halogen; and Ar stands for 4-cyano-2,5-difluoro-phenyl, 2,6-dimethoxy-phenyl, 2-bromo-3-trifluoro-methyl-phenyl, 2-bromo-5-trifluoromethyl-phenyl, 6-chloro-pyridine-3-yl-methyl or one of the 5- or 6-member (hetero)cyclic groups mentioned in the description. The invention also concerns salts of these substances, a process for preparing the novel compounds, and their use as plant-treatment agents.

Abstract: The novel compounds of formula I: (R1, R2, R3, L1, L2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.

Abstract: The novel compounds of formula I: wherein (R1, R2, R3, A, X, L and n through L5 are defined in the specification) show high fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: The novel compounds of formula I: wherein (R1, R2, Hal and L1 through L5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with carriers and adjuvants to produce fungicidal compositions.

Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Abstract: The novel compounds of formula I: (R1 to R5 and X are defined in the specification) show selective fungicidal activity, in particular against rice blast disease. The new compounds are processed with carriers and, optionally, an adjuvant to provide fungicidal compositions.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof are provided, which have adenosine A2A receptor antagonism and are useful for the treatment or prevention of various diseases induced by hyperactivity of adenosine A2A receptors (for example, Parkinson's disease or senile dementia): wherein R1 represents substituted or unsubstituted aryl, or the like; R2 represents hydrogen, halogen, lower alkyl, substituted or unsubstituted aryl, or the like; R3 represents hydrogen, halogen, XR10 (wherein X represents O or S; and R10 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic ring, substituted or unsubstituted aralkyl, lower alkyl, or hydroxy lower alkyl), or the like; and Q represents hydrogen or 3,4-dimethoxybenzyl.

Abstract: The novel optically active compounds of formula I: (R1, Hal and L1 through L5 are defined in the specification) wherein the enantiomeric excess of the (S)-enantiomer is at least 70%., show enhanced selective fungicidal activity. The new compounds are processed with carriers, and optionally with adjuvants, to form fungicidal compositions.

Abstract: The present invention is concerned with pyrazolopyrimidines and pyrazolotriazines of the general formula and their pharmaceutically acceptable salts. Surprisingly, these compounds evidence selective affinity to 5HT-6 receptors. They are accordingly suitable for use in the treatment and prevention of central nervous disorders such as, for example, psychoses, schizophrenia, manic depressions, depressions, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.

Abstract: A compound represented by the general formula (I) and a salt thereof: ##STR1## wherein: Rf represents a (C.sub.1 -C.sub.4)haloalkyl group; X.about.Y represents N.dbd.N or CH.dbd.N or the like; A represents a nitrogen atom or CH; Z represents an oxygen or sulfur atom; Rg represents a hydrogen or halogen atom and the like; R1, R2, R3, R4 and R5 are each independently represent a hydrogen or halogen atom or a nitro or cyano group or the like.

Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.

Abstract: Adjuvants selected from liquid polyalkoxylated aliphatic alcohols, solid sodium hydrocarbyl sulfonates and polyalkoxylated trisiloxanes enhance the efficacy of fungicidal triazolopyrimidines. They can be incorporated into formulations of the fungicidal compounds or be added to spray mixtures (tank mix) as separately formulated additives in order to improve the efficacy, systemicity and spectrum of these fungicides.

Abstract: Disclosed are enantiomers diastereomers, salts, solvates, hydrates and mixtures thereof, of formula I: ##STR1## The core moiety is non-cyclic or at least one five- to seven-membered ring, n is an integer from about 4 to about 16, R.sub.1 and R.sub.2 are hydrogen, halogen or C.sub.1-12 alkyl or alkenyl, and (CH.sub.2).sub.n may be substituted by a hydroxyl, halogen, oxygen, a (C.sub.1-4) alkyl group or a dimethylamino group. The compounds and pharmaceutical composition thereof are useful in methods for treating an individual having a disease or treatment-induced toxicity, mediated by second messenger activity.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

