Showing papers by "Roussel Uclaf published in 1973"
TL;DR: The specificity of estradiol binding to EBP and the decrease in the number of specific binding sites with age have been used to show that a plasma protein may modulate a tissue response by controlling the free steroid concentration.
164 citations
TL;DR: The use of a highly active progestin, 17, 21-dimethyl-19-nor-4, 9-pregnadiene-3, 20-dione, as a tag has established that progesterone binds to a specific “7–8S” uterus cytosol component in both the immature mouse and rat.
138 citations
Journal Article•
TL;DR: By comparing 16 estradiol derivatives, it has been possible to assess the relative influence of distribution, metabolism, uterine uptake, and plasma and tissue binding on uterotrophic activity in the rat and revealed that all active compounds are bound in vivo to the 8 S uterus cytosol receptor.
Abstract: By comparing 16 estradiol derivatives, it has been possible to assess the relative influence of distribution, metabolism, uterine uptake, and plasma and tissue binding on uterotrophic activity in the rat. This comparison has revealed that all active compounds are bound in vivo to the 8 S uterus cytosol receptor, but that their activity cannot be related to binding in vitro, owing to the many factors acting on the compound in vivo prior to the triggering of the biological response. It is suggested that only the free molecule in the plasma is active on the uterus and that consequently activity is modulated by plasma binding.
106 citations
TL;DR: A lack of correspondence between clinical antidepressant activity and classical pharmacological tests suggests that the system described may serve as a valuable model for antidepressant activity.
62 citations
TL;DR: The computer print-out not only gives the binding parameter values, but also a graphical representation of the experimental and calculated binding curve in a Proportion Graph thus illustrating the adequacy of fit.
30 citations
TL;DR: The Be-induced blockade of the reticulo-endothelial system (RES) is considerably more pronounced than that exerted by carbon and may be maintained for several weeks, and seems to depend on the physicochemical properties of beryllium.
20 citations
Patent•
18 Jul 1973TL;DR: In this article, a group consisting of HYDROGEN, FLUORINE, CHLORINE and BROMINE and their non-to-XIC, PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS is considered.
Abstract: 1. A COMPOUND SELECTED FROM THE GROUP CONSISTING OF A COMPOUND OF THE FORMULA 1-R1,2-R2,3-(X-(1,4-PHENYLENE)-CO-(CH2)N-(PIPERIDIN-1,4- YLENE)-),R-INDOLE WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKOXY OF 1 TO 5 CARBON ATOMS, R1 AND R2 ARE INDIVIDUALLY SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL OR 1 TO 5 CARBON ATOMS, N IS 2 OR 3 AND X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, FLUORINE, CHLORINE AND BROMINE AND THEIR NON-TOXIC, PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS.
14 citations
Patent•
04 Sep 1973TL;DR: In this paper, a novel organo-phosphorus compounds of the formula where R is selected from the group consisting of methine and nitrogen, R1 is selecting from the groups consisting of hydrogen, alkyl of 1 to 3 carbon atoms and NO2, R2 is selected, R3 is branched or straight chain alkyls of 1-to-3 carbon atoms.
Abstract: Novel organo-phosphorus compounds of the formula WHEREIN R is selected from the group consisting of methine and nitrogen, R1 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and NO2, R2 is selected from the group consisting of hydrogen, straight or branched alkyl of 1 to 3 carbon atoms, chlorine, bromine, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl and thioalkyl of 1 to 4 carbon atoms, R3 is branched or straight chain alkyl of 1 to 3 carbon atoms and R4 is selected from the group consisting of straight and branched chain alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms and wherein R5 and R6 are individually selected from the group consisting of hydrogen and branched and straight chain alkyl of 1 to 3 carbon atoms having pesticidal properties and their preparation.
11 citations
TL;DR: The results establish that the in vitro inhibitory effect of estradiol and of three of its estrogenic and non-estrogenic derivatives on 5α-reductase activity in rat prostate microsomes is not correlated with their uterotrophic activity, nor with their in vitro affinity for the uterus cytosol estrogen receptor.
10 citations
Patent•
07 Sep 1973TL;DR: In this paper, a cyclopropanecarboxylic acid and esters of the formula "STR1" are selected from the group consisting of hydrogen, alkyl, alkynyl, alkenyl, aryl, aralkyl, arabinyl, cycloalkenyl and heterocyclic, with the proviso that when Z 1 and Z 2 are methyl and R 1 is other than methyl and their preparation.
