专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07407981B2 Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 失效
标题翻译：氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US07407981B2
公开(公告)日：2008-08-05
申请号：US11683452
申请日：2007-03-08
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
IPC分类号： A61K31/415 , C07D231/00
CPC分类号： C07D231/56 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D405/12
摘要： 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.
摘要翻译：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。

2. 发明授权

US07166629B2 Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
标题翻译：氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US07166629B2
公开(公告)日：2007-01-23
申请号：US10654703
申请日：2003-09-04
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to 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 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, 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.
摘要翻译：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，芳基或杂芳基（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 激进; R 5和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8， -OC（O）R8，NR8R9，NHC（O）R8，C（O）NR8R9，NHC（S）R8，C（S）NR8R9，SR8，S（O） R 8，NHSO 2 R 8，SO 2 NR 8 R 9，-O-SO 2 R 8，-SO 2 -O （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，链烯基，炔基，金刚烷基或多环烷基。

3. 发明授权

US07582669B2 Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
标题翻译：氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US07582669B2
公开(公告)日：2009-09-01
申请号：US11567442
申请日：2006-12-06
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to 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 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, 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.
摘要翻译：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，芳基或杂芳基（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和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8，-OC（O）R 8，NR 8 R 9，NHC（O）（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。

4. 发明申请

US20070093479A1 NOVEL AMINOINDAZOLE DERIVATIVES AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM 有权
标题翻译：作为药物和药物组合物的新型氨基咔唑衍生物包括它们
公开(公告)号：US20070093479A1
公开(公告)日：2007-04-26
申请号：US11567442
申请日：2006-12-06
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/427 , A61K31/416
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to 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 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, 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.
摘要翻译：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，芳基或杂芳基（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 激进; R 5和R 6彼此独立地选自以下基团：卤素，CN，NO 2，NH 2，OH，COOH，C（O）OR 8， -OC（O）R8，NR8R9，NHC（O）R8，C（O）NR8R9，NHC（S）R8，C（S）NR8R9，SR8，S（O） R 8，NHSO 2 R 8，SO 2 NR 8 R 9，-O-SO 2 R 8，-SO 2 -O （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，链烯基，炔基，金刚烷基或多环烷基。

5. 发明授权

US07629374B2 Use of aminoindazole derivatives for the inhibition of tau phosphorylation 失效
标题翻译：氨基吲唑衍生物用于抑制tau磷酸化
公开(公告)号：US07629374B2
公开(公告)日：2009-12-08
申请号：US12143070
申请日：2008-06-20
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
IPC分类号： A61K31/415
CPC分类号： C07D231/56 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D405/12
摘要： 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.
摘要翻译：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. 发明授权

US07196109B2 Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 失效
标题翻译：氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US07196109B2
公开(公告)日：2007-03-27
申请号：US11285874
申请日：2005-11-23
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
IPC分类号： A61K31/415 , C07D403/00 , C07D417/00 , C07D413/00 , C07D211/32
CPC分类号： C07D231/56 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D405/12
摘要： 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.
摘要翻译：本发明涉及通式（I）的新型衍生物，

7. 发明申请

US20060074122A1 Novel aminoindazole derivatives as medicaments and pharmaceutical compositions including them 失效
标题翻译：新型氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US20060074122A1
公开(公告)日：2006-04-06
申请号：US11285874
申请日：2005-11-23
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
IPC分类号： A61K31/4162
CPC分类号： C07D231/56 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D405/12
摘要： 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.
摘要翻译：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。

8. 发明授权

US07019011B2 Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 失效
标题翻译：氨基吲唑衍生物作为药物和药物组合物，包括它们
公开(公告)号：US07019011B2
公开(公告)日：2006-03-28
申请号：US10654698
申请日：2003-09-04
申请人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
发明人： Dominique Lesuisse , Gilles Dutruc-Rosset , Franck Halley , Didier Babin , Thomas Rooney , Gilles Tiraboschi
IPC分类号： C07D231/56 , C07D241/10 , A61K31/416
CPC分类号： C07D231/56 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D403/12 , C07D405/12
摘要： The present invention relates to 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.
摘要翻译：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，芳基或杂芳基（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 激进; 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。

9. 发明申请

US20080125418A1 Benzimidazole derivatives and their use as kdr kinase protein inhibitors 审中-公开
标题翻译：苯并咪唑衍生物及其作为kdr激酶蛋白抑制剂的用途
公开(公告)号：US20080125418A1
公开(公告)日：2008-05-29
申请号：US11943008
申请日：2007-11-20
申请人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
发明人： Didier Babin , Alain Le Brun , Laurence Gauzy-Lazo , Herve Bouchard
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4196 , A61K31/4184 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04 , C07D491/04
摘要： The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitotic agents.
摘要翻译：本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物，和一个或多个。抗有丝分裂剂。

10. 发明授权

US06897208B2 Benzimidazoles 有权
标题翻译：苯并咪唑
公开(公告)号：US06897208B2
公开(公告)日：2005-05-24
申请号：US10279834
申请日：2002-10-24
申请人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
发明人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D521/00 , A61K31/33 , A61K31/415 , C07D231/00 , C07D235/00 , C07D487/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式