Abstract: The compounds of the formula: ##STR1## wherein Y is bond or alkylene;Z is bond, alkylene or vinylene;E is(i) 4-15 membered, unsaturated, partially saturated or fully saturated, mono or bicyclic hetero ring containing as hetero atoms, one or two nitrogen atoms, one or two oxygen atoms or one sulfur atom,(ii) 4-15 membered, unsaturated or partially saturated, mono or bicyclic carbocyclic ring, or(iii) --OR.sup.4 (in which R.sup.4 is hydrogen atom, alkyl or alkyl substituted by a hydroxy group);Cyc is benzene, pyridine or imidazole;R.sup.1 is hydrogen or alkyl;R.sup.2 is hydrogen, alkyl, alkoxy or halogen atom;R.sup.3 is hydrogen, alkyl, alkoxy or --COOR.sup.5 (in which R.sup.5 is hydrogen or alkyl);with the proviso that(1) a Cyc ring should not bond to Z through a nitrogen atom in the Cyc ring when Z is vinylene and that(2) Y is not a single bond, when E is --OR.sup.

Abstract: A method for the preparation of 2'-modified nucleosides is provided. The method comprises a novel intramolecular nucleophilic displacement reaction. Included in the invention are novel 2'-modified pyrimidines and purines prepared according to the method of the invention, novel pyrimidines and purines bearing a 2',3' heterocyclic substituent and oligonucleotides containing said 2'-modified pyrimidines and purines. The 2'-modified nucleosides are useful as anti-viral and anti-neoplastic agents.

Abstract: The novel compounds of formula I: whereinR.sup.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, or aryl group, or an optionally substituted cycloalkyl or cycloalkenyl group, in which one CH.sub.2 group may also be replaced by O, S or NR.sup.2, in which R.sup.2 represents a hydrogen atom or an alkyl group;X represents a hydrogen or halogen atom, or an alkoxy, aryloxy, aralkyloxy, haloalkoxy, alkylthio, cyano, amino, alkylamino or dialkylamino group;L.sup.1, L.sup.2, L.sup.3, L.sup.4 and L.sup.5 each independently represent an hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group or a nitro or cyano group show selective fungicidal activity. The new compounds are processed with carriers and, optionally, adjuvants, to afford fungicidal compositions, useful in agricultural applications.

Abstract: N-(Triazoloazinyl)arylsulfonamide compounds, such as 2,6-dimethoxy-N-(8-chloro-5-methoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)b enzenesulfonamide, 2-methoxy-4-(trifluoromethyl)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrim idin-2-yl)pyridine-3-sulfonamide, and 2-methoxy-6-methoxycarbonyl-N-(5,8-dimethoxy[1,2,4]triazolo[1,5-a]pyridin- 2-yl)benzenesulfonamide were prepared from appropriately substituted 2-amino[1,2,4]triazolo-[1,5-c]pyrimidine and 2-amino[1,2,4]triazolo[1,5-a]-pyridine compounds and appropriately substituted benzenesulfonyl chloride and pyridine-3-sulfonyl chloride compounds. The compounds were found to be useful as herbicides.

Abstract: The compounds of the formula: ##STR1## wherein ring ##STR2## is a hetero ring containing nitrogen atom, optionally selected from ##STR3## n is 0-2; Y is bond or alkylene;Z is bond, alkylene or vinylene;E is(i) 4-15 membered, unsaturated, partially saturated or fully saturated, mono or bicyclic hetero ring containing as hetero atoms, 1 or 2 N atoms, 1 or 2 O atoms or 1 S atom,(ii) 4-15 membered, unsaturated or partially saturated, mono or bicyclic carbocyclic ring, or(iii) --OR.sup.4 (in which R.sup.4 is hydrogen atom, alkyl or alkyl substituted by a hydroxy group);Cyc is 5-7 membered, unsaturated, partially saturated or fully saturated, monocyclic hetero ring containing as hetero atoms, 1 or 2 N atoms or 5-7 membered, unsaturated or partially saturated, monocyclic carbocyclic ring;R.sup.1 is H or alkyl;R.sup.2 is H, alkyl, alkoxy or halogen atom;R.sup.3 is H, alkyl, alkoxy or --COOR.sup.5 (in which R.sup.

