Abstract: Compounds of the formula I ##STR1## in which A is CH and D is N.sup.+ R, A is nitrogen and D is N.sup.+ R or A is N.sup.+ R and D is nitrogen, R is --CR.sup.4 R.sup.5 --E--R.sup.6, Q.sup.n- is an inorganic or organic anion, n is 1, 2, 3 or 4 and R.sup.1 -R.sup.6, E, X, Y and Z are each as defined in the description, processes for their preparation and their use as pesticides.

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

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

Abstract: The present invention relates to a process for the preparation of 2,5-diamino-4,6-dichloropyrimidine.

Abstract: The present invention is related to a process of making of 2,6-diaminopurines wherein the 6-amino group is substituted by R.sup.4 and R.sup.5, by reacting a compound of formula (VI) ##STR1## with an excess of amine NHR.sup.4 R.sup.5.

Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.

Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is O, S or NH;R and R.sup.1 are each independently selected from H and C.sub.1 -C.sub.4 alkyl or taken together represent C.sub.2 -C.sub.6 alkylene;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;R.sup.3 is a 6-membered heterocyclic ring containing 2N hetero-atoms, said ring being linked to X by a ring carbon atom, optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by C.sub.1 -C.sub.6 alkyl, hydroxy, --OR.sup.5, halo, --S(O).sub.m R.sup.5, oxo, amino, --NHR.sup.5, --N(R.sup.5).sub.2, cyano, --CO.sub.2 R.sup.5, --CONH.sub.2, --CONHR.sup.5 or --CON(R.sup.5).sub.2, with the proviso that R.sup.3 is not an N--(C.sub.1 -C.sub.6 alkyl)pyridonyl group;R.sup.4 is phenyl substituted by a hydroxy group and optionally further substituted by 1 or 2 substitutents each independently selected from hydroxy, C.sub.1 -C.sub.6 alkyl, --OR.sup.5, halo, cyano and nitro;R.sup.5 is C.sub.1 -C.sub.6 alkyl;R.sup.

Abstract: This invention relates to methods of inhibiting sorbitol dehydrogenase, lowering fructose levels, and treating or preventing diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic microangiopathy or diabetic macroangiopathy in a mammal using pyrimidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined as below, and to pharmaceutical compositions containing such derivatives. It also relates to certain novel substituted pyrimidines having the above formula. It also relates to mutual prodrugs of compounds of the formula I and aldose reductase inhibiting compounds, and to pharmaceutical compositions comprising a compound of the formula I and an aldose reductase inhibitor.

Abstract: An N-benzoylamino acid compound of the formula (I), ##STR1## wherein R.sup.3 is an NR.sup.4 R.sup.5 group where R.sup.4 and R.sup.5 which are the same or different are selected from the group consisting of hydrogen, a hydroxyl group, a C.sub.1-12 alkyl group, a C.sub.1-4 alkyl group substituted by a hydroxyl group and a C.sub.1-4 alkyl group substituted by an amino group;R.sup.4 and R.sup.5 when taken together with the adjacent nitrogen form a substituted or unsubstituted 5- or 6-membered heterocyclic group, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom, a 5- or 6-membered heterocyclic group containing an additional nitrogen atom and being substituted by an oxo group, a phenyl-substituted C.sub.1-4 alkyl group or C.sub.

Abstract: Aminotetrazole derivatives of the formula (I) wherein the variables are as defined in the disclosure are useful as nitric oxide synthase inhibitors.

Abstract: Cyclohexylamino and cycloalkoxy nitrogen heterocycles, processes for their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formulaAr--X-E-Qin which Ar is substituted or unsubstituted 4-pyridyl or 4-pyrimidinyl; X is NH, O, S, SO or SO.sub.2 ; E is a bond or alkanediyl; and Q is a substituted cycloalkyl or 4-piperidyl.The invention also relates to processes and intermediates for their preparation, to compositions comprising them and to their use as pesticides and fungicide.

