Abstract: Compounds of the fomrula (I): ##STR1## and sterioisomers thereof, wherein X is halogen, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, alkenyl, alkynyl, aryl, amino, arylazo, heteroarylalkyl, heteroaryloxyalkyl, acylamino nitro, nitride, trifluoromethyl, -OR.sup.1, -SR.sup.1, -CO.sub.2 R.sup.2, -CONR.sup.3 R.sup.4, -COR.sup.5, -CR.sup.6 .dbd.NR.sup.7, -N.dbd.CR8R.sup.9, -SOR.sup.10 or -SO.sub.2 R.sup.11 ; W, Y and Z, which may be the same or different, are any of the atoms or groups listed for X above and, in addition, may be hydrogen atoms; or any two of the groups W, X, Y and Z, in adjacent positions on the phenyl ring, optionally join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; R.sup.1 is alkyl, or cycloalkyl optionally containing a heteroatom in the cycloalkyl ring, alkenyl, acyl, aryl, heteroaryl, aralkyl or heteroarylalkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, R.sup.9, R.sup.10 and R.sup.

Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.

Abstract: A process is provided for obtaining quaternary ammonium or phosphonium substituted carbonic acid esters. The first step involves reacting the hydroxyl predecessor compound of the ester with phosgene in an aprotic organic solvent to obtain a solution of chloroformate/hydrogen chloride complex. In a second step, the chloroformate/hydrogen chloride complex in solution is admixed with a salt whose conjugate anion, normally a phenol sulfonate, has structure L. During the admixing step, pH is maintained no lower than 6 until all reactants have been combined to form the product ester. Thereupon, pH is lowered to less than 5.5 to stabilize product against hydrolysis.

Abstract: A process is described for obtaining sulfophenyl quaternary ammonium or phosphonium substituted carbonic acid esters. These esters are prepared through sulfonation with sulfur trioxide of aromatic chloroformates followed by reaction of the sulfonated aromatic chloroformate with quaternary ammonium or phosphonium substituted alcohols. The resultant sulfophenyl esters are useful as bleach precursors in combination with peroxygen compounds such as sodium perborate or percarbonate.

Abstract: The 2-piperazinones are made by reacting a 1-cyano-1-hydroxyalkane with ethylenediamine or a substituted ethylenediamine in aqueous solution. The process to make the 2-piperazinones suitable as a regenerable sulfur dioxide absorbing medium requires that the cyano compound be present in at least a molar equivalent amount to the diamine and that the resulting 2-piperazinone product be sparged with an inert gas.

Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.

Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.

Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=1 or 2, a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2-, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.

Abstract: A sulfonamide compound represented by the following formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are identical or different, and each represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R.sup.4 represents a hydrogen atom, a lower alkyl group, or a substituted or unsubstituted aralykyl group; R.sup.5 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted aralkyl group; R.sup.6 and R.sup.7 are identical or different and each represents a hydrogen atom, a lower alkyl group or a lower alkoxy group; and n is an integer of 1 to 8,and an acid addition salt thereof. The compounds of formula (I) provided by this invention have some useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular disorders such as angina pectoris, cerebral circulation disorder and thrombosis.

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as anti-hypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##

Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.

Abstract: A process for the preparation of 4-(2-hydroxyalkyl)-2-piperazinones and their substituted derivatives comprising reacting an N-hydroxyalkylalkylenediamine, e.g. 2-[(2-aminoethyl)amino]ethanol, or a hydrocarbyl substituted derivative thereof with an .alpha.,.beta.-dicarbonyl compound, e.g. glyoxal, an alkyl-substituted derivative of glyoxal or a glyoxal equivalent. Certain hexahydro-4-(hydroxyalkyl)-2H-1,4-diazepin-2-ones have been made which are new compounds.

Abstract: Certain polysubstituted piperazinones (PSP) having two or three methylene groups linking the N.sup.1 atom of the ring to the N atom of a terminal amine group, are found to be peculiarly prone to decomposition when subjected to elevated temperature after being contacted with water, and sensitive to the amount of base used in the base-induced ketoform reaction which generates the PSP represented by the structure ##STR1## These PSP are therefore produced by a modification of the ketoform reaction under essentially anhydrous conditions, using enough ketone to dissolve the PSP formed and a molar ratio of solid alkali metal hydroxide/diamine reactant in the range from at least 5 but less than 7. The PSP produced is recovered as a solution in the ketone, without contacting the PSP with water. The PSP product obtained after the ketone is distilled, is essentially pure.

Abstract: The 4-(2-hydroxyalkyl)-2-piperazinones and their substituted derivatives are prepared by reacting a decahydropyrazino[2,3-b]pyrazine or its substituted derivative having at least one active amine hydrogen, with an alkylene oxide having 2 to 4 carbon atoms.

