Patents Assigned to Laboratoire Theramex
  • Patent number: 9084796
    Abstract: 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: Grant
    Filed: April 17, 2012
    Date of Patent: July 21, 2015
    Assignee: LABORATOIRE THERAMEX
    Inventors: Jacques Paris, Jean-Louis Thomas
  • Patent number: 9012667
    Abstract: 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: Grant
    Filed: February 8, 2011
    Date of Patent: April 21, 2015
    Assignee: Laboratoire Theramex
    Inventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
  • Patent number: 8476455
    Abstract: 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: Grant
    Filed: December 15, 2004
    Date of Patent: July 2, 2013
    Assignee: Laboratoire Theramex
    Inventors: Jean Lafay, Benoit Rondot, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti, Francois Puccio, Christian Blot, Philippe Maillos
  • Publication number: 20130137885
    Abstract: 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: Application
    Filed: February 8, 2011
    Publication date: May 30, 2013
    Applicant: LABORATOIRE THERAMEX
    Inventors: Jean-Luc Moutou, Florent Mouton, Gilles Pellegrino, Jean-Marc Dillenschneider, Jean Lafay
  • Patent number: 8168619
    Abstract: 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: Grant
    Filed: October 29, 1999
    Date of Patent: May 1, 2012
    Assignee: Laboratoire Theramex
    Inventors: Jacques Paris, Jean-Louis Thomas
  • Publication number: 20110237624
    Abstract: 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: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: LABORATOIRE THERAMEX
    Inventors: Benoit RONDOT, Jean LAFAY, Paule BONNET, Thierry CLERC, Igor DUC, Eric DURANTI, François PUCCIO, Jacqueline SHIELDS, Christian BLOT, Philippe MAILLOS
  • Publication number: 20090023779
    Abstract: 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: Application
    Filed: October 14, 2005
    Publication date: January 22, 2009
    Applicant: Laboratoire Theramex
    Inventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos
  • Patent number: 7476691
    Abstract: 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: Grant
    Filed: May 16, 2003
    Date of Patent: January 13, 2009
    Assignee: Laboratoire Theramex
    Inventors: Jean Lafay, Benoît Rondot, Denis Carniato, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti
  • Patent number: 7030104
    Abstract: 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: Grant
    Filed: September 14, 2001
    Date of Patent: April 18, 2006
    Assignee: Laboratoire Theramex
    Inventors: Georges Gray, Bertrand Villet, Jacques Paris, Jean-Louis Thomas
  • Patent number: 6906049
    Abstract: 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: Grant
    Filed: October 25, 1999
    Date of Patent: June 14, 2005
    Assignee: Laboratoire Theramex
    Inventors: Jacques Paris, Jean Louis Thomas
  • Patent number: 6831073
    Abstract: 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: Grant
    Filed: March 17, 1999
    Date of Patent: December 14, 2004
    Assignee: Laboratoire Theramex
    Inventors: Michel Lanquetin, Jacques Paris, Jean-Louis Thomas
  • Publication number: 20040220163
    Abstract: 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: Application
    Filed: January 8, 2004
    Publication date: November 4, 2004
    Applicant: Laboratoire Theramex
    Inventors: Jacques Paris, Jean-Louis Thomas, Michel Lanquetin
  • Patent number: 6803380
    Abstract: 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: Grant
    Filed: May 17, 2002
    Date of Patent: October 12, 2004
    Assignee: Laboratoire Theramex
    Inventors: Jean-Claude Pascal, Denis Carniato
  • Patent number: 6737433
    Abstract: 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: Grant
    Filed: December 16, 2002
    Date of Patent: May 18, 2004
    Assignee: Laboratoire Theramex
    Inventors: Nathalie Adje, Paule Bonnet, Denis Carniato, Remi Delansorne, Jean Lafay, Jean-Claude Pascal
  • Patent number: 6586402
    Abstract: 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: Grant
    Filed: November 30, 1999
    Date of Patent: July 1, 2003
    Assignee: Laboratoire Theramex
    Inventors: Rémi Delansorne, Jacques Paris
  • Patent number: 6548715
    Abstract: 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 indep
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: April 15, 2003
    Assignee: Laboratoire Theramex S.A.
    Inventors: Roger Bouillon, Maurits Vandewalle, Pierre Jean De Clercq
  • Patent number: 6191292
    Abstract: 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: Grant
    Filed: December 8, 1999
    Date of Patent: February 20, 2001
    Assignee: Laboratoire Theramex
    Inventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
  • Patent number: 6180803
    Abstract: 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: Grant
    Filed: November 5, 1998
    Date of Patent: January 30, 2001
    Assignee: Laboratoire Theramex
    Inventors: Alain Piasco, Jean Lafay, R{acute over (e)}mi Delansorne, Jacques Paris, Jean-Claude Pascal
  • Patent number: 6153587
    Abstract: 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: Grant
    Filed: May 24, 1999
    Date of Patent: November 28, 2000
    Assignee: Laboratoire THERAMEX
    Inventors: Remi Delansorne, Jacques Paris
  • Patent number: 6017907
    Abstract: 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: Grant
    Filed: June 28, 1996
    Date of Patent: January 25, 2000
    Assignee: Laboratoire Theramex S.A.
    Inventors: Roger Bouillon, Maurits Vandewalle, Pierre Jean de Clercq