公开(公告)号：US20160058774A1

公开(公告)日：2016-03-03

申请号：US14464536

申请日：2014-08-20

申请人： Mohamed EL-ALFY ,  Fernand LABRIE ,  Louise BERGER

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

IPC分类号： A61K31/5685 ,  A61K31/453

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.

摘要翻译： 在涉及施用性类固醇前体的易感染的温血动物（包括人）中治疗或减少获得阴道功能障碍的可能性的更多方法，特别是阴道干燥和性交痛，导致性功能障碍和性欲降低和表现。 进一步施用雌激素或选择性雌激素受体调节剂，特别是选自雷洛昔芬，阿唑西芬，他莫昔芬，德洛昔芬，托瑞昔芬，碘多昔芬，GW 5638，TSE-424，ERA-923和拉索昔芬的那些，更具体地， 一般结构：具体公开用于治疗和/或抑制某些上述疾病的发展。 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。

公开(公告)号：US20140045806A1

公开(公告)日：2014-02-13

申请号：US13942977

申请日：2013-07-16

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685

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.

摘要翻译： 阴道内DHEA用于治疗女性中至少一种选择的女性性欲欲障碍，女性性唤起障碍，女性性高潮障碍和女性性兴趣觉醒障碍中的至少一种病症，其中（1）不患有 外阴阴道萎缩的症状和/或（2）不患有中度至重度的性交疼痛。

公开(公告)号：US20120283230A1

公开(公告)日：2012-11-08

申请号：US13544407

申请日：2012-07-09

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685 ,  A61P15/02 ,  A61K31/568

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 also disclosed.

摘要翻译： 用于治疗或减少由绝经期，绝经后妇女，特别是骨质疏松症，阴道萎缩和干燥，性腺机能减退，性欲降低，皮肤萎缩，结缔组织病，尿失禁，乳腺，子宫内膜，卵巢等症状或疾病的可能性的新方法 公开了涉及施用性类固醇前体的敏感性温血动物，包括人类的易感温血动物，子宫癌，热潮红，肌肉量减少，胰岛素抵抗，疲劳，能量损失，衰老，身体症状的体征。 所述方法包括给予和给药脱氢表雄酮（DHEA）的新方法，以便利用阴道层薄层和/或肌层中的阳性雄激素作用，而不会不期望地引起全身性雌激素作用，以避免乳房和 子宫癌。 还公开了用于递送用于本发明的活性成分的药物组合物。

公开(公告)号：US20090042844A1

公开(公告)日：2009-02-12

申请号：US12100372

申请日：2008-04-09

申请人： Fernand LABRIE ,  Sylvain GAUTHIER ,  Julie CLOUTIER ,  Josee MAILHOT ,  Steeves POTVIN ,  Sylvain DION ,  Jean-Yves SANCEAU

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

IPC分类号： A61K31/58 ,  A61P35/00 ,  C07J43/00 ,  A61K31/56 ,  C07J3/00

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.

摘要翻译： 具有结构，其盐或N-氧化物衍生物的化合物用于治疗或减少获得雄激素依赖性疾病的可能性，例如前列腺癌，良性前列腺增生症，多囊卵巢综合征，痤疮，多毛症，皮脂溢，雄激素性脱发，以及 男性秃发。 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它方式制成任何药物剂型。 还公开了与其它活性药剂的组合。

公开(公告)号：US20150175576A1

公开(公告)日：2015-06-25

申请号：US14567970

申请日：2014-12-11

申请人： Fernand LABRIE ,  Shankar Mohan SINGH ,  Richard LABRECQUE ,  Liviu Constantin CIOBANU

发明人： Fernand LABRIE ,  Shankar Mohan SINGH ,  Richard LABRECQUE ,  Liviu Constantin CIOBANU

IPC分类号： C07D403/12 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/496 ,  A61K31/517 ,  A61K31/444 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/4725 ,  C07D401/12 ,  C07D401/14

