Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.

Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which an ether group forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1 -C.sub.8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1 -C.sub.4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.

Abstract: Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacterial infections therewith. Also described is a method of manufacture of the quinolones and naphthyridones as well as the starting materials, the optically pure pyrrolidine moieties for attachment at the 7-position.

Abstract: Selected analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.

Abstract: The present invention relates to pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as herein. The compounds are useful as anti-amnestic agent.

Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

Abstract: A process for the separation of a racemic mixture of certain aliphatic carboxylic acids or esters thereof is disclosed. The process comprises (i) forming a salt solution comprising said racemic mixture of a C.sub.1 to C.sub.6 linear or branched aliphatic carboxylic acid and an organic or inorganic base (ii) treating said salt solution with one-half molar equivalent of a chiral organic nitrogenous base having a base strength no stronger than said organic or inorganic base (iii) precipitating from the reaction solution formed in step (ii) the less soluble diastereomeric salt and (iv) separating said precipitated diastereomeric salt.

Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 -OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.

Abstract: There are provided novel esters of 2-arylmethyl-1-naphthol derivatives useful as anti-inflammatory agents. Also provided are pharmaceutical compositions containing these compounds and methods of using the compounds to treat inflammatory diseases in man.

Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.

Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.

Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula ##STR1## where R.sub.2 is a radical selected from the group consisting of ##STR2## where m is an integer from 0 to 3.

Abstract: Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.

Abstract: In one embodiment this invention provides a nonlinear optical medium whcih is a transparent film of a thermoplastic polymer composed of recurring monomeric units corresponding to the formula: ##STR1##

Abstract: Memory enhancing 1-(benzenesulfonyl)-2-oxo-5-alkoxy-pyrrolidines are prepared by alkylation of the corresponding pyrrolidones or pyrrolidone precursors.

Abstract: A method for racemizing an optically active amino acid, which comprises heating the optically active amino acid in an aqueous solution under an alkaline condition in the presence of an alkali metal salt.

Abstract: This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; whereinAr is phenyl, naphthyl or sulfur, oxygen or nitrogen heterocyclic;X is O, S, NR.sub.5, or a chemical bond;R is H, lower alkoxy, aryloxy, hydroxy, lower alkyl, aryl or lower aralkyl;R.sub.1 and R.sub.2 are independently hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl, aryloxy, lower aralkyl, lower aralkoxy, formyl, lower alkanoyl, benzoyl, and lower aralkanoyl;R.sub.3 and R.sub.4 are independently hydrogen, halogen, hydroxy, lower alkoxy, aryloxy, lower aralkoxy, trifluoromethyl, lower carbalkoxy, carboxy, cyano, nitro, lower alkyl, lower alkenyl, lower alkynyl, aryl or lower aralkyl;R.sub.5 is H, lower alkyl, lower aralkyl or aryl;R.sub.6 is hydroxy or hydroxy-substituted lower alkyl;n and m are independently 0, 1, 2 or 3.

Abstract: Aromatic tetrahydroazepinones and thoines having the formula: ##STR1## wherein Q is carbon or nitrogen;B is oxygen or sulfur;R is loweralkyl, cycloalkyl or phenylloweralkyl;Z is an amino or a heterocyclic amino containing radical; andY is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, phenyl or trifluorophenyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.

Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## and pharmaceutically acceptable salts thereof are disclosed.

Abstract: A new class of anti-spasmodic compounds having two branch chains and containing quaternary nitrogen is provided. The compounds have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are defined hereinbelow and m is an integer from 0 to 3.

Abstract: A new class of anti-spasmodic thioester compounds having a heterocyclic ring containing the nitrogen atom of a secondary or tertiary amine or a bicycloheterocyclic ring system containing the nitrogen atom of a secondary or tertiary amine. These compounds have the general formula I ##STR1## wherein: n is an integer from 0 to 2;R.sub.1 is aryl or cycloalkyl;R.sub.2 is hydrogen or hydroxyl; andR.sub.

Abstract: Compound of the formula ##STR1## wherein n is 1 or 2, Y is OH, R.sup.1 COO--, R.sup.2 R.sup.3 NCOO-- or R.sup.4 O whereby R.sup.1 is an alkyl group, or a possibly substituted phenyl group, R.sup.2 is an alkyl, phenethyl, or benzyl or phenyl group, R.sup.3 is H or an alkyl group and R.sup.4 is an allyl or benzyl group, and R is an alkyl, hydroxyalkyl, dimethylaminoalkyl or methylthioalkyl group or alkenyl group, processes for their preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent a straight-chain or branched alkyl group of 1 to 15 carbon atoms, a cycloalkyl group of 3 to 6 carbon atoms, a 2-furyl, 3-furyl, 3-pyridyl, 4-pyridyl or 2-thienyl group or an aromatic group of the formula ##STR2## wherein X, Y and Z are the same or different and represent hydrogen, alkyl of 1 to 3 carbon atoms, trifluoromethyl, alkoxy with 1 to 4 carbon atoms, halogen, nitro or hydroxy groups are useful as pharmaceutical, veterinary and cosmetic agents.

