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1. 发明专利

CA2130515A1 11-BENZALDOXIME-17 -METHOXY-17.-METHOXYMETHYLESTRADIENE DERIVATIVES, METHODS FOR THEIR PRODUCTION AND PHARMACEUTICALS CONTAINING THESE SUBSTANCES 未知
公开(公告)号：CA2130515A1
公开(公告)日：1995-03-21
申请号：CA2130515
申请日：1994-08-19
申请人： SCHUBERT GERD , KAUFMANN GUENTER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
发明人： SCHUBER GERD , KAUFMANN GUENTER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
IPC分类号： A61K31/565 , A61K31/56 , A61P5/24 , A61P13/02 , A61P15/00 , A61P35/00 , C07J1/00 , C07J41/00 , C07J75/00
摘要： Novel 11-benzaldoxime-estra-diene derivatives of the general Formula I and their pharmaceutically-acceptable salts, processes for their production, and pharmaceutical composition containing such compounds, are provided herein. I n such compounds of Formula I, Z is -CO-CH3, -CO-0-C2H5, -CO-NH-phenyl, -CO-NH-C2H5 , -CO-C2H5, CH3, or -CO-phenyl. Such compounds of the general, Formula I are produced by the esterification or the urethane formation of a compound of the general Formula II with a compound of the general Formula II by the reaction of that compound with an esterifying, or an etherifying or a n urethane- forming agent which contains the group Z, or its precursor. Such compounds show strong antigestagenic effects combined with reduced glucocorticoid activity.

2. 发明专利

CA2130516C NEW 11-BENZALDOXIME-ESTRADIENE DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICALS CONTAINING THESE SUBSTANCES 未知
公开(公告)号：CA2130516C
公开(公告)日：2003-04-15
申请号：CA2130516
申请日：1994-08-19
申请人： SCHUBERT GERD , KAUFMANN GUNTHER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
发明人： SCHUBERT GERD , KAUFMANN GUNTHER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
IPC分类号： A61K31/56 , A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , C07J41/00 , C07J75/00
摘要： Novel 11-benzaldoxime-estra-diene derivatives of the general Formula I (see formula I) or their pharmaceutically acceptable salts are provided herein, as well as processes for their production, and pharmaceuticals containing such compounds. In such compound of the general Formula I, Z, R1, R2 and R3 are specifically defined . Such compounds show strong antigestagenic effects combined with reduced glucocorticoid activity, and thus provide novel uses of such compounds.

3. 发明专利

CA2130516A1 NEW 11-BENZALDOXIME-ESTRADIENE DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICALS CONTAINING THESE SUBSTANCES 未知
公开(公告)号：CA2130516A1
公开(公告)日：1995-03-21
申请号：CA2130516
申请日：1994-08-19
申请人： SCHUBERT GERD , KAUFMANN GUENTHER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
发明人： SCHUBERT GERD , KAUFMANN GUENTHER , SOBECK LOTHAR , OETTEL MICHAEL , ELGER WALTER , KURISCHKO ANATOLI
IPC分类号： A61K31/56 , A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , C07J41/00 , C07J75/00
摘要： Novel 11-benzaldoxime-estra-diene derivatives of the general Formula I (see formula I) or their pharmaceutically acceptable salts are provided herein, as well as processes for their production, and pharmaceuticals containing such compounds. In such compound of the general Formula I, Z, R1, R2 and R3 are specifically defined . Such compounds show strong antigestagenic effects combined with reduced glucocorticoid activity, and thus provide novel uses of such compounds.

