Patents by Inventor Fernand Labrie

Fernand Labrie has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5728688
    Abstract: Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment of vaginal atrophy, hypogonadism, diminished libido, loss of collagen or connective tissues in the skin, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these precursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 17, 1998
    Assignee: Endoreoherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 5712251
    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.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 27, 1998
    Assignee: Roussel Uclaf
    Inventors: Fernand Labrie, Jean-Pierre Raynaud
  • Patent number: 5688769
    Abstract: A method for inhibiting ovarian steroidogenesis in women comprising administering to women an ovarian steroidogenesis inhibitorilly effective amound of D Ser (tbu).sup.6 des Gly NH.sub.2 .sup.10 LH-RH ethylamide.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: November 18, 1997
    Assignee: Roussel Uclaf
    Inventors: Fernand Labrie, Jean-Pierre Raynaud
  • Patent number: 5686437
    Abstract: Novel derivatives of estrogenic nuclei, contain a side-chain substitution of the formula --R.sup.1 ?B--R.sup.2 --!.sub.x L--G and may be used in pharmaceutical compositions as sex steroid activity inhibitors useful in the treatment of both androgen-related and estrogen-related diseases.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5686465
    Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5631249
    Abstract: Novel compounds for the inhibition of sex steroid activity for the treatment of both androgen-related and estrogen-related diseases include for example 15- and 16-halo substituted compounds such as: ##STR1## The compounds are characterized by an estrogenic nucleus substituted with a substituent of the formula --R.sup.1 [B--R.sup.2 --].sub.x L--Gwherein at least one of n and G is a polar moiety distanced from a ring carbon of the estrogenic nucleus by at least three intervening atoms:x is an integer from 0--6;R.sup.1 and R.sup.2 are independently either absent or selected from the group consisting of straight- or branched-chain alkylene, straight- or branched-chain alkynylene, straight- or branched-chain alkenylene, phenylene, and fluoro-substituted analogs of the foregoing; andB is either absent or selected from the group consisting of --O-- --Se--, --SO--, --SO.sub.2 --, --NR.sup.3 --, --SiR.sup.3.sub.2, --CR.sup.3 OR.sup.3 --, NR.sup.3 CO--, NR.sup.3 CS--, --CONR.sup.3 --, CSNR.sup.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: May 20, 1997
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves M erand
  • Patent number: 5629303
    Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration)administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: May 13, 1997
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Martin Lepage
  • Patent number: 5610150
    Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 11, 1997
    Assignee: Endorecherche Inc.
    Inventor: Fernand Labrie
  • Patent number: 5595985
    Abstract: A combination therapy for the prophylaxis and/or treatment of benign prostatic hyperplasia in susceptible warm-blooded animals which comprises administering a combination of two or more compounds selected from the group consisting of an inhibitor of 5.alpha.-reductase activity, an antiestrogen, an inhibitor of aromatase activity, an inhibitor of 17.beta.-hydroxysteroid dehydrogenase activity and, in some cases, an anti-androgen and/or an LHRH agonist. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such compositions are disclosed.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: January 21, 1997
    Assignee: Endorecherche Inc.
    Inventor: Fernand Labrie
  • Patent number: 5593981
    Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: January 14, 1997
    Assignee: Endorecherche Inc.
    Inventor: Fernand Labrie
  • Patent number: 5585405
    Abstract: Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibition of androgen or estrogen activity is desired. Preferred inhibitors also possess antiestrogenic activity, thus providing the advantage of a double inhibitory action both on estrogen formation and on estrogen action (blockade of estrogen receptors by antiestrogenic action).
