Showing papers by "Rhône-Poulenc published in 1987"
Patent•
16 Jul 1987TL;DR: Taxol derivatives of formula STR1 are useful antitumor agents as mentioned in this paper, in which R represents hydrogen or acetyl, one of R 1 or R 2 represents hydroxy and the other represents tert-butoxy carbonylamino.
Abstract: Taxol derivatives of formula ##STR1## in which R represents hydrogen or acetyl, one of R 1 or R 2 represents hydroxy and the other represents tert-butoxycarbonylamino and their isomers are useful antitumor agents.
380 citations
Patent•
05 Jan 1987TL;DR: In this paper, plants are developed which are resistant to bromoxynil and are capable of expressing the nitrilase enzyme to provide detoxification of an environment and protect benzonitrile herbicide-sensitive cells from its cytotoxic effect.
Abstract: Nitrilase enzymes specific for the hydrolysis of the nitrile group of benzonitriles, eg. bromoxynil or ioxynil, nucleotide sequences encoding for such enzymes, and transformed cells in which the nitrilase expression is foreign are provided. The transformed cells are capable of expressing the nitrilase enzyme to provide detoxification of an environment and protect benzonitrile herbicide-sensitive cells from its cytotoxic effect. Plants are developed which are resistant to bromoxynil.
293 citations
TL;DR: In this article, the influence of surface area and additives on the transformation of transition aluminas into alpha alumina was studied using differential thermal analysis and by measuring the rate of transformation by X-ray diffraction of samples calcined at numerous intervals during a 50 hour period.
224 citations
TL;DR: Genetic transformation by root inducing (Ri) T-DNA from Agrobacterium rhizogenes increased biomas and tropane alkaloid production in axenic root cultures of Calystegia sepium and Atropa belladonna and is suggested to improve the production of secondary metabolites in vitro.
157 citations
TL;DR: The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function.
135 citations
TL;DR: Radioautographic studies of [125I-Tyr3]NT binding to rat brain tissue sections in the absence and presence of levocabastine revealed markedly different regional distributions of the two NT binding components.
133 citations
TL;DR: In this paper, a theoretical model for spherical particeles based on the annihilation of vacancies as the rate-determining step leads to a kinetic law involving the initial specific surface area, the valency of the foreign cation, and a parameter which depends on its ionic radius.
130 citations
TL;DR: It is demonstrated that viral RNAs are specific targets for the oligonucleotide-acridine conjugate that inhibits the cytopathic effect of type A influenza viruses.
Abstract: Oligodeoxynucleotides covalently linked to an acridine derivative were targeted to part of the 3'-terminal sequence which is common to the eight RNAs of type A influenza viruses. The cytopathic effect of the virus on MDCK cells in culture was strongly decreased by a heptanucleotide covalently attached to the acridine ring. Control experiments using other oligonucleotide sequences showed that the effect was specific for the complementary sequence of the 3'-terminal region of the viral RNAs. The RNA transcriptase reaction of a type A virus was also selectively inhibited in vitro by the heptanucleotide-acridine conjugate. A type B influenza virus was used as a control. The common sequence at the 3' end of its eight viral RNAs is different from that of type A viruses. Three mismatches were expected with the heptanucleotide which was fully complementary to type A viral RNAs. This heptanucleotide had no effect on the cytopathic effect of a type B influenza virus. These results demonstrate that viral RNAs are specific targets for the oligonucleotide-acridine conjugate that inhibits the cytopathic effect of type A influenza viruses.
113 citations
Patent•
29 Jun 1987TL;DR: In this article, the authors propose to use a semipermeable polyvinylidene fluoride (PVFD) and a hydrophilic polymer compatible therewith, e.g., a cellulose acetate or sulfonated polysulfone.
Abstract: Hydrophilic semipermeable membranes which retain their capacity for filtration, even after drying, and which are well adapted for either ultrafiltration or microfiltration, are comprised of at least 70% by weight of polyvinylidene fluoride (PVFD) and up to 30% by weight of a hydrophilic polymer compatible therewith, e.g., a cellulose acetate or sulfonated polysulfone.
90 citations
TL;DR: Some tripeptides obtained by enzymic digestion of caseins possess immunomodulating properties and X‐ray analysis has been applied to two of them Leu‐Leu‐Tyr and Gly‐Leo‐Phe in order to correlate activity and structure.
80 citations
Patent•
16 Jul 1987TL;DR: Taxol and 10-deacetyltaxol are derived from a compound of formula: STR 1, in which R' represents acetyl or 2,2,2-trichloroethoxy carbonyl radical, by removal of the t-butoxycarbonyls radical, benzoylation of the amine product obtained, and removal of 2.2, 2, 2, 2,1,2 trichlorosophosphoric acid group(s).