4. 发明申请

WO9965228A2 PHARMACEUTICAL COMBINATIONS FOR COMPENSATING FOR A TESTOSTERONE DEFICIENCY IN MEN WHILE SIMULTANEOUSLY PROTECTING THE PROSTATE 审中-公开
标题翻译： AT THE MAN补偿睾酮亏缺的药物组合，与前列腺法同时保护
公开(公告)号：WO9965228A2
公开(公告)日：1999-12-16
申请号：PCT/DE9901652
申请日：1999-06-07
申请人： JENAPHARM GMBH , HUEBLER DORIS , OETTEL MICHAEL , SOBEK LOTHAR , ELGER WALTER , AL MUDHAFFAR ABDUL ABBAS
发明人： HUEBLER DORIS , OETTEL MICHAEL , SOBEK LOTHAR , ELGER WALTER , AL-MUDHAFFAR ABDUL-ABBAS
IPC分类号： A61K31/56 , A61K31/565 , A61K31/568 , A61K31/569 , A61K31/57 , A61K45/06 , A61P13/08 , A61P35/00 , H04N5/00
CPC分类号： A61K31/565 , A61K31/57 , A61K31/585 , A61K45/06 , A61K2300/00
摘要： The invention relates to pharmaceutical combinations for compensating for an absolute and relative testosterone deficiency in men while simultaneously preventing the development of benign prostatic hypertrophy (BPH) or of prostatic cancer. The inventive combinations contain a natural or synthetic androgen combined with a gestagen, an antigestagen, an antiestrogen, a GnRH analog, a testosterone-5 alpha -reductase inhibitor, an alpha -adrenergic blocking agent or a phosphodiesterase inhibitor. Compared to the inventive combinations, each active ingredient cannot carry out the desired objective alone.
摘要翻译：本发明涉及药物组合用于人在同时预防补偿的绝对和相对睾酮赤字或前列腺癌的前列腺增生的发展（BPH）。本发明的组合包含在组合的天然或合成的雄激素与孕激素，一个antigestagen，抗雌激素药，一个GnRH的类似物，睾酮5的α还原酶抑制剂，α--Andrenorezeptorblocker或磷酸二酯酶抑制剂。相比于单独每种药物的新组合无法实现预期目标。

5. 发明申请

WO0219971A9 4-HALOGENATED 17-METHYLENE STEROIDS, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 审中-公开
标题翻译： 4卤代17甲基甾类，方法生产它们和药物组合物含
公开(公告)号：WO0219971A9
公开(公告)日：2002-08-08
申请号：PCT/EP0109943
申请日：2001-08-29
申请人： JENAPHARM GMBH , MENZENBACH BERND , ELGER WALTER , DROESCHER PETER , HILLISCH ALEXANDER , KAUFMANN GUENTER , SCHWEIKERT HANS-UDO , MUELLER GERD
发明人： MENZENBACH BERND , ELGER WALTER , DROESCHER PETER , HILLISCH ALEXANDER , KAUFMANN GUENTER , SCHWEIKERT HANS-UDO , MUELLER GERD
IPC分类号： A61K31/569 , A61K31/57 , A61P5/24 , A61P5/28 , A61P5/34 , A61P13/08 , A61P15/16 , A61P15/18 , A61P17/10 , A61P17/14 , A61P43/00 , C07J13/00 , C07J17/00 , A61K31/56
CPC分类号： C07J13/007
摘要： The invention relates to 17-Methylene steroids. Method for the production thereof and pharmaceutical compositions containing these compounds. The inventive compounds have an active profile with a hybrid character of such that they act as inhibitors of the 5 alpha -reductase and, at the same time, as gestagens. Said compounds are thus suited for treating medical disorders that, in men and women, are a result of an increased androgen level in certain organs and tissues. The inventive compounds combined with other hormonal substances such as estrogen, testosterone or a potent androgen are suited as contraceptives for women and men.
摘要翻译：本发明涉及17-亚甲基甾类，处理用于含有这些化合物和药物组合物及其制备。本发明的化合物具有与在它们用作5α还原酶的抑制剂，并在同一时间作为孕激素的方式混合字符的有效简表。因此，它们适用于治疗男性疾病和女性在某些器官和组织，从而提高雄激素水平。与其它激素物质如雌激素，睾甾酮或强雄激素结合，本发明的化合物适合作为避孕药的妇女和男性。

