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1. 发明申请

WO2012087389A1 NOVEL 19-NOR-STEROIDS AND THEIR USE FOR TREATING PROGESTERONE-DEPENDENT CONDITIONS 审中-公开
标题翻译：新一代19-非甾体化合物及其用于治疗依赖前列腺素的条件
公开(公告)号：WO2012087389A1
公开(公告)日：2012-06-28
申请号：PCT/US2011/050859
申请日：2011-09-08
申请人： REPROS THERAPEUTICS INC. , PODOLSKI, Joseph, S. , WIEHLE, Ronald, D.
发明人： PODOLSKI, Joseph, S. , WIEHLE, Ronald, D.
IPC分类号： C07J9/00 , A61K31/57 , A61P5/36
CPC分类号： C07J7/008 , C07J5/0053 , C07J7/0045
摘要： The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.
摘要翻译：本发明的主题涉及激素依赖性病症的治疗领域。公开了用于处理这些条件的新化合物和方法。本发明的实施方案公开了治疗子宫内膜异位症，痛经，乳腺癌，子宫肌瘤和子宫内膜过度增生的方法。

2. 发明申请

WO2011157443A1 (11B,17A)-11-(4-(2-11C-ACETYL)PHENYL)-17,23-EPOXY-19,24-DINORCHOLA-4,9,20-TRIEN-3-ONE 审中-公开
标题翻译：（11B，17A）-11-（4-（2-11C - 乙酰基）苯基）-17,23-EPOXY-19,24-DINORCHOLA-4,9,20三烯-3-酮
公开(公告)号：WO2011157443A1
公开(公告)日：2011-12-22
申请号：PCT/EP2011/003012
申请日：2011-06-17
申请人： N.V. ORGANON , BRANDS, Franciscus Theodorus Leonardus , HAMERSMA, Johannes, Antonius, Maria , WIEGERINCK, Peter, Hermanus, Gerardus
发明人： BRANDS, Franciscus Theodorus Leonardus , HAMERSMA, Johannes, Antonius, Maria , WIEGERINCK, Peter, Hermanus, Gerardus
IPC分类号： C07J21/00 , A61K31/58 , G01N33/74 , A61P5/36
CPC分类号： C07J53/001 , A61K51/0493 , C07J21/00
摘要： The present invention relates to (11β,17α)-11-(4-(2- 11 C-acetyl)phenyl)-17,23- epoxy-19,24-dinorchola-4,9,20-trien-3-one, an 11 C-labelled ORG 33628; a process for the preparation thereof, intermediates used in this process and the use of this compound as a PET tracer for the detection of breast cancer.
摘要翻译：本发明涉及（11β，17a）-11-（4-（2-11C-乙酰基）苯基）-17,23-环氧-19,24-二肉豆蔻-4,9,20-三烯-3-酮， 11C标记的ORG 33628; 其制备方法，该方法中使用的中间体以及该化合物作为PET示踪剂用于检测乳腺癌的用途。

3. 发明申请

WO2011015892A3 NOVEL CRYSTAL FORM OF CDB - 4124 AND PROCES S FOR THE PREPARATION THEREOF 审中-公开
标题翻译： CDB的新型晶体形式 - 4124及其制备方法
公开(公告)号：WO2011015892A3
公开(公告)日：2011-03-31
申请号：PCT/HU2010000088
申请日：2010-08-05
申请人： RICHTER GEDEON NYRT , BALAZS ATTILA , CSOERGEI JANOS , DEMETER ADAM , SANTA CSABA
发明人： BALAZS ATTILA , CSOERGEI JANOS , DEMETER ADAM , SANTA CSABA
IPC分类号： C07J41/00 , A61K31/573 , A61P5/36
CPC分类号： A61K31/573 , C07J41/0083
摘要： The present invention relates to novel crystalline Form II of 17a-acetoxy-21-methoxy-11ß-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical composition comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof.
摘要翻译：本发明涉及17a-乙酰氧基-11-甲氧基-11β-[4-N，N-二甲基氨基苯基] -19-去甲基-4,9-二烯-3,20-二酮的新型结晶形式II（也称为 CDB-4124），其制备方法和包含它的药物组合物。 II型可以从不同的介质如C1-C4醇和羧酸，酮，环己烷，乙腈，二甲基甲酰胺，二甲基亚砜，水及其任何混合物中结晶出来。