Abstract: A process for the preparation of 4-(2-hydroxyalkyl)-2-piperazinones and their substituted derivatives comprising reacting an N-hydroxyalkylalkylenediamine, e.g.2-[(2-aminoethyl)amino]ethanol, or a hydrocarbyl substituted derivative thereof with an .alpha.,.beta.-dicarbonyl compound, e.g. glyoxal, an alkyl-substituted derivative of glyoxal or a glyoxal equivalent. Certain hexahydro-4-(hydroxyalkyl)-2H-1,4-diazepin-2-ones have been made which are new compounds.

Abstract: N-(substituted)-1-(piperazinealkyl)-.alpha.-(3,5-dialkyl-4-hydroxyphenyl)-. alpha.,.alpha.-disubstited acetamides, are novel compounds prepared by a novel modification of the ketoform process. The compounds are useful as stabilizers for organic materials subject to degradation in an environment in which the materials are exposed to heat, oxidation and light, particularly ultraviolet light. The compounds are especially useful in combination with known secondary stabilizers.

Abstract: The trans isomeric form of 1,3,4,6,7,11b-hexahydro-7-aryl-2H-pyrazino[2,1-a]isoquinolines are prepared using novel 3-phenyl-4-arylacyl-2-piperazinones and 3-phenyl-4-(2-hydroxy-2-arylethyl) piperazines as intermediates. The process involves reacting a nove piperazinone with a reducing agent such as aluminum hydrides, borane or lithium borohydrides, and then reacting the resulting piperazine with a strong acid, such as polyphosphoric or sulfuric acid.

Abstract: N-substituted piperazinones are prepared by reacting an N-substituted ethylenediamine such as N,N'-dimethylethylenediamine with a 2-oxoaldehyde such as glyoxal. N-substituted piperazinones are useful as flue gas desulfurization agents.

Abstract: Compounds of the formula (T).sub.g -E where T is a substituted 4-acyl-2-piperazinone group, g is 1 or 2 and E is a selected terminal or linking group, are effective light stabilizers for polyolefins and other organic polymers, particularly thermoset acrylic or alkyd acrylic resins.

Abstract: The disclosure deals with novel synthesis involving (a) hydrogenation of a cis-3,3-dialkyl-3,4-dihydroquinoxaline-2-one in the presence of a suitable hydrogenation catalyst, at elevated temperature and pressure, to yield a cis-3,3-dialkyl decahydroquinoxaline-2-one; (b) reaction of trans-1,2-diaminocyclohexane with acetone cyanohydrin in the presence of water to yield trans-3,3-dimethyl-decahydroquinoxaline-2-one; and (c) a reaction of 1,2-diamine with a saturated acyclic or cyclic monoketone or aldehyde and a holoform, in the presence of (i) a phase transfer catalyst (ii) an organic solvent, and (iii) solid or aqueous alkali to yield 2-keto-1,4-diazacycloalkanes. Such compounds exhibit exceptional UV light stabilizing property.

Abstract: The invention relates to a novel process for the preparation of the optically pure 2S- or 2R-indolinecarboxylic acid of the formula ##STR1## and salts thereof. The process comprises forming the heterocyclic 5-membered ring in formula I from an open chain precursor by diastereoselective cyclization.

Abstract: A bis-polysubstituted piperazinone ("bis-PSP") in which two PSP moieties are closely coupled through an ethylene linkage, may be esterified so as to incorporate particular moieties in a macromolecule which may have only one bis-PSP unit, or may be esterified to form an oligomer having plural esterified bis-PSP repeating units. The macromolecule not only exhibits excellent UV-stabilization and antioxidant properties in synthetic resinous materials thus performing a highly effective dual function, but also is resistant to extraction with solvents, particularly polar solvents.

Abstract: Hydroxylamines derived from hindered amines are effective in stabilizing polyolefin compositions containing a stabilizer or mixture of stabilizers selected from the group consisting of the phenolic antioxidants, the hindered amine light stabilizers, the alkylated hydroxybenzoate light stabilizers, the ultraviolet light absorbers, the organic phosphorus compounds, the alkaline metal salts of fatty acids and the thiosynergists, against degradation upon high temperature extrusion, exposure to the combustion products of natural gas, gamma irradiation or upon storage for extended periods.

Abstract: Novel piperazinones having the formula ##STR1## are useful UV stabilizers and are purified by fractional distillation in the presence of an inorganic base.

Abstract: Novel hindered 2-keto-1,4-diazacycloalkane-triazine oligomers having the general formula ##STR1## are useful antioxidants and UV stabilizers for various polymers.

Abstract: Compounds of the formula (T).sub.g -E where T is a substituted 4-acyl-2-piperazinone group, g is 1 or 2 and E is a selected terminal or linking group, are effective light stabilizers for polyolefins and other organic polymers.

