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1. 发明公开

EP3083590A4 NON-STEROIDAL ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS WITH A PYRIDYL MOIETY 有权
标题翻译： NICHTSTEROID-ANTIANDROGENE ANDD SELEKTIVE ANDROGENREZEPTORMODULATOREN MIT EINEM PYRIDYLANTEIL
公开(公告)号：EP3083590A4
公开(公告)日：2017-05-03
申请号：EP14872056
申请日：2014-12-16
申请人： ENDORECHERCHE INC
发明人： LABRIE FERNAND , SINGH SHANKAR MOHAN , LABRECQUE RICHARD , CIOBANU LIVIU CONSTANTIN
IPC分类号： C07D401/12 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61P5/26 , A61P35/00 , C07D233/74 , C07D401/14 , C07D403/12
CPC分类号： C07D403/12 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/58 , A61K38/09 , A61K45/06 , C07D401/12 , C07D401/14 , A61K2300/00
摘要： Compounds having the structure or their salts: are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia, male baldness, muscle atrophy and weakness, sarcopenia, male hypogonadism, erectile dysfunction, female sexual dysfunction and osteoporosis. 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.
摘要翻译：具有结构或其盐的化合物：用于治疗或减少获得雄激素依赖性疾病如前列腺癌，良性前列腺增生，多囊卵巢综合征，痤疮，多毛症，皮脂溢出，雄激素性脱发，男性秃顶，肌肉萎缩肌无力症，男性性腺功能减退症，勃起功能障碍，女性性功能障碍和骨质疏松症。它们可以与药学上可接受的稀释剂或载体一起配制或以其他方式制成任何药物剂型。还公开了与其他活性药剂的组合。

2. 发明授权

EP2147014B1 17ALPHA-SUBSTITUTED STEROIDS AS SYSTEMIC ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS 有权
标题翻译： 17α-乙烯取代的类固醇全身抗雄激素和选择性雄激素受体调节剂
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

3. 发明公开

EP2877183A1 IMPROVEMENT OF SEXUAL AROUSAL, SEXUAL DESIRE, ORGASM AND/OR PLEASURE FOLLOWING INTRAVAGINAL PRASTERONE (DHEA) ADMINISTRATION IN WOMEN NOT SUFFERING OR INDEPENDENTLY FROM DYSPAREUNIA OR OTHER SYMPTOMS OF VULVO-VAGINAL ATROPHY 有权
标题翻译：受影响或不管性刺激，性欲，高潮和/或休闲阴道内的阴道内普拉睾酮（DHEA）管理其中没有性交或阴道萎缩等症状的女性改进
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.

4. 发明授权

EP1623712B1 Selective estrogen receptor modulator in combination with dehydroepiandrosterone (DHEA) or analogues 有权
标题翻译：选择性雌激素受体调节剂，和脱氢表雄酮或组合的类似物
公开(公告)号：EP1623712B1
公开(公告)日：2012-12-12
申请号：EP05018115.5
申请日：1999-06-10
申请人： ENDORECHERCHE INC.
发明人： Labrie, Fernand
IPC分类号： A61K31/565 , A61K45/06 , A61P3/06 , A61P9/00
CPC分类号： A61K31/565 , A61K31/57 , A61K31/66 , A61K45/06 , A61K31/445 , A61K31/41 , A61K31/40 , A61K31/38 , A61K31/135 , A61K2300/00

5. 发明授权

EP1196163B1 PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF INSULIN RESISTANCE 有权
标题翻译：药物制剂INSULINRESITENZ的治疗
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.

6. 发明公开

EP1802312A1 SEX STEROID PRECURSORS ALONE OR IN COMBINATION WITH A SELECTIVE ESTROGEN RECEPTOR MODULATOR AND/OR WITH ESTROGENS AND/OR A TYPE 5 CGMP PHOSPHODIESTERASE INHIBITOR FOR THE PREVENTION AND TREATMENT OF VAGINAL DRYNESS AND SEXUAL DYSFUNCTION IN POSTMENOPAUSAL WOMEN 有权
标题翻译： PRE有性类固醇结合选择性雌激素受体调节绝经后妇女的预防与处理阴道萎缩的
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.

7. 发明授权

EP0615448B1 SEX STEROID ACTIVITY INHIBITORS 失效
标题翻译： SEX STEROIDE INHIBITONEN
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。

8. 发明公开

EP1028731A2 STABLE ANTIANDROGENIC GEL COMPOSITION 审中-公开
标题翻译：稳定抗雄激素GELZUSAMMENSETZUNG
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.

9. 发明公开

EP0595796A1 METHOD OF TREATMENT OF ANDROGEN-RELATED DISEASES 失效
标题翻译： METHOD FOR THE治疗雄激素疾病。
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.

10. 发明公开

EP3116510A4 TREATMENT OF MALE ANDROGEN DEFICIENCY SYMPTOMS OR DISEASES WITH SEX STEROID PRECURSOR COMBINED WITH SERM 审中-公开
标题翻译： BEHANDLUNG VONMÄNNLICHENANDROGENMANGELSYMPTOMEN ODER -ERKRANKUNGEN MITSEXSTEROIDVORLÄUFERN在KOMBINATION MIT SERMERM
公开(公告)号：EP3116510A4
公开(公告)日：2017-08-16
申请号：EP15761680
申请日：2015-03-09
申请人： ENDORECHERCHE INC
发明人： LABRIE FERNAND , GAUTHIER SYLVAIN
IPC分类号： A61K31/5685 , A61K31/352 , A61P5/26 , A61P5/32 , C07D311/60 , C07J1/00
CPC分类号： A61K31/5685 , A61K9/0019 , A61K9/0031 , A61K9/0053 , A61K31/453 , A61K38/24 , A61K45/06 , A61K2300/00
摘要： Novel methods for prevention, reduction or elimination of the incidence of male androgen deficiency symptoms or diseases including male hypogonadism-associated symptoms and diseases associated with low serum testosterone and/or low DHEA or low total androgens in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and a selective estrogen receptor modulator (SERM) (particularly acolbifene), an antiestrogen or a prodrug of the two. The symptoms or diseases are loss of libido, erectile dysfunction, tiredness, loss of energy, depression, bone loss, muscle loss, muscle weakness, fat accumulation, memory loss, cognition loss, Alzheimer's disease, dementia, loss of body hair, fertility problems, insomnia, gynecomastia, anemia, hot flushes, sweats, decreased sense of well-being, obesity, osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, cardiovascular disease and type 2 diabetes. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
摘要翻译：包括人类在内的包括人在内的预防，减少或消除男性雄激素缺乏症状或疾病包括男性性腺功能减退症相关症状和与低血清睾酮和/或低DHEA或低总雄激素相关疾病发病率的新方法一定量的性类固醇前体，特别是脱氢表雄酮（DHEA）和选择性雌激素受体调节剂（SERM）（特别是阿考比芬），这两者的抗雌激素或前药。症状或疾病是性欲减退，勃起功能障碍，疲倦，精力不集中，抑郁症，骨质流失，肌肉损失，肌肉无力，脂肪堆积，记忆丧失，认知丧失，阿尔茨海默病，痴呆，体毛脱落，生育问题，失眠，男子女性型乳房，贫血，热潮红，汗水，幸福感减退，肥胖，骨质疏松症，高胆固醇血症，高脂血症，动脉粥样硬化，高血压，胰岛素抵抗，心血管疾病和2型糖尿病。还公开了用于递送用于本发明的活性成分和试剂盒的药物组合物。

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