Abstract: A novel photocurable monomer having the formula: ##STR1## wherein: Ar is arylene;R.sup.1 is H, alkyl, alkoxy, amino, halogen, sulfide, sulfoxide, sulfonate, aryl or heterocyclic;R.sup.2 is H, alkyl, aryl or aralkyl; andR.sup.3 is H or methyl,is useful in preparing a polymer having a high refractive index. The polymer is useful in optical components, such as lenses.

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: Optically active compounds of formula ##STR1## in which R is either a H.sub.3 C--, (CH.sub.3).sub.3 C--, (CH.sub.3).sub.3 CO--, C.sub.6 H.sub.5 CH.sub.2 O--, C.sub.6 H.sub.5 --, o-NO.sub.2 C.sub.6 H.sub.4 --, p-NO.sub.2 C.sub.6 H.sub.4 -- or a p-CH.sub.3 C.sub.6 H.sub.4 -group, or salts or lower alkyl esters thereof. The compounds are prepared by the following sequence of reaction steps:(a) there is started from a racemic mixture of a compound according to said formula in which R=a C.sub.6 H.sub.5 group,(b) cinchonidine, D(--)-2-aminobutanol-1 or a derivative thereof is added to this compound as resolving agent,(c) the D(--)-salt of the resolving agent formed is crystallized out and isolated,(d) if necessary, this salt is further purified of the L-isomer by recrystallization,(e) the pure D(--)-salt is hydrolysed in order to remove the resolving agent,(f) the D(--)-S-benzoyl-.beta.-mercaptoisobutyric acid thus liberated is won and, if necessary, purified, and(g) if desired, the C.sub.6 H.sub.

Abstract: A method for the preparation of an ester of .alpha.-thio-.alpha.-aromatic propionic acid derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, phenyl or benzothiazolyl, R.sup.2 is alkyl and Ar is an aromatic substituent.The method comprises reacting an ester of .alpha.-chloro-.alpha.-thiopropionic acid of the formula: ##STR2## with an aromatic compound of the formula ARH, in the presence of a Lewis acid. The method provides good reactivity and positional selectivity in the Friedel-Crafts reaction. Many esters of the formula (2) are useful as pharmaceuticals, agricultural chemicals, perfumes or their intermediates.

Abstract: A method for the extraction of certain amino acids from aqueous solutions by contacting said solutions with various dithiophosphinates in conjunction with a polar diluent is disclosed.

Abstract: Novel processes for making arylpropionic acids are described. One process comprises carboxylating particular Grignard compounds which are the products of a catalyzed reaction between corresponding arylmagnesium bromides and ethylene. Furthermore, the reaction making the particular Grignard compounds is itself novel. Also, an improved method is disclosed for making coupled aryl compounds useful as intermediates for making compounds having a pharmaceutical use. For example, particular biaryls may be used to make some of the Grignard compounds herein from which the arylpropionic acids are made. Finally, an improved bromination is disclosed giving high yields of 4-bromo-2-fluoroaniline, which is thereafter coupled with benzene, then used to make the arylmagnesium bromide reacted with ethylene to obtain the particular Grignard compound and subsequent desired arylpropionic acid, i.e. 2-(2-fluoro-4-biphenylyl)propionic acid.

Abstract: N-Substituted pyrrolidineacetic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an esters of an N-unsubstituted pyrrolidineacetic acid followed by hydrolysis of the ester.

Abstract: DL-.alpha.-amino acids or a salt thereof can be obtained by racemizing an optically active .alpha.-amino acid or a salt thereof in the presence of an aliphatic acid and an aldehyde.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein Hal is bromine or chlorine; R is C.sub.1-4 alkyl, straight or branched chain; and one of R.sup.1 and R.sup.2 is hydrogen and the other is selected from the group consisting of C.sub.3-8 cycloalkyl; C.sub.3-8 cycloalkyl C.sub.1-3 alkyl; phenyl; phenyl C.sub.1-3 alkyl; mono- or disubstituted phenyl or phenyl C.sub.1-3 alkyl wherein the substituents are halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, or trifluoromethyl; a heterocyclic radical selected from the group consisting of thienyl, furanyl, pyrrolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, pyrazolyl, imidazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, and pyridinyl, and N-oxides thereof; and a saturated heterocyclic radical selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, thiazolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, and piperidinyl.