Abstract: Taxol and 10-deacetyltaxol are prepared from a compound of formula: ##STR1## in which R' represents acetyl or 2,2,2-trichloroethoxycarbonyl radical, by removal of the t-butoxycarbonyl radical, benzoylation of the amine product obtained, and removal of the 2,2,2-trichloroethoxycarbonyl group(s).
TL;DR: In vitro permeability studies of water, butanol, and a representitive peptide through oral mucosa from hamster and dog reveal similar permeability characteristics for these tissues, and preliminary experiments confirm that the buccal route has substantial potential for administration of peptides.
TL;DR: Methods for producing axenic spores of the VA mycorrhizal fungus Glomus mosseae are described and the spores did not readily germinate on agar but the soil actinomycete Streptomyces orientalis stimulated germination.
Abstract: Methods for producing axenic spores of the VA mycorrhizal fungus Glomus mosseae are described. The spores did not readily germinate on agar but the soil actinomycete Streptomyces orientalis stimulated germination. Spores stored in moist atmosphere at 4° can remain viable for 4 years; under dry conditions, the death of spores seemed to be directly related to water activity.
TL;DR: The data presented here suggest that the successful treatment of paraquat poisoning will not be achieved by modification of toxicokinetics, and that when these techniques of elimination are initiated, potentially lethal concentrations of paraaquat have already been attained in the highly vascular tissues of vital organs and in pneumocytes.
Abstract: 1 There is a striking discrepancy between the efficacy of the kidneys, haemodialysis and haemoperfusion in removing paraquat from the body and the poor prognosis of paraquat poisoning even when the...
Patent•
02 Sep 1987TL;DR: In this paper, the authors present a composition for coating a biologically active substance which is stable in a medium in which the pH is greater than or equal to 5 and which permits the release of the active substance in the medium which is less than, or equal, to 3.5.
Abstract: A composition for coating a biologically active substance which is stable in a medium in which the pH is greater than or equal to 5 and which permits the release of the active substance in a medium in which the pH is less than or equal to 3.5, comprises a film-forming, water-insoluble binder which possesses controlled hydrophilicity and is optionally slightly sensitive to pH variations, and a substance which is sensitive to pH variations (e.g. an inorganic filler, simple aminated substance, basic polymer or copolymer, chitosan). Pellets for feeding to ruminants consist of a core containing the biologically active substance, e.g. methionine or lysine, coated with this substance.
Patent•
09 Nov 1987TL;DR: In this article, stable factor VIII and other plasma protein formulations are provided in low ionic strength media which comprises: sodium chloride, potassium chloride or mixtures thereof; lysine hydrochloride; and histidine as the buffering agent.
Abstract: Stable factor VIII and other plasma protein formulations are provided in low ionic strength media which comprises: sodium chloride, potassium chloride or mixtures thereof; lysine hydrochloride; and histidine as the buffering agent.
TL;DR: The recombinant HSA is produced essentially as an insoluble aggregate and differs from natural HSA by the presence of a methionine at the N-terminus, but the Met-HSA could be re-natured, purified and was found to be very similar to the natural protein.
Abstract: Significant synthesis of Human Serum Albumin (HSA) was demonstrated in E. coli using efficient bacterial expression signals. The recombinant HSA is produced essentially as an insoluble aggregate and differs from natural HSA by the presence of a methionine at the N-terminus. However, the Met-HSA could be re-natured, purified and was found to be very similar to the natural protein. A procedure was devised to produce mature HSA starting with the authentic N-terminal sequence from E. coli. By analogy with the maturation of the HSA propeptide, a plasmid expressing a fusion between the first six residues of the bacteriophage λcII protein (Val-Arg-Ala-Asn-Lys-Arg-) and the sequence of mature HSA was constructed. After renaturation, this fusion protein was cleaved by trypsin in vitro to yield a mature refolded HSA with native N-terminal sequence. This protein could not be distinguished by several criteria from authentic natural HSA.
Patent•
04 Mar 1987TL;DR: In this paper, the use of a malonic acid derivative compound for inducing synergistic plant growth regulating responses or ethylene responses was discussed. But the use was restricted to a single plant growth regulator.
Abstract: This invention relates to synergistic plant growth regulator compositions containing (1) an ethylene response or ethylene-type response inducing agent and (11) a malonic acid derivative compound This invention also relates to the use of said compositions for inducing synergistic plant growth regulating responses or ethylene responses or ethylene-type responses
TL;DR: The purified angiogenin was demonstrated to be active as an angiogenic factor and exhibited a characteristic RNase activity.