4. 发明申请

WO2010142705A1 SUBSTITUTED 16,17-ANNELLATED STEROID COMPOUNDS FOR USE IN WOMEN'S HEALTHCARE 审中-公开
标题翻译：用于妇女健康服用的16,17-ANNELLATED STEROID化合物
公开(公告)号：WO2010142705A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/058042
申请日：2010-06-09
申请人： N.V. ORGANON , DIJCKS, Fredericus, Antonius , LOOZEN, Hubert, Jan, Jozef , ADDO, Samira , EDERVEEN, Antonius, Gerardus, Hendrikus
发明人： DIJCKS, Fredericus, Antonius , LOOZEN, Hubert, Jan, Jozef , ADDO, Samira , EDERVEEN, Antonius, Gerardus, Hendrikus
IPC分类号： C07J53/00 , A61K31/57 , A61P5/30 , A61P5/32 , A61P5/34 , A61P5/36
CPC分类号： C07J53/002
摘要： The present invention relates to substituted steroid compounds having the formula (I) Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
摘要翻译：本发明涉及具有式（I）的取代的类固醇化合物，其中R1是H或卤素; R2是H，（1C-4C）烷基，（1C-4C）酰基，葡糖醛酸或氨磺酰基; R3是H或卤素; R4是H，（1C-4C）烷基，（2C-4C）烯基或（2C-4C）炔基; R5是甲基或乙基; R6是H或甲基; R7是H或甲基; R8是H或酰基，用于治疗和预防子宫内膜异位，避孕，绝经期和绝经后妇女的激素治疗，治疗骨质疏松症和治疗子宫肌瘤和其他月经相关疾病，如功能障碍崩漏。

5. 发明申请

WO2008113851A3 NOVEL C11 MODIFIED RETROSTEROIDS AS PROGESTERONE RECEPTOR MODULATOR COMPOUNDS 审中-公开
标题翻译：新型C11改性复方作为孕激素受体调节剂化合物
公开(公告)号：WO2008113851A3
公开(公告)日：2008-11-20
申请号：PCT/EP2008053365
申请日：2008-03-20
申请人： SOLVAY PHARM GMBH , MESSINGER JOSEF , BOECKER CHRISTIANE , HUSEN BETTINA , THOLE HEINRICH-HUBERT , HINAJE MARIA , BUCHHOLZ MONIKA
发明人： MESSINGER JOSEF , BOECKER CHRISTIANE , HUSEN BETTINA , THOLE HEINRICH-HUBERT , HINAJE MARIA , BUCHHOLZ MONIKA
IPC分类号： C07J15/00 , A61K31/57 , A61P5/34 , A61P5/36
CPC分类号： C07J15/005
摘要： Described herein arenew retrosteroidal compounds of general formula (I), representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. Saidcompounds are preferably used for the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for HRT.
摘要翻译：本文描述了代表孕酮受体调节剂及其制备的通式（I）的新型逆甾体化合物和含有这些化合物的药物制剂。所述化合物优选用于治疗良性妇科疾病，例如子宫内膜异位症和子宫肌瘤，以及用于女性避孕和HRT。

