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    • 5. 发明授权
    • Use of aminoindazole derivatives for the inhibition of tau phosphorylation
    • 氨基吲唑衍生物用于抑制tau磷酸化
    • US07629374B2
    • 2009-12-08
    • US12143070
    • 2008-06-20
    • Dominique LesuisseGilles Dutruc-RossetFranck HalleyDidier BabinThomas RooneyGilles Tiraboschi
    • Dominique LesuisseGilles Dutruc-RossetFranck HalleyDidier BabinThomas RooneyGilles Tiraboschi
    • A61K31/415
    • C07D231/56A61K31/416A61K31/4178A61K31/422A61K31/427A61K31/454A61K31/496A61K31/5377A61K31/541C07D403/12C07D405/12
    • The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.
    • 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或 与(1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1基团稠合的杂芳基) R 5,R 6和R 7彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,OR 8,COOH,C(O)OR 8,-OC(O)R 8,NR 8 R 9,NHC )R8,C(O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O)R8,SO2R8,NHSO2R8,SO2NR8R9,-O-SO2R8,-SO2-O-R8,三氟甲基,三氟甲氧基 ,(1-6C)烷基,(1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基,炔基,金刚烷基或多环烷基, 选自以下的疾病:神经变性疾病,中风,颅脑和脊髓创伤和周围神经病变,肥胖症,代谢疾病,II型糖尿病,原发性高血压,动脉粥样硬化性心血管疾病,多囊卵巢综合征,综合征X,免疫缺陷和癌症。
    • 6. 发明申请
    • USE OF AMINOINDAZOLE DERIVATIVES FOR THE INHIBITION OF TAU PHOSPHORYLATION
    • 氨基吖啶衍生物用于抑制TAO磷酸化的用途
    • US20080261997A1
    • 2008-10-23
    • US12143070
    • 2008-06-20
    • Dominique LESUISSEGilles DUTRUC-ROSSETFranck HALLEYDidier BABINThomas ROONEYGilles TIRABOSCHI
    • Dominique LESUISSEGilles DUTRUC-ROSSETFranck HALLEYDidier BABINThomas ROONEYGilles TIRABOSCHI
    • A61K31/496A61K31/454A61K31/415A61P25/00
    • C07D231/56A61K31/416A61K31/4178A61K31/422A61K31/427A61K31/454A61K31/496A61K31/5377A61K31/541C07D403/12C07D405/12
    • The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.
    • 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或 与(1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C( - NH)NR1基; R 5,R 6和R 7彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,OR 8,COOH,C( O)OR 8,-OC(O)R 8,NR 8 R 9,NHC(O)R 8,C(O)NR 8 R 9,NHC(S)R 8,C(S)NR 8 R 9,SR 8,S(O)R 8,SO 2 R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2, (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基 ,炔基,金刚烷基或多环烷基,以治疗选自以下的疾病:神经变性疾病,中风,颅脑和脊髓创伤和周围神经病变,肥胖症,代谢疾病,II型糖尿病,原发性高血压,动脉粥样硬化心血管疾病,多囊卵巢综合征 ,综合征X,免疫缺陷和癌症。
    • 7. 发明授权
    • Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    • 氨基吲唑衍生物作为药物和药物组合物,包括它们
    • US07407981B2
    • 2008-08-05
    • US11683452
    • 2007-03-08
    • Dominique LesuisseGilles Dutruc-RossetFranck HalleyDidier BabinThomas RooneyGilles Tiraboschi
    • Dominique LesuisseGilles Dutruc-RossetFranck HalleyDidier BabinThomas RooneyGilles Tiraboschi
    • A61K31/415C07D231/00
    • C07D231/56A61K31/416A61K31/4178A61K31/422A61K31/427A61K31/454A61K31/496A61K31/5377A61K31/541C07D403/12C07D405/12
    • The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.
    • 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或 与(1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C( - NH)NR1基; R 5,R 6和R 7彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,OR 8,COOH,C( O)OR 8,-OC(O)R 8,NR 8 R 9,NHC(O)R 8,C(O)NR 8 R 9,NHC(S)R 8,C(S)NR 8 R 9,SR 8,S(O)R 8,SO 2 R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2, (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基 ,炔基,金刚烷基或多环烷基,以治疗选自以下的疾病:神经变性疾病,中风,颅脑和脊髓创伤和周围神经病变,肥胖症,代谢疾病,II型糖尿病,原发性高血压,动脉粥样硬化心血管疾病,多囊卵巢综合征 ,综合征X,免疫缺陷和癌症。