Patent•
03 Sep 1987TL;DR: In this article, a composition for coating a biologically active substance, which is stable in a medium with a pH greater than or equal to 5 and which enables the active substance to be released from a mixture of a basic amino copolymer and a hydrophobic substance with a melting point greater than 60° C.
Abstract: A composition for coating a biologically active substance, which is stable in a medium with a pH greater than or equal to 5 and which enables the active substance to be released in a medium with a pH less than or equal to 3.5, consisting of a basic amino copolymer (preferably vinyl-pyridine/styrene copolymer) and a hydrophobic substance with a melting point greater than 60° C. (preferably stearic acid), the hydrophobic substance content being between 50 and 90% of the total mass of the coating, and granules comprising a nucleous containing the biologically active substance, coated with this composition.
Patent•
16 Nov 1987TL;DR: In this paper, a biologically active substance water-soluble, stable in a medium whose pH is greater than or equal to 5 and allowing the release of the active substance in medium with pH less than 3.5 is described.
Abstract: Composition pour l'alimentation des ruminants contenant une substance biologiquement active hydrosoluble, stable dans un milieu dont le pH est superieur ou egal a 5 et qui permet la liberation de la substance active dans un milieu dont le pH est inferieur a 3,5 comprenant : Composition for ruminant feed containing a biologically active substance water-soluble, stable in a medium whose pH is greater than or equal to 5 and allowing the release of the active substance in a medium whose pH is less than 3.5 comprising: - un noyau contenant la substance active, ayant eventuellement subi un traitement de surface - a core containing the active substance, which has optionally undergone a surface treatment - une premiere couche d'enrobage constituee d'une substance filmogene sensible aux variations du pH eventuellement associee a une charge minerale, et - a first coating layer of a substance sensitive film changes in pH may be associated with an inorganic filler, and - une seconde couche d'enrobage constituee d'une substance hydrophobe eventuellement associee a une charge minerale. - a second coating layer consisting of a hydrophobic substance optionally combined with an inorganic filler.
TL;DR: Gelfiltration of 35S-heparin and35S-PK 10169 before and after binding to endothelial cells demonstrated a selective binding of high molecular weight molecules from polydisperse heparinand PK 10169 preparations.
Patent•
08 Jun 1987TL;DR: In this article, a polyamide-based molding composition having enhanced flexibility and resilience, especially at low temperatures, are prepared from (1) semirigid copolyamides prepared from fatty acid dimers, (2) elastomers containing moieties compatible or reactive with such copoly amides, and (3) conventional polyamides.
Abstract: Polyamide-based molding compositions having enhanced flexibility and resilience, especially at low temperatures, are prepared from (1) semirigid copolyamides prepared from fatty acid dimers, (2) elastomers containing moieties compatible or reactive with such copolyamides (1) and comprising olefinic copolymers bearing carboxyl and/or carboxylate groups, copolyester-amides, polyurethanes, organopolysiloxane and polyurethane block copolymers, and copolymers produced from a latex which comprises suitable functional groups, and, optionally, (3) conventional polyamides.
TL;DR: A randomized, double-blind, comparative trial of zopiclone versus nitrazepam was conducted in 74 geriatric chronic insomniac patients, finding that zopicLone was devoid of effect on neurological function and the condition on awakening was better with zopic lone.
Abstract: A randomized, double-blind, comparative trial of zopiclone versus nitrazepam was conducted in 74 geriatric chronic insomniac patients. Following a 7-day wash-out period, two parallel groups, successively received a placebo for 7 days, then either 7.5 mg zopiclone or 5 mg nitrazepam for another 7-day period. Efficacy on sleep was assessed by a sleep analogue scale and the Spiegel Sleep Questionnaire, residual effects by psychometric tests and tolerance by a standardized question, as well as by clinical and laboratory tests. Zopiclone and nitrazepam were more active than placebo on all tests of efficacy. In contrast with nitrazepam, zopiclone was devoid of effect on neurological function. In addition, the condition on awakening was better with zopiclone.
Patent•
18 Dec 1987TL;DR: In detergent or rinsing compositions containing an antisoiling and anti-redeposition latex consisting of vinyl copolymers characterized in that they consist either of copolymer of vinyl acetates with unsaturated carboxylic acids grafted with sulphonic polyesters in which the acetate functions are optionally at least partially saponified as mentioned in this paper.
Abstract: 1. Detergent or rinsing compositions containing an antisoiling and anti-redeposition latex consisting of vinyl copolymers characterized in that these copolymers consist either of copolymers of vinyl acetates with unsaturated carboxylic acids grafted with sulphonic polyesters in which the acetate functions are optionally at least partially saponified, or of copolymers of (meth)acrylic esters grafted with sulphonic polyesters.