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.

Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: Compounds having utility as antinflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds are pyrimidine- or pyrazine-containing compounds and, in one embodiment, are carboxyamides of the same. Methods are also disclosed for preventing and/or treating inflammatory conditions by administering to an animal in need thereof an effective amount of a compound of this invention, preferably in the form of a pharmaceutical composition.

Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.

Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.

Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.

Abstract: Described herein are compounds of Formula (XX) and Formula (XXIV), shown below, and processes of making same. ##STR1## wherein p is 0 ##STR2## wherein p is 1, and Y is chlorine or bromine.

Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.

Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.

Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formammide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylamino-methylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: 4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: This invention relates to methods of inhibiting sorbitol dehydrogenase, lowering fructose levels, and treating or preventing diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic microangiopathy or diabetic macroangiopathy in a mammal using pyrimidine derivatives of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined as below, and to pharmaceutical compositions containing such derivatives. It also relates to certain novel substituted pyrimidines having the above formula. It also relates to mutual prodrugs of compounds of above formula (I) and aldose reductase inhibiting compounds, and to pharmaceutical compositions comprising a compound of above formula (I) and an aldose reductase inhibitor.

Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: This invention relates to compounds of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X, m and n are defined as in the specification, their pharmaceutically acceptable salts and pharmaceutical compositions containing such compounds or their salts.

Abstract: The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.

Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichloropyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide.

Abstract: Di-, tri- and tetrachromophoric perylene-3,4:9,10-tetracarboxylic acid imides of the formula I ##STR1## in which A is, for example, 1,4-phenylene,R is 1-hexylheptyl andm is 2,are readily accessible by reaction of a perylene-3,4:9,10-tetracarboxylic acid monoanhydride monoimide with 1,4-diaminobenzene-bisformamide. The preparation process and also a specific process for the preparation of monochromic perylene-3,4:9, 10-tetracarboxylic acid bisimides are also claimed. These processes are particularly suitable for reaction of highly electron-rich aromatic amines, which cannot be reacted under conventional condensation conditions.

Abstract: Compounds of general Formula I ##STR1## wherein R.sup.3 is a saturated, unsaturated, straight- or branched-chain or cyclic aliphatic hydrocarbon residue of up to 16 carbon atoms or, if R.sup.4 is a hydrogen atom, a cycloalkyl group or an aryl or aralkyl group optionally substituted by one or several C.sub.1 -C.sub.6 -dialkylamino groups or by one or several C.sub.1 -C.sub.6 -alkoxy groups,R.sup.4 is a hydrogen atom, a saturated, unsaturated, straight- or branched-chain or cyclic hydrocarbon residue of up to 16 carbon atoms, orR.sup.3 and R.sup.4 jointly mean a saturated or unsaturated 5- or 6-membered ring optionally substituted or containing an O, S, N atom or oxo substituent, and Y is COOX or CONR.sub.3 R.sub.4,are valuable complexing agents, complexes or complex salts, e.g., for use as NMR or X-ray diagnostic image-enhancement agents or radioactive diagnostic agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each individually are lower-alkyl or amino,A is ##STR2## B is hydrogen in A.sup.4, A.sup.5 and A.sup.6 ; ##STR3## in A.sup.1 -A.sup.6 ; lower-alkoxy in A.sup.4 -A.sup.6 ;and lower-alkyl, styryl, phenylethynyl or benzoyloxy-lower-alkyl in A.sup.1 and A.sup.2 ;n is 0, 1 or 2;m, p are, independently 0, 1 andR.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, lower-alkyl, trifluoromethyl, lower-alkoxy or nitro,and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the control or prevention of illnesses which are caused by disorders of the dopamine system, in particular psychotic illnesses such as schizophrenia.

Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia in a subject in need of such treatment. The methods comprise administering to a subject in need thereof, a pyrimidine of Formula I. ##STR1## wherein the variables are as defined in the specification.

