Patents Assigned to Laboratoire Theramex
-
Patent number: 9084796Abstract: A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17?-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems.Type: GrantFiled: April 17, 2012Date of Patent: July 21, 2015Assignee: LABORATOIRE THERAMEXInventors: Jacques Paris, Jean-Louis Thomas
-
Patent number: 9012667Abstract: The invention relates to a process for the preparation of a compound of formula (I): wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.Type: GrantFiled: February 8, 2011Date of Patent: April 21, 2015Assignee: Laboratoire TheramexInventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
-
Patent number: 8476455Abstract: The invention relates to the compounds of formula (I): in which R1, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds.Type: GrantFiled: December 15, 2004Date of Patent: July 2, 2013Assignee: Laboratoire TheramexInventors: Jean Lafay, Benoit Rondot, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti, Francois Puccio, Christian Blot, Philippe Maillos
-
Publication number: 20130137885Abstract: The invention relates to a process for the preparation of a compound of formula wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.Type: ApplicationFiled: February 8, 2011Publication date: May 30, 2013Applicant: LABORATOIRE THERAMEXInventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
-
Patent number: 8168619Abstract: A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17?-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems.Type: GrantFiled: October 29, 1999Date of Patent: May 1, 2012Assignee: Laboratoire TheramexInventors: Jacques Paris, Jean-Louis Thomas
-
Publication number: 20110237624Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: LABORATOIRE THERAMEXInventors: Benoit RONDOT, Jean LAFAY, Paule BONNET, Thierry CLERC, Igor DUC, Eric DURANTI, François PUCCIO, Jacqueline SHIELDS, Christian BLOT, Philippe MAILLOS
-
Publication number: 20090023779Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: October 14, 2005Publication date: January 22, 2009Applicant: Laboratoire TheramexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
-
Patent number: 7476691Abstract: The present invention relates to sulfamate benzothiophene compounds of the formula: (I) wherein R1, R2, R3, m and n are as defined in the specification. The invention also relates to pharmaceutical compositions containing these compounds and to methods of using them.Type: GrantFiled: May 16, 2003Date of Patent: January 13, 2009Assignee: Laboratoire TheramexInventors: Jean Lafay, Benoît Rondot, Denis Carniato, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti
-
Patent number: 7030104Abstract: The present invention relates to the field of therapeutic chemistry and more especially to the realization of new galenic forms intended to be applied on the skin. More particularly it relates to a topical hormonal composition with a systemic effect for the hormonal treatment of the perimenopause and of the menopause as well as for the treatment of the ovarian hormonal deficiencies in women with amenorrhea, characterized in that it comprises, as active ingredients, a progestogen derived from 19-nor progesterone and estradiol or one of its derivatives, a vehicle which allows the systemic passage of said active ingredients, chosen from the group constituted by a solubilizing agent, an absorption promoting agent, a film-forming agent, a gelling agent and their mixtures, in combination or in a mixture with suitable excipients for the realization of a gelled and/or film-forming pharmaceutical form.Type: GrantFiled: September 14, 2001Date of Patent: April 18, 2006Assignee: Laboratoire TheramexInventors: Georges Gray, Bertrand Villet, Jacques Paris, Jean-Louis Thomas
-
Patent number: 6906049Abstract: The present invention relates to the field of chemistry and more particularly to that of therapeutic chemistry. The invention relates more particularly to novel contraceptive compositions formed from a progestative agent and an oestrogen. The invention relates specifically to novel pharmaceutical contraceptive compositions, characterized in that they contain, as active ingredients, a nomegestrol ester and oestradiol, in combination or admixture with an inert, non-toxic, pharmaceutically-acceptable vehicle or diluent which is suitable for oral administration.Type: GrantFiled: October 25, 1999Date of Patent: June 14, 2005Assignee: Laboratoire TheramexInventors: Jacques Paris, Jean Louis Thomas
-
Patent number: 6831073Abstract: A method of treating estrogenic deficiencies in women while further avoiding the appearance of osteoporosis, withdrawal bleeding and cardiovascular diseases in post-menopausal women without any androgenic effect, and no deleterious effects on blood vessels comprising continuously without interruption administering to said women, a combination of 0.5 to 3 mg of an estrogenic compound and 1.5 to 3.75 mg of nomegestrol acetate.Type: GrantFiled: March 17, 1999Date of Patent: December 14, 2004Assignee: Laboratoire TheramexInventors: Michel Lanquetin, Jacques Paris, Jean-Louis Thomas
-
Publication number: 20040220163Abstract: The present invention relates to a method of achieving contraception in a woman, comprising daily administering to said woman, from the first day of her cycle, a pharmaceutical composition comprising (i) estradiol, an ester thereof or an equine conjugated estrogen and (ii) nomegestrol acetate.Type: ApplicationFiled: January 8, 2004Publication date: November 4, 2004Applicant: Laboratoire TheramexInventors: Jacques Paris, Jean-Louis Thomas, Michel Lanquetin