Abstract: Heterocyclic dihaloacetamides of the formula ##STR1## where R.sup.1 to R.sup.6, Z and n have the meanings given in the description, are antagonistic agents which increase the toleration of herbicidal acetanilides by crops.

Abstract: A telomeric acid, a tertiary amine, and an epoxide are reacted in the absence of added water. The product recovered is effective in improving the filterability and reducing the pour point of diesel fuel. Alternatively the product can be prepared by reacting a quaternary ammonium hydroxide and a telomeric acid.

Abstract: Aryl-substituted piperazinones and their physiologically-acceptable acid-addition salts have a useful nootropic action. They are administered enterally or parenterally in conventional dosage forms.

Abstract: Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.

Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

Abstract: The invention includes novel dicarboxylic acids derived from alkylene or arylene diaminetetraacetec acid corresponding to the formula ##STR1## These dicarboxylic acids derived from alkylene or arylene diaminetetraacetic acid are useful in the preparation of polyamides.Another aspect of the invention is a polymer prepared from between about 1 and 100 mole percent of the diamine salt of the compound represented by formula (I) ##STR2## These polymers are useful in preparing molded articles.

Abstract: The compounds of the following formulas ##STR1## where W is hydrogen, benzyloxycarbonyl, or t-butoxycarbonyl useful as intermediates for preparing piperazine, piperazinone, 1,4-diazepine and 1,4-diazepin-2-one polypeptide compound.

Abstract: 2-Acyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino-[2,1-a]-4-isoquinoleinones having anthelmintic activity of the formula ##STR1## are prepared from 4-acyl-2,6-dioxopierazines by reaction with a phenethyl halide, selective reduction of one of the oxo groups and cyclization, by the novel intermediates of formula ##STR2## in which Y represents O or H, OH.

Abstract: Heterocyclic dihaloacetamides of the formula ##STR1## where R.sup.1 to R.sup.6, Z and n have the meanings given in the description, are antagonistic agents which increase the toleration of herbicidal acetanilides by crops.

Abstract: Novel analgesic and antipsychotic agents having the formula ##STR1## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR2## or the group ##STR3## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.

Abstract: Disclosed are stabilizer compounds of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.6 are independently selected from the group consisting of alkyl of 1-8 carbon atoms, aryl, cycloalkyl, and alkalene of 2-6 carbon atoms;R.sup.2 is alkyl of 1-6 carbon atoms and can, in conjunction with an acyclic substituent of R.sup.1, form a cyclic substituent;R.sup.4 is hydrogen of 1-6 carbon atoms and can, in conjunction with an acyclic substituent of R.sup.3, form a cyclic substituent;R.sup.5 is hydrogen or alkyl of 1-6 carbon atoms;R is hydrogen or alkyl of 1-6 carbon atoms;Y is oxygen, nitrogen or sulfur;m is 0 to 6;n is 0 to 3; andX is 1 to 3.The foregoing stabilizers are highly effective in the stabilization of polymeric materials against ultraviolet light and the oxygen present in the environment. Due to the relative bulk of these stabilizers, their resistance to migration within an extraction from the stabilized polymer is similar to the more difficult to prepare polymeric stabilizer.

Abstract: A known base-induced catalytic ketoform synthesis can now be carried out without sacrificing the directivity of the prior art process, but non-catalytically, that is, in the absence of the phase transfer catalyst heretofore required, provided the ketone/araldehyde is present in large excess from about 2 to about 25 times the calculated molar amount necessary to yield the reaction product. This synthesis obviates the problems of separating and recovering a phase transfer catalyst used in the prior art process.

Abstract: Novel polysubstituted 2-keto-1,4-diazacycloalkanes are powerful stabilizers for materials subject to ultraviolet (UV) light degradation, particularly for polyolefins. The cyclic 2-keto compounds of this invention have (a) a fixed two-carbon bridge between the N.sup.1 and N.sup.4 atoms of the diaza ring, the remaining portion of the ring having a variable length bridge of two or more carbon atoms, (b) and N-adjacent carbonyl in the fixed two-carbon bridge, and (c) at least one N.sup.4 -adjacent carbon atom of the diaza ring is polysubstituted, that is, has two substituents which may be cyclizable.Compositions containing (a) the polysubstituted 2-keto-1,4-diazacycloalkanes of this invention, and (b) prior art polysubstituted 2-keto-1,4-diazacycloalkanes, exhibit excellent stability to UV light.

