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Pharmacodynamic binding includes antagonism to progesterone receptor and antiestrogen

机译:药效学结合包括对孕激素受体和抗雌激素的拮抗作用

摘要

IT REFERS TO PHARMACEUTICAL COMPOSITIONS THAT INCLUDE: a) 11B- (4-ACETILFENIL) -17B-HIDROXI-17A- (1,1,2,2,2-PENTAFLUOROETIL) -ESTRA-4,9-DIEN-3-ONA, OR AN ANALOG; b) A PURE ANTIESTROGEN, SUCH AS I, WHERE Hal IS F O Cl, AND WHICH IS ATTACHED TO THE STRATRENE SKELETON IN POSITION 11B; R3 IS H, (C1-C4) ALKYL, (C1-C4) ALCANYL OR A (C3-C7) CYCLE ETHER WITH AN ATOM OF O; R17 'IS H, (C1-C4) ALKYL OR (C1-C4) ALKYLNYL; R17 '' IS (C1-C4) ALKYL, (C1-C4) ALKYNYL; SK IS THE GROUP U-V-W-X-Y-Z-E THAT IS ATTACHED TO THE STRATRIENE SKELETON THROUGH U IN POSITION 7A; U IS (C1-C13) ALKYLENE OR -ALKENYLENE; V IS CH2-O C (O);W is n (R6),N + (o -) (R6) group,AN AZOLIDINYLENE N-OXIDE RING, AMONG OTHERS; R6 IS H, CH2-R7 O C (O) -R7; R7 IS H, (C1-C14) ALKYL, (C3-C10) CYCLLOALKYL, AMONG OTHERS; X IS (C1-C12) ALKYLENE, ALKYLENE OR ALKYLENE; AND IT IS A DIRECT LINK, (C3-C10) CICLOALQUILO, (C7-C20) ARALQUILO, AMONG OTHERS; Z IS A DIRECT LINK, (C1-C9) ALKYLENE, ALKYLENE OR ALKYLENE; E IS A GROUP CF3 OR A GROUP ARILO PARTIALLY FLOWERED; 11B-FLUORO-17A-METHYL-7A- {5- [METHYL- (8,8,9,9,9-PENTAFLUORONONYL) AMINO] PENTIL} -ESTRA-1,3,5 (10) -TRIEN-3 ARE SELECTED , 17B-DIOL, 7A- [9- (4,4,5,5,5-PENTAFLUOROPENTIL-SULFINIL) -NONIL] -ESTRA-1,3,5 (10) -TRIEN-3,17 BETA-DIOL,There are others He also mentioned a preparatory process These compounds contribute to the treatment and / or prevention of gastric cancer, breast cancer, sclerosis, polio, etc.
机译:它是指包含以下成分的药物成分:a)11B-(4-乙炔苯)-17B-HIDROXI-17A-(1,1,2,2,2-五氟甲酚)-ESTRA-4,9-DIEN-3-ONA,或模拟; b)纯抗雌激素,例如I,Hal是F O Cl,并且连接在位置11B的STRATRENE骨架上; R 3为H,(C 1 -C 4)烷基,(C 1 -C 4)烷酰基或具有O原子的(C 3 -C 7)环醚; R17'IS H,(C1-C4)烷基或(C1-C4)烷基; R17'是(C1-C4)烷基,(C1-C4)炔基; SK是U-V-W-X-Y-Z-E组,它通过位置7A上的U连接到STRATRIENE骨架上; U为(C1-C13)亚烷基或-亚烯基; V是CH 2 -O C(O); W是n(R6),N +(o-)(R6)基,氮杂亚烷基N-氧化物环,以及其他。 R6是H,CH2-R7OC(O)-R7; R7是H,(C1-C14)烷基,(C3-C10)环烷基,以及其他; X为(C1-C12)亚烷基,亚烷基或亚烷基;并且它是(C3-C10)CICLOALQUILO,(C7-C20)ARALQUILO等的直接链接; Z是直接链,(C1-C9)亚烷基,亚烷基或亚烷基; E是CF3组或部分流过的ARILO组;选择11B-FLUORO-17A-甲基-7A- {5- [甲基-(8,8,9,9,9-五氟膦酰基)氨基]戊}}-ESTRA-1,3,5(10)-TRIEN-3 ,17B-DIOL,7A- [9-(4,4,5,5,5-五氟opentil-sulfinil)-nonil] -ESTRA-1,3,5(10)-TRIEN-3,17 BETA-DIOL,There他还提到了制备过程。这些化合物有助于治疗和/或预防胃癌,乳腺癌,硬化症,小儿麻痹症等。

著录项

  • 公开/公告号PE20090152A1

    专利类型

  • 公开/公告日2009-04-30

    原文格式PDF

  • 申请/专利权人 BAYER SCHERING PHARMA AKTIENGESELLSCHAFT;

    申请/专利号PE19870200800

  • 发明设计人 HOFFMANN JENS;KORR DANIEL;

    申请日2008-04-22

  • 分类号A61K31/567;A61K31/57;A61P5/32;A61P5/36;A61P35;

  • 国家 PE

  • 入库时间 2022-08-21 19:26:00

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