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降低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，皮脂溢性，雄激素性脱发，男性秃发，肌肉萎缩的可能性 肌无力，男性性腺功能减退，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它方式制成任何药物剂型。 还公开了与其它活性药剂的组合。

公开(公告)号：US20130244989A1

公开(公告)日：2013-09-19

申请号：US13875027

申请日：2013-05-01

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685 ,  A61K31/453

CPC分类号： A61K31/5685 ,  A61K31/453 ,  A61K31/568

摘要： Novel methods for reduction or elimination the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly compounds having the general structure: Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

摘要翻译： 用于减少或消除热潮红，血管舒缩症状和盗汗发生的新方法，同时降低获得乳腺，子宫或子宫内膜癌的风险，并通过抑制骨质疏松，高胆固醇血症，高脂血症，动脉粥样硬化，高血压， 胰岛素抵抗，2型糖尿病，失去肌肉质量，肥胖，阿尔茨海默病，认知丧失，记忆丧失或易感温血动物包括人类的阴道干燥，包括施用一定量的性类固醇前体，特别是脱氢表雄酮 DHEA）和抗雌激素或选择性雌激素受体调节剂，特别是具有一般结构的化合物：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。

公开(公告)号：US20130005700A1

公开(公告)日：2013-01-03

申请号：US13602602

申请日：2012-09-04

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685 ,  A61P5/24

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 also disclosed.

摘要翻译： 用于治疗或减少由绝经期，绝经后妇女，特别是骨质疏松症，阴道萎缩和干燥，性腺机能减退，性欲降低，皮肤萎缩，结缔组织病，尿失禁，乳腺，子宫内膜，卵巢等症状或疾病的可能性的新方法 公开了涉及施用性类固醇前体的敏感性温血动物，包括人类的易感温血动物，子宫癌，热潮红，肌肉量减少，胰岛素抵抗，疲劳，能量损失，衰老，身体症状的体征。 所述方法包括给予和给药脱氢表雄酮（DHEA）的新方法，以便利用阴道层薄层和/或肌层中的阳性雄激素作用，而不会不期望地引起全身性雌激素作用，以避免乳房和 子宫癌。 还公开了用于递送用于本发明的活性成分的药物组合物。

公开(公告)号：US20120322778A1

公开(公告)日：2012-12-20

申请号：US13602503

申请日：2012-09-04

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685 ,  A61P15/12 ,  A61P5/24 ,  A61P19/10 ,  A61P3/08 ,  A61P17/00 ,  A61P19/04 ,  A61P13/00 ,  A61P35/00 ,  A61P21/00 ,  A61K31/568 ,  A61P15/02

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 also disclosed.

公开(公告)号：US20100317635A1

公开(公告)日：2010-12-16

申请号：US12791174

申请日：2010-06-01

申请人： Fernand LABRIE

发明人： Fernand LABRIE

IPC分类号： A61K31/5685 ,  A61K31/568 ,  A61P35/00 ,  A61P19/10 ,  A61P25/28 ,  A61P21/00 ,  A61P9/10 ,  A61P9/12 ,  A61P3/06 ,  A61P3/10 ,  A61P15/02 ,  B65D69/00

CPC分类号： A61K31/5685 ,  A61K31/453 ,  A61K31/568

摘要： Novel methods for reduction or elimination the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly compounds having the general structure: Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

摘要翻译： 用于减少或消除热潮红，血管舒缩症状和盗汗发生的新方法，同时降低获得乳腺，子宫或子宫内膜癌的风险，并通过抑制骨质疏松，高胆固醇血症，高脂血症，动脉粥样硬化，高血压， 胰岛素抵抗，2型糖尿病，失去肌肉质量，肥胖，阿尔茨海默病，认知丧失，记忆丧失或易感温血动物包括人类的阴道干燥，包括施用一定量的性类固醇前体，特别是脱氢表雄酮 DHEA）和抗雌激素或选择性雌激素受体调节剂，特别是具有一般结构的化合物：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。