Abstract: The invention relates to oligonucleotides and their derivatives to inhibit the expression of isoprenyl protein transferases, therapeutic compositions containing such compounds and the use of such compositions of oligonucleotides for the treatment or therapy of diseases of the human or animal body induced by an abnormal and/or uncontrolled cellular proliferation.
Type:
Grant
Filed:
June 23, 1995
Date of Patent:
January 5, 1999
Assignee:
Societe De Conseils De Recherches Et D'Applications Scientifiques (S.C.R.A.S.)
Abstract: The invention relates to a method of treating and a therapeutical composition for the treatment of Acquired Immuno Deficiency Syndrome (AIDS) and related infections. The composition comprises from 1 to 100% of a complex of Poly(A).Poly(U), preferably associated with other anti-AIDS coagents which act on the HIV virus according to a different mechanism from that of the complex of Poly(A).Poly(U). The composition is suitably administered in 100 to 4000 mg doses and at 3 to 5 day intervals.
Type:
Grant
Filed:
March 13, 1997
Date of Patent:
April 7, 1998
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Ara G. Hovanessian, Evelyne Deschamps de Paillette
Abstract: Peptides derived from the C terminal sequence of sorbin, but containing at least one D-amino acid residue, inhibit pepsin release and are therefore likely to be useful in the treatment of ulcers or oesophagitis. Their salts and substitution derivatives are also claimed as a pharmaceutical compositions containing them. A method for the treatment of a patient suffering from gastric ulcers or oesophagitis comprising the administration of said peptides, is also claimed.
Type:
Grant
Filed:
March 15, 1995
Date of Patent:
September 16, 1997
Assignee:
Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)
Abstract: A two-step process for converting ginkgolide C into ginkgolide B is disclosed. In the first step, ginkgolide C is reacted with a sulfonic anhydride to obtain a C-7 sulfonate of ginkgolide C. In the second step, the C-7 sulfonate of ginkgolide C is reacted with a borohydride, and this reaction eliminates the C-7 radical of the C-7 sulfonate of ginkgolide C, thus producing ginkgolide B.
Type:
Grant
Filed:
August 4, 1994
Date of Patent:
February 4, 1997
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S)
Abstract: The invention relates to thieno-triazolo-diazepine derivatives of the formula: ##STR1## wherein Y stands for oxygen or sulphur and R stands for various substituents, to a preparation process of said compounds and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-asthmatic, anti-allergic and gastro-intestinal protectors.
Type:
Grant
Filed:
February 18, 1992
Date of Patent:
February 20, 1996
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Braquet, Andre Esanu, Jean-Pierre Laurent, Alain Rolland
Abstract: The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein:A represents a cyclooxygenase inhibitor having an accessible acidic function andB represents the L-form of arginine analogues of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent various substituents, process for the preparation of such compounds and pharmaceutical composition thereof.
Type:
Grant
Filed:
December 23, 1992
Date of Patent:
January 2, 1996
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Pierre-Etienne Chabrier De Lassauniere, Pierre Braquet, Colette Broquet, Serge Auvin
Abstract: The invention relates to a N-(2,4- or 2,5-disubstituted tetrahydrofuryl alkyl)-N-(phenylethyl-.beta.-ol)amine derivative, under a racemic or enantiomer form, of general formula I ##STR1## wherein R represent various radicals and n is of from 1 to 10, to a process for the preparation of said derivative, and to pharmaceutical compositions comprising the same.
Type:
Grant
Filed:
July 13, 1993
Date of Patent:
September 5, 1995
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Serge Auvin, Pierre Braquet, Colette Broquet
Abstract: The invention relates to benzofuranylimidazole derivatives of the general formula (1) ##STR1## wherein R.sub.1 and R.sub.2 represent various radicals, to a process for their preparation and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 2, 1993
Date of Patent:
October 11, 1994
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Jesus A. Garcia Sevilla, Jose J. Meana Martinez, Fernando Barturen Fernandez, Fernando A. Geijo Caballero, Angel Menargues Banos, Rosendo Obach Vidal, Francesc Pla Rodas
Abstract: The invention relates to benzofuranylimidazole derivatives of the general formula (1) ##STR1## wherein R.sub.1 and R.sub.2 represent various radicals, to a process for their preparation and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 23, 1992
Date of Patent:
May 10, 1994
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S)
Inventors:
Jesus A. G. Sevilla, Jose J. M. Martinez, Fernando B. Fernandez, Fernando A. G. Caballero, Angel M. Banos, Rosendo O. Vidal, Francesc P. Rodas
Abstract: An osmotic pump comprises a housing (2) within which is a delivery chamber (5) separated from an osmotic salt chamber (7) by impermeable moveable pressure responsive means such as a piston (6) or a flexible membrane. The osmotic salt chamber (7) is separated from a source of osmotic fluid, e.g. an osmotic fluid chamber (12), by a semipermeable membrane (96,36), optionally mounted in a piston (9,23). A fluid barrier isolates the osmotic salt chamber (7) from the source of osmotic fluid for storage of the pump, and may be inactivated when the pump is to be used. The fluid barrier may be a foil sheet (10), inactivatable by rupture, or a piston and a fluid bypass arrangement (21,23). Activation of the osmotic pump may be effected in some embodiments by loading the discharge chamber (5) with the agent to be delivered and in other embodiments by movement of a plunger (16), under manual control or, if the plunger is pre-biassed, by release of a locking means (18) which holds it in position.
