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    • 2. 发明申请
    • 2-METHYLENE-20(21)-DEHYDRO-19-NOR-VITAMIN D ANALOGS
    • 2-亚甲基-20(21) - 脱氢-19-维生素D类似物
    • WO2010006172A2
    • 2010-01-14
    • PCT/US2009050110
    • 2009-07-09
    • WISCONSIN ALUMNI RES FOUNDDELUCA HECTOR FTADI BULLI PADMAJAPLUM LORI ACLAGETT-DAME MARGARET
    • DELUCA HECTOR FTADI BULLI PADMAJAPLUM LORI ACLAGETT-DAME MARGARET
    • C07C401/00A61K31/593A61P3/04A61P17/00A61P17/06A61P29/00A61P35/00A61P37/02
    • C07C401/00
    • This invention discloses 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs, and specifically 2-methylene-20(21)-dehydro-19-nor-1a,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows lower activity in vivo on bone calcium mobilization and similar in vivo intestinal calcium transport activity compared to the native hormone 1a,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基-20(21) - 脱氢-19-去甲 - 维生素D类似物,特别是2-亚甲基-20(21) - 脱氢-19-去甲-1a,25-二羟基维生素D3及其药物用途 。 该化合物表现出相对高的转录活性以及明显的抑制未分化细胞增殖和诱导其向单核细胞分化的活性,因此证明其用作抗癌剂并用于治疗皮肤疾病例如牛皮癣以及皮肤病 如皱纹,皮肤松弛,皮肤干燥和皮脂分泌不足。 与天然激素1a,25-二羟基维生素D 3相比,该化合物在体内对骨钙动员和体内肠钙转运活性也表现出较低的活性,因此可用于治疗人类以及肾中的自身免疫病症或炎性疾病 性骨病。 该化合物也可用于治疗或预防肥胖症。
    • 3. 发明申请
    • 2-METHYLENE-(17Z)-17(20)-DEHYDRO-19,21-DINOR-VITAMIN D ANALOGS
    • 2-甲基 - (17Z)-17(20)-DEHYDRO-19,21-维生素D类似物
    • WO2010006135A3
    • 2010-04-15
    • PCT/US2009050060
    • 2009-07-09
    • WISCONSIN ALUMNI RES FOUNDDELUCA HECTOR FTADI BULLI PADMAJAPLUM LORI ACLAGETT-DAME MARGARET
    • DELUCA HECTOR FTADI BULLI PADMAJAPLUM LORI ACLAGETT-DAME MARGARET
    • C07C401/00A61K31/593A61P3/04A61P17/00A61P17/06A61P29/00A61P35/00A61P37/02
    • C07C401/00C07C2601/14C07C2602/24
    • This invention discloses 2-methylene-(17Z)-17(20)-dehydro-19,21 -dinor-vitamin D analogs, and specifically 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-1a,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits relatively high transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has significant calcemic activity in vivo having about the same bone calcium mobilization activity and intestinal calcium transport activity as the native hormone 1a,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
    • 本发明公开了2-亚甲基 - (17Z)-17(20) - 脱氢-19,21-维生素D类似物,特别是2-亚甲基 - (17Z)-17(20) - 脱氢-19,21-二 -1a,25-二羟基维生素D 3及其药物用途。 该化合物显示相对较高的转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的明显活性,从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症 如皱纹,皮肤松弛,皮肤干燥和皮脂分泌不足。 该化合物在体内也具有显着的钙活性,其具有与天然激素1a,25-二羟基维生素D 3大致相同的骨钙动员活性和肠钙转运活性,因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及 肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。