Rhône-Poulenc

About: Rhône-Poulenc is a based out in . It is known for research contribution in the topics: Alkyl & Catalysis. The organization has 8909 authors who have published 8934 publications receiving 182241 citations. The organization is also known as: Rhone-Poulenc.

Diversity Profiling and Design Using 3D Pharmacophores: Pharmacophore-Derived Queries (PDQ)

Abstract: The current interest in combinatorial chemistry for lead generation has necessitated the development of methods for design and evaluation of the diversity of the resultant compound libraries. Such methods also have application in selecting diverse sets of compounds for general screening from corporate databases and in the analysis of large sets of structures to identify common patterns. In this paper we describe a novel methodology for calculating diversity and identifying common features based on the three-point pharmacophores expressed by a compound.1 The method has been implemented within the environment of the Chem-X molecular modeling package (ChemDBS-3D), using a systematic analysis of 3D distance space with three point combinations of six pharmacophoric groups. The strategy used to define the pharmacophores is discussed, including an in-house developed atom type parameterization. The method is compared with the related approach being developed into the ChemDiverse module of Chem-X. Results from an ...

Low-Molecular-Weight Heparins: An Overview of their Pharmacodynamics, Pharmacokinetics and Metabolism in Humans

Abstract: Low-molecular-weight heparins (LMWHs) comprise a group in the class of antithrombotic medications, a class headed by unfractionated heparin (UFH). The LMWHs, with mean molecular weights of 4.0-6.0 kD, differ in their individual manufacturing processes, the distribution of their fragment molecular weights, their in vitro potency (anti-Xa, antithrombin and anticoagulant activities) and, consequently, in their biodynamic patterns, recommended dose regimen, and efficacy/safety ratio. Their drug disposition profiles have been evaluated using two significant markers of their pharmacodynamic activity, namely anti-Xa and anti-IIa activities. Since they are mainly administered subcutaneously, then compared to UFH, they are almost completely absorbed (F > or = 90%) and, in contrast to UFH, those for which data are available in the literature exhibit linear pharmacokinetics with proportionality between anti-Xa (and anti-IIa in some cases) plasma concentration and dose, and stationary distribution volume and clearance processes when the dosage is increased. Their distribution volume is close to the blood volume, they are partially metabolized by desulphatation and depolymerization, but urinary excretion of anti-Xa activity for enoxaparin, dalteparin and nadroparin, all given at doses for prevention of venous thrombosis, is between 5 and 10% of the injected dose. However, these LMWHs differ in the extent of their non-renal clearance, resulting in different apparent elimination half-life values and relative apparent bioavailability. When considering certain at-risk situations, using doses for preventing thromboembolism, the LMWHs do not significantly cross the placenta of pregnant women and their excretion profiles are only slightly altered in severe (endogenous creatinine clearance less than 15 ml/min) renal disease patients when given at doses recommended for prevention of venous thromboembolism. Because of the differences among LMWHs, the clinical profile of a given LMWH cannot be extrapolated to another one or generalized to the whole LMWH family.

Nucleic acid-containing composition, preparation and use thereof

Abstract: Pharmaceutical composition useful for transfecting a nucleic acid and characterised in that it contains, in addition to said nucleic acid, at least one transfecting agent and a compound causing the condensation of said nucleic acid, wherein said compound is totally or partly derived from a histone, a nucleoline, a protamine and/or a derivative thereof. The use of said composition for transferring nucleic acids in vitro, ex vivo and/or in vivo is also described.