Type:
Grant
Filed:
December 4, 1991
Date of Patent:
January 18, 1994
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: The invention relates to a process for the preparation of ginkgolide B from ginkgolide C and to ginkgolide B thus obtained, the process comprising the following succession of four steps:protecting the 10-hydroxy group of ginkgolide C by conversion to an alkyl ester, the reaction being effected in dimethylformamide at a temperature of from 15.degree. to 50.degree. C. for from 4 to 10 hours;activating the 7-hydroxy group of the resultant 10-protected ginkgolide C by conversion to a (R)thiocarbonyl ester, the activation being effected in basic conditions at a temperature of from 0.degree. to 40.degree. C. for from 1 to 24 hours;deoxygenating the 7-activated group in the resultant 10-protected 7-activated ginkgolide C by treating it with tributyltin hydride or tris-(trimethylsilyl)silane, in an aprotic solvent, in the presence of a free-radical generator, the reaction being effected at a temperature of from 70.degree. to 110.degree. C.
Type:
Grant
Filed:
March 30, 1992
Date of Patent:
August 31, 1993
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: The invention relates to a preparation process of particles designed to release an effective amount of active ingredient over a predetermined period of time, said particles comprising one ore more active ingredients in admixture with a bioresorbable and/or biodegradable polymer or copolymer, and the particles thus obtained in a substantially spheroidal form and substantially deprived of active ingredient on the external covering.
Type:
Grant
Filed:
July 23, 1991
Date of Patent:
May 25, 1993
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: The invention relates to pyrrolo-pyridine derivatives of the formula: ##STR1## wherein R represents a phenyl group, optionally substituted by one or more of various groups and therapeutically acceptable salts of these compounds, to a preparation process of the same comprising reacting, in an inert atmosphere and in a protic solvent, the 2-methyl 3-hydroxy 4,5-diboromomethyl pyridine, on a stoichiometric excess of the compound of the formula NH.sub.2 -R.The invention relates also to therapeutic compositions containing said derivatives as active ingredient.The compounds according to the invention have antiallergic activity.
Type:
Grant
Filed:
May 31, 1991
Date of Patent:
December 1, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: A method for inhibiting blood vessel blockage in a mammal particularly after a procedure such as angioplasty, an arterial bypass operation or an allograft transplant operation which comprises: administering to a mammal before, during and/or after the procedure an effective blood vessel blockage inhibiting amount of an octapeptide having the formula ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o-, m- or, more preferably, p-substituted X-Phe (where X is a halogen, H, NH.sub.2, NO.sub.2, OH , or C.sub.1-13 alkyl), pentafluoro-Phe, or .beta.
Type:
Grant
Filed:
March 28, 1989
Date of Patent:
September 15, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: The invention relates to 3-(N-methyl-N-alkyl)-amino 2-methoxymethylene propan 1-ol derivatives of the formula ##STR1## wherein R stands for an alkyl chain, A stands for: ##STR2## and Y represents various quaternary ammonia, to a preparation process of said compounds and to therapeutic compositions containing the same.
Type:
Grant
Filed:
November 27, 1990
Date of Patent:
June 2, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Braquet, Colette Broquet, Benedicte Vandamme, Paola Principe-Nicolas
Abstract: The invention relates to glycerol derivatives of general formulae Ia, Ib and Ic ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, A and Y stand for various substituents, to a preparation process of said compounds and to therapeutical compositions containing the same.
Type:
Grant
Filed:
December 19, 1990
Date of Patent:
May 26, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Braquet, Colette Broquet, Benedicte Vandamme, Paola Principe-Nicolas
Abstract: The invention relates to a therapeutical composition of matter for the treatment by perfusion of shock states comprising as an essential ingredient therein, an effective amount either, of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.4 stant for H or CH.sub.3 or C.sub.2 H.sub.5,R.sub.2 stands for H or NO.sub.2 andR.sub.3 stands for NHR.sub.4 or CH.sub.3 or C.sub.2 H.sub.5alone or of a mixture of said compound with a cyclooxygenase blocker.
Type:
Grant
Filed:
December 19, 1990
Date of Patent:
January 14, 1992
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Braquet, Pierre-Etienne Chabrier de Lassauniere, Jean-Michel Guillon, Michel Auguet
Abstract: The invention relates to new selenophen derivatives of the formulae, ##STR1## to a preparation process of said compounds and to therapeutic compositions containing the same.
Type:
Grant
Filed:
November 14, 1990
Date of Patent:
December 24, 1991
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Abstract: This invention relates to thieno-triazolo-diazepine derivatives of the formula ##STR1## wherein R represents various substituents, to a preparation process of these compounds consisting in reacting the thieno-triazolo-diazepine compound of the formula ##STR2## on RSO.sub.2 Cl and to therapeutic compositions containing the same. The compounds are particularly interesting as anti-PAF and anti-ischemic agents.
Type:
Grant
Filed:
March 20, 1990
Date of Patent:
September 17, 1991
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
Inventors:
Andre Esanu, Pierre Braquet, Christiane Martin, Jean-Pierre Laurent