公开(公告)号：EP3178480A1

公开(公告)日：2017-06-14

申请号：EP17151727.9

申请日：2010-06-16

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand

IPC分类号： A61K31/453 ,  A61K31/085 ,  A61K31/4025 ,  A61K31/56 ,  A61K31/5685 ,  A61K31/568 ,  A61P15/12

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

摘要： Novel methods for reduction or elimination of 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 benzopyran compounds. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

摘要翻译： 潮热，血管舒缩症状，并同时降低获取具有有益效果通过抑制骨质疏松症，高胆固醇血症，高脂血症，动脉粥样硬化的发展乳腺癌，子宫癌或子宫内膜癌和进一步更危险盗汗，高血压的发病率的减少或消除的新颖方法 ，胰岛素抵抗，2型糖尿病，在易感温血动物包括人类涉及性类固醇前体的量的施用肌肉质量，肥胖，阿尔茨海默氏病，认知的丧失，记忆丧失，或阴道干燥的损失，特别是去氢 （DHEA）和抗雌激素在一个或选择性雌激素受体调节剂，特别是苯并吡喃化合物。 用于递送活性成分（S）和试剂盒（或多个）本发明有用的药物组合物因此是游离缺失盘。

公开(公告)号：EP3116510A1

公开(公告)日：2017-01-18

申请号：EP15761680.6

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。

公开(公告)号：EP2386304B9

公开(公告)日：2014-11-05

申请号：EP11174925.5

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 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

公开(公告)号：EP2399582B9

公开(公告)日：2014-09-10

申请号：EP11174930.5

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 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

公开(公告)号：EP2441456A1

公开(公告)日：2012-04-18

申请号：EP11191361.2

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 ,  A61K9/02

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

摘要： A sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone-sulfate, androst-5-ene-3β,17β-diol, and 4-androsten-3,17-dione for use in a method of treating and/or reducing the likelihood of acquiring symptoms or diseases due to the menopause, or vaginal diseases or problems, in postmenopausal women is provided, said method comprising administering the sex steroid precursor to a patient in need of said treatment at a therapeutic amount which increases the level of circulating androgen metabolites, as part of a combination therapy with a therapeutically effective amount of a Selective Estrogen Receptor Modulator in order to decrease the risk of breast and uterine cancer normally present in postmenopausal women and to prevent bone loss, fat accumulation and diabetes type 2. Pharmaceutical compositions and kits for delivery of active ingredients useful to the invention are disclosed.

摘要翻译： 选自脱氢表雄甾酮，脱氢表雄酮硫酸酯，雄甾-5-烯-3,2,17,22-二醇和4-雄甾-3,17-二酮的性甾族前体，用于治疗和/或减少 提供了在绝经后妇女中获得由于更年期或阴道疾病或问题引起的症状或疾病的可能性，所述方法包括以增加循环雄激素水平的治疗量对需要所述治疗的患者施用性类固醇前体 代谢物，作为与治疗有效量的选择性雌激素受体调节剂的组合疗法的一部分，以降低通常存在于绝经后妇女中的乳腺和子宫癌的风险，并预防骨丢失，脂肪蓄积和2型糖尿病。药物组合物 并且公开了用于递送用于本发明的活性成分的试剂盒。

公开(公告)号：EP2399582A1

公开(公告)日：2011-12-28

申请号：EP11174930.5

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 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or inhibition of the development of breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3ß,17ß-diol, and compounds converted in vivo to one of the foregoing precursors.
Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursors is disclosed. Pharmaceutical compositions for delivery of active ingredients and kits useful to the invention are disclosed.

摘要翻译： 涉及施用选择性雌激素受体调节剂的敏感温血动物（包括人）在内的用于治疗和/或抑制乳腺癌发展，高胆固醇血症，高脂血症或动脉粥样硬化的新方法，以及选自以下组中的一种性类固醇前体 的脱氢表雄甾酮，硫酸脱氢表雄酮，雄甾-5-烯-3β，17β-二醇，以及在体内转化成前述前体之一的化合物。 公开了将二膦酸盐与选择性雌激素受体调节剂和/或性类固醇前体组合的进一步给药。 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。

公开(公告)号：EP2386305A3

公开(公告)日：2011-12-07

申请号：EP11174933.9

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 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or inhibition of the development of breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3β,17β-diol, and compounds converted in vivo to one of the foregoing precursors.
Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursors is disclosed. Pharmaceutical compositions for delivery of active ingredients and kits useful to the invention are disclosed.

摘要翻译： 用于治疗和/或抑制敏感性温血动物包括人类中的乳腺癌，高胆固醇血症，高脂血症或动脉粥样硬化发展的新方法包括给予选择性雌激素受体调节剂和一定量的性类固醇前体，所述性类固醇前体选自： 脱氢表雄酮，脱氢表雄酮硫酸盐，雄甾-5-烯-3β，17β-二醇，以及体内转化成前述前体之一的化合物。 披露了进一步施用双膦酸盐与选择性雌激素受体调节剂和/或性类固醇前体的组合。 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：EP1623712A3

公开(公告)日：2009-12-16

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 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or inhibition of the development of breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warmblooded animals including humans involving administration of selective estrogen receptor modulator and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3β,17β-diol, and compounds converted in vivo to one of the foregoing precursors.
Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursors is disclosed. Pharmaceutical compositions for delivery of active ingredients and kits useful to the invention are disclosed.

摘要翻译： 用于治疗和/或抑制涉及施用选择性雌激素受体调节剂的敏感温血动物（包括人）中的乳腺癌，高胆固醇血症，高脂血症或动脉粥样硬化发展的新方法，以及选自脱氢表雄酮 ，脱氢表雄酮硫酸酯，雄甾-5-烯-3,2α-二醇，以及在体内转化成前述前体之一的化合物。 公开了将二膦酸盐与选择性雌激素受体调节剂和/或性类固醇前体组合的进一步给药。 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。

公开(公告)号：EP1899305A1

公开(公告)日：2008-03-19

申请号：EP06752811.7

申请日：2006-06-16

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand ,  BRETON, Rock ,  SINGH, Shankar, Mohan ,  MALTAIS, Rene

IPC分类号： C07D233/42 ,  A61K31/4178 ,  A61K31/4166 ,  A61K31/5377 ,  C07D403/12 ,  C07D413/12

CPC分类号： C07D417/12 ,  C07D207/40 ,  C07D211/48 ,  C07D233/74 ,  C07D233/86

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 and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

公开(公告)号：EP1807062A1

公开(公告)日：2007-07-18

申请号：EP05799216.6

申请日：2005-10-31

申请人： ENDORECHERCHE INC.

发明人： EL-ALFY, Mohamed ,  LABRIE, Fernand ,  AZZI, Lamia

IPC分类号： A61K31/00

CPC分类号： A61K31/57 ,  A61K8/63 ,  A61K31/568 ,  A61Q19/08

摘要： Novel methods of treating or reducing the likelihood of acquiring skin diseases due to age-related androgen deficiency, particularly skin atrophy, loss of collagen, loss of elastic fibers, loss of connective tissue, cellulite, and formation of wrinkles, in susceptible warm-blooded animals including humans involving administration of an androgen or/and a sex steroid precursor. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.