Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.

Abstract: The invention relates to compounds represented by the following general formula (1): ##STR1## wherein R.sup.1 represents an alkyl group, R.sup.2 represents an amino group, alkyl group or the like, and R.sup.3 represents a nitro group, amino group, heterocyclic group, alkylsulfonylamino group or the like, or salts thereof, medicines comprising such a compound, a preparation process of the compounds, and intermediates useful for preparation thereof. The compounds (1) are useful for the prevention and treatment of a respiratory disease.

Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.

Abstract: This invention is directed to tricyclic pteridinones of formula (I): ##STR1## where R, R.sup.1, A, B and D are described herein. These compounds and their pharmaceutically acceptable salts are disclosed as being combined inotropic and vasodilator agents.

Abstract: Purine or triazolopurine compounds are disclosed represented by formula (I) or (II): ##STR1## wherein R.sup.1 and R.sup.4 represent each hydrogen, halogeno, hydroxy, mercapto, or amino; R.sup.2 represents alkyl or aryl; and R.sup.3 and R.sup.5 represent each hydrogen, alkyl, or aryl; and pharmaceutical compositions comprising these compounds as xanthine oxidase inhibitors, remedies for hyperuricemia, or remedies or preventive agents for gout.

Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which 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 drugs, and enhancement of memory.

Abstract: The invention relates to compounds represented by the following general formula (1): ##STR1## wherein R.sup.1 represents an alkyl group, R.sup.2 represents an amino group, alkyl group or the like, and R.sup.3 represents a nitro group, amino group, heterocyclic group, alkylsulfonylamino group or the like, or salts thereof, medicines comprising such a compound, a preparation process of the compounds, and intermediates useful for preparation thereof. The compounds (1) are useful for the prevention and treatment of a respiratory disease.

Abstract: Antihypertensive and bronchodilating compounds of the formula or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein:R.sub.1, R.sub.2, R.sub.3, R.sup.a, R.sup.b and R.sup.c as defined in the disclosure;pharmaceutical compositions containing said compounds;methods of treatment using said compounds; anda process for preparing polycyclic guanines comprisinga) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine;b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine;c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; andd) closing the ring of the substituted aminopurine with a suitable dehydrating agent.

Abstract: Disclosed are adenosine A.sub.2a receptor antagonists of the formula ##STR1## wherein A is pyrazole, imidazole or triazole ring; R is ##STR2## R.sub.1 and R.sub.2 are independently H, OH, halogen, alkoxy, alkyl, nitro, amino, CN, haloalkyl, haloalkoxy, carboxy or carboxamido; or the OH group together with one of R.sub.1 or R.sub.2, or R.sub.1 and R.sub.2 together, form a methylenedioxy group;and n is 0-4;said compounds are useful in the treatment of cardiovascular, central nervous system, and respiratory diseases.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.

Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.

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: The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds. The bicyclic aminoimidazole compounds of the invention have anti-tumor and anti-microbial activity.

Abstract: The synthesis and the application of new dyes is described. In particular said new dyes can be incorporated in non-migratory state in hydrophilic colloid layers of photographic materials wherefrom they can be rapidly removed after being quickly decolorised in alkaline aqueous liquids used in the processing of said materials. In photographic applications dyes of the general formula (I) are provided with at least one ionisable group which permits solubilization in aqueous and/or alkaline medium. ##STR1## The meanings of the symbols are as defined in the claims and in the description.

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.

Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Abstract: A process for the preparation of acyclovir by alkylation of N.sup.2 -formylguanine with 2-oxa-1,4-diacyloxybutane and hydrolysis of the resulting intermediate is described.

Abstract: The present invention relates to imidazoquinazoline derivatives represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, R.sup.2 and R.sup.3 represent independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroarylalkyl, or substituted or unsubstituted heteroaryl, or R.sup.2 and R.sup.3 are combined to represent a heterocyclic group containing a nitrogen atom, R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl, X represents O or S, Y represents a single bond or O, n represents 0, 1, 2, or 3, and pharmaceutically acceptable salts thereof.

Abstract: Compounds of general formula (Ia), (Ib) and (II), wherein R.sup.1 and R.sup.2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R.sup.3 R.sup.4 NS(O).sub.2 -- and R.sup.3 and R.sup.4 signify lower alkyl, and R.sup.2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH.sub.2 NHCH.sub.3, a bicyclic heterocycle with 1-3N atoms or a group --NR.sup.5 R.sup.6 or --OR.sup.5 in which R.sup.5 and R.sup.6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH.dbd.CH--, --CH.dbd.N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II).

