Abstract: 2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 --CHOH--CH.sub.2, CH.sub.2 --S--CH.sub.2 or C(CH.sub.3).sub.2 --S--CH.sub.2,excluding 2,7-diazabicyclo[3.3.0]octane.Also their preparation by the reaction ##STR2## Intermediates II are also new.

Abstract: Intermediates are described for preparing conformationally constrained tricyclic thienothiopyran compounds that are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Abstract: The present invention relates to substituted phenylcarbamate or naphthylcarbamate tricyclic compounds which provide highly potent and selective cholinergic agonist and blocking activity and their use as pharmaceutical agents. The invention further relates to improvements in therapy relative to cholinergic diseases such as glacuoma, Myasthenia Gravis, Alzheimer's disease and to improvements in therapy and organophosphate poisoning. The invention further provides for a selective acetylcholinesterase and butyrylcholinesterase agents and a method for inhibiting these esterases.

Abstract: Squarylium compounds having the following formula (I), ##STR1## and an optical information recording medium comprising a substrate, and a recording layer formed on the substrate, comprising a squarylium compound having formula (II) are disclosed: ##STR2##

Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.

Abstract: The present invention provides a cyanine compound represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 is an optionally substituted lower alkyl group, X and Y are the same or different and each represent a methylene group or an oxygen atom, Z is an acidic residue, and n is 2 or 3. This cyanine compound is suitable for use as a near infrared light-absorbing organic dye useful as an optical disc recording medium for semiconductor laser recording.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The present invention provides an indolenine derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, X and Y are the same or different and each represent a methylene group or an oxygen atom. This indolenine derivative is useful as an intermediate for synthesizing a cyanine compound suitable for use as an organic near infrared light-absorbing dye useful as an optical disc recording medium adapted for semiconductor laser recording.

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## R.sup.3 and R.sup.4 are hydrogen; R.sup.5 is 2-pyridinyl, 2-pyrazinyl, 2-pyrimidinyl, 3-pyridazinyl or any of the foregoing R.sup.5 moieties substituted by lower alkyl, lower alkoxy, halo lower alkyl, cyano, nitro or halo;X, Y and Z are, independently, N, S, O, NR.sup.6, SO, SO.sub.2, CR.sup.6 or CH.sub.2 ;A is lower alkylene, O or S;R.sup.6 is hydrogen, lower alkyl, aryl, aralkyl;m is 3-7;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/-anxiolytic agents having a low liability for extrapyramidal side effects.

Abstract: The invention relates to compounds of general formula: ##STR1## in which A, B, G, D which may be identical or different, each denote a hydrogen atom or a halogen atom, a lower alkoxy group or alternatively a lower alkyl group optionally substituted with one or more halogen atoms,X denotes a hydrogen atom, a linear or branched lower alkyl group or a group SO.sub.2 E in which E denotes a linear or branched lower alkyl group or an aryl group optionally substituted with a linear or branched lower alkyl group,T denotes a hydrogen atom or a lower alkyl group,R.sub.3 denotes a hydrogen atom or a linear or branched lower alkyl group or an aryl group optionally substituted with one or more linear or branched lower alkyl groups,n and m, which may be identical or different, each denote 0 or 1,R.sub.1 and R.sub.2, which may be identical or different, each denote a hydrogen atom or a linear or branched lower alkyl group,or alternatively,R.sup.1 and R.sup.

Abstract: Indole and indole derivatives are prepared by contacting under mild reaction conditions an N-(2-toly)formidate, N-(3-methyl-2-pyridyl)formimidate, or N-methyldiazyl formimidate with an alkali metal amide.

Abstract: Swainsonine and analogs, namely, 1,4-dideoxy-1,4-imino-D-mannitol and the novel ring contacted swainsonines, (1S,2R,7R,7aR)-1,2-trihydroxypyrrolizidine and (1S,2R,7S,7aR)-1,2,7-trihydroxypyrrolizidine, are synthesized from the divergent intermediate, 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol. These novel compounds are glycosidase inhibitors.