Patent•
16 Jan 1987TL;DR: In this paper, a process for the production of precipitation silica by maintaining a constant-volume reaction medium to provide suitable colloids of silica, reacting the colloids with an electrolyte and consolidating the resulting product by the addition of a solution of silicate and an acidifying agent to obtain a precipitationsilica.
Abstract: Precipitation silicas, in the form of aggregates as shown in FIG. 1, having a mean projected area of the aggregates which is higher than about 8,000 nm 2 and preferably is higher than about 15,000 nm 2 . The present invention also concerns a process for the production of precipitation silica by maintaining a constant-volume reaction medium to provide suitable colloids of silica, reacting the colloids with an electrolyte and consolidating the resulting product by the addition of a solution of silicate and an acidifying agent to obtain a precipitation silica.
TL;DR: The kinetics of induced crystallization during uniaxial stretching of amorphous poly(ethylene terephthalate) films and annealing of oriented samples were studied in this paper.
TL;DR: This method has been successfully applied to pharmacokinetic studies of zopiclone and its two main metabolites in healthy subjects and patients with chronic renal failure.
TL;DR: Results indicate that DA-1 and DA-2 dopamine receptor agonists can be easily discriminated on the basis of their cardiovascular profiles.
Abstract: This report summarizes studies aimed to characterize pharmacologically, hemodynamically and biochemically DA-1 (fenoldopam) and DA-2 (quinpirole) dopamine receptor agonists in anesthetized rats. Fenoldopam (20 micrograms/kg/min i.v. over 15 min) and quinpirole (10 micrograms/kg/min i.v. over 15 min) share the common property of decreasing mean carotid artery blood pressure by lowering peripheral vascular resistance. Fenoldopam increased mesenteric and renal blood flows whereas quinpirole decreased the former blood flow, but enhanced the latter. These effects of quinpirole were antagonized selectively by S-sulpiride, but not SCH 23390; however, with fenoldopam the reverse was found. In chlorisondamine-pretreated rats with blood pressure supported by vasopressin, fenoldopam, but not quinpirole, caused hypotension. In nephrectomized rats, the blood pressure effects of fenoldopam (assessed as area under the infusion time-response curve) were more pronounced than in sham-operated controls. The hypotensive effects due to an i.v. bolus injection of fenoldopam, but not to acetylcholine, histamine, salbutamol or quinpirole, were significantly inhibited in rats pretreated with an infusion of fenoldopam. In pithed rats, quinpirole reduced the pressor responses to electrical stimulation of the spinal cord without affecting those to exogenous norepinephrine, angiotensin II or 5-hydroxytryptamine which, on the contrary, were inhibited by fenoldopam. The plasma renin activity (in intact rats) was reduced by quinpirole, but elevated by fenoldopam. The latter effect also occurred in pithed rats and was blocked by SCH 23390. Quinpirole lowered heart rate, whilst fenoldopam produced tachycardia. These effects of quinpirole and fenoldopam were significantly inhibited by S-sulpiride and SCH 23390, respectively. In chlorisondamine-pretreated rats quinpirole failed to change heart rate whereas fenoldopam still increased it. In conclusion, these results indicate that DA-1 and DA-2 dopamine receptor agonists can be easily discriminated on the basis of their cardiovascular profiles.
Patent•
17 Jun 1987TL;DR: In this paper, an analysis assembly consisting of at least two analysis stations having different characteristics, and a module delimiting temporary storage slots for receptacles containing different substances to be analyzed by different methods applicable to each of said substances, is presented.
Abstract: Apparatus for automatically taking and analyzing samples of substances made available in random manner, is of the type comprising an analysis assembly including at least two analysis stations having different characteristics, and a module delimiting temporary storage slots for receptacles containing different substances to be analyzed by different methods applicable to each of said substances, said apparatus comprising: receptacles each bearing a code identifying the substance contained therein, the analysis treatment to which is is to be subjected, and a treatment priority attributed thereto; means for detecting the in-use or available status of each analysis station; means for scanning the slots in the storage module for reading the codes of the receptacles and for storing them in priority order in conjuction with the characteristics of the corresponding treatment and the addresses of the slots; means for seeking in priority order correspondence between the treatments to be performed and a currently available compatible analysis station; means for displacing an insertion system into relationship with the available analysis station; means for bringing the selected sample receptacle into relationship with an extraction station; means for extracting at least a portion of the sample from the selected receptacle and for transferring it into the insertion system; means for inserting the sample into the analysis station; means for controlling the operating conditions of the analysis station as a function of the analysis treatment to be performed; and means for returning the insertion system to its home position in readiness for a new operating cycle.