Abstract: This polysaccharide consists of repeating units which are composed of a backbone, comprising 2 radicals of D-mannose, 2 of D-glucose, 1 of D-galactose, 1 of D-glucuronic acid, 1 of D-xylose, 1 of L-lyxose and 1 of L-fucose, on which pyruvic acid groups may be grafted and of which certain of the saccharide hydroxyl groups are esterified as acetate. It can be employed as a viscosity agent for thickening and gelling.
Type:
Grant
Filed:
September 24, 1992
Date of Patent:
October 3, 1995
Assignee:
Elf Sanofi
Inventors:
Thierry Fontaine, Bernard Fournet, Marie France Planard
Abstract: Recombinant DNA which codes for a protein with endochitinase activity or for a precursor thereof, comprising the sequence (a1) (SEQ ID NO. 1).
Type:
Grant
Filed:
September 8, 1992
Date of Patent:
August 29, 1995
Assignees:
Elf Sanofi, Societe Nationale Elf Aquitaine
Inventors:
Pierre-Louis Blaiseu, Richard Legoux, Jean-Jacques Leguay, Michel Schneider
Abstract: The subject of the invention is 2-(1-bromoethyl)benzo[b]thiophene of formula: ##STR1## as well as a process for the preparation thereof, characterised in that 2-ethylbenzo[b]thiophene is reacted, in a solvent, with a brominating agent in the presence of a free radical initiator, which provides the desired compound, and the use thereof in the preparation of 2-(1-(benzyloxyamino)ethyl)benzo[b]thiophene and of N-hydroxy-N-{1-(benzo[b]thien-2-yl)ethyl}urea.No figure.
Abstract: The invention relates to N-alkylenepiperidino compounds of formula ##STR1## as well as their enantiomers, and pharmaceutical compositions containing them that are useful as antagonists of neurokinin receptors in the treatment of substance P- and/or neurokinin-independent pathologies.
Type:
Grant
Filed:
May 4, 1992
Date of Patent:
May 2, 1995
Assignee:
Elf Sanofi
Inventors:
Xavier Edmonds-Alt, Serge Martinez, Vincenzo Proietto, Didier Van Broeck
Abstract: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group, each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.
Abstract: The subject of the invention is 4-hydroxyphenylthio derivatives of general formula: ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, each represent hydrogen, a methyl or ethyl radical or a halogen atom,R represents a (C.sub.1 -C.sub.6) alkyl, (C.sub.3 -C.sub.6) cycloalkyl or phenyl radical,R.sub.3 represents hydrogen or a halogen atom, X represents --O--, --S-- or --NR.sub.4 -- in which R.sub.4 represents hydrogen or a (C.sub.1 -C.sub.4) alkyl group, useful as synthetic intermediates, especially for the preparation of aminoalkoxyphenylsulphonyl derivatives which are pharmaceutically active compounds.
Abstract: The subject of the invention is new high molecular mass N,O-sulphated heparosans consisting of chains or of a mixture of chains having a molecular mass of between 1.5.times.10.sup.4 and 4.0.times.10.sup.6 D, characterized by a repeating disaccharide structure of formula I: ##STR1## in which E represents, in 0 to 80% of the disaccharide units of the said N,O-sulphated heparosan, an acetyl group and, in the remaining disaccharide units, a sulphate group and optionally a hydrogen atom, G represents a hydrogen atom and a sulphate group, and the pharmaceutically acceptable salts of the said N,O-sulphated heparosans.