Abstract: Novel cyclopropanecarboxylic acids and esters of the formula ##STR1## wherein Z 1 and Z 2 are selected from the group consisting of hydrogen, alkyl, aralkyl, aryl, alkenyl non-conjugated with the cyclopropane ring, alkenyl non-conjugated with the cyclopropane ring, cycloalkyl, cycloalkenyl and heterocyclic; R is selected from the group consisting of OH and OR' in which R' is selected from the group consisting of lower alkyl which may be substituted, benzyl which may be substituted on the phenyl or methylene portion, N-methylene-dicarboximide, (5-benzyl-furyl-3) methyl, and a cyclopentene of the formula ##STR2## WHEREIN R" is selected from the group consisting of alkyl, alkynyl, alkenyl, aryl, aralkyl, cycloalkyl, cycloalkenyl and heterocyclic; A is a bivalent alkyl radical selected from the group consisting of ##STR3## WHEREIN R 1 is selected from the group consisting of hydrogen and lower alkyl, R 2 and R 3 are selected from the group consisting of alkyl, alkynyl, alkenyl, aryl, aralkyl, cycloalkyl, cycloalkenyl and heterocyclic and taken together with the carbon atom to which they are attached form a ring selected from the group consisting of carbon homo rings and unsaturated carbon homo rings of 3 to 7 carbon atoms and heterocyclic rings which may be substituted with lower alkyl or lower alkoxy and R 2 and R 3 may together form a polycyclic aromatic radical, R 4 is lower alkyl, R 5 is selected from the group consisting of hydrogen and lower alkyl and R 4 and R 5 together with the carbon atoms to which they are attached may form a saturated or unsaturated carbon homo ring or a heterocyclic ring, Y is selected from the group consisting of methylene and a saturated or unsaturated carbon chain and Y' is selected from the group consisting of methine and a saturated or unsaturated carbon chain with the proviso that when Z 1 and Z 2 are methyl and R 1 is hydrogen, R 2 is other than methyl and their preparation.
8 citations
Patent•
09 Jul 1973TL;DR: In this paper, the authors present a list of novel or optically active mixed alkali metal or ammonium phosphate salts with vincanol, methods for their preparation, and their pharmaceutical use.
Abstract: Novel racemic or optically active mixed alkali metal or ammonium phosphate salts with vincanol, methods for their preparation, and their pharmaceutical use.
Patent•
02 Jan 1973TL;DR: In this article, desacetoxycephalosporin derivatives of the formula QU1## in racemic or optically active form or cis and trans forms and mixtures thereof are presented.
Abstract: Novel desacetoxycephalosporin derivatives of the formula ##EQU1## in racemic or optically active form or cis and trans forms and mixtures thereof wherein R is selected from the group consisting of aminophenyl and R', R' is selected from the group consisting of phenyl optionally substituted with at least one member of the group consisting of halogen and nitro and a 5 to 6 member heterocyclic group, Y is selected from the group consisting of amino, NHCOOR" where R" is alkyl of 1 to 5 carbon atoms, hydrogen and hydroxy, A is selected from the group consisting of alkyl of 2 to 5 carbon atoms and cycloalkyl of 3 to 7 carbon atoms optionally containing a heteroatom and R 1 is selected from the group consisting of hydrogen, easily acid hydrolyzable group and easily hydrogenolysis removable group, with the proviso that when R is aminophenyl Y is other than amino and NHCOOR" and R 1 is hydrogen and when Y is amino, R 1 is hydrogen and the non-toxic pharmaceutically acceptable addition salts of with organic and inorganic bases and acids where appropriate which have antibacterial activity and a novel process for their preparation and novel intermediates therefor.
Patent•
12 Mar 1973TL;DR: Novel thiazolcarboxamides of the formula D R A W I N G WHEREIN R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and phenyl, R1 is selected, n is a whole number from 2 to 5 and X and X1 are individually selected.
Abstract: Novel thiazolcarboxamides of the formula D R A W I N G WHEREIN R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and phenyl, R1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, n is a whole number from 2 to 5 and X and X1 are individually selected from the group consisting of hydrogen, halogen, trifluoromethyl and alkyl, alkoxy and alkylthio of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having Alpha -adrenolytic activity and their preparation.
Patent•
24 Oct 1973TL;DR: In this paper, the 4-(alkylaminoalkyl)-(4H)-thieno-(3,2-b)(f)-benzazepines of the formula where R1 and R2 are selected from the group consisting of hydrogen, halogen, -CF3, lower alkoxy optionally substituted, lower alkylthio and arloweralkyl.
