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1. 发明申请

WO2008065100A1 SUBSTITUTED ESTRATRIEN DERIVATIVES AS 17BETA HSD INHIBITORS 审中-公开
标题翻译：取代的ESTRATRIEN衍生物作为17BETA HSD抑制剂
公开(公告)号：WO2008065100A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062856
申请日：2007-11-27
申请人： SOLVAY PHARMACEUTICALS GMBH , MESSINGER, Josef , HUSEN, Bettina , SCHOEN, Uwe , THOLE, Heinrich-Hubert , KOSKIMIES, Pasi , UNKILA, Mikko
发明人： MESSINGER, Josef , HUSEN, Bettina , SCHOEN, Uwe , THOLE, Heinrich-Hubert , KOSKIMIES, Pasi , UNKILA, Mikko
IPC分类号： C07J41/00 , C07J43/00 , C07J51/00 , A61K31/565 , A61K31/58 , A61K31/566 , A61P5/32
CPC分类号： C07J51/00 , C07J41/0005 , C07J41/0044 , C07J43/003
摘要： This invention relates to novel substituted estratrien derivatives of general formula (I) useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17- HSD) type 1, type 2 and/or type 3 enzyme, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds.
摘要翻译：本发明涉及可用于治疗的通式（I）的新型取代的雌三醇衍生物，特别是用于治疗和/或预防需要抑制17β-羟类固醇脱氢酶（17-HSD）1型的类固醇激素依赖性疾病，2型和/或3型酶及其盐，含有这些化合物的药物制剂和这些化合物的制备方法。

2. 发明申请

WO2008034796A2 THERAPEUTICALLY ACTIVE TRIAZOLES AND THEIR USE 审中-公开
标题翻译：治疗活性三唑及其使用
公开(公告)号：WO2008034796A2
公开(公告)日：2008-03-27
申请号：PCT/EP2007/059785
申请日：2007-09-17
申请人： SOLVAY PHARMACEUTICALS GMBH , MESSINGER, Josef , SCHOEN, Uwe , HUSEN, Bettina , THOLE, Heinrich-Hubert , KOSKIMIES, Pasi , KALLIO, Lila
发明人： MESSINGER, Josef , SCHOEN, Uwe , HUSEN, Bettina , THOLE, Heinrich-Hubert , KOSKIMIES, Pasi , KALLIO, Lila
IPC分类号： C07J43/00 , A61K31/58 , A61P35/00 , A61P13/00 , A61P5/32
CPC分类号： C07J43/003
摘要： This invention relates to novel estratrien-triazoles of general formula (I) useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) such as 17β-HSD type 1, type 2 or type 3 enzyme.
摘要翻译：本发明涉及可用于治疗，特别是用于治疗和/或预防类固醇激素依赖性病症，优选类固醇激素依赖性疾病或病症的通式（I）的新颖的雌三醇 - 三唑，其需要抑制17β- 羟基类固醇脱氢酶（17β-HSD），如17β-HSD 1型，2型或3型酶。

3. 发明申请

WO2008113851A2 NOVEL C11 MODIFIED RETROSTEROIDS AS PROGESTERONE RECEPTOR MODULATOR COMPOUNDS 审中-公开
标题翻译：新的C11修饰型RETROSTEROIDS作为孕酮受体调节剂化合物
公开(公告)号：WO2008113851A2
公开(公告)日：2008-09-25
申请号：PCT/EP2008/053365
申请日：2008-03-20
申请人： SOLVAY PHARMACEUTICALS 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
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：本文描述了新的通式（I）的反甾体化合物，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，如子宫内膜异位和子宫肌瘤，以及女性节育和HRT。

