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    TREATMENT OF MALE ANDROGEN DEFICIENCY SYMPTOMS OR DISEASES WITH SEX STEROID PRECURSOR COMBINED WITH SERM
    51.
    发明申请
    TREATMENT OF MALE ANDROGEN DEFICIENCY SYMPTOMS OR DISEASES WITH SEX STEROID PRECURSOR COMBINED WITH SERM 审中-公开
    治疗与雄性不育症状或疾病与SEM STEROID前列腺素联合SERM

    公开(公告)号：WO2015135061A1

    公开(公告)日：2015-09-17

    申请号：PCT/CA2015/000142

    申请日：2015-03-09

    Applicant: ENDORECHERCHE, INC.

    Inventor： LABRIE, Fernand ,  GAUTHIER, Sylvain

    IPC: A61K31/5685 ,  A61K31/352 ,  A61P5/26 ,  A61P5/32 ,  C07D311/60 ,  C07J1/00

    CPC classification number: A61K31/5685 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0053 ,  A61K31/453 ,  A61K38/24 ,  A61K45/06 ,  A61K2300/00

    Abstract: 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.

    Abstract translation: 用于预防，减少或消除男性雄激素缺乏症状或疾病的发生率的方法，包括男性性腺机能减退相关症状和与低血清睾酮和/或低DHEA或低总雄激素相关的疾病，包括涉及给药的易感温血动物 一类量的类固醇前体，特别是脱氢表雄酮（DHEA）和选择性雌激素受体调节剂（SERM）（尤其是阿曲比芬），二者的抗雌激素或前药。 症状或疾病是性欲丧失，勃起功能障碍，疲劳，能量损失，抑郁，骨丢失，肌肉损失，肌肉无力，脂肪堆积，记忆丧失，认知丧失，阿尔茨海默氏病，痴呆，身体毛发丧失，生育问题 ，失眠，男子女性发育不良，贫血，潮热，汗水，健康感，肥胖症，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。 还公开了用于递送本发明有用的活性成分和试剂盒的药物组合物。

    USE OF AN AROMATASE INHIBITOR FOR THE TREATMENT OF HYPOGONADISM AND RELATED DISEASES
    54.
    发明申请
    USE OF AN AROMATASE INHIBITOR FOR THE TREATMENT OF HYPOGONADISM AND RELATED DISEASES 审中-公开
    使用芳香酶抑制剂治疗高血压和相关疾病

    公开(公告)号：WO2013036562A1

    公开(公告)日：2013-03-14

    申请号：PCT/US2012/053844

    申请日：2012-09-06

    Applicant: NOVARTIS AG ,  TAYLOR, Ann ,  KLICKSTEIN, Lloyd B.

    Inventor： TAYLOR, Ann ,  KLICKSTEIN, Lloyd B.

    IPC: A61K9/48 ,  A61K31/4196 ,  A61P5/26 ,  A61P15/08

    CPC classification number: A61K31/4196 ,  A61K9/4833 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866

    Abstract: This invention relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile. The present invention further relates to a method of increasing testosterone levels and treating hypogonadism and related diseases with the aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile in a particular dosing regimen. The invention also relates to pharmaceutical compositions comprising said aromatase inhibitor 4,4'-[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, optionally in combination with other active ingredients. Furthermore, the present invention relates to kits comprising said pharmaceutical compositions together with instructions how to administer them.

    Abstract translation: 本发明涉及一种增加睾丸激素水平和用芳香酶抑制剂4,4' - [氟 - （1-H-1,2,4-三唑-1-基）亚甲基]双苄腈治疗性腺机能减退和相关疾病的方法。 本发明还涉及使用芳香酶抑制剂4,4' - [氟 - （1-H-1,2,4-三唑-1-基）亚甲基]双苄腈来增加睾丸激素水平和治疗性腺机能减退和相关疾病的方法 在特定的给药方案中。 本发明还涉及包含所述芳香酶抑制剂4,4' - [氟 - （1-H-1,2,4-三唑-1-基）亚甲基]双苄腈的药物组合物，任选与其它活性成分组合。 此外，本发明涉及包含所述药物组合物的试剂盒以及如何施用它们的说明书。