Abstract: A compound having the formula: ##STR1## wherein R is a hydrogen atom, a lower alkyl group, an alkanoyl group, an aralkyl group, an alkylsulfonyl group or an arylsulfonyl group, and R.sup.1 is a hydrogen atom or a protecting group for a hydroxyl group, or a salt thereof.

Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathocromically shifted absorption peaks.

Abstract: A method of preparing indole carboxylic acid derivatives from aniline derivatives is described which can be carried out in a single reaction vessel without any isolation of intermediate products. The method involes reacting an aniline derivative with a soluble nitrite in an acid medium, reducing the resulting nitrosamine by treating the acidic nitrosamine containing reaction solution with zinc in the presence of sufficient acid, optionally with addition of additional acid and/or a solvent such as a lower alcohol, reacting the resulting hydrazine derivative containing solution with a lower alkyl ester of pyruvic acid to obtain a corresponding hydrazone which cyclizes to yield an indole carboxylic acid ester, and if desired, hydrolyzing the ester to obtain the corresponding carboxylic acid.

Abstract: Fungicidal 3-cyano-4-phenyl-pyrrole= derivatives of the formula ##STR1## in which Ar stands for phenyl which is trisubstituted to pentasubstituted andR stands for alkyl, alkoxy or alkoxyalkyl.Claimed are compounds of the formula (I) wherein Ar is phenyl which is trisubstituted by halogen, at least one of which is fluorine, and R is alkyl, alkoxy or alkoxyalkyl each having 1 to 6 carbon atoms in the individual alkyl moieties, fungicidal compositions containing the compounds, and a method of combating fungi comprising administering the compounds to the fungi or their habitat.

Abstract: A process for producing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or an aralkyl group, and R.sup.2 is a hydrogen atom or a hydroxyl-protecting group, or a salt thereof, which comprises removing from a compound of the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or a hydroxyl-protecting group, R.sup.4 and R.sup.5 which may be the same or different are N-protecting groups selected from the group consisting of lower alkyl groups and aralkyl groups, and X.sup..crclbar. is an anion, the N-protecting group(s), if necessary, together with the hydroxyl-protecting group.

Abstract: Compounds of the general formula (I) ##STR1## (R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO, R.sup.1 and R.sup.2 are independently halogen, alkyl, alkoxy, hydroxyl, cyano, nitro or --NR.sup.3 R.sup.4 where R.sup.3 and R.sup.4 are independently H or alkyl and R.sup.2 may be H) and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action.The compounds may be prepared by amination of compounds of the general formula (II) ##STR2## (where R.sup.1 and R.sup.2 are as defined above and X is a leaving group.

Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.

Abstract: Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration.

Abstract: A compound of formula (I) ##STR1## is prepared by cyclizing a compound of formula (IIa) or (IIb) or a mixture thereof ##STR2## wherein X is hydroxyl or halogen and R.sup.1 and R.sup.2 independently, represent hydroxy protecting groups) followed by removal of the protecting groups R.sup.1 and R.sup.2.The compound (I) is of use as an intermediate in the stereoselective preparation of (.+-.) trans-5-fluoro-2,3,3a,9a-tetrahydro-1H-[1,4]benzodioxino[2,3-c] pyrrole, which is a selective .beta..sub.2 -adrenoreceptor antagonist and is thus of potential value, in particular, for the treatment or prevention of depression.

Abstract: The present invention relates to novel tricyclo ether derivative compounds, to compositions containing these ether derivative compounds, and to methods of using these compounds or compositions to control the growth of undesired vegetation.

Abstract: Dyeing compositions for keratinous fibres based on indole derivatives, and new compounds.Dyeing composition for keratinous fibres, and especially human hair, characterized in that it contains, in a cosmetically acceptable medium suitable for dyeing these fibres, at least one dye corresponding to the formula: ##STR1## in which R.sub.1 denotes a hydrogen atom or a lower alkyl group or a group --SiR.sub.9 R.sub.10 R.sub.11 ;R.sub.2 and R.sub.3, which may be identical or different, denote a hydrogen atom, a lower alkyl group, a carboxyl group, a lower alkoxycarbonyl group or a group -COOSiR.sub.9 - R.sub.10 R.sub.11 ; and R.sub.5, which may be identical or different, denote at least one linear or branched C.sub.1 -C.sub.20 alkyl group, a formyl group, a linear or branched C.sub.2 -C.sub.20 acyl group, a linear or branched C.sub.3 -C.sub.20 alkenoyl group, a group --SiR.sub.9 R.sub.10 R.sub.11, a group --P(O)(OR.sub.6).sub.2 or a group R.sub.6 OSO.sub.2 --, the other group R.sub.4 or R.sub.

Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen, cyano or halogen (fluorine, chlorine, bromine or iodine) or optionally substituted alkyl; V is either oxygen or sulphur; W, X, Y and Z, which may be the same or different, are hydrogen, halogen, nitro, cyano, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryl, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted arylalkoxy, optionally substituted alkenyl S(O).sub.n R.sup.3 (wherein n is 0, 1 or 2), or optionally substituted heteroaryl, or W, X or X, Y or Y, Z together form methylenedioxy; and R.sup.3 is optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heteroaryl.

Abstract: Compounds of the general formula (I) ##STR1## (wherein R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO; and R.sup.1 and R.sup.2 each represents H, fluorine or chlorine);and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action.The compounds may be prepared by amination of compounds of the general formula (II): ##STR2## (wherein X is a leaving group).

Abstract: Indole derivatives of formula I ##STR1## R is hydrogen, one or two halogen atoms or one or two organic radicals in the 4-, 5-, 6- or 7-position(s),R.sup.1 and R.sup.4 are the same or different and each is hydrogen, alkyl of 1 to 3 carbon atoms or alkoxyalkyl of 1 to 3 carbon atoms in each of the alkoxy and alkyl portions,R.sup.3 is phenyl, --COOalkyl, --PO.sub.3 (alkyl).sub.2, --SO.sub.2 aryl, --SO.sub.2 alkyl, ##STR2## each of 1 to 3 carbon atoms in each alkyl group, and A and B each independently is alkyl of 1 to 3 carbon atoms or together with the connecting N-atom form a pyrrolidono, piperidino, morpholino or piperazino group,are valuable intermediates for preparing valuable tryptophans and .beta.-carbolines.

Abstract: There are provided benzopyrans of formula I, ##STR1## wherein the substituents, R.sub.5 -R.sub.8 and EA are as defined in the specification. These compounds are useful as anti-asthmatic agents.

Abstract: The present invention relates as new industrial product to a derivative of pyrano-indole chosen from the group constituted by:(i) the pyrano[2,3-g]indoles of general formula: ##STR1## in which: X represents a group ##STR2## (where R is a lower alkyl group, OH, lower alkoxy, tosyloxy, NH.sub.2) or ##STR3## (where R' and R", which are identical or different, each represent H or a lower alkyl);R.sub.1 represents an atom of hydrogen, a lower alkyl group, or COY.sub.1(where Y.sub.1 is a lower alkyl group, an amino acid group CH.sub.2 CH(COOH) NH.sub.2 or an aminoalkylene group -(CH.sub.2).sub.n -NR'R" in which is a whole number between 1 and 4 and R' and R" are defined as hereinabove);R.sub.2 represents an atom of hydrogen, or a COY.sub.2 group (where Y.sub.2 is OH or lower alkoxy;R.sub.3 represents an atom of hydrogen, an atom of halogen, a CHO group, lower alkyl, CF.sub.3, (CH.sub.2).sub.n NR'R" or CO-CONR'R"(where n, R' and R" are defined as hereinabove), andR.sub.

Abstract: 1-(Carbamyl, thiocarbamyl, and iminocarbamyl)-indoline derivatives of the formula ##STR1## where each R.sub.1 is independently alkyl, alkoxy, acyloxy, hydroxy, halo or trifluoromethyl, n is 0, 1, 2 or 3, R.sub.2 and R.sub.3 are independently hydroxy, alkoxy, amino or substituted amino, R.sub.4 and R.sub.5 are independently hydrogen, alkyl or substituted alkyl, R.sub.6 is hydrogen, alkyl or substituted alkyl, and Y is O, S or N--R.sub.7 where R.sub.7 is hydrogen, alkyl, cyano or substituted alkyl, and salts thereof, which are useful as antihypertensive and cardioactive agents, methods of preparing the same, and pharmaceutical compositions thereof, are provided.

