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1. 发明授权

US06388109B1 14,15-cyclopropano steroids of the 19-norandrostane series, method for the production thereof and pharmaceutical preparations containing said compounds 失效
标题翻译： 19-去雄孕烷系列的环丙糖类固醇，其制备方法和含有所述化合物的药物制剂
公开(公告)号：US06388109B1
公开(公告)日：2002-05-14
申请号：US09719910
申请日：2000-12-20
申请人： Sigfrid Schwarz , Gerd Schubert , Sven Ring , Walter Elger , Birgitt Schneider , Günter Kaufmann , Lothar Sobek
发明人： Sigfrid Schwarz , Gerd Schubert , Sven Ring , Walter Elger , Birgitt Schneider , Günter Kaufmann , Lothar Sobek
IPC分类号： C07J5300
CPC分类号： C07J53/004
摘要： Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.
摘要翻译：描述了通式（I）的19-去雄孕烷系列及其药学上可接受的盐的新的14,15-环丙烷类固醇，其制备方法和含有这些化合物的药物制剂。化合物的特征是激素（孕激素和/或雄激素）活性。

2. 发明授权

US06534490B1 Unsaturated 14, 15-cyclopropanoandrostanes, method for the production thereof and pharmaceutical preparations containing said compounds 失效
标题翻译：不饱和14,15-环丙烷雄甾烷，其制备方法和含有所述化合物的药物制剂
公开(公告)号：US06534490B1
公开(公告)日：2003-03-18
申请号：US09720135
申请日：2000-12-21
申请人： Sven Ring , Sigfrid Schwarz , Walter Elger , Birgitt Schneider , Günter Kaufmann , Lothar Sobek
发明人： Sven Ring , Sigfrid Schwarz , Walter Elger , Birgitt Schneider , Günter Kaufmann , Lothar Sobek
IPC分类号： A61K3156
CPC分类号： C07J53/004
摘要： Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.
摘要翻译：描述了通式（I）的新的不饱和14,15-环丙烷 - 雄甾烷及其药学上可接受的盐，它们的制备方法和含有这些化合物的药物制剂。化合物的特征在于激素（孕激素和/或雄激素）活性，可用于激素替代疗法。

3. 发明授权

US07473709B2 11β-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones 失效
标题翻译： D-丁基-4,9-二烯-3-酮的11β-苯甲醛肟衍生物
公开(公告)号：US07473709B2
公开(公告)日：2009-01-06
申请号：US11635076
申请日：2006-12-07
申请人： Sven Ring , Gerd Schubert , Lothar Sobek
发明人： Sven Ring , Gerd Schubert , Lothar Sobek
IPC分类号： A61K31/15 , C07C251/32
CPC分类号： C07J41/0083
摘要： The present patent application relates to 11β-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of formula I bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.
摘要翻译：本专利申请涉及式I的D-homoestra-4,9-二烯-3-酮的11b-苯甲醛肟衍生物：其中R1是氢原子或C1-C6-烷基，C1-C6-酰基，C1- C 1 -C 6 - 烷基氨基羰基或芳基氨基羰基; 并且R 2是氢原子或C 1 -C 6烷基或C 1 -C 6酰基。式I化合物比孕酮受体更强地结合糖皮质激素受体，并且是有效的抗糖皮质激素。根据本发明，它们适用于治疗和/或预防可归因于由糖皮质激素，特别是皮质醇引起的雄激素缺乏症的症状和/或疾病。

4. 发明申请

US20070149621A1 11Beta-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones 失效
标题翻译： D-丁基-4,9-二烯-3-酮的11β-苯甲醛肟衍生物
公开(公告)号：US20070149621A1
公开(公告)日：2007-06-28
申请号：US11635076
申请日：2006-12-07
申请人： Sven Ring , Gerd Schubert , Lothar Sobek
发明人： Sven Ring , Gerd Schubert , Lothar Sobek
IPC分类号： A61K31/15 , C07C251/48
CPC分类号： C07J41/0083
摘要： The present patent application relates to 11β-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of formula I bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.
摘要翻译：本专利申请涉及式I的D-均聚-4,9-二烯-3-酮的11b-苯甲醛肟衍生物：其中R 1是氢原子或C 1 - C 1 -C 6 - 烷基，C 1 -C 6 - 酰基，C 1 -C 3 - 烷基，C 1 -C 6 - 酰基，C 1 -C 6 - C 1-4烷氧基羰基，C 1 -C 4 - 烷硫基羰基，C 1 -C 6亚烷基烷基氨基羰基或芳基氨基羰基; 且R 2是氢原子或C 1 -C 6 - C 6 - 烷基或C 1 -C 3 - SUB> 6 - 酰基。式I化合物比孕酮受体更强地结合糖皮质激素受体，并且是有效的抗糖皮质激素。根据本发明，它们适用于治疗和/或预防可归因于由糖皮质激素，特别是皮质醇引起的雄激素缺乏症的症状和/或疾病。

5. 发明授权

US06670493B2 Methods and compositions for treating diseases due to androgen deficiency with glucocorticoid receptor antagonist compounds and new compounds 失效
公开(公告)号：US06670493B2
公开(公告)日：2003-12-30
申请号：US10218085
申请日：2002-08-13
申请人： Vladimir Patchev , Lothar Sobek , Gerd Schubert
发明人： Vladimir Patchev , Lothar Sobek , Gerd Schubert
IPC分类号： C07J100
CPC分类号： C07J1/00 , C07J41/0083
摘要： The method of treating or preventing a disease in a human male or a male animal caused by a decreased production of androgens, such as testosterone, in the human male or male animal includes administering an effective amount of a glucocorticoid receptor antagonist to the human male or the male animal in order to increase production of the androgens. These diseases include male sexual dysfunction, infertility and hypogonadism. Novel androgen receptor antagonist compounds and methods of synthesis are also described.