4. 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。

5. 发明申请

WO2007082891A1 PROCESS FOR THE PREPARATION OF 11BETA-HYDR0XY-9BETA, 10ALPHA -STEROIDS EMPLOYING AMYCOLATOPSIS MEDITERRANEI CELLS 审中-公开
标题翻译：制备11BETA-HYDROXY-9BETA的方法，使用AMYCOLATOPSIS MEDITERRANEI细胞的10ALPHA-酪蛋白
公开(公告)号：WO2007082891A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050412
申请日：2007-01-16
申请人： SOLVAY PHARMACEUTICALS GMBH , MESSINGER, Josef , THOLE, Heinrich-Hubert , RASCHE, Heinz-Helmer , SCHMIDT, Michael , HAKALA, Juha
发明人： MESSINGER, Josef , THOLE, Heinrich-Hubert , RASCHE, Heinz-Helmer , SCHMIDT, Michael , HAKALA, Juha
IPC分类号： C12P33/08 , C07J7/00
CPC分类号： C07J7/00 , C12P33/08
摘要： The invention relates to the use of bacterial strains of the species Amycolatopsis mediterranei for the microbial transformation of 9β,10α-steroids of general Formula (I) to their corresponding 11β-hydroxyl analogues, as well as to specific strains of that species. In addition, the present invention relates to the process of transforming 9β,10α-steroids to their corresponding 11β-hydroxyl derivatives using bacterials strains of the species Amycolatopsis mediterranei , and to the subsequent isolation of the 11β-hydroxyl derivatives from the bacterial culture medium. The resultant 11β-hydroxylated products are useful intermediates for the preparation of novel steroidal compounds with 9β,10α-confirmation carrying different kind of substituents in the 11β-position.
摘要翻译：本发明涉及物种Amycolatopsis地塞米松的细菌菌株用于将通式（I）的9β，10α-类固醇与其相应的11β-羟基类似物以及该物种的特定菌株的微生物转化。此外，本发明涉及使用中性粒细菌的细菌菌株将9β，10α类固醇转化为相应的11β-羟基衍生物的方法，随后从细菌培养基中分离出11β-羟基衍生物。所得的11β-羟基化产物是制备具有9β，10a-确认在11β位置携带不同种类的取代基的新型甾体化合物的有用中间体。

6. 发明申请

WO2008116920A2 17BETA-HYDROXYSTEROID-DEHYDROGENASE-TYP1-INHIBITOREN ZUR BEHANDLUNG HORMONABHÄNGIGER ERKRANKUNGEN 审中-公开
标题翻译： 17β-羟基类固醇脱氢酶1抑制剂用于治疗激素相关性疾病
公开(公告)号：WO2008116920A2
公开(公告)日：2008-10-02
申请号：PCT/EP2008/053672
申请日：2008-03-27
申请人： UNIVERSITÄT DES SAARLANDES , HARTMANN, Rolf , FROTSCHER, Martin , OBERWINKLER, Sandrine , ZIEGLER, Erika , MESSINGER, Josef , THOLE, Heinrich-Hubert
发明人： HARTMANN, Rolf , FROTSCHER, Martin , OBERWINKLER, Sandrine , ZIEGLER, Erika , MESSINGER, Josef , THOLE, Heinrich-Hubert
IPC分类号： A61K31/015 , A61K31/498 , A61P15/00
CPC分类号： A61K31/015 , A61K31/498
摘要： Die Erfindung betrifft die Verwendung von nicht-steroidalen 17Beta-Hydroxysteroid-Dehydrogenase Typ1 Inhibitoren zur Behandlung und Prophylaxe hormonabhängiger, insbesondere estrogenabhängiger Erkrankungen. Weiterhin werden geeignete Inhibitoren sowie ein Verfahren zu deren Herstellung zur Verfügung gestellt.
摘要翻译：本发明涉及使用非甾体类的17β-羟基类固醇脱氢酶类型1抑制剂用于治疗和激素依赖性的预防的，特别是雌激素依赖性疾病。提供了进一步的合适的抑制剂和它们的制备的方法。