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which 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 drugs, and enhancement of memory.

Abstract: Pyrimido[4,5-g]quinazoline quinone derivatives were synthesized as anthranone-like reductive alkylating agents. Like many naturally-occurring antibiotics, these quinone derivatives are designed to afford an alkylating quinone methide species upon reduction and leaving group elimination. Kinetic studies of pyrimido[4,5-g]quinazoline hydroquinones provided evidence of quinone methide intermediates able to trap nucleophiles (alkylation) and protons. The rate of quinone methide formation is determined by the hydroquinone free energy. Thus, a linear free energy relationship for quinone methide formation was obtained by plotting rates of quinone methide formation, as the log, versus the quinone reduction potential. The pyrimido[4-5-g]quinazoline quinone methides fall on this free energy plot, showing that these species are formed by the same mechanism as the other structurally-diverse quinone methides previously studied in this research group.

Abstract: Novel triazoloquinazolines of the formula I ##STR1## where A, X R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The compounds are suitable for controlling diseases.

Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and W, X, A, B, C, D, E, R.sub.3, R.sub.4 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, over-dose with benzodiaziepine drugs, and enhancement of memory.

Abstract: The use of triazoloquinazolines for the production of drugs for controlling central nervous disorders is described. The triazoloquinazolines have the formula ##STR1## where R.sup.1, R.sup.2 and X have the meanings stated in the description.

Abstract: Compounds for treating cardiovascular or circulatory disorders of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.7, Ar.sup.1, Ar.sup.2, X, Y, and n are defined herein.

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: The present invention relates to a compound selected from these of formula (I): ##STR1## in which A and R.sub.1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT.sub.3 receptors.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a tricyclic heterocyclic ring system; which is an .alpha.-1 adrenergic antagonist and is useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.

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.

Abstract: The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R.sup.1 and R.sup.2 together form an optionally substituted group of the formula --N.dbd.CH--NH--, --N.dbd.CH--O--, --N.dbd.CH--S--, --N.dbd.N--NH--, --NH--N.dbd.CH--, --NH--CH.dbd.CH--. --NH--CO--NH--, --NH--CO--O--, --NH--CO--S--, --NH--NH--CO--, --N.dbd.CH--CH.dbd.N--, --N.dbd.N--CH.dbd.CH--, --N.dbd.CH--N.dbd.CH--, --N.dbd.CH--CH.dbd.N--, --NH--CO--CH.dbd.CH-- or --N.dbd.CH--CO--NH--; m is 1, 2 or 3 and R.sup.3 includes hydrogen, halogeno and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds. in the treatment of cancer.

Abstract: Compounds of formulaA(B).sub.x, (I),whereinx is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores am distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.

Abstract: Pyrazolothiazolopyrimidine derivatives represented by the Formula ##STR1## and pharmaceutically acceptable salts thereof are useful as anti-inflammatory, analgesic, immunomodulatory and anti-ulcer agents.

Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein n is 0, 1, or 2, X is ##STR2## Z is H.sub.2, oxygen or sulfur, and R.sub.1, R.sub.2, R.sub.3, R.sub.4, T, W, and Y are defined variables.These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepinc type drugs, and enhancement of alertness.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 -R.sup.4, X, Y, and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Substituted ring annulated 5-alkoxy-N-aryl-[1,2,4]triazolo[1,5-c]pyrimidine-2-sulfonamide compounds, such as N-(2,6-dichlorophenyl)-5-methoxycyclopenteno[d]-[1,2,4]triazolo[1,5-c]pyri midine-2-sulfonamide, were prepared by condensation of an appropriate 2-chloro-sulfonyl-5-alkoxy[1,2,4]triazolo[1,5-c]pyrimidine compound, such as 2-chlorosulfonyl-5-methoxycyclopenteno[d][1,2,4]triazolo[1,5-c]pyrimidine, with a substituted arylamine compound, such as 2,6-dichloroaniline, and found to possess herbicidal utility.

Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.

Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and X represents hydrogen, halogen, or hydroxy;W represents an aryl group unsubstituted or substituted with various organic and inorganic substituents;A, B, C, D, and E represent carbon or nitrogen substituted with hydogen or varous organic and inorganic substituents; andR.sub.3, and R.sub.4 are variables representing various organic and inorganic substituents.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 drugs, and enhancement of memory.