Type:
Grant
Filed:
February 3, 1994
Date of Patent:
January 24, 1995
Assignee:
Elf Sanofi
Inventors:
Jean-Claude Lormeau, Bruno Chevallier, Marc L. V. Salome
Abstract: Heterocyclic substituted 2-acylamino-5-thiazoles, their preparation and pharmaceutical compositions containing them.A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
Type:
Grant
Filed:
March 3, 1994
Date of Patent:
January 10, 1995
Assignee:
Elf Sanofi
Inventors:
Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
Abstract: Compounds of formula ##STR1## in which R.sub.1 represents OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, benzyl, phenyl, (C.sub.1 -C.sub.4)alkylNZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; R.sub.2 represents OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio or NZ.sub.1 Z.sub.2 ; R.sub.3 represents H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl or benzyl; A represents N and R represents H or (C.sub.1 -C.sub.4)alkyl which can be substituted by phenyl or NZ.sub.1 Z.sub.2 ; B represents phenyl which is coupled to the pyridyl ring and is optionally substituted by one or more groups chosen from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; and Z.sub.1 and Z.sub.2 represent, independently of each other, H, (C.sub.1 -C.sub.6) alkyl, formyl or benzyl, or they form with the nitrogen atom to which they are attached an optionally substituted saturated heterocycle and their salts.
Type:
Grant
Filed:
August 19, 1993
Date of Patent:
November 1, 1994
Assignee:
Elf Sanofi
Inventors:
Andre Bachy, Laurent Fraisse, Peter Keane, Etienne Mendes, Jean-Claude Vernieres, Jacques Simiand
Abstract: The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1## wherein the substituents are as described in the specification, and to intermediates. The compounds are useful for antagonizing angiotensin II.
Type:
Grant
Filed:
June 23, 1993
Date of Patent:
October 4, 1994
Assignee:
Elf Sanofi
Inventors:
Claude Bernhart, Jean-Claude Breliere, Jacques Clement, Dino Nisato, Pierre Perreault, Claude Muneaux, Yvette Muneaux
Abstract: The microbeads are composed of a core containing the active ingredient and a microporous membrane, insoluble in aqueous medium, consisting of a film-forming polymer, a plasticizer and a filling material.The membrane has a thickness such that diltiazem is released in vitro at an approximately constant rate for at least 6 hours after a latent period of less than one hour.The active ingredient can be intimately mixed with the core or included in a polyvinyl pyrrolidone layer coating an inert grain.The sustained-release microbeads are formed by application to the core of a dispersion of the constituents of the membrane in a solvent and evaporation of the solvent.The pharmaceutical compositions consist of capsules containing the microbeads. They are administered orally one or twice per day, depending on the dose, for the treatment of angina or hypertension.
Abstract: Cycloaminoalkoxyphenyl derivatives useful for the treatment of certain pathological syndromes of the cardiovascular system and ocular diseases of formula: in which:B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denotes hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine,A denotes a straight or linear alkylene radical, having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical,Am denotes a group: ##STR1## in which: R.sub.3, R'.sub.3 and R".sub.3, which are identical or different, each denotes hydrogen, a halogen atom such as chlorine or bromine, a lower alkyl group or a lower alkoxy group, R.sub.4 denotes hydrogen or an alkyl radical,n and m, identical or different, each denotes 0, 1, 2 or 3,Cy represents a group of formula: ##STR2## pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
March 2, 1992
Date of Patent:
August 23, 1994
Assignee:
Elf Sanofi
Inventors:
Jean Gubin, Pierre Chatelain, Jean Lucchetti
Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## where Y. m. Ar', n, p, Q, T, q and Z are defined herein. The invention also relates to methods of making the compounds of formula (I) and pharmaceutical compositions which contain the compounds of formula (I). The inventive compounds are useful as neurokinin receptor antagonists, and are useful for the treatment of any substance P-dependent and neurokinin-dependent pathological condition.
Type:
Grant
Filed:
May 4, 1992
Date of Patent:
August 23, 1994
Assignee:
Elf Sanofi
Inventors:
Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Pierre Goulaouic, deceased, by Marie Bousquet, heir, by Catherine M. L. Goulaouic, heir
Abstract: The invention relates to N-sulfonyl derivatives of formulae (I)" and (I)' ##STR1## and to pharmaceutical compositions in which they are present. The compounds have an affinity for the vasopressin and ocytocin receptors.