Abstract: New sulfonylurea compounds of the formula: ##STR1## in which n is 1 or 2,R is thienyl, furyl, pyridyl or phenyl optionally mono or disubstituted,R.sub.1 and R.sub.2, the same or different, each are hydrogen, halogen, (C.sub.1 to C.sub.5)-alkyl, (C.sub.1 to C.sub.5)-alkoxy, or trifluoromethyl, or together represent --CH.sub.2 --O--CH.sub.2 --,R.sub.3 is hydrogen, or hydroxy, andR.sub.4 is (C.sub.1 to C.sub.5)-alkyl, (C.sub.3 to C.sub.8)-cycloalkyl or azacycloalkyl of the formula: ##STR2## in which p is zero or an integer from 1 to 5, or azabicycloalkyl of the formula: ##STR3## in which m is 1, 2, or 3. These new compounds and physiologically tolerable salts thereof may be used as medicines especially in the treatment of diabetes.

Abstract: Novel 4Hfuro[3,2-b]indoles which are useful for treating allergies are disclosed. Also disclosed are methods for preparing said indoles, pharmaceutical compositions containing said indoles and methods for using said pharmaceutical compositions.

Abstract: Compounds are disclosed of general formula ##STR1## where R is H, C.sub.1-6 alkyl optionally substituted by C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl or alkynyl, C.sub.3-7 cycloalkyl, aralkyl or --CHOand the physiologically acceptable salts thereof. The compounds have selective .alpha..sub.2 -adrenoreceptor antagonist action and are indicated as potentially useful for the treatment or prevention of migraine, thrombosis, diabetes, obesity, hypertension, constipation, paralytic ileus, senile dementia and analepsis, and for use in appetite suppression and for the treatment of depression; they may be formulated as pharmaceutical compositions in conventional manner. The compounds may be prepared, for example, by amination of a compound of formula ##STR2## where X is a leaving group such as halogen or a hydrocarbylsulphonyloxy group.

Abstract: 1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula ##STR1## R=H, alkyl, alkoxy, halogeno or CF.sub.3 ; R'=H or R-phenyl;m=0 or 1;p,q=0 to 2;and derivatives thereof, are antihypertensive and cardioactive agents.

Abstract: Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

Abstract: A compound of formula (I): ##STR1## wherein: R is C.sub.1-4 alkyl;R.sub.1 is hydrogen or C.sub.1-4 alkyl;one of A and B is sulphur, and the other of A and B is carbon doubly bound to the carbon spacing A and B; andthe dotted line represents an optionally present double bond;and pro-drugs thereof; and pharmaceutically acceptable salts thereof;have useful anti-inflammatory and analgesic activity.

Abstract: Benzo[4,5]pyrano[2,3c]pyrrole derivatives of the general formula: ##STR1## or pharmaceutically acceptable acid addition salts thereof, in which R.sub.1 and R.sub.2 represent hydrogen, alkyl, alkoxy, aralkoxy, hydroxy, halogen, methylenedioxy or acyloxy, and R.sub.3 represents hydrogen, alkyl, aralkyl or aminoalkyl, are potent dopamine agonists.

Abstract: Improved yields of Benzoxepino- or Benzthiapino[4,3-b]pyrrole-2-acetic acids have been achieved from processes based on modifications performed on a pyrrole carboxylic ester rather than on a pyrrole-.alpha.-oxoacetate.

Abstract: 1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula ##STR1## R=H, alkyl, alkoxy, halogeno or CF.sub.3 ; R'=H or R-phenyl;m=0 or 1;p,q=0 to 2;and functional derivatives thereof, are antihypertensive and cardioactive agents.

Abstract: A method of preparation and/or purification of acid anhydrides is disclosed. Dicarboxylic or polycarboxylic acids contained in the anhydrides to be treated, are dehydrated in an organic solvent in the presence of activated carbon.