6. 发明申请

WO0226759A3 17 alpha FLUOROALKYL STEROIDS, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译： 17α-氟烷基stareroids，它们的制备方法和含有这些化合物的药物组合物
公开(公告)号：WO0226759A3
公开(公告)日：2002-06-20
申请号：PCT/DE0103732
申请日：2001-09-28
申请人： JENAPHARM GMBH , RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
发明人： RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
IPC分类号： A61K31/569 , A61K31/58 , A61P5/26 , A61P15/00 , A61P15/10 , A61P15/16 , A61P35/00 , C07J1/00 , C07J11/00 , C07J43/00 , C07J71/00 , A61K31/565
CPC分类号： C07J71/0047 , C07J1/0037 , C07J1/0085 , C07J11/00 , C07J71/0063 , C07J71/0084
摘要： The invention relates to 17 alpha fluoroalkyl steroids of the general formula (I), STEROID (I), wherein R3 represents a group of the formula CnFmHo, wherein n = 1, 2, 3, 4, 5 or 6, m > 1 and m+o = 2n+1. The invention further relates to methods for producing the same and to compositions that contain said compounds. The inventive composition of the general formula (I) possess androgenic activity.
摘要翻译：本发明涉及17阿尔法-Fluoraklylsteroide通式（I）其中R 3是下式基团的CnFmHo，其中n = 1，2，3，4，5或6，M> 1，且m + O = 2N + 1 其制备方法和含有这些化合物的药物组合物。根据本发明的通式（I）的化合物具有雄激素活性。

7. 发明申请

WO0134126A2 MESOPROGESTINS (PROGESTERONE RECEPTOR MODULATORS) AS A COMPONENT OF COMPOSITIONS FOR HORMONE REPLACEMENT THERAPY (HRT) 审中-公开
标题翻译：作为激素替代疗法（HRT）组分的组分的孕酮（孕酮受体调节剂）
公开(公告)号：WO0134126A2
公开(公告)日：2001-05-17
申请号：PCT/US0023771
申请日：2000-08-31
申请人： JENAPHARM GMBH , ELGER WALTER , CHWALISZ KRISTOF , SCHUBERT GERD
发明人： ELGER WALTER , CHWALISZ KRISTOF , SCHUBERT GERD
IPC分类号： A61K45/00 , A61K31/565 , A61P5/30 , A61K31/00
CPC分类号： A61K31/565
摘要： The present invention refers to the use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as component for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
摘要翻译：本发明涉及中孕酮作为药物组分用于制备用于激素替代疗法（HRT）的药物和作为与雌激素一起用于组合使用的组分用于制备用于HRT以及相应HRT的药物的用途 - 治疗激素缺乏和激素不规则症状的方法和方法。中孕酮被定义为在体内孕激素受体（PR）具有激动和拮抗活性的化合物。它们将PR的功能稳定在激动和拮抗的中等水平。孕激素或抗孕激素不能达到相应的功能状态。 J867，J912，J956和J1042是根据本发明优选的中孕酮。

8. 发明申请

WO0134126A9 MESOPROGESTINS (PROGESTERONE RECEPTOR MODULATORS) AS A COMPONENT OF COMPOSITIONS FOR HORMONE REPLACEMENT THERAPY (HRT) 审中-公开
标题翻译：作为激素替代治疗组合物的组分（HRT）的MESOPROGESTINS（孕酮受体调节剂）
公开(公告)号：WO0134126A9
公开(公告)日：2002-09-12
申请号：PCT/US0023771
申请日：2000-08-31
申请人： JENAPHARM GMBH , ELGER WALTER , CHWALISZ KRISTOF , SCHUBERT GERD
发明人： ELGER WALTER , CHWALISZ KRISTOF , SCHUBERT GERD
IPC分类号： A61K45/00 , A61K31/565 , A61P5/30
CPC分类号： A61K31/565
摘要： The present invention refers to the use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as component for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
摘要翻译：本发明涉及使用中孕烯孕酮作为制备用于激素替代疗法（HRT）的药物的药物成分的用途，以及与雌激素联合使用的组分用于制备用于HRT的药物以及相应的HRT 治疗激素缺乏症和激素不规则症状的方法和方法。中孕烯孕素被定义为在体内孕酮受体（PR）具有激动作用和拮抗活性的化合物。他们将PR的功能稳定在激进和对抗的中间水平。孕激素或抗孕激素不能达到相应的功能状态。 J867，J912，J956和J1042是根据本发明优选的中孕妇。