Abstract: A process for the preparation of salts of (6R)-N(5),N(10)-methenyl-5,6,7,8-tetrahydrofolic acid of a particular formula (I). The process comprises:(i) mixing at least one acid S.sub.1 with an aqueous solution having dissolved therein an ammonium- or alkali metal-salt of (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid of a particular formula (II) until a pH in the range of about 5.5 to 7.5 is obtained;(ii) adding a water-soluble alkaline earth metal salt to the mixture obtained from step (i);(iii) precipitating a solid and isolating the solid;(iv) providing a solid of formula (I) by suspending the solid obtained from step (iii) in water, adding an acid S.sub.2, which will not precipitate with an alkaline earth metal cation, until the pH stabilizes to a value of 1.0 to 2.0, and separating the resulting solid.

Abstract: Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl;R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino;R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one.The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.

Abstract: Pyrazolo[5,1-b]quinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for treating neurodegenerative disorders, tumors of neuronal origin, inflammation, allergy, and pain, and methods for screening compounds that interact with the neurotrophic receptors using said compositions are disclosed.

Abstract: A process for the preparation of alkaline earth metal salts of (6R)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid. An alkaline earth metal salt, either in the form of a solid, or in the form of an aqueous solution, is added, preferably under an inert gas atmosphere, to an ammonium salt or alkali metal salt of (6RS)-N(10)-formyl-5,6,7,8-tetrahydrofolic acid dissolved in water or an aqueous buffer solution. II is added an alkaline earth metal salt either in the form of a solid or in the form of an aqueous solution. The obtained mixture is allowed to crystallize, and the obtained solid is separated. The product is known to be cytostatic.

Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein n is 0, 1, or 2, X is ##STR2## Z is H.sub.2, oxygen or sulfur, and R.sub.1, R.sub.2, R.sub.3, R.sub.4, T, W, and Y are defined variables.These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and X represents hydrogen, halogen, or hydroxy;W represents an aryl group unsubstituted or substituted with various organic and inorganic substituents;A, B, C, D, and E represent carbon or nitrogen substituted with hydrogen or various organic and inorganic substituents; andR.sub.3, and R.sub.4 are variables representing various organic and inorganic substituents..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 drugs, and enhancement of memory.

Abstract: Salts of 5,10-methylene-(6R)-, (6R,S)-, and (6S)-tetrahydrofolic acid with sulfuric acid or a sulfonic acid are stable in solid form and can be used as a constituent and/or as a starting material for the production of pharmaceutical compositions.

Abstract: There are disclosed condensed purine derivatives represented by formula; ##STR1## in which R.sup.3 represents hydrogen, lower alkyl or benzyl; each of X.sup.1 and X.sup.2 independently represents hydrogen, lower alkyl, aralkyl or phenyl; and n is an integer of 0 or 1; R.sup.1 represents hydrogen, lower alkyl, alicyclic alkyl, noradamantan-3-yl, dicyclopropylmethyl or styryl; and R.sup.2 represents hydrogen, lower alkyl or alicyclic alkyl; or a pharmaceutically acceptable salt thereof. The derivatives and pharmaceutically acceptable salts are useful as diuretics, renal protecting agents, antiallergic agents and hypotensives.

Abstract: A novel process for producing 5-[(substituted)amino]-8-[phenyl or substituted-phenyl]-3H,6H-1,4,5a,8a-tetraazaace-naphthylen-3-ones of the formula: ##STR1## Where R.sub.1, R.sub.2 and R.sub.3 are defined in the specification by reacting a 4,5-dihydro-7-[phenyl or substituted phenyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide with carbon disulfide and a suitable base and a lower alkyl iodide to give a 5-(lower alkylthio)-8-[phenyl or substituted phenyl]-3H,6H-1,4,5a,8a-tetraazaacenaphthylen-3-one which is further reacted with an amine of the formula: ##STR2## to give the desired compounds is disclosed as well as 5-(loweralkylthio)-8-phenyl-3H,6H,1,4,5a,8a-tetra azaacenaphthylen-3-ones useful as intermediates in the process.

Abstract: The present invention relates to a novel method of preparing diastereoisomers derived from tetrahydrofolic acid. By reacting (i) (6RS)-folinic acid or one of its salts, or (ii) 5,10-methenyl-5,6,7,8-tetrahydrofolic acid, with HCOOH at pH 2.0-2.6, a precipitate is obtained which consists of a mixture of two diastereoisomers of orthoamide structure and of the formulae ##STR1## in which R is the p-benzoyl-(L)-glutamic acid residue, in a molar ratio IV/III of about 7/3, compound III being of so-called natural configuration and compound IV being of so-called unnatural configuration. The pure compound IV is isolated from said precipitate and the pure compound III is isolated from the corresponding filtrate. The diastereoisomers of the reduced folates and their salts of natural and unnatural configuration are prepared from compounds III and respectively IV.