Abstract: Novel 4-(alkylaminoalkyl)-(4H)-thieno-(3,2-b)(f)-benzazepines of the formula WHEREIN R1 and R2 are selected from the group consisting of hydrogen, halogen, -CF3, lower alkoxy optionally substituted, lower alkylthio, lower alkyl, optionally substituted sulfonamido, diloweralkylamino and acylamino wherein the acyl is derived from an organic carboxylic acid of one to 18 carbon atoms, R is selected from the group consisting of hydrogen and lower alkyl, A is alkylene of two to five carbon atoms, optionally substituted by lower alkyl, B is selected from the group consisting of hydrogen, lower alkyl and arloweralkyl, C is selected from the group consisting of lower alkyl and arloweralkyl and B and C taken together are alkylene of two to six carbon atoms optionally interrupted with one or two heteroatoms, Y is selected from the group consisting of hydrogen, hydroxy, lower alkoxy and lower alkanoyloxy, X is hydrogen and taken together with Y forms a carbon-carbon double bond, Z'' is selected from the group consisting of hydrogen and lower alkyl and Z is selected from the group consisting of hydrogen, lower alkyl and lower alkoxy and taken with Y forms a member of the group consisting of 0, lower alkylenedioxy, loweralkylenedithio and thioloweralkyleneoxy and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant activity with a large therapeutic index and their preparation and novel intermediates.
Patent•
24 May 1973Patent•
19 Oct 1973TL;DR: In this article, a novel 10-(piperidino-alkyl)-phenothiazines of the formula "STR1##" was proposed, in which X is selected from the group consisting of hydrogen, chlorine, --CF 3, --OCH 3 and SCH 3, B and R are individually selected from a group of hydrogen and alkyl of 1 to 4 carbon atoms.
Abstract: Novel 10-(piperidino-alkyl)-phenothiazines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, chlorine, --CF 3 , --OCH 3 and SCH 3 , B and R are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, Z' is selected from the group consisting of hydrogen and alkyl of 1 to 10 carbon atoms, p is 0 or 1, n is 0, 1 or 2 and A is selected from the group consisting of hydrogen, --COOR 2 and --COR 1 , R 2 is linear alkyl of 1 to 15 carbon atoms and R 1 is selected from the group consisting of alkyl of 1 to 18 carbon atoms optionally containing a double bond or --O-- and a polymethoxyphenyl and their non-toxic, pharmaceutically acceptable acid addition salts having neuroleptic, analgesic, spasmolytic and antihistaminic activity and their preparation and novel intermediates.
Patent•
11 Jan 1973TL;DR: In this paper, a novel process for the preparation of alkali metal, alkaline earth metal and ammonium salts of alpha -D-glucose-1-phosphoric acid by reaction of phosphoric acid and pentaacetyl-beta -Dglugose and to novel salts.
Abstract: Novel process for the preparation of alkali metal, alkaline earth metal and ammonium salts of alpha -D-glucose-1-phosphoric acid by reaction of phosphoric acid and pentaacetyl- beta -D-glucose and to novel salts.
Patent•
05 Feb 1973TL;DR: In this article, the authors present an analysis of the effect of an estimated amount of a component of the formulae on the results of an internal competition, which is based on an estimate of the average effect of the component on the entire formulaa.
Abstract: 1. AN INSECTIDAL COMPOSITION COMPRISING AN INSECTICIDALLY EFFECTIVE AMOUNT OF A COMPOUND SELECTED FROM THE GROUP CONSISTING OFF OPTICALLY ACTIVE AND RACEMIC MIXTURES OF A COMPOUND OF THE FORMULA 1-((-CO-X-CH2-CH2-)>C=CH-),2-(R-OOC-),3,3-DI(H3C-)- CYCLOPROPANE WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF OXYGEN AND SULFUR AND R IS SELECTED FROM THE GROUP CONSISTING OF ALKYL OF 1 TO 6 CARBON ATOMS, A RADICAL OF THE FORMULA -CH2-(FURYLENE)-CH2-Y3 WHEREIN Y3 IS PHENYL, AND A RADICAL OF THE FORMULA WHEREIN Z IS SELECTED FROM THE GROUP CONSISTING OF ALKENYL OF 2 TO 7 CARBON ATOMS AND ALKADIENYL OF 4 TO 7 CARBON ATOMS; AND AN INERT CARRIER.
Patent•
21 May 1973TL;DR: In this paper, a novel 2-phenyl ethanol derivatives of the formula WHEREIN X is selected from the group consisting of oxygen and sulfur, Hal is halogen, R is chosen from the groups consisting of hydrogen and alkyl of 1 to 4 carbon atoms, and Y is selected by combining hydrogen and acyl of an organic carboxylic acid of one to 18 carbon atoms.
Abstract: Novel 2-phenyl ethanol derivatives of the formula WHEREIN X is selected from the group consisting of oxygen and sulfur, Hal is halogen, R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and Y is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms and when R is alkyl, they exist in the form of racemates or optically active isomers having analgesic and anti-inflammatory activity.
Patent•
04 Oct 1973Patent•
04 Oct 1973Patent•
09 Aug 1973Patent•
28 Mar 1973TL;DR: In this paper, the authors proposed a method of treating pepsic hyperactivity in warm-blooded animals by oral administration of alkali metal salts of the sulfuric acid ester of a high molecular weight polysaccharide extracted from Furcellaria fastigiata algae.
