公开(公告)号：US20090275590A1

公开(公告)日：2009-11-05

申请号：US12351561

申请日：2009-01-09

申请人： Peter Robert GUZZO ,  Matthew David SURMAN ,  Alan John HENDERSON ,  May Xiaowu JIANG ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

发明人： Peter Robert GUZZO ,  Matthew David SURMAN ,  Alan John HENDERSON ,  May Xiaowu JIANG ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D401/10 ,  A61K31/501 ,  A61P3/04

CPC分类号： C07D471/04 ,  C07D519/00 ,  C07D521/00

摘要： Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R6, —C(═O)—O—R7, or —C(═O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH═CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

摘要翻译： 用于并入用于治疗各种疾病的药物组合物中的取代的吡啶并吲哚对应于其中R 1为H或任选取代的烷基的式（I） R 2，R 3，R 4各自独立地选自H，-O-烷基，-S-烷基，烷基，卤素，-CF 3和-CN; G是-CR 12 R 13 -NR 5 - 或-NR 5 -CR 12 R 13; R5; （O）-R 6，-C（ - O）-O-R 7或-C（ - ） - NR 19 R 20;任选取代的杂环， R6和R7各自为任选取代的烷基或任选取代的杂环; R 8，R 9，R 10，R 11，R 12，R 13，R 19和R 20各自独立地选自H或任选取代的烷基; R 14和R 15各自独立地为H或卤素; L是-CH 2 -O-，-CH 2 CH 2 - ， - CH-CH-或键; 和B是芳基或杂芳基或环烷基; 条件是当L是直接键时，B不能是被氟单取代的未取代的杂芳基或杂芳基。

公开(公告)号：US08716308B2

公开(公告)日：2014-05-06

申请号：US12351561

申请日：2009-01-09

申请人： Peter Guzzo ,  Matthew David Surman ,  Alan John Henderson ,  May Xiaowu Jiang ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

发明人： Peter Guzzo ,  Matthew David Surman ,  Alan John Henderson ,  May Xiaowu Jiang ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/00

CPC分类号： C07D471/04 ,  C07D519/00 ,  C07D521/00

摘要： Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R6, —C(═O)—O—R7, or —C(═O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH═CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

摘要翻译： 用于并入用于治疗各种疾病的药物组合物中的取代的吡啶并吲哚对应于其中R 1为H或任选取代的烷基的式（I） R 2，R 3，R 4各自独立地选自H，-O-烷基，-S-烷基，烷基，卤素，-CF 3和-CN; G为-CR12R13-NR5-或-NR5-CR12R13; R5; 是任选取代的烷基，任选取代的杂环，-C（= O）-R 6，-C（= O）-O-R7或-C（= O）-NR 19 R 20; R6和R7各自为任选取代的烷基或任选取代的杂环; R 8，R 9，R 10，R 11，R 12，R 13，R 19和R 20各自独立地选自H或任选取代的烷基; R 14和R 15各自独立地为H或卤素; L是-CH 2 -O-，-CH 2 CH 2 - ， - CH = CH-或键; 和B是芳基或杂芳基或环烷基; 条件是当L是直接键时，B不能是被氟单取代的未取代的杂芳基或杂芳基。

公开(公告)号：US20100331339A9

公开(公告)日：2010-12-30

申请号：US12351561

申请日：2009-01-09

申请人： Peter Robert GUZZO ,  Matthew David SURMAN ,  Alan John HENDERSON ,  May Xiaowu JIANG ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

发明人： Peter Robert GUZZO ,  Matthew David SURMAN ,  Alan John HENDERSON ,  May Xiaowu JIANG ,  Mark Hadden ,  James Grabowski ,  Alexander Usyatinsky

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D401/10 ,  A61K31/501 ,  A61P3/04

CPC分类号： C07D471/04 ,  C07D519/00 ,  C07D521/00

摘要： Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(═O)—R6, —C(═O)—O—R7, or —C(═O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH═CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

摘要翻译： 用于并入用于治疗各种疾病的药物组合物中的取代的吡啶并吲哚对应于其中R 1为H或任选取代的烷基的式（I） R 2，R 3，R 4各自独立地选自H，-O-烷基，-S-烷基，烷基，卤素，-CF 3和-CN; G为-CR12R13-NR5-或-NR5-CR12R13; R5; 是任选取代的烷基，任选取代的杂环，-C（= O）-R 6，-C（= O）-O-R7或-C（= O）-NR 19 R 20; R6和R7各自为任选取代的烷基或任选取代的杂环; R 8，R 9，R 10，R 11，R 12，R 13，R 19和R 20各自独立地选自H或任选取代的烷基; R 14和R 15各自独立地为H或卤素; L是-CH 2 -O-，-CH 2 CH 2 - ， - CH = CH-或键; 和B是芳基或杂芳基或环烷基; 条件是当L是直接键时，B不能是被氟单取代的未取代的杂芳基或杂芳基。