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.

Steroids including a spiro ring in position 17, the process for their preparation and their use

Abstract: ##STR1## Products having the formula (I) wherein R1 is an aryl or aralkyl, R2 is a hydrocarbonated radical (1-18 carbon atoms), the dotted lines indicate an optional bond, the cycles A, B and C represent (II), (III), (IV), (V), (VI); R' and R" are H, alkyl (1-4 carbon atoms). Re is H, alkyl (1-6 carbon atoms), acyl, and their salts, their preparation, their application as medicaments, the pharmaceutical compositions containing them and intermediaries.

19-Nor or 19-nor D-homo steroids substituted at position 11 beta by a phenyl group substituted by an alkynyl group, process for their preparation, their use in medicaments and pharmaceutical compositions containing them

Abstract: 1. The products of formula I : see diagramm : EP0245170,P90,F1 in which R1 represents an alkynyl radical having from 2 to 8 carbon atoms optionally substituted by a radical selected from the radicals, hydroxyl, halogen, trialkylsilyl, alkoxy, alkylthio, dialkylamino and oxo, R2 represents an alkyl radical having from 1 to 3 carbon atoms, the rings _A and _B have one of the following structures ; a/. either _A and _B represent the group : see diagramm : EP0245170,P90,F2 in which R' and R" identical or different represent a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms ; b/. or _A and _B represent the group : see diagramm : EP0245170,P90,F3 in which Rx represents a hydrogen atom or an ORe group in which Re represents a hydrogen atom, an alkyl radical containing from 1 to 6 carbon atoms optionally substituted by a dialkylamino radical or an acetyl or propionyl radical ; c/. or _A and _B represent the group : see diagramm : EP0245170,P90,F4 d/. or _A and _B represent the group : see diagramm : EP0245170,P90,F5 e/. or _A and _B represent the group : see diagramm : EP0245170,P91,F1 in which R3 represents a hydrogen atom, an alkyl radical having from 1 to 8 carbon atoms or an aralkyl radical having from 7 to 15 carbon atoms ; - the group of formula : see diagramm : EP0245170,P91,F2 represents : a/. either : see diagramm : EP0245170,P91,F3 in which R3 and R4 , identical or different, represent either a hydrogen atom, a hydroxyl radical, an Oalk4 , or see diagramm : EP0245170,P91,F4 radical, alk4 and alk5 representing an alkyl radical having from 1 to 8 carbon atoms or a benzyl radical ; an alkyl, alkenyl or alkynyl radical having at the most 8 carbon atoms or a phenyl, benzyl or phenylethyl or pyridylethynyl, thienyl or furyl radical, each of these radicals being optionally substituted by one or more radicals selected from the group formed by the radicals hydroxy, alkoxy and alkylthio having from 1 to 4 carbon atoms, the halogen atoms and the dialkylamino radical, or R3 and R4 together form the following radicals : see diagramm : EP0245170,P91,F5 see diagramm : EP0245170,P91,F6 see diagramm : EP0245170,P91,F7 see diagramm : EP0245170,P91,F8 see diagramm : EP0245170,P91,F9 see diagramm : EP0245170,P91,F10 see diagramm : EP0245170,P91,F11 see diagramm : EP0245170,P91,F12 see diagramm : EP0245170,P91,F13 see diagramm : EP0245170,P91,F14 see diagramm : EP0245170,P91,F15 see diagramm : EP0245170,P91,F16 see diagramm : EP0245170,P91,F17 see diagramm : EP0245170,P91,F18 in which R5 and R6 together form a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms, M represents a hydrogen, sodium or potassium or lithium atom, R20 represents an alkyl radical optionally substituted by hydroxyl and R17 represents a hydrogen atom or an acetyl radical, Y and Z represent the following groups : see diagramm : EP0245170,P92,F1 see diagramm : EP0245170,P92,F2 see diagramm : EP0245170,P92,F3 see diagramm : EP0245170,P92,F4 see diagramm : EP0245170,P92,F5 in which R7 and R8 represent an alkyl radical having from 1 to 4 carbon atoms ; b/. or : see diagramm : EP0245170,P92,F6 in which R3 , R4 and Y-Z have the definitions previously indicated, the wavy lines meaning that the substituents R2 , R7 and R8 acan be found in one or other of the possible configurations, as well as the addition salts of the products of formula I with acids and bases.

Sun filter microcapsules

Abstract: Microcapsules containing at least one sun filter having been hardened so as to be impervious with a size of 1 to 1250 micrometers whereby the sun filters do not come in contact with the skin.

RU486: The French experience

Abstract: RU486 (mifepristone) followed by a prostaglandin (PG) analogue has been marketed in France since April 1990 as a medical alternative to surgery for early pregnancy termination. By law, the drug is used only in the centres approved for voluntary pregnancy termination, and its distribution is strictly controlled. Before being marketed, it was distributed to more than 20,000 women, as part of a training programme for the prescribers. Analysis confirmed an efficacy rate of 95.3%. Failures included incomplete ovular expulsion (2.8%), premature vacuum aspiration (0.7%) and ongoing pregnancy (1.2%). Pelvic pain and malaise were reported as side-effects in 1.6 and 1.2% of the cases respectively. Infectious complications were reported in 0.2% of the cases. Three severe adverse events (one of which was fatal) occurred, including myocardial infarction and ventricular arhythmia, in the hours following PG administration and justify a careful medical monitoring in the centre 3-4 h after administration of PG. For this reason, a trial was undertaken to evaluate the efficacy of an oral form of a PGE1 analogue (misoprostol). When RU486 was followed 36-48 h later by 400 micrograms of misoprostol, the efficacy rate was 96.9%, indicating an efficacy equivalent to that obtained with the other PG analogues. The distribution procedures were adequately followed by the prescribers and by the patients. In summary, RU486 constitutes a safe and efficient medical means of pregnancy termination, provided that the manufacturer's recommendations are properly followed.

Intrapleural immunotherapy with escalating doses of interleukin-2 in metastatic pleural effusions

Abstract: Background. The authors assessed the tolerance and efficacy of intrapleural interleukin-2 (IL-2) in patients with malignant effusion. Methods. Twenty-three patients had a total of 25 metastatic pleural effusions; the patients were treated with recombinant IL-2 by means of a continuous intrapleural infusion for 5 days. The daily dosage used in this Phase I/II trial initially was 3 × 106 IU/m2/day; the dosage was increased with every third patient, culminating in a dosage of 24 × 106 IU/m2/day. Results. One patient who had received the highest dosage died of renal failure on day 8. Ninety-six percent of patients had Grade 2–3 fever, which was easily controlled with paracetamol administration. Two (8%) patients had pleural empyema. All other side effects were mild and resolved spontaneously by the end of treatment. The objective response rate was 21.7%. The five patients who responded to IL-2 therapy were alive 7–24 months after treatment, and the survival rate of the whole group was 59% after 13 months. Conclusion. A daily dose of 10–24 × 106 IU/m2/day of IL-2 administered intrapleurally gave response rates similar to those reported in the literature using the intravenous route, but a much lower morbidity rate was recorded.