9. 发明申请

WO0126603A3 MESOPROGESTINS (PROGESTERONE RECEPTOR MODULATORS) AS A COMPONENT OF FEMALE CONTRACEPTIVES 审中-公开
标题翻译：雌激素受体调节剂（孕激素受体调节剂）作为雌激素受体的组分
公开(公告)号：WO0126603A3
公开(公告)日：2002-01-17
申请号：PCT/IB0002053
申请日：2000-08-31
申请人： JENAPHARM GMBH , CHWALISZ KRISTOF , ELGER WALTER , SCHUBERT GERD
发明人： CHWALISZ KRISTOF , ELGER WALTER , SCHUBERT GERD
IPC分类号： A61K45/00 , A61K31/565 , A61P5/30 , A61P15/18 , A61K31/567
CPC分类号： A61K31/567 , A61K31/565 , A61K2300/00
摘要： The present invention relates to the use of mesoprogestins for the production of a pharmaceutical for female contraception, to a pharmaceutical preparation for female contraception and to a method of female contraception administering effective amounts of a mesoprogestin in a female desiring contraception. Optionally the mesoprogestin can be used in combination with an estrogen. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
摘要翻译：本发明涉及中孕烯孕酮用于制造女性避孕药物的用途，涉及一种女性避孕药物制剂，以及一种女性避孕方法，在雌性避孕方法中施用有效量的中孕妇。任选地，中孕酮可以与雌激素联合使用。中孕烯孕素被定义为在体内孕酮受体（PR）具有激动作用和拮抗活性的化合物。他们将PR的功能稳定在激进和对抗的中间水平。孕激素或抗孕激素不能达到相应的功能状态。 J867，J912，J956和J1042是根据本发明优选的中孕妇。

10. 发明申请

WO0115679A3 MESOPROGESTINS FOR THE TREATMENT AND PREVENTION OF BENIGN HORMONE DEPENDENT GYNECOLOGICAL DISORDERS 审中-公开
标题翻译：治疗和预防胆固醇依赖性心脏病的MOPOPOS
公开(公告)号：WO0115679A3
公开(公告)日：2001-11-22
申请号：PCT/US0023770
申请日：2000-08-31
申请人： JENAPHARM GMBH , CHWALISZ KRISTOF , ELGER WALTER , SCHUBERT GERD
发明人： CHWALISZ KRISTOF , ELGER WALTER , SCHUBERT GERD
IPC分类号： A61K45/00 , A61K31/4365 , A61K31/57 , A61K38/00 , A61K45/06 , A61P15/00 , A61P15/04 , A61P35/00 , A61K31/00 , A61K31/567 , A61K38/08 , A61K38/09 , A61K38/14
CPC分类号： A61K31/57 , A61K45/06
摘要： This present invention disclosed the use of mesoprogestins, a new class of progesterone receptor modulators (PRMs), for the treatment and prevention of benign hormone dependent gynecological disorders: a) for the treatment of gynecological disorder such as endometriosis, uterine fibroids, postoperative peritoneal adhesions, dysfunctional bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; b) for the prevention of gynecological disorders such as postoperative, peritoneal adhesions, dysfunctional uterine bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; and c) a method of treatment and prevention of the above mentioned disorders in a female, preferably in a human female, in need of treatment or prevention of one or more of these disorders, with an effective amount of a mesoprogestin. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. The daily dose of mesoprogestin is 0.5 to 100 mg, preferably 5.0 to 50 mg and most preferably 10 to 25 mg. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
摘要翻译：本发明公开了用于治疗和预防良性激素依赖性妇科疾病的新型孕激素受体调节剂（PRM）的使用：a）用于治疗妇科疾病如子宫内膜异位症，子宫肌瘤，术后腹膜粘连功能障碍性出血（metrorrhagia，月经过多）和痛经; b）用于预防妇科疾病如术后，腹膜粘连，功能障碍性子宫出血（metrorrhagia，月经过多）和痛经; 和c）有效量的中孕酮治疗和预防女性，优选在人类女性中需要治疗或预防这些疾病中的一种或多种的上述病症的方法。中孕烯孕素被定义为在体内孕酮受体（PR）具有激动作用和拮抗活性的化合物。他们将PR的功能稳定在激进和对抗的中间水平。孕激素或抗孕激素不能达到相应的功能状态。中孕酮的日剂量为0.5〜100mg，优选为5.0〜50mg，最优选为10〜25mg。 J867，J912，J956和J1042是根据本发明优选的中孕妇。

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