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

Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichlororpyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylamino-methylene) pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene) pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine.

Abstract: Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

Abstract: Disclosed is a process for the preparation of 5-formylaminopyrimidines of the general formula: ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and signify H, OH, SH, NH.sub.2, alkylamino, halogen, O-alkyl, S-alkyl or alkyl, as well as aryl, and alkyl is an aliphatic radical containing up to 4 carbon atoms, from the corresponding 5-nitrosopyrimidines of the general formula: ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 have the same meanings as above, wherein the starting compound is subjected to a reductive formylation in the presence of a noble metal catalyst, as well as of formic acid and of a salt thereof.

Abstract: Fungicidal 2-imidazolin-5-ones and 2-imidazoline-5-thiones, processes for their preparation, fungicidal compositions containing them and methods of using them to treat or prevent fungal disease in crops.

Abstract: This invention relates to derivatives of acrylic acid useful in agriculture (especially as fungicides but also as plant growth regulators, insecticides and nematocides), to processes for preparing them, to agricultural (especially fungicidal) compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants, to regulate plant growth and to kill or control insect or nematode pests. The invention provides a compound having the formula (I): ##STR1## and stereoisomers thereof, wherein W is a substituted pyridinyl or substituted pyrimidinyl group linked to A by any of its ring carbon atoms; A is either an oxygen atom or S(O).sub.

Abstract: Pyrimidine-cyanoguanidine compounds of Formula I and its pharmaceutically acceptable acid addition salts ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5, hydroxy methyl, cycloalkyl methoxy-C.sub.1 -C.sub.5 alkyl, or R.sub.1 and R.sub.2 are combined to form a C.sub.3 -C.sub.6 carbocyclic ring;R.sub.3 and R.sub.4 are each independently selected to be hydrogen, C.sub.1 -C.sub.4 alkyl, F, Cl, Br, I or CF.sub.3 ;R.sub.5 is hydrogen, F or Cl;R.sub.6 is hydrogen, --NH.sub.2, --NHCH.sub.3, --NHC.sub.2 H.sub.5, --NHCH(CH.sub.3) .sub.2, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2, NH(CH.sub.2).sub.m --OC.sub.1 --C.sub.3 alkyl (where m is 2 or 3), --NHC(O)C.sub.1 -C.sub.3 alkyl, Cl or Br; and n is 0 or 1.The compounds of Formula I are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.

Abstract: The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10, wherein R.sub.8 is loweralkyl, and R.sub.9 and R.sub.10 are each independently selected from the group consisting of H and lower alkyl;R.sub.

Abstract: The present invention provides methods for treating Cryptosporidium parvum in a subject in need of such treatment.

Abstract: The present invention provides compounds useful for treating Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum in a subject in need of such treatment.

Abstract: This invention relates to novel tricyclic pteridinones, their aza analogs and their pharmaceutically acceptable salts. Further encompassed by the invention is a novel process for the production of the tricyclic pteridinones and their aza analogs. The compounds of the invention exhibit cardiovascular properties, particularly mixed vasodilation and selective venous and arterial dilation. Pharmaceutical compositions are proposed for the compounds.

Abstract: Herbicidal 3-substituted pyridine compounds and derivatives thereof of the formula: ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 1, 2 or 3 ring nitrogen atoms with the remainder of the ring atoms being carbon; a substituted or unsubstituted 5-membered heteroaryl group having a ring heteroatom of oxygen or sulfur with the remainder of the ring atoms being carbon; or a substituted or unsubstituted 5-membered heteroaryl group having one ring nitrogen atom and either an oxygen or sulfur ring heteroatom with the remainder of the ring atoms being carbon. Herbicidal compositions containing such 3-substituted pyridine compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed 3-substituted pyridine derivatives.

Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.

Abstract: This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1 or 2, and R.sub.1, R.sub.2, X, Y and W are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.