Abstract: Crystallized anhydrous zilpaterol hydrochloride having less than 5% of the crystals with a size of less than 15 microns and at least 95% of the crystals having a size of less than 250 microns and a process for its preparation and novel intermediates.
Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are as set forth below.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
March 17, 1998
Assignee:
Roussel Uclaf
Inventors:
Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.
Abstract: Described herein are compounds of the formula ##STR1## wherein the substituents are defined as in the specification having inhibiting activity on the effects of angiotensin II.
Type:
Grant
Filed:
August 1, 1994
Date of Patent:
February 3, 1998
Assignee:
Roussel Uclaf
Inventors:
Alain Corbier, Jean Paul Vevert, Jidong Zhang
Abstract: A protein having sucrose phosphate synthetase (SPS) activity is isolated from plants, preferably maize. The protein has a molecular weight of 110-130 dK and contains at least one peptide selected from Thv Trp Ile Lys, Try Val Val Glu Leu Ala Arg, Ser Met Pro Pro Ile Trp Ala Glu Val Met Arg, Leu Arg Pro Asp Gln Asp Try Leu Met His Ile Ser His Arg and Trp Ser His Asp Gly Ala Arg. Isolation is carried out by obtaining an extract from the plant by grinding, centrifugation and filtration; enriching the extract in SPS protein by precipitation in an appropriate solvent such as polyethylene glycol, centrifugation and solubilization of the precipitate obtained in a buffer solution; subjecting the protein thus obtained to low pressure anion exchange chromatography, chromatography on heparin Sepharose and high pressure anion exchange chromatography; and purifying the active fractions obtained by passage through two high pressure chromatography columns.
Type:
Grant
Filed:
January 23, 1995
Date of Patent:
February 3, 1998
Assignee:
Roussel UCLAF
Inventors:
Charles Van Assche, Danielle Lando, Jean Michel Bruneau, Toni Alois Voelker, Monica Gervais
Abstract: A method of treating prostate cancer in warm-blooded animals comprising administering to warm-blooded animals an effective amount of a peptide of Formula I and an anti-androgen.
Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
January 27, 1998
Assignee:
Roussel Uclaf
Inventors:
Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
Abstract: The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having a very good antibiotic activity.
Abstract: A soft capsule containing a) a capsule casing containing gelatin and optionally a plasticizer and other additives, b) a compound of the formula ##STR1## wherein R1, R2 and R3 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --CF3, --NO2, --NH2, alkylamino and dialkylamino of 1 to 5 alkyl carbon atoms and acylamino of acyl of an aliphatic carboxylic acid of 1 to 6 carbon atoms or a non-toxic, pharmaceutically acceptable acid addition salt thereof and c) at least one mineral oil and optionally a pharmaceutical carrier.
Type:
Grant
Filed:
February 28, 1996
Date of Patent:
January 13, 1998
Assignee:
Roussel Uclaf
Inventors:
Philippe Becourt, Jean-Luc Dubois, Pierre Metziger
Abstract: A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##
Type:
Grant
Filed:
May 28, 1993
Date of Patent:
January 13, 1998
Assignee:
ROUSSEL UCLAF
Inventors:
Andre Claussner, Daniel Philibert, Lucien Nedelec, Patrick Van De Velde, Francois Nique, Jean-Georges Teutsch
Abstract: Disclosed is a method of inducing anti-estrogenic activity in warm-blooded animals by the administration of a compound of the formula ##STR1## wherein the substituents are as defined in the specification.
Type:
Grant
Filed:
August 8, 1995
Date of Patent:
January 6, 1998
Assignee:
Roussel-Uclaf
Inventors:
Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
Type:
Grant
Filed:
March 1, 1996
Date of Patent:
January 6, 1998
Assignee:
Roussel Uclaf
Inventors:
Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
Abstract: A sequence of anti-direction, anti-messenger RNA oligonucleotides of .alpha.-TNF characterized in that it possesses the structure of the formula ##STR1## wherein X is hydrogen, or a sequence of 1 to 17 oligonucleotides in free form, in alkylated form, in sulfurated form or in the form of a poly L-lysine derivative useful for stopping the production of .alpha.-TNF.
Type:
Grant
Filed:
November 18, 1994
Date of Patent:
January 6, 1998
Assignee:
Roussel Uclaf
Inventors:
Abdel Karim Braham, Pierre Smets, Rene Zalisz
Abstract: A process for the preparation of granules containing at least one active principle with a melting point above 70.degree. C. selected from the group consisting of herbicides, fungicides and insecticides comprising dissolving the active principle in an aromatic solvent or pyrrolidone, absorbing the resulting solution on a support, optionally adding water thereto and drying the resulting product to form the granules and the granules produced thereby which have a superior biological activity than a granule dispersible in water with good stability.
Abstract: Described herein are novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
Type:
Grant
Filed:
August 12, 1996
Date of Patent:
January 6, 1998
Assignee:
Roussel Uclaf
Inventors:
Andre Claussner, Francois Goubet, Jean-Georges Teutsch
Abstract: The present invention relates to new nucleotide sequences coding for variable regions of .beta. chains of human T lymphocyte receptors, corresponding peptide segments and the diagnostic and therapeutic uses.
Abstract: A method of treating male sterility linked to insufficient fertilizing power of the spermatozoa in warm-blooded animals comprising administering to warm-blooded animals an amount of a compound of formula I or its acid addition salts sufficient to increase the fertilizing power of spermatozoa.
Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is cyclopropyl or --CH.sub.2 --CH.dbd.CH.sub.2, R.sub.2 is --S(O).sub.n --(CF.sub.2).sub.x --CF.sub.3, n is 1 or 2, x is 0 or 1, R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms, m is 0 or 1 and its non-toxic, pharmaceutically acceptable addition salts with a base having anti-inflammatory activity.
Type:
Grant
Filed:
September 26, 1996
Date of Patent:
December 2, 1997
Assignee:
Roussel UCLAF
Inventors:
David Paul Kay, Elizabeth Anne Kuo, Richard Alexander Williamson
Abstract: The bicyclic derivatives of pyridines of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts and a process and intermediates for their preparation which compounds are inhibitors of angiotensin II effects, particularly a vasoconstrictor activity.
Type:
Grant
Filed:
April 20, 1995
Date of Patent:
November 25, 1997
Assignee:
Roussel Uclaf
Inventors:
Alain Corbier, Michel Fortin, Jacques Guillaume, Jean-Luc Haesslein, Jean-Paul Vevert