Abstract: There are disclosed compounds ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.12 alkoxy group, a C.sub.5 -C.sub.8 cycycloalkyl group, a C.sub.5 -C.sub.8 cycycloalkoxy group, a C.sub.5 -C.sub.8 cycloalkylthio group, a C.sub.6 -C.sub.10 aryl group, a C.sub.6 -C.sub.10 aryloxy group, a C.sub.6 -C.sub.10 arylthio group, nitro, halogen, cyano, --COOH, --COOR.sub.7, --NR.sub.8 R.sub.9 or --CONR.sub.8 R.sub.9, where R.sub.7 is C.sub.1 -C.sub.20 alkyl, C.sub.5 -C.sub.8 cycloalkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, and R.sub.8 and R.sub.9 are each independently of the other hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, X is nitrogen or CR.sub.4, Y is nitrogen or CR.sub.5 and Z is nitrogen or CR.sub.6, and R.sub.4, R.sub.5 and R.sub.6 are each independently of one another hydrogen, a straight-chain or branched C.sub.1 -C.sub.12 alkyl group or a C.sub.6 -C.sub.

Abstract: There is disclosed a process for the preparation of 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias which comprises treating a 1-phthalimidopyrrole of the formula ##STR2## with a base to yield a 1-aminopyrrole of the formula ##STR3## which is reacted with a compound of the formula ##STR4## to obtain the compound of Formula (I).

Abstract: New N-nitro, 3 substituted azetidine compounds are disclosed and these are sed in processes to prepare TNAZ.

Abstract: Method for optically resolving an enantiomeric mixture of ethodolic acid to produce the S (+) enantiomer is provided wherein the enantiomeric mixture is salified with at least 0.5 moles per mole of a mixture of alpha-(+)-phenethylamine enantiomers in an organic solvent. The resulting precipitate containing the salt of optically active phenethylamine and the S-(+)-enantiomer of the ethodolic acid is separated followed by isolation of the optically enantiomer. Salification of the acid with organic and inorganic bases, selected from basis amino acids, morpholine, aminopyridine and benzylalkyltrimethylammonium derivatives provides new therapeutically effective derivatives.

Abstract: The invention provides novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein A, R.sup.1, R.sup.2, m and n are as defined in the specification, and the group --(CH.sub.2)n--A--R.sup.1 is at the 3- or 4-position, together with their pharmaceutically acceptable salts. These phenyl-alkyl-imidazoles and salts have valuable pharmacological properties, especially CNS activities and activity against inflammatory disease.

Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

Abstract: The present invention provides an enantiomerically selective process and intermediates for preparing certain 4,5-disubstituted pyrazolidinones and intermediates which are useful for treating diseases of the central nervous system.

Abstract: One aspect of the present invention provides for the separation of a racemic mixture or a mixture enriched with one or other enantiomer, said mixture comprising the enantiomers of the compound of the formula: ##STR1## wherein R is CN or CONHR' where R' is a C.sub.1 -C.sub.6 alkyl, hydrogen, or benzyl, and R.sub.1 is C.sub.1 -C.sub.6 alkyl or benzyl. Another aspect of the present invention provides a method of preparing a compound of the formula: ##STR2## wherein R is H, C.sub.1 -C.sub.6 alkyl or benzyl, and wherein R.sub.2, R.sub.3, and R.sub.4 are C.sub.1 -C.sub.6 alkyl or benzyl.

Abstract: The present invention relates to 4-amino-3-hydroxy-phthalimidine, an important intermediate for the synthesis of 3-substituted 5-quinoline-carboxylic acid amides, and a process for the preparation thereof.

Abstract: The areno[e]indols have the formula (I). The methods comprises: (a) reacting (VI) with an aldehyde Ar"--CHO to obtain (VII); (b) oxidizing (VII) to yield the cetone (VIII); (c) reating (VIII) with a strong base and thereafter with an acycle chloride ClCOR, to produce (IX); (d) subjecting to a photochemical cyclization (IX) to produce (I). In said formulas Ar is phenyl or substituted phenyl; Ar' is radical (i) or (ii); R is an acyle group, Ar" is a phenyl, pyrolyl, furanyl or thiophenyl group substituted up to three times by any of the radials R, R.sup.1, R.sup.2, or R.sup.3. The compounds (I) are useful as intermediates in the synthesis of hexahydroareno(e)cyclopropa(c)indol-4-ones with antitumoral activity.