6. 发明授权

US07250408B2 Glucocorticoid receptor antagonists for prophylaxis and therapy of glucocorticoid-mediated hypogonadism, of sexual dysfunction and/or infertility 失效
标题翻译：糖皮质激素受体拮抗剂用于预防和治疗糖皮质激素介导的性腺机能减退症，性功能障碍和/或不育症
公开(公告)号：US07250408B2
公开(公告)日：2007-07-31
申请号：US10735487
申请日：2003-12-12
申请人： Ulrich Bothe , Gerd Schubert , Guenter Kaufmann , Lothar Sobek , Vladimir Patchev , Alexander Hillisch
发明人： Ulrich Bothe , Gerd Schubert , Guenter Kaufmann , Lothar Sobek , Vladimir Patchev , Alexander Hillisch
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： A61K31/00 , A61K31/567 , A61K31/573 , C07J1/00
摘要： The novel glucocorticoid receptor antagonists are 11β-substituted steroid compounds of formula (I): wherein R1 denotes a methyl group, a methoxy group, or an ethoxy group; wherein R2 denotes a tert.-butyl group, a 1-hydroxy-1-methylethyl group, a 1-methoxy-1-methylethyl group, an ethyl isocrotonate group, or a substituted phenyl group. The method of treating an individual suffering from glucocorticoid-mediated hypogonadism, sexual dysfunctions, and/or infertility includes administering a daily dosage consisting of an effective amount of one of these 11β-substituted steroid compounds.
摘要翻译：新型糖皮质激素受体拮抗剂是式（I）的11b取代的类固醇化合物：其中R 1表示甲基，甲氧基或乙氧基; 其中R 2表示叔丁基，1-羟基-1-甲基乙基，1-甲氧基-1-甲基乙基，异巴豆酸乙酯基或取代的苯基。治疗患有糖皮质激素介导的性腺机能减退，性功能障碍和/或不孕症的个体的方法包括施用由有效量的这些11b取代的类固醇化合物之一组成的每日剂量。

7. 发明申请

US20070078091A1 Pharmaceutical combinations for compensating for a testosterone deficiency in men while simultaneously protecting the prostate 审中-公开
标题翻译：用于补偿男性睾酮缺乏症的药物组合，同时保护前列腺
公开(公告)号：US20070078091A1
公开(公告)日：2007-04-05
申请号：US11517301
申请日：2006-09-08
申请人： Doris Hubler , Michael Oettel , Lothar Sobek , Walter Elger , Abdul-Abbas Al-Mudhaffar
发明人： Doris Hubler , Michael Oettel , Lothar Sobek , Walter Elger , Abdul-Abbas Al-Mudhaffar
IPC分类号： A61K38/09 , A61K31/57 , A61K31/56 , A61K31/519 , A61K31/517 , A61K31/4709 , A61K31/138
CPC分类号： A61K31/565 , A61K31/57 , A61K31/585 , A61K45/06 , A61K2300/00
摘要： This invention relates to pharmaceutical combinations for compensating for an absolute and relative testosterone deficiency in men with simultaneous prophylaxis for the development of a benign prostatic hyperplasia (BPH) or prostate cancer. The combinations according to the invention contain a natural or synthetic androgen in combination with a gestagen, an antigestagen, an antiestrogen, a GnRH analog, a testosterone-5α-reductase inhibitor, an α-andreno-receptor blocker or a phosphodiesterase inhibitor. In comparison to the combinations according to the invention, any active ingredient by itself cannot achieve the desired goal.
摘要翻译：本发明涉及用于补偿男性绝对和相对睾酮缺乏的药物组合，同时预防良性前列腺增生（BPH）或前列腺癌的发展。根据本发明的组合含有天然或合成的雄激素与孕激素，抗原成分，抗雌激素，GnRH类似物，睾酮-5α-还原酶抑制剂，α-肾上腺素受体阻断剂或磷酸二酯酶抑制剂的组合。与根据本发明的组合相比，任何活性成分本身都不能实现期望的目标。

8. 发明申请

US20070010514A1 Non-steroidal progesterone receptor modulators 审中-公开
标题翻译：非甾体孕激素受体调节剂
公开(公告)号：US20070010514A1
公开(公告)日：2007-01-11
申请号：US11473325
申请日：2006-06-23
申请人： Ulrich Bothe , Alexander Hillisch , Peter Droescher , Gunter Kaufmann , Lothar Sobek , Ulrike Fuhrmann , Norbert Schmees , Wolfgang Schwede , Carsten Moeller
发明人： Ulrich Bothe , Alexander Hillisch , Peter Droescher , Gunter Kaufmann , Lothar Sobek , Ulrike Fuhrmann , Norbert Schmees , Wolfgang Schwede , Carsten Moeller
IPC分类号： A61K31/538 , C07D265/02
CPC分类号： C07D413/12 , C07D265/02
摘要： The present invention relates to non-steroidal progesterone receptor modulators of the general formula I, a process for their preparation, the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions comprising these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
摘要翻译：本发明涉及通式I的非甾体孕激素受体调节剂，其制备方法，孕酮受体调节剂用于生产药物的用途，以及包含这些化合物的药物组合物。根据本发明的化合物适用于治疗和预防妇科疾病如子宫内膜异位症，子宫平滑肌瘤，功能障碍性出血和痛经，以及用于治疗和预防激素依赖性肿瘤和用于女性生育控制和激素替代疗法。

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