    Type: Grant
    Filed: August 1, 1994
    Date of Patent: December 17, 1996
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5567695
    Abstract: A method of treatment or prevention of breast and endometrial cancer, osteoporosis and endometriosis in susceptible warm-blooded animals comprising administering a low dose of a progestin or other steroid derivative having androgenic activity and low masculinizing activity. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such compositions are disclosed. An in vitro assay permitting specific measurements of androgenic activity of potentially useful compounds is also disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 22, 1996
    Assignee: Endorecherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 5550107
    Abstract: A method of treatment of breast and endometrial cancer in susceptible warm-blooded animals may include inhibition of ovarian hormonal secretion by surgical (ovariectomy) or chemical (use of an LHRH agonist, e.g. [D-Trp.sup.6, des-Gly-NH.sub.2.sup.10 ]LHRH ethylamide or antagonist) as part of a combination therapy comprising administering an antiestrogen together with at least one compound selected from the group consisting of an androgen, a progestin, at least one inhibitor of sex steroid formation, especially 17.beta.-hydroxysteroid dehydrogenase and aromatase activity, at least one inhibitor of prolactin secretion, one inhibitor of growth hormone secretion and one inhibitor of ACTH secretion. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such composition are disclosed.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: August 27, 1996
    Assignee: Endorecherche Inc.
    Inventor: Fernand Labrie
  • Patent number: 5545634
    Abstract: A method of treatment or prevention of breast and endometrial cancer, osteoporosis and endometriosis in susceptible warm-blooded animals comprising administering a low dose. Of a progestin or other steroid derivative having androgenic activity and low masculinizing activity. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such compositions are disclosed. An in vitro assay permitting specific measurements of androgenic activity of potentially useful compounds is also disclosed.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: August 13, 1996
    Assignee: Endorecherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 5541172
    Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 30, 1996
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Martin Lepage
  • Patent number: 5494914
    Abstract: Inhibitors of testosterone 5.alpha.-reductase activity, for example those of formula: ##STR1## wherein novel substituents are provided at the R.sup.4, R.sup.6, R.sup.7, R.sup.17.alpha. and/or R.sup.17.beta. positions are useful for the treatment of diseases whose progress is aided by activation of androgen receptors, e.g., prostate cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, androgenic alopecia and the like.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: February 27, 1996
    Assignee: Endorecherche
    Inventors: Fernand Labrie, Yves M. Merand, Shankar M. Singh
  • Patent number: 5434146
    Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolaR serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: July 18, 1995
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Martin Lepage
  • Patent number: 5395842
    Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
    Type: Grant
    Filed: December 2, 1991
    Date of Patent: March 7, 1995
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5393785
    Abstract: Novel antiestrogenic compounds are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified diphenylethane and diphenylethylene analogs which show strong affinity for estrogen receptors but substantially lack the capacity to activate such receptors or otherwise act as agonists.
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: February 28, 1995
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5389613
    Abstract: A novel method of treating prostate adenocarcinoma, prostate benign hypertrophia, endometriosis, dysmenorrhea, hirsuitism, hormono-dependant mammary tumors, treatment and prevention of precocious puberty, induction of a retardation of the appearance of puberty and treatment of acne of mammals comprising administering to warm-blooded animals an effective amount of a peptide of the formulaP Glu-His-Trp-Ser-Tyr-X-Y-Arg-Pro-Z (I)wherein (a) Z is Gly--NH.sub.2, Y is Leu and X is Gly, (b) Z is Gly--NH.sub.2, Y is Leu, X is DN Leu, DN Val, D Abu (.alpha.-aminobutyric acid), D Phe, D Ser, D Thr, D Met, D Pgl, D Lys, Leu, Ile, Nle, Val, N Val, Met, Phe, D Leu, D Arg, D Ser (tbu), D Thr (tbu), D Cys (tbu), D Asp (O tbu), D Glu (Otbu), D Orn (boc), D Lys (boc), D Trp, Trp, 2-methyl Ala, D Tyr, D Met .epsilon.-lauryl D Lys, .epsilon.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: February 14, 1995
    Assignees: Roussel Uclaf, Shering Corporation
    Inventors: Fernand Labrie, Jean-Pierre Raynaud