Type:
Grant
Filed:
August 3, 1992
Date of Patent:
August 16, 1994
Assignee:
Elf Sanofi
Inventors:
Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
Abstract: The iontophoresis device for transcutaneous administration of the active principle to the subject comprises electrodes, at least one of which is a consumable electrode formed of an electrochemically consumable material associated either with an insulating support or with a particular electronically conducting support. The single consumable electrode or one of the consumable electrodes holds a limited quantity of electrochemically consumable material, the said limited quantity being chosen so that the quantity of electricity necessary for its electrochemical consumption corresponds to the quantity of electricity necessary for administering the given total quantity of active principle to the subject and the active principle is present at the start of the operation in a quantity greater than the said given total quantity.
Type:
Grant
Filed:
February 12, 1993
Date of Patent:
June 14, 1994
Assignees:
Societe Nationale Elf Aquitaine, Elf Sanofi
Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
Type:
Grant
Filed:
May 29, 1992
Date of Patent:
May 24, 1994
Assignee:
Elf Sanofi
Inventors:
Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
Abstract: The subject of the invention is new high molecular mass N,O-sulphated heparosans consisting of chains or of a mixture of chains having a molecular mass of between 1.5.times.10.sup.4 and 4.0.times.10.sup.6 D, characterised by a repeating disaccharide structure of formula I: ##STR1## in which E represents, in 0 to 80% of the disaccharide units of the said N,O-sulphated heparosan, an acetyl group and, in the remaining disaccharide units, a sulphate group and optionally a hydrogen atom, G represents a hydrogen atom and a sulphate group, and the pharmaceutically acceptable salts of the said N,O-sulphated heparosans.
Type:
Grant
Filed:
November 30, 1992
Date of Patent:
May 24, 1994
Assignee:
Elf Sanofi
Inventors:
Jean-Claude Lormeau, Bruno Chevallier, Marc L. V. Salome
Abstract: The invention relates to 2-amino-7-hydroxytetralin carboxyalkyl ethers of formula ##STR1## wherein Alk represents a straight or branched (C.sub.3 -C.sub.5)alkylene group, and R is hydrogen or (C.sub.1 -C.sub.4)alkyl, useful as starting materials in the synthesis of 7-substituted phenylethanolaminotetralins of formula (XII) ##STR2## wherein X represents hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, or trifluoromethyl which are useful as spasmolytics and anti-glaucoma agents.The new 7-substituted phenylethanolaminotetralins (XII) as well as the intermediates in the preparation of the compounds (I), the N-protected 2-amino-7-hydroxytetralin carboxyalkyl ethers, are also claimed.
Abstract: The invention relates to intermediates in the production of dialkylenepiperidino compounds and their enantiomers and their use for the treatment of substance p- and neurokinin-dependent pathology.
Type:
Grant
Filed:
May 4, 1992
Date of Patent:
April 5, 1994
Assignee:
Societe Anonyme: Elf Sanofi
Inventors:
Xavier Emonds-Alt, Isabelle Grossriether, Vincenzo Proietto, Didier Van Broeck
Abstract: The present invention relates to a kit for the specific assay of Angiotension II, comprising:the anti-Ang II antibody,a solution of labelled Ang II,solutions containing the Ang II standards at known and increasing concentrations,the requisite washing solution(s),a solution of anti-Ang III antibody, the said antibody exhibiting a cross-reaction with Ang II of less than 10% and preferably less than 5%,and, optionally, a solution of anti-Ang I antibody and/or a solution of anti-pentapeptide antibody and/or a solution of anti-hexapeptide antibody, the said antibodies exhibiting a cross-reaction with Ang II of less than 10% and preferably less than 5%.
Type:
Grant
Filed:
July 5, 1991
Date of Patent:
March 22, 1994
Assignee:
Elf Sanofi
Inventors:
Dominique Simon, Jean Marchand, Gabriel Badouaille, Bernard Romestand, Jean-Alain Fehrentz