Roussel Uclaf

About: Roussel Uclaf is a based out in . It is known for research contribution in the topics: Alkyl & Alkoxy group. The organization has 1888 authors who have published 2338 publications receiving 36508 citations.

4H-triazolo [4,3-a][1,4] benzodiazepines, process for their preparation, their use as medicaments and compositions containing them

Abstract: 1. Claims for the contracting States CH, DE, GB, IT, LI, NL The compounds of formula (I) : see diagramm : EP0227539,P11,F1 in which R1 and R2 represent a hydrogen atom or an alkyl radical containing from 1 to 5 carbon atoms, R3 , R4 , R5 , R6 , identical or different, in any position on the benzene nuclei, represent a hydrogen atom, a hydroxyl radical, an alkyl radical containing from 1 to 4 carbon atoms, an Oalk1 radical, alk1 representing an alkyl radical containing from 1 to 4 carbon atoms, an NH2 , NHalk2 radical, alk2 representing an alkyl radical containing from 1 to 4 carbon atoms, an see diagramm : EP0227539,P11,F2 radical, alk3 and alk'3 , identical or different representing an alkyl radical containing from 1 to 4 carbon atoms, a halogen atom, a CF3 or an NO2 radical, on the condition that R5 and R6 does not represent at the same time a hydrogen atom, in all the racemic or optically active forms, as well as their addition salts with acids. 1. Claims for the contracting State ES Preparation process for compounds of formula (I) : see diagramm : EP0227539,P12,F2 in which R1 and R2 represent a hydrogen atom or an alkyl radical containing from 1 to 5 carbon atoms, R3 , R4 , R5 , R6 , identical or different, in any position on the benzene nuclei, represent a hydrogen atom, a hydroxyl radical, an alkyl radical containing from 1 to 4 carbon atoms, an Oalk1 radical, alk1 representing an alkyl radical containing from 1 to 4 carbon atoms, an NH2 , NHalk2 radical, alk2 representing an alkyl radical containing from 1 to 4 carbon atoms, see diagramm : EP0227539,P12,F3 radical, alk3 and alk'3 , identical or different, representing an alkyl radical containing from 1 to 4 carbon atoms, a halogen atom, a CF3 radical or an NO2 radical, on the condition that R5 and R6 do not represent at the same time a hydrogen atom, in all racemic or optically active forms, as well as their addition salts with acids, characterised in that a compound of formula II : see diagramm : EP0227539,P13,F1 in which R1 , R2 , R3 and R4 have the previous meanings, in the racemic or optically active form, is subjected to the action of a compound of formula (III) : see diagramm : EP0227539,P13,F2 in which R5 and R6 have the previous meanings, so as to obtain a compound of formula (I) in the racemic or optically active form, which is converted, if desired, into salts by the action of an acid.

Steroids substituted in position 10, their preparation and intermediates obtained in their preparation, their use as medicaments and pharmaceutical compositions containing them

Abstract: L'invention concerne les produits The invention relates to products ou X est -CH 2 - et R est un aryie eventuellement substitue, ou vinyle ou ethynyie eventuellement substitue ; where X is -CH 2 - and R is an optionally substituted aryie, or vinyl or ethynyl optionally substituted; ou X est un soufre ou une liaison et R est un aryle eventuellement substitue ; or X is a sulfur or a bond and R is an optionally substituted aryl; R 2 est methyle ou ethyle ; R 2 is methyl or ethyl; R 3 est alkyle, alkenyle ou alkynyle (1-8c) eventuellement substitue ; R 3 is alkyl, alkenyl or alkynyl (1-8C), optionally substituted; R 4 est H ou acyle ; R 4 is H or acyl; . . le trait pointlle indique la presence eventuelle d'une liaison ; the pointlle line indicates the optional presence of a bond; leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions les renfermant. their process and intermediates for preparation, their use as medicaments and compositions containing them. Les produits (I) possedent une remarquable activite anti-glucocorticoide et, pour certains, glucocorticoide. The products (I) have a remarkable anti-glucocorticoid activity and, for some, glucocorticoid.

17-Aryl steroids, their preparation and intermediates for their preparation, their use as medicines and pharmaceutical compositions containing them

Abstract: Products of the formula … … in which… R1 = C1-18 organic radical… R2 = CH3 or C2H5… A and B … … Re = H, C1-6 Alk or acyl … … R3 or R4 denote: one optionally protected or acylated OH or alkoxy and the other optionally substituted aryl,… R5: optionally substituted aryl,… process and intermediates for their preparation, their application as medications and the pharmaceutical compositions containing them

Emulsified spray formulations

Abstract: A formulation suitable for spraying or for dilution with water to form a sprayable preparation, the formulation comprising an active ingredient, optionally a carrier or solvent for the active ingredient, an emulsifier and an evaporation retardant where the formulation satisfies the following formula ##EQU1## where L is less than or equal to 15, A=700376, B=-1.51, C=0.8472, M oil is the weighted average relative molar mass of the oil phase M retardant is the weighted average relative molar mass of the retardant, and X=(M oil ) 1.8/Y, where Y is the molar solubility ratio of the formulation, defined as the minimum number of moles of the oil phase which will dissolve the retardant, divided by the number of moles of retardant, provided that, in the formula above, any solvent which has no liquid phase at 27° C. at atmospheric pressure is extruded. The formulation may include a pesticide or herbicide. The action of the evaporation retardant is improved.

Early events in human B cell activation: metabolic pathways vary according to the first signal used.

Abstract: The effects of the calcium channel blocking drug Verapamil and of palmitoyl-carnitine (PTC), an inhibitor of protein-kinase C activity, on human B cell activation were measured. Both Verapamil and PTC inhibited the B cell proliferation induced by costimulation with anti-mu antibody and with 3 different growth factors: interleukin 2, 20-kDa B cell growth factor and 50-kDa B cell growth factor. Both uridine and thymidine incorporation induced by costimulation with ionomycin and phorbol 12-myristate 13-acetate (PMA) were inhibited by Verapamil and PTC. In contrast, B cell proliferation was resistant to Verapamil (while being still inhibited by PTC) in two situations: when B cells were costimulated with PMA and growth factors and when B cells previously activated in vitro (by anti-mu antibody or PMA) were stimulated with growth factors. These results confirm that the late stage (G1----S transition) of B cell activation is independent of Ca2+ entry. More importantly, they show that the initial events induced by anti-mu antibody and by PMA are based on different biochemical pathways: PMA would act on a subpopulation of B cells which has already received an early signal of activation in vivo. This emphasizes the functional and biochemical heterogeneity of the G0 stage among circulating B cells.