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    • 1. 发明申请
    • COMPOUNDS HAVING PROGESTOGENIC ACTIVITY AND THEIR USE
    • 具有致孕活性的化合物及其用途
    • WO2006107273A8
    • 2006-12-28
    • PCT/SG2005000116
    • 2005-04-06
    • UNIV SINGAPOREYONG EU LEONGLIM LIS SA ELISSASHEN PINGGONG YINHAN
    • YONG EU LEONGLIM LIS SA ELISSASHEN PINGGONG YINHAN
    • A61K31/343A61K31/381A61K31/407A61K36/00A61P5/30C07D487/02C07D491/02C07D493/22C07D495/02C07D497/02C07D498/02C07D513/02
    • A61K36/236A61K31/343A61K31/381A61K31/407C07D493/04C07D493/10
    • The invention relates to compounds having progestogenic activity and to their use. The invention discloses a compound having the general formula (I) wherein Y, Y', X and X' are independently selected from the group consisting of O, S and N; R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C4-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from the group consisting of hydrogen, optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C 1-6 thioalkyl, optionally substituted C 5-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; ---- indicates an optional double bond.
    • 本发明涉及具有孕激素活性的化合物及其用途。 本发明公开了具有通式(I)的化合物,其中Y,Y',X和X'独立地选自O,S和N; R 1选自任选取代的C 1-8烷基,任选取代的C 2-6烯基,任选取代的C 1-6烷基, 炔基,任选取代的C 1-6烷氧基,任选取代的C 1-6硫代烷基,任选取代的C 4-10芳基,任选取代的C 6-12芳基, 烷基芳基,任选取代的C 1-6烷基氨基,任选取代的C 1-6烷基羰基,任选取代的C 1-6烷基磺酰氨基, 任选取代的(C 1 -C 6)烷基亚磺酰基,任选取代的C 1-6烷基羰基氨基,任选取代的杂(C 5 -C 5) 芳基,羟基,卤素,氰基,硝基,氨基,甲酰基和巯基; R SUB 3,SUB 3,SUB 4,SUB 5,SUB 6,SUB和 R 7独立地选自氢,任选取代的C 1-8烷基,任选取代的C 2-6烯基,任选取代的 取代的C 2-6炔基,任选取代的C 1-6烷氧基,任选取代的C 1-6硫代烷基,任选取代的C≡C1-6烷基, 5-10芳基,任选取代的C 6-11烷基芳基,任选取代的C 1-6烷基氨基,任选取代的C 1-6烷基, 任选取代的C 1-6烷基磺酰氨基,任选取代的(C 1 -C 6)烷基亚磺酰基,任选取代的C 1 -C 4烷基磺酰基, 任选取代的杂芳基,羟基,卤素,氰基,硝基,氨基,甲酰基和巯基; ----表示可选的双键。
    • 2. 发明申请
    • COMPOUNDS HAVING PROGESTOGENIC ACTIVITY AND THEIR USE
    • 具有原发性活性的化合物及其使用
    • WO2006107273A1
    • 2006-10-12
    • PCT/SG2005/000116
    • 2005-04-06
    • NATIONAL UNIVERSITY OF SINGAPOREYONG, Eu LeongLIM, Lis Sa ElissaSHEN, PingGONG, YinHan
    • YONG, Eu LeongLIM, Lis Sa ElissaSHEN, PingGONG, YinHan
    • A61K31/343A61P5/30A61K31/381A61K31/407A61K36/00C07D495/02C07D487/02C07D491/02C07D493/22C07D497/02C07D498/02C07D513/02
    • A61K36/236A61K31/343A61K31/381A61K31/407C07D493/04C07D493/10
    • The invention relates to compounds having progestogenic activity and to their use. The invention discloses a compound having the general formula (I) wherein Y, Y', X and X' are independently selected from the group consisting of O, S and N; R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C1-6 thioalkyl, optionally substituted C4-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are independently selected from the group consisting of hydrogen, optionally substituted C 1-8 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, optionally substituted C 1-6 alkoxy, optionally substituted C 1-6 thioalkyl, optionally substituted C 5-10 aryl, optionally substituted C 6-11 alkylaryl, optionally substituted C 1-6 alkylamino, optionally substituted C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkylsulfonamino, optionally substituted (C 1 -C 6 )alkylsulfinyl, optionally substituted C 1-6 alkylcarbonylamino, optionally substituted hetero(C 5 -C 10 )aryl, hydroxyl, halogen, cyano, nitro, amino, formyl, and thiol; ---- indicates an optional double bond.
    • 本发明涉及具有孕激素活性及其应用的化合物。 本发明公开了具有通式(I)的化合物,其中Y,Y',X和X'独立地选自O,S和N; R 1选自任选取代的C 1-8 - 烷基,任选取代的C 2-6 - 烯基,任选取代的C 1 -C 6 - 任选取代的C 1-6烷氧基,任选取代的C 1-6硫烷基,任选取代的C 4-10芳基,任选取代的C 6-11 - 烷基芳基,任选取代的C 1-6烷基氨基,任选取代的C 1-6烷基羰基,任选取代的C 1-6烷基亚磺酰氨基, 任选取代的(C 1 -C 6 -C 6)烷基亚磺酰基,任选取代的C 1-6烷基羰基氨基,任选取代的杂(C 5 -C 6 - 芳基,羟基,卤素,氰基,硝基,氨基,甲酰基和硫醇; R 2,R 3,R 4,R 5,R 6和R 5, R 7独立地选自氢,任选取代的C 1-8 - 烷基,任选取代的C 2-6 - 烯基,任选地 取代的C 2-6 - 炔基,任选取代的C 1-6烷氧基,任选取代的C 1-6烷硫基,任选取代的C 1 -C 6 - 任选取代的C 6-11烷基芳基,任选取代的C 1-6烷基氨基,任选取代的C 1-6 - 任选取代的C 1 -C 6烷基亚磺酰基,任选取代的C 1 -C 6烷基亚磺酰基,任选取代的C 1 -C 6烷基亚磺酰基, 1-6烷基羰基氨基,任选取代的杂原子(C 5 -C 10)芳基,羟基,卤素,氰基,硝基,氨基,甲酰基和硫醇; ----表示可选双键。