-
Patent number: 6803380Abstract: 5-aryl-1H-triazole compounds of the formula are potent and selective COX-2 inhibitors. The invention further relates to pharmaceutical compositions containing these compounds.Type: GrantFiled: May 17, 2002Date of Patent: October 12, 2004Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Denis Carniato
-
Patent number: 6737433Abstract: Imidazole derivatives of the formula: in which R1 and R2 are each independently hydrogen, (C1-C6)alkyl or (C3-C8)cycloalkyl; n is 0, 1 or 2; R3, R4, R5 and R6 are each independently hydrogen or a (C1-C6)alkyl, halogen, cyano, (C1-C6)alkoxy, trifluoromethyl, (C1-C6)alkylthio, (C1-C6)alkylsulfonyl, sulfonamido, acyl, (C1-C6)alkoxycarbonyl, or carboxamido group; R3 and R6 together with the phenyl ring bearing them can also form a benzofurane, or a N-methylbenzotriazole. The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.Type: GrantFiled: December 16, 2002Date of Patent: May 18, 2004Assignee: Laboratoire TheramexInventors: Nathalie Adje, Paule Bonnet, Denis Carniato, Remi Delansorne, Jean Lafay, Jean-Claude Pascal
-
Patent number: 6586402Abstract: The invention relates to LH-RH peptide analogues with excellent affinity for LH-RH receptors, of the formula: A1-A2-A3-A4-A5-A6-HAA-A7-Pro-Z (I) The invention also relates to the uses of said peptide analogues and to the pharmaceutical compositions containing them.Type: GrantFiled: November 30, 1999Date of Patent: July 1, 2003Assignee: Laboratoire TheramexInventors: Rémi Delansorne, Jacques Paris
-
Patent number: 6548715Abstract: A compound of the formula I: in which P is hydrogen or alkyl; Y and Y′ are each hydrogen or, when taken together, represent a group ═CH2; W and W′ are each hydrogen; X is selected from the group consisting of a hydroxyalkyl, a hydroxyalkoxy, an alkoxy optionally comprising an epoxide function, a hydroxyalkene, a hydroxyalkadiene, a hydroxyalkyne and isomeric forms thereof; and a) either R1 and R3 or R′3 form a saturated 5- or 6-membered carbocyclic ring and R2, R′2, R3 or R′3, R4, R′4, R5 and R′5 are each independently hydrogen or alkyl; or b) R2 or R′2 and R4 or R′4 form a saturated 5- or 6-membered carbocyclic ring, and R1, R2 or R′2, R3, R′3, R4 or R′4, R5 and R′5 are each independently hydrogen or alkyl; or c) R3 or R′3 and R5 or R′5 form a saturated or unsaturated 5- or 6-membered carbocyclic ring, and R1, R2, R′2, R3 or R′3, R4, R′4, and R5 or R′5 are each indepType: GrantFiled: October 28, 1999Date of Patent: April 15, 2003Assignee: Laboratoire Theramex S.A.Inventors: Roger Bouillon, Maurits Vandewalle, Pierre Jean De Clercq
-
Patent number: 6191292Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.Type: GrantFiled: December 8, 1999Date of Patent: February 20, 2001Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
-
Patent number: 6180803Abstract: The invention relates to compounds of the formula: in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.Type: GrantFiled: November 5, 1998Date of Patent: January 30, 2001Assignee: Laboratoire TheramexInventors: Alain Piasco, Jean Lafay, R{acute over (e)}mi Delansorne, Jacques Paris, Jean-Claude Pascal
-
Patent number: 6153587Abstract: LH-RH analogues with excellent affinity for LH-RH receptors, of the formula A.sub.1 -A.sub.2 -W-A.sub.3 -A.sub.4 -SPL-A.sub.5 -A.sub.6 -Pro-Z(I) in which:-A.sub.1 is pGlu, AcSar or an aromatic D-amino acid;-A.sub.2 is a direct bond, His, DPhe, DpFPhe or DpClPhe;*W is an aromatic L- or D-amino acid;-A.sub.3 is Ala, Thr, Ser, DSer, Ser(OBzl) or MeSer;-A.sub.4 is Tyr, Phe, cPzACAla, L- or D-PicLys, L- or D-NicLys or L- or D-IprLys;*SPL is the spirolactam of formula: ##STR1## -A.sub.5 is an amino acid with a (C.sub.1 -C.sub.8)alkyl or (C.sub.3-C.sub.6)cycloalkyl side chain;-A.sub.6 is L- or D-(Arg, HArg, Lys, HLys, Orn, Cit, HCit or Aph), where L- or D-(Arg and HArg) can be substituted by one or two (C.sub.1 -C.sub.4)alkyl groups and L- or D-(Lys, HLys, Orn and Aph) can be substituted by an isopropyl, nicotinoyl or picolinoyl group; and*Z is GlyNH.sub.2, DAlaNH.sub.2, AzaGlyNH.sub.2 or --NHR.sub.1 where R.sub.1 is a (C.sub.1 -C.sub.Type: GrantFiled: May 24, 1999Date of Patent: November 28, 2000Assignee: Laboratoire THERAMEXInventors: Remi Delansorne, Jacques Paris
-
Patent number: 6017907Abstract: The present invention relates to analogues of vitamin D, which lack the combined presence of the trans-fused six-membered C-ring and of five-membered D-ring, but still possess a central part consisting of a substituted chain of five atoms, atoms which correspond to positions 8, 14, 13, 17 and 20 of vitamin D, and at the ends of which are connected, at position 20 a structural moiety representing part of the side-chain of vitamin D or of an analogue of vitamin D, and at position 8 the .DELTA.(5,7)-diene moiety connected to the A-ring of the active 1-alpha-hydroxy metabolite or of an established vitamin D analogue, to their preparation process, to preparation intermediates, to pharmaceutical preparations comprising these compounds and to their use in medicine.Type: GrantFiled: June 28, 1996Date of Patent: January 25, 2000Assignee: Laboratoire Theramex S.A.Inventors: Roger Bouillon, Maurits Vandewalle, Pierre Jean de Clercq