Abstract: This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.

Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group,A represents a hydrogen atom, and in this case B represents a group CO-G, G being:either a heteroaryl group selected from furan, indole, pyrrole, pyridine, quinoline, isoquinoline and benzofuran, optionally substituted with one or more lower alkyl or lower alkoxy groups or a halogen atoms,or a linear or branched lower alkyl group substituted with a carboxyl group,or a linear or branched lower alkenyl group substituted with a carboxyl group,or a phenyl or naphthyl group substituted with a carboxyl group,or alternatively A forms with B a group CO(CH.sub.2).sub.n CH(CH.sub.

Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.

Abstract: This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).

Abstract: Disclosed is a process for synthesis of a dipeptide such as N-acetyl-L-.alpha.-aspartyl-L-phenylalanine methyl ester wherein one amino acid serves as a chiral template which allows for synthesis of a second amino acid residue to form said dipeptide. The process involves several novel steps such as a nucleophile addition step. In addition, several novel intermediates are described.

Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds are carbamates represented by the general formula ##STR1## wherein Ar and Ar' represent phenyl, naphthyl or heteroaryl, each of which may be substituted; Z and W are hydrogen, aliphatic hydrocarbon, heterocyclic, aryl or carbocyclic containing groups.

Abstract: A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.

Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.

Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.

Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, and its use in the treatment of a number of disease states.

Abstract: A process is described for isolating tetrahydrofuran from mixtures containing tetrahydrofuran, 1,4-butanediol, -butyrolactone and succinic acid esters, in which the mixtures are heated to from 150.degree. to 250.degree. C. in the presence of phyllosilicates, the resultant tetrahydrofuran and water of reaction are removed from the reaction mixture by distillation, and the tetrahydrofuran is separated from the distillate.

Abstract: The present invention relates to heterocyclic compounds characterized in that they correspond to the general formula I: ##STR1## in which R.sub.1 represents a hydrogen atom or a halogen, n can have the values 1 to 6 and Het represents an azole, or one of its derivatives selected from among imidazole, indazole, tetrahydroindazoles, pyrazole or pyrazoline and which can be represented by the general formula II: ##STR2## in which A and B, always different, represent a carbon atom or a nitrogen atom, the dashed line indicates the possible presence of a double bond between positions 4 and 5, and R.sub.2, R.sub.3 and R.sub.

Abstract: The present invention relates to novel bicyclo ether derivatives, to compositions containing them, and to their method of use especially to control the growth of undesired vegetation in rice.

Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 0 or 1; andAr is an aromatic amide moiety, which compound exhibits prokinetic activity and is a 5-HT3 antagonist.

Abstract: N-acyltetrahydroisoquinolines including novel compounds of the formula ##STR1## wherein R.sup.1 is a C10-C25 alkyl chain; a substituted C10-C25 alkyl chain; an interrupted C10-C25 alkyl chain; a substituted interrupted C10-C25 alkyl chain; diphenylamino; di-(R.sup.2 -substituted phenyl)amino; di-(heteroaryl)amino; di-R.sup.2 -substituted heteroary)amino; diphenylmethyl; or di-(R.sup.2 -substituted phenyl)methyl;R.sup.2 is hydroxy, lower alkyl, lower alkoxy, halogeno, amino, lower alkylamino or di-(lower alkyl)amino;R.sup.3, R.sup.4 and R.sup.5 are independently H or --(CH.sub.2 .sub.n --Ar;Ar is phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl;n=0,1 or 2;m=0,1 or 2;or a pharmaceutically acceptable salt thereof, useful in the treatment of atherosclerosis are disclosed.

Abstract: An aminopyrimidine compound of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a cycloalkyl group or a halogen atom;R.sup.2 and R.sup.3 each represent an alkyl group or a halogen atom, or R.sup.2 and R.sup.3 represent a saturated or unsaturated 5- or 6-membered ring;R.sup.4 represents a hydrogen atom or --CONR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 represent an unsaturated 5-membered ring; andR.sup.5 represents ##STR2## where m represents an integer of 1 to 10; m' represents an integer of 1 to 15;n represents an integer of 0, 1 or 2;R.sup.8 represents a hydrogen atom, an alkyl group or a cycloalkyl group;R.sup.9 represents an alkyl group, an alkenyl group, an alkynyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted aralkyl group or an alkyl group,and acid addition salts thereof. Such compound is useful for combatting insects, acarids, nematodes and fungus.

Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.

Abstract: Anxiolytic agents which are racemic or optically active pyrido[1,2-a]pyrazine derivatives of the formula ##STR1## wherein x is N or CH and Y represents one of certain pyrazolo, triazolo, tetrazolo or cyclic imido radicals; and intermediates therefor.

Abstract: A compound of the formula: ##STR1## (wherein R is phenoxy optionally substituted by a halogen, methoxy, or methyl group, ##STR2## one of A and B is ##STR3## and the other is >CH.sub.2 ;R.sup.1 is hydrogen or C.sub.1 -C.sub.5 alkyl;Z.sup.1 is phenyl, benzyl, or isoxazolyl each optionally substituted by a halogen, methoxy, or methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, or phenyl optionally mono-, di-, or tri-substituted by a halogen, methoxy, or methyl group; or Z.sup.1 and Z.sup.2 taken together with the adjacent nitrogen atom may form 5-membered heterocyclic group; Z.sup.3 is C.sub.1 -C.sub.5 hydroxyalkyl, di(C.sub.1 -C.sub.5 alkyl) sulfamoyl, 6-membered heterocyclic group, phenyl, benzyl, or phenylsulfonyl each phenyl moiety of the last three members being optionally substituted by a halogen, methoxy, or methyl group; Z.sup.