Abstract: The invention concerns novel N-(iminomethyl)amine derivatives comprising in their skeleton the aminophenylamine, oxodiphenylamine, carbazole, phenazine, phenoxazine or oxodiphenyl motif, their use as medicines and pharmaceutical compositions containing them. The invention concerns in particular the following compounds: -4-{[2-thienyl(imino)methyl]amino}-N-[2-(phenylamino)phenyl]-benzenebutanamide; -4-{[2-thienyl(imino)methyl]amino}-N-[4-(phenylamino)phenyl]-benzenebutanamide; -N-′[4-(10H-phenothiazin-2-yloxy)phenyl]-2-thiophenecarboximidamide; -4-(4-{[amino(2-thienyl)methylidene]amino}phenyl)-N-(10H-phenothiazin-3-ylH)butanamide; -3-[(3-{[amino(2-thienyl)methylidene]amino}-benzyl)amino]-N-(4-anilinophenyl)propanamide; -N′-(4-{2-[(10H-phenothiazin-3-ylmethyl)amino]ethyl}phenyl-2-thiophene carboximidamide.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
November 19, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
Abstract: The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino [1,2-b] quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.
Type:
Grant
Filed:
June 20, 2000
Date of Patent:
August 20, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Abstract: A method for implanting or inserting a solid or semisolid formulation containing at least one active principle uses a device comprising one part set inside the body of the patient and which conditions the solid or semisolid form, brings these conditioning action to the deposit site, injects or inserts in this deposit site, and withdraws after injection or insertion, with one part remaining outside and activating the functions of the device. The invention also concerns a sustained-release solid formulation for parenteral administration comprising a homogeneous mixture of an active principle in non-dispersed state and of a biologically compatible and biodegradable excipient, in which the amount of active principle is at least 50% by weight.
Type:
Application
Filed:
February 1, 2002
Publication date:
August 15, 2002
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION
Abstract:
The present invention is directed to imidazolyl derivatives of formula (I), wherein the variables are defined in the specification, which are useful as prenyl transferase inhibitors.
Type:
Grant
Filed:
May 22, 2001
Date of Patent:
July 16, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques, S.A.S.
Abstract: A compound of the formula XXV (H) wherein the substituents are defined as set forth in the specification which are useful intermediates for the production of derivatives of 2-(iminomethyl)-imino-phenyl having inhibitory activity on NO-synthase enzymes.
Type:
Application
Filed:
September 17, 2001
Publication date:
April 11, 2002
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
Inventors:
Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
Abstract: A method comprising the following steps: preparing in a vacuum a dry form (18) of an active principle, as well as a liquid (22), and drawing this liquid into the dry form, by the action of the vacuum to obtain an injectable preparation. The device comprises a gastight syringe (19) to condition under vacuum the dry form, a reservoir (12) containing the liquid (22) and a cap (29) forming a connector between the syringe and the liquid reservoir, the injection needle (25) of the syringe being driven into the septum (24) of the cap (29). The invention enables a preparation which is directly injectable by an automatic rehydration step to be obtained; indeed, after activation, the extemporaneous preparation is automatic since the device elements move by themselves under the action of the liquid which is drawn by suction into the volume under vacuum containing the solid formulation (18).
Type:
Grant
Filed:
February 18, 1999
Date of Patent:
February 26, 2002
Assignee:
Societe de Conseils de Recherches et D'Applications
Scientifiques SCRAS
Abstract: The invention concerns novel phenylcyclidine derivatives with selective affinity for low affinity receptors, methods for preparing them, pharmaceutical compositions containing them and their use as protective agents for central or peripheral nervous system cells against acute or chronic degeneration, or as an anticonvulsant.
Type:
Grant
Filed:
November 30, 1999
Date of Patent:
January 29, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Jean-Marc Kamenka, Jacques Hamon, Jacques Vignon
Abstract: A compound of the formula
wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
Type:
Grant
Filed:
September 22, 1999
Date of Patent:
January 22, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet
Abstract: The invention concerns the use of a flavoniodic extract of ginkgo biloba leaves, and more specifically an extract devoid of terpenes for oral hygiene. The invention also concerns a composition for oral hygiene containing such an extract.
Type:
Grant
Filed:
June 23, 2000
Date of Patent:
January 22, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Abstract: A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula 1
Type:
Application
Filed:
June 15, 2001
Publication date:
January 17, 2002
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D' APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
Inventors:
Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
Abstract: The compound of the formula
wherein the substituents are defined as in the specification and its non-toxic, pharmaceutically acceptable salts which are useful for the treatment of viral infections, parasitic diseases and the treatment of cancer.
Type:
Grant
Filed:
June 14, 1999
Date of Patent:
January 15, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
Abstract: A compound selected from the group consisting of a compound of the formula
wherein A is selected from the group consisting of
and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.
Type:
Grant
Filed:
December 7, 1999
Date of Patent:
January 1, 2002
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
Abstract: A method of inhibiting effects of exogenous neurotoxic or neurotoxinic products in warm-blooded animals comprising administering to warm-blooded animals before exposure to said products an inhibitorily effective amount of reversible cholinesterase inhibitor selected from the group consisting of pyridostigmine and physostigmine followed by administration of an inhibitorily effective amount of 2-methyl-1-(1-piperidinyl)-1-(2-thienyl)-cyclohexane in substantially pure racemic, diastereoisomeric or enantiomeric form.
Type:
Application
Filed:
April 13, 2001
Publication date:
December 27, 2001
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S)
Inventors:
Guy Lallement, Pierre D'Arbigny, Jean-Marc Kamenka
Abstract: A process for preparing a flavonoid extract from the leaves of ginkgo biloba comprising multiple distractions of the leaves of the ginkgo biloba with solvents wherein at least one of the extraction stages is a deterpenation step using a solvent of the formula RC(O)OR′ wherein R and R′ are individually lower alkyl.
Type:
Application
Filed:
April 18, 2001
Publication date:
November 22, 2001
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)
Abstract: The invention features an implantable device for the automatic delivery of an active ingredient according to an adjustable delivery profile. The device includes a housing; a reservoir operatively connected to the housing and arranged to store a solid composition including the active ingredient; an actuator arranged within the housing to move the solid composition from the reservoir to a transit area, wherein the solid composition exits the housing at the transit area; a controller that acts on the actuator to adjust movement of the solid composition out of the housing according to the adjustable delivery profile; and a power source arranged to provide energy to the actuator and the controller. The solid composition can be an elongate, solid composition comprising a drug, and up to 90% of a carrier, wherein the composition has a cross-section of less than 0.
Type:
Grant
Filed:
May 19, 2000
Date of Patent:
October 23, 2001
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques, S.A.S.
Abstract: The invention concerns novel compounds having the elements of group 11, 12 or 14; and a tridentate ligand, a method for preparing them and their use in particular as polymerisation catalyst.
Type:
Grant
Filed:
December 23, 1999
Date of Patent:
October 16, 2001
Assignees:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.), Centre National de la Recherche Scientifique
(C.N.R.S.)