6. 发明申请

WO2008128791A2 PROGESTERONE-RECEPTOR ANTAGONIST FOR USE IN BRCA ALONE OR AS COMBINATION WITH ANTIESTROGEN 审中-公开
标题翻译：用于BRCA的PROGESTERONE-RECEPTOR ANTAGONIST或与ANENSTROGEN组合使用
公开(公告)号：WO2008128791A2
公开(公告)日：2008-10-30
申请号：PCT/EP2008003333
申请日：2008-04-21
申请人： BAYER SCHERING PHARMA AG , HOFFMANN JENS , KORR DANIEL
发明人： HOFFMANN JENS , KORR DANIEL
IPC分类号： A61K31/00 , A61K31/567 , A61K31/573 , A61K45/06 , A61P5/32 , A61P5/36
CPC分类号： A61K45/06 , A61K31/00 , A61K31/567 , A61K31/573 , A61K2300/00
摘要： The present invention relates to the single use of the progesterone-receptor antagonist 11ß-(-4-acetylpheny)-17 ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)- estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, as well as to a combination comprising the progesterone- receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2- pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one pure antiestrogen, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer.endometriosis, myeloma, myoma and meningioma. The present invention also relates to a combination of the progesterone-receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)-estra-4,9- dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one EGF or EGFR targeting drug, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer, endometriosis, myeloma, myoma and meningioma.
摘要翻译：本发明涉及孕酮 - 受体拮抗剂11β-（ - 4-乙酰基苯基）-17β-羟基-17a-（1,1,2,2,2-五氟乙基） - 雌甾-4,9- 二烯-3-酮或其药学上可接受的衍生物或类似物，用于预防和治疗BRCA1或BRCA2介导的乳腺癌，以及包含孕酮受体拮抗剂11β-（4-乙酰基苯基）-17β （1,1,2,2,2-五氟乙基） - 雌-4,9-二烯-3-酮或其药学上可接受的衍生物或类似物以及至少一种纯抗雌激素用于预防和BRCA1或BRCA2介导的乳腺癌，卵巢癌子宫内膜癌，胃癌，结肠直肠癌，子宫内膜异位症，骨髓瘤，肌瘤和脑膜瘤的治疗。本发明还涉及孕酮受体拮抗剂11β-（4-乙酰基苯基）-17β-羟基-17a-（1,1,2,2,2-五氟乙基） - 雌-4,9-二烯 -3-或其药学上可接受的衍生物或类似物，以及至少一种EGF或EGFR靶向药物，用于预防和治疗BRCA1或BRCA2介导的乳腺癌，卵巢癌子宫内膜癌，胃癌，结肠直肠癌，子宫内膜异位症，骨髓瘤，肌瘤和脑膜瘤。

7. 发明申请

WO2007118717A3 METHOD FOR PREPARING 4-[17β-METHOXY-17α-METHOXYMETHYL-3-OXOESTRA-4,9-DIEN-11β-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL) 审中-公开
公开(公告)号：WO2007118717A3
公开(公告)日：2007-10-25
申请号：PCT/EP2007/003723
申请日：2007-04-17
申请人： BAYER SCHERING PHARMA AKTIENGESELLSCHAFT , GRAWE, Detlef , GLIESING, Sabine , GERECKE, Hagen , HOESEL, Peter , MUELLER, Uwe , MICHEL, Thomas , EILERS, Robert , KNABE, Uwe , ERHART, Bernd , MOSEBACH, Michael , VOIGTLAENDER, David , TILSTAM, Ulf , JACKE, Juergen , BAHL, Klaus , BOHLMANN, Ulf , WEHMEIER, Dieter , SANDER, Michael
发明人： GRAWE, Detlef , GLIESING, Sabine , GERECKE, Hagen , HOESEL, Peter , MUELLER, Uwe , MICHEL, Thomas , EILERS, Robert , KNABE, Uwe , ERHART, Bernd , MOSEBACH, Michael , VOIGTLAENDER, David , TILSTAM, Ulf , JACKE, Juergen , BAHL, Klaus , BOHLMANN, Ulf , WEHMEIER, Dieter , SANDER, Michael
IPC分类号： C07J41/00 , C07J1/00 , C07J21/00 , C07J71/00 , A61K31/565 , A61P5/36
摘要： The present invention relates to a method for the reliable and reproducible preparation of 4-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-llβ- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

8. 发明申请

WO2007098382A3 17-PHOSPHOROUS STEROID DERIVATIVES USEFUL AS PROGESTERONE RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2007098382A3
公开(公告)日：2007-08-30
申请号：PCT/US2007/062274
申请日：2007-02-16
申请人： JANSSEN PHARMACEUTICA N.V. , JIANG, Weiqin , SUI, Zhihua
发明人： JIANG, Weiqin , SUI, Zhihua
IPC分类号： C07J51/00 , A61K31/56 , A61P5/36 , A61P5/46
摘要： The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.

