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1. 发明申请

US20080045561A1 Novel Bis-Azaindole Derivatives, Preparation And Pharmaceutical Use Thereof As Kinase Inhibitors 失效
标题翻译：新型双 - 阿魏那衍生物，其制备和药物用途作为激酶抑制剂
公开(公告)号：US20080045561A1
公开(公告)日：2008-02-21
申请号：US11692321
申请日：2007-03-28
申请人： Conception NEMECEK , William METZ , Sylvie WENTZLER , Dominique LESUISSE , Youssef EL-AHMAD
发明人： Conception NEMECEK , William METZ , Sylvie WENTZLER , Dominique LESUISSE , Youssef EL-AHMAD
IPC分类号： A61K31/5375 , A61K31/435 , A61P35/00 , C07D413/14 , C07D471/02
CPC分类号： C07D519/00
摘要： Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
摘要翻译：公开了式（I）化合物：其中R1，R2，R3，R4和R5具有说明书中给出的含义及其盐，包含所述化合物的药物组合物及其作为蛋白激酶抑制剂的用途。

2. 发明申请

US20100256141A1 NOVEL BIS-AZAINDOLE DERIVATIVES, PREPARATION AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS 审中-公开
标题翻译：新型双嘧啶衍生物，其作为激酶抑制剂的制备和药物使用
公开(公告)号：US20100256141A1
公开(公告)日：2010-10-07
申请号：US12821371
申请日：2010-06-23
申请人： Conception NEMECEK , William A. METZ , Sylvie WENTZLER , Dominique LESUISSE , Youssef EL-AHMAD
发明人： Conception NEMECEK , William A. METZ , Sylvie WENTZLER , Dominique LESUISSE , Youssef EL-AHMAD
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , C07D413/14 , C07D403/14 , A61K31/497 , A61P35/00 , A61P3/00 , A61P11/06 , A61P37/08 , A61P7/02 , A61P25/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P27/02 , C12N9/99
CPC分类号： C07D519/00
摘要： Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
摘要翻译：公开了式（I）化合物：其中R1，R2，R3，R4和R5具有说明书中给出的含义及其盐，包含所述化合物的药物组合物及其作为蛋白激酶抑制剂的用途。

3. 发明申请

US20080108654A1 Cyclic Urea Compounds, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors 失效
标题翻译：循环脲类化合物，其制备方法及其药物用途作为激酶抑制剂
公开(公告)号：US20080108654A1
公开(公告)日：2008-05-08
申请号：US11972314
申请日：2008-01-10
申请人： Marcel PATEK , Anil NAIR , Augustin HITTINGER , Conception NEMECEK , Daniel BOND , Greg HARLOW , Herve BOUCHARD , Jacques MAUGER , Jean-Luc MALLERON , Mark PALERMO , Fahad AL-OBEIDI , Thomas FAITG , Hartmut STROBEL , Sven RUF , Kurt RITTER , Youssef EL-AHMAD , Dominique LESUISSE
发明人： Marcel PATEK , Anil NAIR , Augustin HITTINGER , Conception NEMECEK , Daniel BOND , Greg HARLOW , Herve BOUCHARD , Jacques MAUGER , Jean-Luc MALLERON , Mark PALERMO , Fahad AL-OBEIDI , Thomas FAITG , Hartmut STROBEL , Sven RUF , Kurt RITTER , Youssef EL-AHMAD , Dominique LESUISSE
IPC分类号： A61K31/47 , C07D401/02 , C07D401/14 , A61K31/444 , A61P11/06 , A61P25/00 , A61P35/00 , C12N9/99 , A61K31/4439
CPC分类号： C07D401/06 , C07D401/14
摘要： The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译：本公开涉及式I的环脲化合物：如本文所定义，其制备方法，包含其的药物组合物及其作为蛋白激酶上的抑制剂的药物用途。因此，式I化合物可用于预防或治疗能够通过抑制蛋白激酶如实体瘤的活性而被调节的生理障碍。

4. 发明申请

US20080261997A1 USE OF AMINOINDAZOLE DERIVATIVES FOR THE INHIBITION OF TAU PHOSPHORYLATION 失效
标题翻译：氨基吖啶衍生物用于抑制TAO磷酸化的用途
公开(公告)号：US20080261997A1
公开(公告)日：2008-10-23
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： A61K31/496 , A61K31/454 , A61K31/415 , A61P25/00
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。

5. 发明申请

US20070155735A1 NOVEL AMINOINDAZOLE DERIVATIVES AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM 失效
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：US20070155735A1
公开(公告)日：2007-07-05
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： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/427 , A61K31/422 , A61K31/416 , A61K31/4178
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。

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