Abstract: A process for pharmaceutically treating a subject with S-(-)-3-morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5-thiadiazol e hemihydrate comprising preparing a composition containing the hemihydrate and topically applying the prepared composition to a surface of the subject.

Abstract: There is disclosed a method for the preparation of the antibacterial (-) piperazine benzoxazine derivative having formula I comprising the steps of reacting (+)2-aminomethylene-3-oxo-3-phenylpropionate derivative of formula II with a base in an organic polar solvent, to give a (-) benzoxazine derivative of formula III: and reacting the (-) benzoxazine derivative of formula III with a piperazine derivative of formula IV in an organic polar solvent.

Abstract: The invention is that of a new triphenodioxazine dye of the formula: ##STR1## wherein: ##STR2## K is independently selected from SO.sub.3 H and COOH; W=a substituted or unsubstituted arylene, alkylene or arylene-alkylene group;Y.sup.1 =Vinyl, .beta.-Sulfatoethyl, .beta.-Thiosulfatoethyl, .beta.-Halogenethyl-group, .beta.-Phosphatoethyl, andX=H.R, R.sub.1 and R.sub.2 are independently selected from hydrogen and substituted or unsubstituted alkyl.T is independently selected from hydrogen, Cl, Br, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, phenyl or phenoxy; andn is selected from 0, 1 or 2.

Abstract: Substituted oxazines and thiazines, arthropodicidal compositions containing them and methods of controlling arthropods are provided. The oxazines and thiazines having the formula ##STR1## wherein Z is O or S; Q is phenyl or pyridyl substituted with alkenyl, alkynyl or substituted phenyl; andA, E, q, R.sup.1 and R.sup.2 are as described.

Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 -- is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Herbicidal compositions of glyphosate, its salts, diquat, or paraquat in combination with a compound of the following formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and n are as defined. Preferred are combinations of glyphosate, its salts, diquat, or paraquat with 2-chloro-5-(4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-4-fluoro benzoic acid, 1-methylethyl ester.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.

Abstract: A condensed thiophene compound represented by general formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R.sup.1 represents hydrogen, halogen, alkyl, etc.; R.sup.2 represents hydrogen, alkyl, acyl, etc.; G represents --CH.sub.2 --, --CH(OH)--, --CO--, etc.; Q represents alkylene; T represents --N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents --CH.sub.2 -- or --S--; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.This compound is useful as an antipsychotic drug having a reduced extrapyramidal side effect.

Abstract: This invention relates to a process for preparing an enantiomerically pure compound of the formula ##STR1## wherein R.sup.1 and R.sup.

Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

Abstract: The disclosure herein relates to a process for the preparation of compounds according to Formula N ##STR1## which comprises using a compound of Formula M ##STR2## as starting material for alkylation to said compounds of Formula N in an inert solvent at temperatures within the range of 0.degree.-200.degree. C. whereinR.sub.1 is C.sub.1-5 alkyl;R.sub.2 is C.sub.1-5 haloalkyl;R.sub.3 is halogen;R.sub.5 is hydrogen or halogen;q is 0-2;R.sub.28 and R.sub.30 are independently an alkyl, alkenyl or alkynyl radical having up to 5 carbon atoms or said radicals substituted with a ##STR3## radical; X is O, S(O).sub.m, NR.sub.19 or CR.sub.20 R.sub.21 ;Y is O, S(O).sub.m or NR.sub.22 ;m is 0-2 andR.sub.13 and R.sub.19 -R.sub.22 are hydrogen or an R.sub.28 member.The above compounds are useful as herbicides.

Abstract: Process for the preparation of optically active 4-(phosphinoethyl)-1,3-oxazolidin-5-one derivatives.The invention relates to a process for preparing optically active compounds of formula (IV) ##STR1## in which the radicals R.sub.1, R.sub.2, R.sub.3 ', R.sub.7, n and m are as defined in the main claim,which comprises reacting a compound of formula (II) ##STR2## with a compound of formula (III) ##STR3## in the presence of catalytical amounts of a radical former.

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: This invention provides compounds having the structure ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, --COR.sup.2, phenyl, or phenylalkyl of 7-10 carbon atoms;the dotted line represents an optional double bond;R.sup.1 is hydrogen, --OH, OR.sup.3, or is absent if the optional double bond is present;R.sup.2 and R.sup.3 are each, independently, alkyl, alkenyl, alkynyl, phenyl, or phenylalkyl;R.sup.4 is hydrogen, --OR.sup.5, alkyl, alkenyl, alkynyl, --COR.sup.5, --CO.sub.2 R.sup.5, --CONR.sup.5 R.sup.6, perhaloalkyl, halogen, phenyl, or phenylalkyl;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, phenyl, or phenylalkyl; andn=0-2or a pharmaceutically acceptable salt thereof that are useful as antipsychotic, antidepressant and anxiolytic agents useful in the treatment and relief of the symptoms of these disease states.

Abstract: A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --0--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat a mental symptoms associated with a cerebrovascular disease.

Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyalkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, alkylaminosulphonyl or dialkylaminosulphonyl; or R.sup.1 and R.sup.2 together form a linking chain-(CH.sub.2).sub.m Op (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups; and Y represents a group selected from (a) or (b) wherein R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.

Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.