Abstract: Novel pharmaceutical compositions having as the active ingredient at least one alkali metal salt of the sulfuric acid ester of a high molecular weight polysaccharide extracted from Furcellaria fastigiata algae (Rhodophyces - gigantinals) and a method of treating pepsic hyperactivity in warm-blooded animals by oral administration of said alkali metal salts.
Patent•
03 Dec 1973TL;DR: Novel steroids of the formula wherein R is alkyl of 1 to 3 carbon atoms and R1 is selected from the group consisting of hydrogen, alkyls of 4 to 6 carbon atoms, and Alpha -tetrahydropyranyl with the proviso that R is not methyl where R 1 is hydrogen having antiandrogenic properties and novel intermediates as discussed by the authors.
Abstract: Novel steroids of the formula WHEREIN R is alkyl of 1 to 3 carbon atoms and R1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and Alpha -tetrahydropyranyl with the proviso that R is not methyl where R1 is hydrogen having antiandrogenic properties and novel intermediates.
Patent•
12 Oct 1973TL;DR: Novel derivatives of maleopimaric acid of the formula are described in this article, where the compounds exhibit hepato-protective activity and have been shown to be hepatic in nature.
Abstract: Novel derivatives of maleopimaric acid of the formula: ##STR1## The compounds of the invention exhibit hepato-protective activity.
Patent•
12 Jan 1973TL;DR: In this article, a method of increasing the number of eggs of poulTRY is proposed to increase the amount of eggs laid by poulliers of poulters.
Abstract: 1. A METHOD OF INCREASING THE CALIBER OF EGGS OF POULTRY COMPRISING ORALLY ADMINISTERING TO EGG LAYING POULTRY AN AMOUNT EFFECTIVE TO INCREASE THE CALIBER OF EGGS OF AT LEAST ONE ACTIVE COMPOUND OF THE FORMULA 3-(O=),13-R,17-R'',17-(HO-)-4,5,9,10,11,12-HEXADEHYDRO- GONANE WHEREIN R IS LOWER ALKYL OF 1 TO 6 CARBON ATOMS AND R'' IS SELECTED FROM THE GROUP CONSISTING OF ALLYL, 2-METHYLALLYL, 2-BUTENYL, TRIFLUOROVINYL, ETHYNYL, PROPARGYL, PROPYNYL CHLOROETHYNYL BUTADIYNYL AND CYCLOPROPYL.
Patent•
29 Jun 1973TL;DR: In this article, the authors present novel biocide compositions having as the active compound an acetophenone of the formula and a method of KILLING BACTERIA AND FUNGI.
Abstract: Novel biocide compositions having as the active compound an acetophenone of the formula AND A METHOD OF KILLING BACTERIA AND FUNGI.
Patent•
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TL;DR: In this paper, the formulae where R is selected from the group consisting of hydrogen and alkali metal useful as anti-inflammatory agents having prolonged activity and their preparation are presented.
Abstract: 21-M-SULFOBENZOATES OF 6,16 Alpha -DIMETHYL-2''-PHENYL- Delta 2,4,6-PREGNATRIENEOLO (3,2-C)-PYRAZOL-11 Beta , 17, 21-TRIOL-20ONE OF THE FORMULA WHEREIN R is selected from the group consisting of hydrogen and alkali metal useful as anti-inflammatory agents having prolonged activity and their preparation.
Patent•
30 Jan 1973TL;DR: As a new compound β-(theophylline ethyl) monosulfite having the formula ##SPC1## and salts thereof with inorganic and organic bases, their process of preparation and as an antibacterial agent, the tetracycline salt of β-theophylla ethyl (THE)-monoSulfite as mentioned in this paper.
Abstract: As a new compound β-(theophylline ethyl) monosulfite having the formula ##SPC1## And salts thereof with inorganic and organic bases, their process of preparation and as an antibacterial agent, the tetracycline salt of β-(theophylline ethyl) monosulfite.
Patent•
06 Mar 1973TL;DR: In this article, a novel process for the preparation of 7α-methyl-13β-R-17α-X-17β-OY-Δ4,9,11 -gonatriene-3-ones of the formula ##SPC1## was proposed.
Abstract: A novel process for the preparation of 7α-methyl-13β-R-17α-X-17β-OY-Δ4,9,11 -gonatriene-3-ones of the formula ##SPC1## Wherein R is lower alkyl of one to four carbon atoms, X is saturated or unsaturated, substituted or unsubstituted, straight or branched aliphatic hydrocarbon of one to four carbon atoms and Y is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of one to 18 carbon atoms and novel intermediates formed therein.