Abstract: 2-Amino-pyrimidininone derivatives possessing antihistaminic and serotonin-antagonistic properties. Compositions containing these compounds as the active ingredient and a method of treating subjects from allergic diseases.

Abstract: The invention discloses certain 5-aryl-substituted,2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines useful as PAF receptor antagonists and for treating tumors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravasation, for controlling hyperreactive airways, for protecting against endotoxin-induced hypotension and death and for treating tumors.

Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.

Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

Abstract: Novel indoloquinoxalines having substituents in 6-position containing cyclic groups, of the general formula I ##STR1## wherein R.sub.1 represents hydrogen or one or several preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, lower alkyl-/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group;X is a group ##STR2## wherein Y is CH.sub.2, NH, O or S and a is 2, 3 or 4 and wherein also the bond --C.dbd.N-- can be saturated; Z is alkyl having 1-6 carbon atoms, Cl, Br or CF.sub.3 andR.sub.3 represents hydrogen, lower alkyl-/cycloalkyl group having not more than 4 carbon atoms,and the physiologically acceptable addition products of the compounds with acids and halogen adducts are described. Also methods for preparing said compounds by reaction of a compound of the formula II ##STR3## with a reactive compound containing the residue --CHR.sub.

Abstract: Phenothiazine derivatives of formula ##STR1## in which R represents --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, hydroxyalkyl or acetyloxyalkyl radicals, or form, together with the nitrogen atom to which they are attached, a heterocycle containing 4 to 7 members which may be substituted by 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, or R represents --N.sup.+ R.sub.1 R.sub.2 R.sub.3 in which R.sub.1 and R.sub.2 are as defined above and R.sub.3 is alkyl or phenylalkyl, their isomeric forms and their mixtures, and their salts, are useful in the field of antidiarrhetics.

Abstract: The invention discloses certain 5-hetero or aryl-substituted-imidazo[2,1-a]isoquinolines useful as platelet activating factor (PAF) receptor antagonists, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravassation and PAF-mediated, endotoxin-induced lung injury, and for controlling hyperreactive airways induced by PAF or allergin. In addition, the invention discloses the use of a select group of said compounds as anti-tumor agents.

Abstract: Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.

Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.

Abstract: 1-Substituted alkyl-2-oxo-hexahydroquinoxaline derivatives of the formula ##STR1## wherein A is lower alkylene; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; and R is selected from the group consisting of 1-methyltetrazole-5-yl-thio, 1-imidazolyl, morpholino, ##STR2## in which R.sub.5 is hydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A and R.sub.1 are as defined above, R.sub.2 and R.sub.3 are each lower alkyl or together form tetramethylene, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.

Abstract: Anti-asthmatically acting compounds of formula ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy and the radical A is the group ##STR2## wherein R.sub.3 is hydrogen, a phenyl radical, an indolyl-(3)-methyl radical, imidazolyl-(4)-methyl radical, a C.sub.1 -C.sub.10 -alkyl group or wherein R.sub.3 represents a C.sub.1 -C.sub.10 -alkyl group which is substituted by a carboxy group, a C.sub.1 -C.sub.6 -alkoxycarbonyl group, an aminocarbonyl group, a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyl-oxy group, a mercapto group, a C.sub.1 -C.sub.6 -alkylthio group, a C.sub.2 -C.sub.6 -alkanoylmercapto group, a phenyl group, a hydroxyphenyl group, a dihydroxyphenyl group, an amino-C.sub.1 -C.sub.6 -alkylthio group, an amino-C.sub.1 -C.sub.6 -alkyloxy group, an amino group, a ureido group (H.sub.2 NCONH--) or a guanidino group or wherein R.sub.

Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.

Abstract: There are provided 4-benzyl-1-(2H)-phthalazinone derivatives having antiallergic activity of the formula ##STR1## wherein R.sub.1 represents fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, C.sub.2 -C.sub.6 -alkanoyl-C.sub.1 -C.sub.6 -alkylamino or a nitro group, R.sub.2 represents hydrogen or has one of the meanings given for R.sub.1, whereby R.sub.1 and R.sub.2 may be the same or different, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy or C.sub.2 -C.sub.6 -alkanoyloxy and A represents an azacycloalkanyl radical, the aza nitrogen of which contains a C.sub.1 -C.sub.6 -alkyl group which is substituted by various radicals, and processes for their manufacture.

Abstract: 1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof.

Abstract: Disclosed herein are derivatives of 5-(lower alkyl)-7-amino-2,3-dihydro-1,4-phthalazinedione having substituents on the amino group. The derivatives have luminescent properties which render them useful as analytical tools in clinical chemistry. Adaptation of the derivatives for luminescent immunoassay provides valuable reagents and assays with outstanding sensitivity.

Abstract: The invention relates to new imidazo-benzoxazinones of formula ##STR1## wherein the substituents are defined herein below, which compounds are useful in the treatment of cardiovascular disorders.

Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.

Abstract: The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.

Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.

Abstract: Novel pyrrol-1-ylphenyldihydropyridazinones of the formula ##STR1## their preparation and their use in the treatment of disorders.

Abstract: This invention relates to novel isoxazolo-pyrido-benzoxazine and isothiazolo-pyrido-benzoxazine derivatives having antibacterial properties.

Abstract: A compound useful as anti-inflammatory agents in warm-blooded animals of the formula ##STR1## wherein X is a member of the class of ethylene and ethenyl and is substituted for hydrogen in the sixth or seventh position of the 1(2H)-phthalazinone ringY is a member of the class of hydrogen and hydroxylR.sub.1 is a member of the class of hydrogen, alkyl, alkoxy, hydroxyl, halogen, nitro, --NR.sub.3 R.sub.4, --COR.sub.5 and --O--A wherein A is a mineral acid residue which with --O-- forms an ester or the alkali metal salt of said ester,R.sub.2 is a member of the class of hydrogen, alkyl, phenyl, substituted phenyl, heteroaryl, hydroxyalkylene, polyhydroxyalkylene, aminoalkylene, alkylaminoalkylene, and carboxyalkylene,R.sub.3, R.sub.4 are independently from the class of hydrogen, alkyl, aminoalkylene or alkylaminoalkylene,R.sub.5 is a member of the class of OR.sub.

Abstract: Certain novel p-aminomethylbenzoyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Preferred member compounds include 2-methyl-4-[4-(morpholinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4-(piperidinomethyl)benzoyloxy]-2H-1, 2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methylpiperazinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxamide 1,1-dioxide and 2-methyl-4-[4-(pyridiniummethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.

Abstract: This invention relates to herbicidal quinoxalinyloxy ethers, herbicidal compositions containing said ethers, and methods of using said compounds as herbicides.