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1. 发明授权

US08193252B1 Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders 有权
标题翻译：美孕激素（孕激素受体调节剂）用于治疗和预防良性激素依赖性妇科疾病
公开(公告)号：US08193252B1
公开(公告)日：2012-06-05
申请号：US10450029
申请日：2000-08-31
申请人： Kristof Chwalisz , Walter Elger , Gerd Shubert
发明人： Kristof Chwalisz , Walter Elger , Gerd Shubert
IPC分类号： A61K31/56
CPC分类号： A61K31/56 , Y10S514/843 , Y10S514/899
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。

2. 发明授权

US07629334B1 Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT) 有权
标题翻译：作为激素替代疗法（HRT）组合物组分的Mesoprogrestins（孕酮受体调节）
公开(公告)号：US07629334B1
公开(公告)日：2009-12-08
申请号：US10433984
申请日：2000-08-31
申请人： Kristof Chwalisz , Walter Elger , Gerd Schubert
发明人： Kristof Chwalisz , Walter Elger , Gerd Schubert
IPC分类号： A61K31/56 , C07J1/00 , C07J6/00
CPC分类号： A61K31/56
摘要： The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components 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 herein.
摘要翻译：使用中孕烯素作为药物组分用于制造用于激素替代疗法（HRT）的药物，以及作为与雌激素联合使用以用于制备用于HRT的药物的组合以及相应的HRT方法和方法治疗激素缺乏和激素不规则症状。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是本文优选的中孕酮。

3. 发明授权

US5719136A Combination of progesterone antagonists and antiestrogens with partial agonistic action for hormone substitution therapy for perimenopausal and postmenopausal women 失效
标题翻译：孕激素拮抗剂和抗雌激素与绝经后和绝经后妇女的激素替代疗法部分激动作用的组合
公开(公告)号：US5719136A
公开(公告)日：1998-02-17
申请号：US628702
申请日：1996-07-05
申请人： Kristof Chwalisz , Klaus Stockemann
发明人： Kristof Chwalisz , Klaus Stockemann
IPC分类号： A61K45/06 , A61K31/135 , A61K31/40 , A61K31/445 , A61K31/565 , A61K31/575 , A61P9/00 , A61P9/10 , A61P19/10 , A61P43/00
CPC分类号： A61K31/565 , A61K31/575 , Y10S514/01
摘要： This invention describes the use of at least one compound having a progesterone-antagonistic (PA) action and at least one compound having an antiestrogenic (AO) action with a simultaneous partial agonistic action for the production of pharmaceutical agents for hormone substitution therapy (HRT) for perimenopausal and postmenopausal women. In the case of combined use of progesterone antagonist and antiestrogen, the stimulation of the endometrium by the progesterone antagonist that is caused by its partial agonistic action when an antiestrogen is used by itself is inhibited. For example, a pharmaceutical agent according to the invention contains onapristone (progesterone antagonist) and tamoxifen (antiestrogen).
摘要翻译： PCT No.PCT / EP94 / 03408 Sec。 371日期：1996年7月5日第 102（e）日期1996年7月5日PCT 1994年10月17日PCT PCT。公开号WO95 / 11013 日期1995年4月27日本发明描述了至少一种具有孕酮拮抗作用（PA）作用的化合物和至少一种具有抗雌激素（AOE）作用的化合物与同时部分激动作用用于产生激素药物的用途围绝经期和绝经后妇女的替代疗法（HRT）。在组合使用孕酮拮抗剂和抗雌激素的情况下，由抗雌激素本身使用时由其部分激动作用引起的孕激素拮抗剂对子宫内膜的刺激被抑制。例如，根据本发明的药剂含有onapristone（孕酮拮抗剂）和他莫昔芬（antestrogen）。

4. 发明授权

US07148213B2 Antigestagenically active steroids with a fluorinated 17α-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US07148213B2
公开(公告)日：2006-12-12
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新的17α-氟烷基类固醇以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用，适用于制备药物制剂。

5. 发明申请

US20050064031A1 Combination contraceptive, kits that contain the latter, and a method that uses the latter 审中-公开
标题翻译：组合避孕药，含有后者的试剂盒，以及使用后者的方法
公开(公告)号：US20050064031A1
公开(公告)日：2005-03-24
申请号：US10982799
申请日：2004-11-08
申请人： Klaus Stockemann , Ulrich Koch , Kristof Chwalisz
发明人： Klaus Stockemann , Ulrich Koch , Kristof Chwalisz
IPC分类号： A61K45/00 , A61K31/00 , A61K31/565 , A61K31/57 , A61P15/00 , A61P15/18 , A61K31/56 , A61K9/20
CPC分类号： A61K31/565 , A61K31/57 , A61K2300/00
摘要： This invention relates to a multi-phase combination preparation that contains at least 28 daily dosage units: with a first phase of at least 21 initial daily dosage units, containing a competitive progesterone antagonist in a dosage which inhibits ovulation during the first above-named phase; and a second phase of 5 to 28 daily dosage units, in which each dosage unit of this second phase contains a gestagen, as well as a corresponding package (contraceptive kit) that contains this combination preparation and a contraceptive method which uses the combination preparation above.
摘要翻译：本发明涉及含有至少28个日剂量单位的多相组合制剂：第一阶段为至少21个初始日剂量单位，其中含有竞争性孕酮拮抗剂，其剂量在第一个上述阶段期间抑制排卵 ; 第二阶段为5〜28日剂量单位，其中第二阶段的每个剂量单位含有孕激素，以及含有该组合制剂的相应包装（避孕药盒）和使用上述组合制剂的避孕方法。

