Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: A process for stabilizing an ethylenically unsaturated monomer or oligomer from premature polymerization is disclosed whereby a stabilizing amount of an N-hydroxy substituted hindered amine is added to said polymerizable monomer or oligomer. The ethylenically unsaturated monomer or oligomer encompass vinyl monomers or oligomers bearing at least one polymerizable moiety. The N-hydroxy substituted hindered amine inhibits premature polymerization in the liquid and/or vapor phase.

Abstract: A particulate composition comprising an isothiazolinone or isothiazolothione or a salt or complex thereof and a water soluble metal salt. The salt is typically a metal salt, for example the sodium salt of 1,2-benzisothiazolin-3-one and the water soluble metal salt is particularly an alkali metal salt such as disodium hydrogen phosphate. A preferred composition can be obtained by stirring together an isothiazolinone or isothiazolothione, a base and an alkali metal phosphate in the presence of water until a dry particulate product is obtained. The particulate product is typically highly and rapidly soluble in water and may be stored in a container formed from a water soluble material, for example a bag formed from polyvinyl alcohol.

Abstract: Pharmaceutical composition for decorporating radioactive isotopes from living organisms comprising as active agent a product prepared by reacting 1,4,10,17-tetraoxa-7,16-diazacyclooctadecane with 2-bromomalonic acid disodium salt.

Abstract: This invention provides a process for preparing amide derivatives of acids by the reaction of haloaminotriazines and acid halides.This invention also provides a process for preparing isocyanates and isocyanate adducts from amide derivatives derived from haloaminotriazines and acid halides such as oxalyl chloride, phosgene and phosgene analogs.Melamine derived acid amides are prepared by reaction of trichloro and hexachloromelamines with chloroformates and acid chlorides. The by-product chlorine may be recycled in this process.Amides, carbamates, sulfonamides, phosphoramides, and related amide derivatives may be prepared by the novel processes of the invention.

Abstract: The present invention relates to a process for the preparation of specifically labelled TTX of high specific activity. In the present process, TTX is oxidized by use of the Pfitzer-Moffat method or Fenton's reagent and the aldehyde obtained is hydrated. The hydrated aldehyde is reduced with alkali metal o alkaline earth metal borotritide. The radioactive TTX so obtained, quite surprisingly, has a specific activity many times greater than previously prepared radioactive TTX.

Abstract: Alkylidene macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: Alkyl and alkenyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and derivitization at C-17. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

Abstract: The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: ##STR1## or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.

Abstract: Disclosed herein are substituted quinazolones and their N.sup.1 -oxide derivatives, methods of synthesizing such compounds, and methods of using them to treat or prevent convulsions in mammals. The substituted quinazolones are represented by the formula: ##STR1## wherein X.sub.1 is N, S, O, or CH, X.sub.2 is N or CH, R.sub.1 and R.sub.2 are H, NO.sub.2, or NH.sub.2 except that when one of R.sub.1 and R.sub.2 is NO.sub.2 or NH.sub.2 the other is H, R.sub.3 and R.sub.4 are alkyl with 1-5 C atoms, and R.sub.5, R.sub.6, and R.sub.7 are H or halogen, provided that when X.sub.1 is N, S, or O, X.sub.2 is CH.

Abstract: The invention relates to a new process for the preparation of (hetero)arylalk(en/in)ylamines of the formula (I) ##STR1## in which A represents ethane-1,2-diyl (ethylene, dimethylene, --CH.sub.2 --CH.sub.2 --) or represents ethene-1,2-diyl (ethenylene, vinylene, --CH.dbd.CH--) or represents ethine-1,2-diyl (ethinylene, --C.ident.C--),characterized in that(a) in the event that, in formula (I), A represents ethine-1,2-diyl, halogeno(hetero)aryl compounds of the general formula (II)Ar--X (II)are reacted with aminoalkinyl compounds of the general formula (III) ##STR2## and, if appropriate, (b) in the event that, in formula (I), A represents ethane-1,2-diyl or ethene-1,2-diyl, the new (hetero)aralkinylamines which are obtained by the process step described under (a), of the general formula (Ia), ##STR3## are reacted with a hydrogenating agent, if appropriate in the presence of a catalyst and if appropriate in the presence of a diluent, the definitions applying to Ar, R.sup.1, R.sup.

