公开(公告)号：EP2147014B1

公开(公告)日：2016-02-17

申请号：EP08748116.4

申请日：2008-04-11

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand ,  GAUTHIER, Sylvain ,  CLOUTIER, Julie ,  MAILHOT, Josée ,  POTVIN, Steeves ,  DION, Sylvain ,  SANCÉAU, Jean-Yves

IPC分类号： C07J43/00 ,  A61K31/565 ,  A61K31/567 ,  A61K31/58 ,  A61P5/28 ,  C07J41/00 ,  C07J63/00

CPC分类号： C07J41/0094 ,  C07J43/003 ,  C07J63/008

公开(公告)号：EP2877183A1

公开(公告)日：2015-06-03

申请号：EP13822094.2

申请日：2013-07-19

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand

IPC分类号： A61K31/5685 ,  A61P15/00 ,  A61P15/02 ,  A61P15/12

CPC分类号： A61K31/5685 ,  A61K9/0034

摘要： Intravaginal DHEA is used for the treatment of at least one condition selected from the group consisting of female hypoactive sexual desire disorder, female sexual arousal disorder, female orgasm disorder and female sexual interest arousal disorder in a woman who either (1) is not suffering from symptoms of vulvo-vaginal atrophy and/or (2) is not suffering from moderate to severe dyspareunia.

公开(公告)号：EP1196163B1

公开(公告)日：2009-11-11

申请号：EP00945483.6

申请日：2000-07-05

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand ,  DESHAIES, Yves ,  RICHARD, Denis ,  MARTEL, Celine ,  MARETTE, Andre

IPC分类号： A61K31/352 ,  A61K31/4025 ,  A61K31/453 ,  A61K31/5377 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06

CPC分类号： A61K31/353 ,  A61K31/352 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/453 ,  A61K31/5377 ,  A61K31/565 ,  A61K45/06 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or prevention of obesity, abdominal fat, and insulin resistance in susceptible warm-blooded animals including humans involves the administration of selective estrogen receptor modulators (SERMs). A combination of a SERM with an amount of estrogen or a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3b,17b-diol and compounds converted in vivo to one of the foregoing precursors or estrogen is also disclosed.

公开(公告)号：EP1802312A1

公开(公告)日：2007-07-04

申请号：EP05797148.3

申请日：2005-10-20

申请人： ENDORECHERCHE INC.

发明人： EL-ALFY, Mohamed ,  LABRIE, Fernand ,  BERGER, Louise

IPC分类号： A61K31/5685 ,  A61K31/566 ,  A61K31/453 ,  A61K31/519 ,  A61P15/02

CPC分类号： A61K31/5685 ,  A61K31/453 ,  A61K31/519 ,  A61K31/566

摘要： Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance , in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure: is specifically disclosed for the medical treatment and/or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

公开(公告)号：EP0615448B1

公开(公告)日：2002-05-02

申请号：EP92923641.2

申请日：1992-12-01

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand ,  MERAND, Yves

IPC分类号： A61K31/352 ,  A61K31/4433 ,  A61K31/4025 ,  C07D311/04

CPC分类号： C07D295/185 ,  A61K31/10 ,  A61K31/135 ,  A61K31/138 ,  A61K31/165 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/382 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  C07C215/64 ,  C07C217/18 ,  C07C235/34 ,  C07C317/18 ,  C07C2602/10 ,  C07D215/14 ,  C07D217/16 ,  C07D235/18 ,  C07D295/088 ,  C07D295/096 ,  C07D311/60 ,  C07D335/06 ,  C07J1/0011 ,  C07J1/0022 ,  C07J1/0025 ,  C07J1/0055 ,  C07J1/0059 ,  C07J1/007 ,  C07J1/0074 ,  C07J1/0081 ,  C07J1/0085 ,  C07J1/0096 ,  C07J17/00 ,  C07J21/006 ,  C07J21/008 ,  C07J41/0072 ,  C07J41/0094 ,  C07J51/00 ,  C07J53/008 ,  C07J71/001 ,  C07J71/0021

摘要： Inhibitors of sex steroid activity, for example those having general structure (A) 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.

摘要翻译： 性类固醇活性的抑制剂，例如具有一般结构的那些可以用作药物组合物的一部分，以提供抗雌激素作用和/或抑制雌激素合成。 这样的药物组合物可用于治疗通过激活性类固醇受体来辅助其进展的乳腺癌或其它疾病。

公开(公告)号：EP1028731A2

公开(公告)日：2000-08-23

申请号：EP98956445.5

申请日：1998-11-05

申请人： SCHERING CORPORATION ,  Endorecherche Inc.

发明人： SEQUEIRA, Joel, A. ,  LABRIE, Fernand ,  MAHASHABDE, Shanshank ,  DeANGELIS, Nicholas ,  MERAND, Yves ,  FOURNIER, Marc

IPC分类号： A61K31/565 ,  A61K9/06 ,  A61K47/10 ,  A61K47/38

CPC分类号： A61K31/569 ,  A61K9/0014 ,  A61K31/575 ,  A61K47/10 ,  A61K47/38 ,  Y10S514/859 ,  Y10S514/861 ,  Y10S514/863 ,  Y10S514/864 ,  Y10S514/944

摘要： Pharmaceutical compositions for the topical treatment of androgen-related conditions, e.g., acne in humans containing an amount of the compound represented by formula (II) effective for the topical treatment of the androgen-related conditions, e.g., acne dissolved in an alcohol-water solvent system, such as ethanol-water [97.6:2.4(w/w)] and having an apparent pH in the range of about 3.5 to 4.5, and containing a gelling agent are disclosed.

公开(公告)号：EP0595796A1

公开(公告)日：1994-05-11

申请号：EP90909601.0

申请日：1990-07-05

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand

IPC分类号： A61K31 ,  A61P35 ,  A61P43 ,  C07J1 ,  C07J17 ,  C07J41

CPC分类号： A61K31/575 ,  A61K31/565 ,  A61K31/57 ,  Y02A50/395 ,  Y10S514/80 ,  A61K2300/00

摘要： 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 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.

公开(公告)号：EP2185157A1

公开(公告)日：2010-05-19

申请号：EP08783354.7

申请日：2008-08-08

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand

IPC分类号： A61K31/5685 ,  A61K31/453 ,  A61K31/56 ,  A61P15/12 ,  A61P5/26 ,  A61P5/32

CPC分类号： A61K31/453 ,  A61K9/0014 ,  A61K9/0034 ,  A61K31/56 ,  A61K31/5685

摘要： Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and/or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are disclosed.

公开(公告)号：EP2147014A1

公开(公告)日：2010-01-27

申请号：EP08748116.4

申请日：2008-04-11

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand ,  GAUTHIER, Sylvain ,  CLOUTIER, Julie ,  MAILHOT, Josée ,  POTVIN, Steeves ,  DION, Sylvain ,  SANCÉAU, Jean-Yves

IPC分类号： C07J43/00 ,  A61K31/565 ,  A61K31/567 ,  A61K31/58 ,  A61P5/28 ,  C07J41/00 ,  C07J63/00

CPC分类号： C07J41/0094 ,  C07J43/003 ,  C07J63/008

摘要： Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

公开(公告)号：EP0595796B1

公开(公告)日：2003-01-15

申请号：EP90909601.8

申请日：1990-07-05

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand

IPC分类号： A61K31/565 ,  A61K31/575 ,  A61K31/57

CPC分类号： A61K31/575 ,  A61K31/565 ,  A61K31/57 ,  Y02A50/395 ,  Y10S514/80 ,  A61K2300/00

摘要： 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 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.