6. 发明授权

US06613757B1 COMBINATION OF PROSTACYCLIN WITH AN ESTROGEN OR PROGESTIN FOR THE PREVENTION AND TREATMENT OF ATHEROSCLEROTIC VASCULAR DISEASE INCLUDING PREECLAMPSIA AND FOR THE TREATMENT OF HYPERTENSION, AND FOR HORMONE REPLACEMENT THERAPY 失效
标题翻译：前列腺素与雌激素或前列腺素联合用于预防和治疗包括前列腺炎和治疗高血压以及霍尔米尔替代治疗的血管性血管疾病的预防和治疗
公开(公告)号：US06613757B1
公开(公告)日：2003-09-02
申请号：US08310950
申请日：1994-09-22
申请人： Robert E. Garfield , Kristof Chwalisz
发明人： Robert E. Garfield , Kristof Chwalisz
IPC分类号： A61K3158
CPC分类号： A61K31/566 , A61K31/565 , A61K31/567 , A61K31/57 , A61K31/5585 , A61K2300/00
摘要： Cardiovascular disease, including preeclampsia in pregnant women and hypertension in both women and men, are prevented or treated by administering thereto prostacyclin or a prostacyclin analog in combination with one or both of an estrogen and a progestin, which combination is also useful for HRT in peri- and post-menopausal women.
摘要翻译：通过与雌激素和孕激素中的一种或两种组合施用前列环素或前列环素类似物，预防或治疗心血管疾病，包括孕妇的先兆子痫和男性和男性的高血压，该组合也可用于围手术期的HRT - 和绝经后妇女。

7. 发明授权

US06316432B1 Antigestagenically active steroids with a flourinated 17 &agr;-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US06316432B1
公开(公告)日：2001-11-13
申请号：US09516359
申请日：2000-03-01
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with acids, and for —CO2R9 radicals with R9 meaning hydrogen as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了具有通式Ⅰ的新的17α-氟烷基类固醇以及它们与酸的生理上相容的盐，对于含有R9的-CO 2 R 9基团以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用适用于药物制剂的生产。

8. 发明申请

US20100004214A1 SEQUENTIAL SPRM/ PROGESTIN TREATMENT 审中-公开
标题翻译：序贯SPRM / PROGESTIN治疗
公开(公告)号：US20100004214A1
公开(公告)日：2010-01-07
申请号：US12558728
申请日：2009-09-14
申请人： Kristof Chwalisz
发明人： Kristof Chwalisz
IPC分类号： A61K31/56
CPC分类号： A61K31/57 , A61K31/56 , A61K31/585 , A61K45/06 , A61K2300/00
摘要： The methods provided herein comprise administering a selective progesterone receptor modulator (SPRM) during a first dosing period and at least one progestogen during a second dosing period. The dosing periods can run concomitantly or sequentially with or without a period where neither the SPRM nor the progestogen is administered.
摘要翻译：本文提供的方法包括在第一给药期间施用选择性孕酮受体调节剂（SPRM）和在第二给药期间施用至少一种孕激素。给药期可以伴随或顺序地伴随或不伴有施用SPRM和孕激素的期间。

9. 发明申请

US20050215535A1 Sequential SPRM/progestin treatment 审中-公开
标题翻译：顺序SPRM /孕激素治疗
公开(公告)号：US20050215535A1
公开(公告)日：2005-09-29
申请号：US10807942
申请日：2004-03-24
申请人： Kristof Chwalisz
发明人： Kristof Chwalisz
IPC分类号： A61K31/565 , A61K31/567 , A61K45/06 , A61K31/57 , A61K31/56
CPC分类号： A61K45/06 , A61K31/565 , A61K31/567 , A61K2300/00
摘要： The methods provided herein comprise administering a selective progesterone receptor modulator (SPRM) during a first dosing period and at least one progestogen during a second dosing period. The dosing periods can run concomitantly or sequentially with or without a period where neither the SPRM nor the progestogen is administered.
摘要翻译：本文提供的方法包括在第一给药期间施用选择性孕酮受体调节剂（SPRM）和在第二给药期间施用至少一种孕激素。给药期可以伴随或顺序地伴随或不伴有施用SPRM和孕激素的期间。

10. 发明申请

US20050080060A1 Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US20050080060A1
公开(公告)日：2005-04-14
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56 , A61P5/36 , C07J1/00 , C07J41/00 , C07J43/00 , C07J53/00
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ═N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen atom, an —OH, —NO2, —N3, —CN, —NR9aR9b, —NHSO2R9, —CO2R9, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R9a and R9b are the same or different and in the same way as R9 represent a hydrogen atom or a C1-C10 alkyl group, and for —NR9aR9b radicals, as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新型17α-氟烷基类固醇，其中R 1代表甲基或乙基，R 2代表式C n F m H o基团，其中n为2,3,4,5或 6，m> 1和m + o = 2n + 1，R 3表示游离的醚化或酯化的羟基，R 4和R 5各自代表氢原子，或一起代表另外的键或亚甲基，St代表部分式A，B或C的甾族ABC-环体系，其中R 6表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基或卤素原子，R 7表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基，或者如果St代表甾族ABC环系统A或B，另外R R 6和R 7一起可以表示另外的键，X表示氧原子，羟基亚氨基= N-OH或两个氢原子，R 8表示任意取代的基团Y或芳基几个地方有一个Y组，Y是一个氢原子，卤素原子，-OH，-NO 2，-N 3，-CN，-NR 9a R 9b，-NHSO 2 R 9，-CO 2 R 9，C 1 -C 10烷氧基，C 1 -C 10 烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟烷基或苯甲酰基，R 9a和R 9b相同或不同，并且R 9表示氢原子或C1- C10烷基，对于-NR 9a R 9b基团，以及它们与酸的生理上相容的盐以及具有R 9表示氢的-CO 2 R 9基团，以及它们与基地新化合物具有非常强的抗前体作用，适用于制备药物制剂。

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