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1. 发明申请

US20110178053A1 AZACARBOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC USE OF SAME 审中-公开
标题翻译：氨基胆碱衍生物，其制备方法及其治疗方法
公开(公告)号：US20110178053A1
公开(公告)日：2011-07-21
申请号：US12997326
申请日：2009-06-11
申请人： Christopher Arendt , Didier Babin , Olivier Bedel , Thierry Gouyon , Mikhail Levit , Ronghua Li , Serge Mignani , Neil Moorcroft , David Papin
发明人： Christopher Arendt , Didier Babin , Olivier Bedel , Thierry Gouyon , Mikhail Levit , Ronghua Li , Serge Mignani , Neil Moorcroft , David Papin
IPC分类号： A61K31/555 , C07D403/14 , A61K31/496 , C07D471/14 , A61K31/4375 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/551 , A61K31/506 , C07F9/92 , A61P35/00
CPC分类号： C07D471/14 , C07D213/73
摘要： The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF3; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C2-C7 alkenyl; optionally substituted linear or branched C2-C6 alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.
摘要翻译：本发明涉及具有式（I）的新型azacarbonline，其中：R 3，R 4独立地表示H; hal CF3; 取代的氧，任选取代的烷氧基; 任选取代的氨基; 取代的羰基; 任选取代的羧基; 任选取代的酰胺; 硫，如任选取代的砜，亚砜或硫化物; 任选地包含任选取代的杂原子的直链，支链或环状C 1 -C 10烷基; 任选取代的直链，支链或环状C 2 -C 7烯基; 任选取代的直链或支链C 2 -C 6炔基; 任选取代的芳基或杂芳基; 可以任选地被取代; 以碱或酸加成盐的形式存在。本发明还涉及其在治疗中用于治疗癌症和合成方法的用途。

2. 发明申请

US20120208809A1 9H-PYRROLO[2,3-B: 5,4-C'] DIPYRIDINE AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译： 9H-吡咯并[2,3-B：5,4-C']二吡啶基咪唑啉衍生物，其制备方法及其治疗用途
公开(公告)号：US20120208809A1
公开(公告)日：2012-08-16
申请号：US13258924
申请日：2009-11-30
申请人： Didier Babin , Olivier Bedel , Thierry Gouyon , Serge Mignani , David Papin
发明人： Didier Babin , Olivier Bedel , Thierry Gouyon , Serge Mignani , David Papin
IPC分类号： A61K31/444 , A61K31/496 , A61K31/5377 , C07D519/00 , A61K31/55 , C07F5/02 , C07D401/04 , C07D213/64 , C07D213/61 , A61P35/00 , A61K31/4545 , A61K31/4375 , C07F5/04 , C07F7/22 , C07D471/14
CPC分类号： C07D471/14 , C07D207/34 , C07D213/24
摘要： The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c′]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers and salts of said substances of formula (I) and to the therapeutic use thereof for treating cancer.
摘要翻译：本发明涉及式（I）的新型9H-吡咯并[2,3-b：5,4-c']二吡啶并吡唑啉，其中：Z2，Z3和Z4为CH，CRa，CRs或N; R3为H，Hal; CF 3，CHF 2; OH，烷氧基; NH 2，NH（烷基），N（烷基）2; C（O）O烷基; CONH（烷基），CON（烷基）2; C1-C10烷基; 芳基; 杂芳基; R6是杂芳基; R a是CONH 2，CONH烷基，CONH环烷基; CONH杂环烷基; CON（烷基）2; CON（烷基）（杂环烷基）; CONHN（烷基）2; C（O）杂环烷基; Rs是H; Hal，OH; O-烷基（C1-C10）; NH2; N（烷基（C1-C10）或环烷基（C3-C7））2; NHC（O）R 3a; N（烷基（C1-C10）C（O）R3a; NHS（O2）R3a; N（烷基）（C1-C10）S（O2）R3a; CO2R3a; SR3a; S（O）R3a; S（O2） ; R a和R 5任选地形成一个周期; R 3a选自Hal，CF 3，C 1 -C 10烷基; C 3 -C 7环烷基; C 2 -C 6烯基; C 2 -C 6炔基; OH; O-烷基（C 1 -C 10） C 3 -C 7烷基（C 3 -C 7）; NH 2; NH-（烷基（C 1 -C 10）或环烷基（C 3 -C 7））; N（烷基（C 1 -C 10） NH-（烷基（C1-C10）或杂环烷基（C3-C7））; N（烷基（C1-C10）或杂环烷基（C3-C7））2，以及所述式 I）及其用于治疗癌症的治疗用途。

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