    CONTROLLED RELEASE NASAL TESTOSTERONE GELS, METHODS AND PRE-FILLED MULTI-DOSE APPLICATOR SYSTEMS FOR PERNASAL ADMINISTRATION
    56.
    发明申请
    CONTROLLED RELEASE NASAL TESTOSTERONE GELS, METHODS AND PRE-FILLED MULTI-DOSE APPLICATOR SYSTEMS FOR PERNASAL ADMINISTRATION 审中-公开
    控制释放NASAL TESTOSTERONE凝胶，方法和预填充多用途施用者系统进行全面管理

    公开(公告)号：WO2012156822A1

    公开(公告)日：2012-11-22

    申请号：PCT/IB2012/001127

    申请日：2012-05-15

    Applicant: TRIMEL PHARMACEUTICALS CORP. ,  KREPPNER, Wayne ,  FOGARTY, Siobhan ,  OBEREGGER, Werner ,  MAES, Paul, José, Pierre, Marie

    Inventor： KREPPNER, Wayne ,  FOGARTY, Siobhan ,  OBEREGGER, Werner ,  MAES, Paul, José, Pierre, Marie

    IPC: A61K9/00 ,  A61K9/06 ,  A61K31/568 ,  A61K47/34 ,  A61K47/44 ,  A61P5/26

    CPC classification number: A61K47/34 ,  A61K9/0043 ,  A61K31/568 ,  A61K47/44

    Abstract: The present invention relates to intranasal testosterone gels for the controlled release of testosterone into the systemic circulation of males and females for providing constant effective testosterone blood levels, without inducing undesired testosterone spike in blood levels, following pernasal administration. The intranasal testosterone gels of the present invention are safe, convenient to use, well tolerated, stable and easily and reproducibly manufactured on scale up. Moreover, because supra- normal and sub-normal testosterone blood levels are believed to be essentially kept to a minimum or avoided and the testosterone serum levels are believed to remain essentially constant during dose life, i.e., the intranasal testosterone gels of the present invention mimic or restore testosterone blood levels to normal physiologic daily rhythmic testosterone levels, the novel intranasal testosterone gels of the present invention are uniquely suited for testosterone replacement or supplemental therapy and effective for treating males diagnosed with, for example, male testosterone deficiency, such as, low sexual libido, low sexual drive, low sexual activity, low fertility, low spermatogenesis, aspermatogenesis, depression and/or hypogonadism, and females who are diagnosed with, for example, female sexual dysfunction, such as, low sexual libido, low sexual drive, low sexual activity, low amygdala reactivity, low sexual stimulation, hypoactive sexual desire disease ("HSDD"), female sexual arousal disorder and/or anorgasmia. The present invention also relates to methods and pre- filled multi-dose airless applicator systems for pernasal administration of the nasal testosterone gels of the present invention.

    Abstract translation: 本发明涉及鼻内睾丸激素凝胶，用于将睾酮控制释放到男性和女性的全身循环中，以提供恒定有效的睾酮血液水平，而不会在经鼻给药后引起血液中不希望的睾酮峰值。 本发明的鼻内睾丸激素凝胶安全，使用方便，耐受性良好，稳定，容易且可重复地按比例制造。 此外，因为认为超正常和亚正常睾酮血液水平基本上保持在最小或避免，并且认为睾酮血清水平在剂量生命期间基本保持不变，即本发明的鼻内睾丸激素凝胶模拟 或将睾酮血液水平恢复至正常的生理日常韵律睾酮水平，本发明的新型鼻内睾丸激素凝胶独特地适用于睾酮替代或补充治疗，并且有效治疗诊断患有例如男性睾酮缺乏症的男性，例如低 性欲低下，性行为低，性活动低，生育能力低，精子发生，精子发生，抑郁和/或性腺机能减退等症状，以及被诊断患有女性性功能障碍的女性，如性欲低下，性欲低下， 低性活动，低杏仁体反应性，低性刺激，低反应性欲欲疾病 （“HSDD”），女性性唤醒障碍和/或动作紊乱。 本发明还涉及用于本发明的鼻睾酮凝胶的鼻内给药的方法和预填充的多剂量无空气涂抹器系统。

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