7. 发明申请

WO2006125800A1 17β-HSD1 AND STS INHIBITORS 审中-公开
标题翻译： 17β-HSD1和STS抑制剂
公开(公告)号：WO2006125800A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062587
申请日：2006-05-24
申请人： SOLVAY PHARMACEUTICALS GMBH
发明人： MESSINGER, Josef , THOLE, Heinrich-Hubert , HUSEN, Bettina , KOSKIMIES, Pasi , PIRKKALA, Lila , WESKE, Michael
IPC分类号： C07J41/00 , C07J71/00 , C07J43/00 , A61K31/565 , A61K31/58 , A61P5/32
CPC分类号： C07J71/0052 , C07J41/0072 , C07J43/003 , C07J71/0068
摘要： The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.
摘要翻译：本发明涉及代表17β-羟类固醇脱氢酶I型（17β-HSD1）的选择性抑制剂的新型取代的类固醇衍生物，此外，其可以代表类固醇硫酸酯酶及其盐的药物制剂含有这些化合物和制备这些化合物的方法。此外，本发明涉及所述新型取代的类固醇衍生物的治疗用途，特别是其用于治疗或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制I型17β-羟类固醇脱氢酶的病症或 /或类固醇硫酸酶和/或需要降低内源性17β-雌二醇浓度。

8. 发明申请

WO2006063615A1 NOVEL SUBSTITUTED THIOPHENEPYRIMIDINONE DERIVATIVES AS INHIBITORS OF 17β-HYDROXYSTEROID DEHYDROGENASE 审中-公开
标题翻译：作为17β-羟基脱氢酶抑制剂的新型取代的噻吩并嘧啶酮衍生物
公开(公告)号：WO2006063615A1
公开(公告)日：2006-06-22
申请号：PCT/EP2004/053424
申请日：2004-12-13
申请人： SOLVAY PHARMACEUTICALS GMBH
发明人： HIRVELÄ, Leena , HUSEN, Bettina , KIVINIEMI, Johanna , KOSKIMIES, Pasi , LEHTOVUORI, Pekka , MESSINGER, Josef , PENTIKÄINEN, Olli Taneli , PIRKKALA, Lila , SAARENKETO, Pauli , THOLE, Heinrich-Hubert , UNKILA, Mikko , VAN STEEN, Bartholomeus Johannes
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： This invention relates to novel substituted thiophenepyrimidinone derivatives and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorder, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译：本发明涉及新的取代的噻吩并嘧啶酮衍生物及其在治疗中的用途，特别是用于治疗和/或预防类固醇激素依赖性疾病或病症，例如需要抑制17β-羟基类固醇脱氢酶的类固醇激素依赖性疾病或病症。

9. 发明申请

WO2005047303A2 NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 审中-公开
标题翻译：新型17β羟基类固醇脱氢酶I型抑制剂
公开(公告)号：WO2005047303A2
公开(公告)日：2005-05-26
申请号：PCT/EP2004/052925
申请日：2004-11-11
申请人： SOLVAY PHARMACEUTICALS GMBH
发明人： MESSINGER, Josef , THOLE, Heinrich-Hubert , HUSEN, Bettina , VAN STEEN, Bartholomeus Johannes , SCHNEIDER, Gyula , HULSHOF, Johannes Bernardus Everardus , KOSKIMIES, Pasi , JOHANSSON, Nina , ADAMSKI, Jerzy
IPC分类号： C07J1/00
CPC分类号： C07J1/0059 , C07J1/00
摘要： The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel 3, 15 substituted estrone derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration. In addition, the present invention relates to the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment and prevention of benign gynaecological disorders, in particular endometriosis.
摘要翻译：本发明涉及代表17β-羟基类固醇脱氢酶I型抑制化合物（17β-HSD1），其盐，包含这些化合物的药物制剂的新型3,15取代雌酮衍生物和制备这些化合物的方法。此外，本发明涉及所述新型3,15取代的雌酮衍生物的治疗用途，特别是它们用于治疗或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β- 和/或需要降低内源性17β-雌二醇浓度。另外，本发明涉及对于雌激素受体没有或仅具有纯拮抗结合亲和力的选择性17β-羟基类固醇脱氢酶1型抑制剂的普遍应用，用于治疗和预防良性妇科疾病，特别是子宫内膜异位。 / p>

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