Abstract: A method for treating trypanosomiases, leishmanioses, filariases and pneumonias caused by Pneumocystis carinii, comprising the step of administering an effective amount of an organometallic compound of the formula: ##STR1## in which: M is arsenic or antimony,Y and Z are identical or different and are each sulfur or oxygen,R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are identical or different and are each hydrogen or a group of the formula: ##STR2## in which X is nitrogen, andA.sub.1 is an alkylene group of 3 to 21 carbon atoms, that is unsubstituted or substituted by: one or more groups which are identical or different and which are of the formula: --(CH.sub.2).sub.n --R.sub.7 in which R.sub.7 is --H, --OH, --COOH, --NH.sub.2 or --SO.sub.3 H and n is an integer of 0 to 10; or one or more Na or K salts of said one or more groups of the formula: --(CH.sub.2).sub.n --R.sub.7, when R.sub.7 is --COOH; or one or more hydrochlorides of said one or more groups of the formula: --(CH.sub.2).sub.n --R.sub.7 when R.

Abstract: Thiazine derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.

Abstract: Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists.

Abstract: A process is described for the preparation of a manganese complex catalyst having the formula: ##STR1## wherein Mn is manganese in the +4 oxidation state; R is a C.sub.1 -C.sub.20 radical selected from the group consisting of alkyl, cycloalkyl, aryl, benzyl and radical combinations thereof;at least two R radicals may also be connected to one another so as to form a bridging unit between two oxygens that coordinate with the manganese;L is a ligand selected from a C.sub.3 -C.sub.60 radical having at least 3 nitrogen atoms coordinating with the manganese; andY is an oxidatively-stable counterion;the process includes the steps of:(i) reacting in an nonaqueous alcoholic medium a manganese (II) salt with the ligand L to form a manganese coordinated substance, a counterion salt M.sub.z Y.sub.

Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitters acetylcholine, dopamine and serotonin; and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found such as in Alzheimer's disease and other conditions involving learning and cognition; and Parkinson's disease.The compounds of this invention can be described as shown in Formula I ##STR1## where A is a heteroaromatic system.

Abstract: Oxazolyl derivatives of formula (I) ##STR1## wherein --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- represents a bivalent radical having the formula--CH.dbd.CH--CH.dbd.CH-- (a-1),--N.dbd.CH--CH.dbd.CH-- (a-2),--CH.dbd.N--CH.dbd.CH-- (a-3),--CH.dbd.CH--N.dbd.CH-- (a-4),--CH.dbd.CH--CH.dbd.N-- (a-5),--N.dbd.CH--N.dbd.CH-- (a-6)or--CH.dbd.N--CH.dbd.N-- (a-7);R represents hydrogen or C.sub.1-4 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or hydroxyC.sub.1-6 alkyl; m represents 1 or 2; D represents C.sub.1-4 alkanediyl; B represents NR.sup.2, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.2 is hydrogen or C.sub.1-4 alkyl; n represents 0, 1 or 2; L represents hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula --Alk--R.sup.3 (b-1); --Alk--Y--R.sup.4 (b-2); --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (b-3); or --CH.sub.2 --CHOH--CH.sub.

Abstract: Compounds having the formula (I) ##STR1## wherein: R.sup.1 is methyl, ethyl or isopropyl; R.sup.2 is alkyl, aralkyl, cycloalkyl, cycloalkylmethyl, aryl, heterocyclic, or heterocyclic-substituted thio; R.sup.3 is hydrogen, methyl or ethyl; or R.sup.2 together with R.sup.3 is --(CH.sub.2).sub.n --, wherein n is 3,4 or 5; and A is aromatic heterocyclic; and salts thereof, are valuable agricultural and horticultural anthelmintic, acaricidal and insecticidal agents.

Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.