9. 发明申请

WO2007039544A1 NOVEL C18 MODIFIED RETROSTEROIDS AS PROGESTERONE RECEPTOR MODULATOR COMPOUNDS 审中-公开
标题翻译：新型C18改性复方作为孕激素受体调节剂化合物
公开(公告)号：WO2007039544A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066842
申请日：2006-09-28
申请人： SOLVAY PHARMACEUTICALS GMBH , MESSINGER, Josef , THOLE, Heinrich-Hubert , HUSEN, Bettina , BOECKER, Christiane , HINAJE, Maria , BUCHHOLZ, Monika , MARK, Christoph , KLINGER-DABRAL, Vibhuti
发明人： MESSINGER, Josef , THOLE, Heinrich-Hubert , HUSEN, Bettina , BOECKER, Christiane , HINAJE, Maria , BUCHHOLZ, Monika , MARK, Christoph , KLINGER-DABRAL, Vibhuti
IPC分类号： C07J15/00 , A61K31/57 , A61P5/34 , A61P5/36
CPC分类号： C07J15/005
摘要： Described herein are new retrosteroidal compounds of general formula (I), representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. Said compounds are preferably used for the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for HRT.
摘要翻译：本文描述了通式（I）的新型逆甾酮化合物，其代表孕酮受体调节剂及其制备，以及含有这些化合物的药物制剂。所述化合物优选用于治疗良性妇科疾病，例如子宫内膜异位症和子宫肌瘤，以及女性避孕和HRT。

10. 发明申请

WO0116108A3 BICYCLIC ANDROGEN AND PROGESTERONE RECEPTOR MODULATOR COMPOUNDS AND METHODS 审中-公开
标题翻译：双环雄性和孕酮受体调节剂化合物及方法
公开(公告)号：WO0116108A3
公开(公告)日：2001-12-20
申请号：PCT/US0023585
申请日：2000-08-25
申请人： LIGAND PHARM INC , ZHI LIN , TEGLEY CHRISTOPHER , PIO BARBARA , ARJAN VAN OEVEREN CORNELIS , MOTAMEDI MEHRNOUCH , MARTINBOROUGH ESTHER , WEST SARAH , HIGUCHI ROBERT , HAMANN LAWRENCE , FARMER LUC
发明人： ZHI LIN , TEGLEY CHRISTOPHER , PIO BARBARA , ARJAN VAN OEVEREN CORNELIS , MOTAMEDI MEHRNOUCH , MARTINBOROUGH ESTHER , WEST SARAH , HIGUCHI ROBERT , HAMANN LAWRENCE , FARMER LUC
IPC分类号： A61K31/37 , A61K31/4025 , A61K31/404 , A61K31/407 , A61K31/416 , A61K31/4178 , A61K31/428 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K31/536 , A61K31/5377 , A61K31/538 , A61K31/55 , A61P5/26 , A61P5/28 , A61P5/34 , A61P5/36 , A61P7/04 , A61P7/06 , A61P13/08 , A61P15/00 , A61P15/04 , A61P15/08 , A61P15/10 , A61P15/16 , A61P15/18 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07D209/34 , C07D209/96 , C07D215/22 , C07D215/227 , C07D215/36 , C07D215/38 , C07D215/48 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , A61K31/352 , A61K31/353 , A61K31/4706 , A61P5/24 , C07D311/08
CPC分类号： C07D215/227 , C07D209/34 , C07D209/96 , C07D215/36 , C07D215/38 , C07D239/80 , C07D265/18 , C07D265/36 , C07D277/68 , C07D311/14 , C07D311/20 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04
摘要： The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要翻译：本发明涉及用于调节由AR和PR介导的过程的化合物，药物组合物和方法。更具体地说，本发明涉及非甾体化合物和组合物，其是AR和PR的高亲和力，高特异性激动剂，部分激动剂（即部分激活剂和/或组织特异性激活剂）和拮抗剂。还提供了制备这些化合物和药物组合物的方法以及它们合成中使用的关键中间体。

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