公开(公告)号：EP1418921A1

公开(公告)日：2004-05-19

申请号：EP02762422.0

申请日：2002-08-01

申请人： Schering AG

发明人： SCHERLITZ-HOFMANN, Ina ,  HOFFMANN, Jens ,  HILLISCH, Alexander ,  UNGER, Eberhard ,  NEUMANN, Tobias ,  SCHWARZ, Sigfrid ,  PETERS, Olaf ,  MICHEL, Thomas

IPC分类号： A61K31/565 ,  C07J31/00 ,  A61P35/00

CPC分类号： A61K31/565 ,  C07J31/006

摘要： The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In said formula, R?1 and R2¿ independently of one another represent H, methyl, C¿1?-C4 acyl or benzyl, R?3¿ represents C¿1?-C4 alkyl, or a group of formula CnFmHo, where n = 1, 2, 3, 4, 5 or 6, m > 1 and m + o = 2n + 1, R?4 and R5¿ independently represent H, or together represent a methylene group or an additional bond, R6 represents H and R7 represents OH, OC¿1?-C4 alkyl, OC1-C11 acyl or OSO2NR?1R2¿, whereby in the B and C ring of the steroid skeleton the broken lines can additionally represent up to two double bonds. The inventive compounds are characterised by a 2-alkoxy substitution in conjunction with a 17-hydroxy substitution. They exhibit the specific activity of inhibiting tubulin polymerisation and can be used, for example, for treating prostatic carcinoma.

摘要翻译： 本发明涉及通式（I）的2-烷氧基雌激素氨基磺酸酯在制备用于治疗肿瘤疾病的药物中的用途，所述肿瘤疾病受抑制微管蛋白聚合的积极影响。 在所述式中，R 1和R 2彼此独立地表示H，甲基，C 1 -C 4酰基或苄基，R 3'表示C 1 -C 4烷基或式C n F m H o的基团，其中 n = 1,2,3,4,5或6，m> 1和m + o = 2n + 1，R 4和R 5独立地代表H，或一起代表亚甲基或另外的键，R 6代表H 并且R 7代表OH，OC 1 -C 4烷基，OC 1 -C 11酰基或OSO 2 NR 1 R 2，其中在类固醇骨架的B和C环中，虚线可另外代表至多两个双键。 本发明化合物的特征在于2-烷氧基取代与17-羟基取代一起。 它们表现出抑制微管蛋白聚合的特异性活性，并且可以用于例如治疗前列腺癌。

公开(公告)号：EP1294402A2

公开(公告)日：2003-03-26

申请号：EP01943329.1

申请日：2001-05-08

申请人： Schering AG

发明人： ELGER, Walter ,  HILLISCH, Alexander ,  HEDDEN, Annemarie ,  SCHWARZ, Sigfrid ,  SCHÖLLKOPF, Klaus

IPC分类号： A61K47/20 ,  A61K31/565 ,  A61K31/566 ,  A61K31/568 ,  A61K31/49 ,  A61K31/4045 ,  A61P43/00

CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula -SO2NR1R2, wherein R?1 and R2¿, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high 'first path' effect, to be administered orally effectively or significantly improve the oral activity thereof.

公开(公告)号：EP1294402B1

公开(公告)日：2006-01-11

申请号：EP01943329.1

申请日：2001-05-08

申请人： Schering AG

发明人： ELGER, Walter ,  HILLISCH, Alexander ,  HEDDEN, Annemarie ,  SCHWARZ, Sigfrid ,  SCHÖLLKOPF, Klaus

IPC分类号： A61K47/20 ,  A61K31/565 ,  A61K31/566 ,  A61K31/568 ,  A61K31/49 ,  A61K31/4045 ,  A61P43/00

CPC分类号： C07J41/0044 ,  C07J41/0038 ,  C07J41/005

摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula -SO2NR R , wherein R and R , independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high "first path" effect, to be administered orally effectively or significantly improve the oral activity thereof.

公开(公告)号：EP0775155B1

公开(公告)日：2004-05-06

申请号：EP95925679.3

申请日：1995-07-03

申请人： Schering AG

发明人： SIEMANN, Hans-Joachim ,  SCHWARZ, Sigfrid ,  ELGER, Walter ,  REDDERSEN, Gudrun ,  SCHNEIDER, Birgitt

IPC分类号： C07J41/00 ,  A61K31/56 ,  C07J53/00 ,  C07J43/00

CPC分类号： C07J43/003 ,  C07J41/0072 ,  C07J51/00 ,  C07J53/004

摘要： The invention concerns novel estra-1,3,5(10)-triene amidosulphamates with an R-SO2-O- group in the 3-position, R being an R1R2N- group in which R?1 and R2¿, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C-atoms or, together with the N-atom, a polymethyleneimino group with 4 to 6 C-atoms or a morpholino group. The compounds described are suitable for use in hormonal contraception and in climacteric hormone-replacement therapy (HRT), as well as in the treatment of gynaecological and andrological conditions. The compounds described thus only have a low hepatic oestrogenicity. Also described are methods of preparing the compounds described, plus the preparation of pharmaceutical compositions containing them.