Abstract: A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: The novel compounds of formula I: ##STR1## (A, L, n and R.sup.1 through R.sup.4 are defined in the specification) show selective fungicidal activity. The new compounds can be combined with carriers and adjuvants to form fungicidal compositions.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2 and Hal are defined in the specification) show selective fungicidal activity, in particular against rice blast disease. The new compounds are processed with carriers, and optionally an adjuvant, to make fungicidal compositions.

Abstract: An improved process for the preparation of (S)-1,1,1-trifluoroalkyl-2-amines of formula IIIA, ##STR1## where R.sup.1 is a C.sub.1-6 alkyl group, from the corresponding racemic mixture, which process includes treating 1 part by mole of the racemic mixture with approximately 0.3 to 0.7 part by mole of D-(-)-tartaric acid in the presence of an inert solvent.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2, R.sup.3, L.sup.1, L.sup.2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.

Abstract: N-arylsulfilimine compounds, such as S,S-dimethyl-N-(2,6-dichlorophenyl)sulfilimine, were prepared and found to catalyze the reaction of aromatic sulfonyl chloride compounds, such as 2-chlorosulfonyl-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]pyrimidine, with aromatic amine compounds, such as 2,6-dichloroaniline, to form N-arylarylsulfonamide compounds, such as N-(2,6-dichlorophenyl)-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]-pyrimidine- 2-sulfonamide. The aryl moiety of the N-arylsulfilimine catalyst and the aryl moiety of the aromatic amine compound were generally chosen to be identical.

Abstract: The novel compounds of formula I ##STR1## (A and R.sup.1 through R.sup.4 are defined in the specification) show selective fungicidal activity. The new compounds are obtainable by a new synthetic method and processed with carriers and adjuvants to fungicidal compositions.

Abstract: N-(substituted aryl)?1,2,4!triazoloazinesulfonamide compounds, such as N-(2,6-difluorophenyl)-8-fluoro-5-methoxy?1,2,4!triazolo?1,5-c!pyrimidine- 2-sulfonamide, were prepared at a good reaction rate and in good yield by the reaction of a chlorosulfonyl?1,2,4!triazoloazine compound, such as 2-chlorosulfonyl-8-fluoro-5-methoxy?1,2,4!triazolo?1,5-c!pyrimidine, and an arylamine compound, such as 2,6-difluoroaniline, in an organic medium containing a relatively acidic alcohol, such as propylene glycol or 2,2,2-trifluoroethanol.

Abstract: The novel compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, Hal and L.sup.1 through L.sup.5, are defined in the specification show selective fungicidal activity.

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Abstract: N-(Triazoloazinyl)arylsulfonamide compounds, such as 2,6-dimethoxy-N-(8-chloro-5-methoxy?1,2,4!-triazolo?1,5-c!pyrimidin-2-yl)b enzenesulfonamide, 2-methoxy-4-(trifluoromethyl)-N-(5,8-dimethoxy?1,2,4!-triazolo?1,5-c!pyrim idin-2-yl)pyridine-3-sulfonamide, and 2-methoxy-6-methoxycarbonyl-N-(5,8-dimethoxy?1,2,4!triazolo?1,5-a!pyridin- 2-yl)benzenesulfonamide were prepared from appropriately substituted 2-amino?1,2,4!triazolo-?1,5-c!pyrimidine and 2-amino?1,2,4!triazolo?1,5-a!-pyridine compounds and appropriately substituted benzene-sulfonyl chloride and pyridine-3-sulfonyl chloride compounds. The compounds were found to be useful as herbicides.