Abstract: The invention is drawn to an antibiotic, NEMATOPHIN, 3-indoleethyl 3'-methyl-2-oxo-pentanamide (+stereoisomer, -stereoisomer and racemic mixture) and its derivatives, 3-indoleethyl 2-oxo-alkanamides, 3-indoleethyl 2-oxo-alkanoates with or without substitute(s) on the indole ring, produced by bacterial symbiont Xenorhabdus nematophilus and/or other Xenorhabdus species or synthesized by reaction of tryptamine or substituted tryptamine and 2-oxo-alkanoic acid or its derivative, the additional salts thereof, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them, including antibiotic-resistant Staphylococcus.

Abstract: A new process is described for the synthesis of the triazolyl tryptamine: ##STR1## and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carded out at high temperature, e.g. 100.degree. C., in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na.sub.2 CO.sub.3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT.sub.1 D receptor agonist having anti-migraine properties.

Abstract: Imidazole, triazole and tetrazole derivatives of formula (I) are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated, wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; R.sup.1 represents a group of formula (i), (ii) or (iii).

Abstract: 5-Cyclohexylmethylhydantoin derivatives may be conveniently prepared by reducing, in the presence of a metal catalyst, a 5-(3-cyclohexene-1-yl)melthylenehydantoin derivative which is obtained by the condensation of a hydantoin derivative and a 3-cyclohexene-1-carbaldehyde derivative in the presence of a monoalkanolamine.

Abstract: The invention relates to use of at least one indole derivative of general formula: ##STR1## or of one of the pharmaceutically acceptable salts thereof, in which: Am is selected from radical (a) and (b) defined as follows: ##STR2## R is a C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl radical R.sub.1 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.2 and R.sub.3, which may be identical or different, represent hydrogen, the methyl or ethyl radical or a halogenR.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen, a C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy radical or a halogenR.sub.7 represents hydrogen or a halogenR.sub.8 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.9 represents hydrogen or, when R.sub.8 and R.sub.9 are taken together, form the methylene radicalm represents 1 or 2n represents 2, 3 or 4for preventing or treating diseases involving a proliferation of smooth muscle cells.

Abstract: A method for producing 3-amino-5-mercapto-1,2,4-triazole, useful as an intermediate compound for a medicine or pesticide, or the intermediate thereof, a salt of N-guanidino thiourea from aminoguanidine thiocyanate or a thiocyanate and an aminoguanidine compound in the presence of an acid in a polar solvent, or even from hydrazine and cyanamide is disclosed.

Abstract: A carboxylate is herein disclosed which is represented by the formula (1) or (2) ##STR1## wherein a ring X is an aromatic residue which may have a substituent; the other substitutents are as defined herein. A heat-sensitive recording material comprising this carboxylate is excellent in the stability of the color image and can provide an optically character-readable sharp color image.

Abstract: The invention relates to indoline compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 denote hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, nitro, hydroxyl, alkoxy or NHR where R can be hydrogen, alkyl, monohydroxyalkyl or polyhydroxyalkyl;X denotes oxygen or sulfur;R.sub.3 represents --OR.sub.4 or NR.sub.5 R.sub.6 whereR.sub.4 denotes alkyl, alkenyl, benzyl, alkoxyalkyl or haloalkyl;R.sub.5 and R.sub.6 denote alkyl;R.sub.1 and R.sub.2 not simultaneously denoting hydrogen or nitro and when R.sub.1 denotes alkyl, alkoxy or mono- or polyhydroxyalkyl, R.sub.2 denotes NHR or hydroxyl,and to their use in dyeing keratinous fibers.

Abstract: A method of forming a crosslinked cellulose product is disclosed wherein cellulose fibers are exposed to a solution that includes a catalyst and a crosslinking agent selected from the group consisting of a cyclic N-sulfatoimide or cyclic N-phosphatoimide; a dimethoxyethanal; a mixture of glyoxal and imidazolidone; a diethanol; or a periodate. Specific examples of the crosslinking agents of the present invention include pyridinium N-sulfatosuccinimide; 2,2'-sulfonyldiethanol; sodium periodate; a mixture of dimethoxyethanal and urea; and a mixture of glyoxal and 2-imidazolidone. An acid or base catalyst, as appropriate, may be used with the crosslinking agent to increase the crosslinking reaction rate. In especially preferred embodiments, cellulose fibers are exposed to the crosslinking agent and catalyst, then separated into individualized fibers in a fiberizer.

Abstract: A process for preparing a water-soluble organic oxide which comprises reacting an oil-soluble organic compound with molecular oxygen in the presence of a water-insoluble sensitizer in an organic solvent phase under irradiation of light to produce a water-soluble organic oxide, and transferring the water-soluble organic oxide to a water phase which forms a layer in contact with said organic solvent phase.