Abstract: Novel compounds have been discovered in which a bis compound of a polysubstituted 2-keto-1,4-diazacycloalkane ("2KDZC") provides a bridge between diisocyanate groups so as to form an oligomeric 2KDZC-urethane ("2K-U" oligomer) having from 2 to about 15 repeating units. The bis compound bridge itself consists essentially of two distally linked polysubstituted 2KDZC moieties, and the 2K-U oligomer formed consists essentially of two 2KDZC moieties linked through their N.sup.1 atoms, which moieties in turn are distally linked to urethane groups through the N.sup.4 atoms of the 2KDZC. Such 2K-U oligomers unexpectedly contain a self-limiting number of 2K-U repeating units which happens to provide 2K-U oligomers which are desirable and highly effective u-v light stabilizers in organic materials.

Abstract: This invention relates to new compounds of value as antibacterial agents. More particularly, it relates to quinoline carboxylic acid derivatives, the hydrates and the acid or alkali addition salts thereof.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R' is hydrogen, straight or branched chain lower alkyl having from 1 to 4 carbon atoms or benzyl, Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms, Y is hydrogen or a nitrogen blocking group selected from the group consisting of tertiary alkoxycarbonyl, benzyloxycarbonyl, cycloalkoxycarbonyl and vinyloxycarbonyl, R.sub.c is hydrogen, halogen or benzyloxy and R.sub.d is hydrogen, or R.sub.c and R.sub.d are benzyloxy; or an individual diastereomer thereof. Said compounds having use as intermediates in the production of enkephalin derivatives which in turn are used as analgesic and antipsychotic agents.

Abstract: Novel compounds are described which are substituted benzophenone hydrazones. They have pesticidal activity, especially against insects and acarids, and pesticidal compositions and methods are described. Methods of making the compounds, and novel intermediates, are also described.

Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.

Abstract: Several novel syntheses have been discovered for preparation of 2-keto-1,4-diazacycloalkanes and their derivatives. Trans isomers of polysubstituted quinoxalin-2-ones may now be prepared.

Abstract: Benzophenone thioethers of the general formula I or Ia ##STR1## in which X is hydrogen, alkyl, alkoxy or --COO-alkyl and X.sub.1 is hydrogen, Cl, Br or --SR, R is an unbranched or branched alkyl radical having 1-20 C atoms, which is unsubstituted or substituted by --OH, --OR.sup.1, --O--C(O)--R.sup.2, --COOR.sup.3, --C(O)-phenyl. --CN, --SR.sup.1, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5 or phenyl, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are monovalent hydrocarbon radicals, R.sub.a is an alkylene radical having 2-10 C atoms, which is unsubstituted or substituted by --OH. --OR.sup.1 or --O--C(O)--R.sup.2 and/or is interrupted by --O--, --NR.sup.4, --O--C(O)--R.sup.6 --C(O)--O--, --C(O)--O--R.sup.7 --O--C(O)-- or phenylene and R.sup.6 and R.sup.7 are divalent hydrocarbon radicals, can be prepared by reacting a mono- or di-halogenobenzophenone of the general formula II ##STR2## in which X.sub.2 is Cl or Br and X.sub.

Abstract: Novel polysubstituted 2-keto-1,4-diazacycloalkanes are powerful stabilizers for materials subject to ultraviolet (UV) light degradation, particularly for polyolefins. The cyclic 2-keto compounds of this invention have (a) a fixed two-carbon bridge between the N.sup.1 and N.sup.4 atoms of the diaza ring, the remaining portion of the ring having a variable length bridge of two or more carbon atoms, (b) an N-adjacent carbonyl in the fixed two-carbon bridge, and (c) at least one N.sup.4 -adjacent carbon atom of the diaza ring is polysubstituted, that is, has two substituents which may be cyclizable.Compositions containing (a) the polysubstituted 2-keto-1,4-diazacycloalkanes of this invention, and (b) prior art polysubstituted 2-keto-1,4-diazacycloalkanes, exhibit excellent stability to UV light.

Abstract: The antistatic composition for application to flat fibrous articles such as textiles, carpets, fabrics and the like which comprises a salt of a polymeric acid with an amine of the general formula ##STR1## wherein A=H, --OR.sub.2, ##STR2## R.sub.1 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.2 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.3 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.

Abstract: A phase transfer catalyzed "soft ion synthesis" is disclosed in which the presence of a "soft ion" generated in situ by a soft ion catalyst has a directive effect which favors the formation of a polysubstituted 2-keto-1,4-diazacycloalkane isomer having substituents on both N.sup.4 -adjacent carbon atoms ("C atoms") of its diaza ring; this isomer is formed at the expense of isomers in which an N.sup.4 -adjacent C atom is not substituted. Such an isomer which has substituents on each N.sup.4 -adjacent C atom is generally more effective as a u-v light stabilizer than an isomer which has an unsubstituted N.sup.4 -adjacent C atom, and therefore the former is more desirable.