公开(公告)号：US20080249080A1

公开(公告)日：2008-10-09

申请号：US11997689

申请日：2006-05-26

申请人： Romano Silvestri ,  Gabriella Marfe' ,  Elisabetta Abruzzese ,  Gianfranco Catalano ,  Carla Di Stefano ,  Ettore Novellino ,  Paola Sinibaldi Salimei ,  Maria Gabriella De Martino ,  Giuseppe La Regina ,  Antonio La-Vecchia

发明人： Romano Silvestri ,  Gabriella Marfe' ,  Elisabetta Abruzzese ,  Gianfranco Catalano ,  Carla Di Stefano ,  Ettore Novellino ,  Paola Sinibaldi Salimei ,  Maria Gabriella De Martino ,  Giuseppe La Regina ,  Antonio La-Vecchia

IPC分类号： A61K31/00 ,  C07D255/00 ,  C07D285/36 ,  A61P43/00 ,  A61K31/33

CPC分类号： C07D513/04

摘要： The invention concerns benzodiazepine derivatives of formula wherein Y it is SO2 or NR, wherein R is H or C1-C6 alkyl; X is H, C1-C12 alkyl, —CO, —SO, —SO2, or —CO—R2, SO—R2, SO2—R2, wherein R2 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, —CN, —NH2, —OH, —NO2, COOR3, wherein R3 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxy carbonyl; phenyl, benzyl, naphtyl, biphenyl, or heterocycle n is 0-6; R4 is selected from H, OH, COOH, CN, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, —CO, —SO, —SO2, or —CO—R5, SO—R5, SO2—R2, —OCO—R5, OSO—R5, SO2—R5, COOR5, SOOR5, SO2OR5, NHR5, NHCOR5, NHSO2R5, SR5, SCOR5, wherein R5 is selected from H, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, —CN, —NH2, OH, —NO2, COOR5′, wherein R5 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxy carbonyl; R6 and R7 independently of each other are selected from the group consisting of H, OH, halogen, CN, NH2, NO2, COOR3, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, and C2-C6 alkoxy carbonyl; R3 is H, C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl or physiologically acceptable salts and uses thereof in medical field, particularly as anti-tumoral agents.

公开(公告)号：US07365090B2

公开(公告)日：2008-04-29

申请号：US10637949

申请日：2003-08-07

申请人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

发明人： Marino Artico ,  Paolo LaColla ,  Romano Silvestri ,  Adel Moussa ,  Jean-Pierre Sommadossi ,  Richard Storer

IPC分类号： A61K31/405 ,  C07D209/14

CPC分类号： C07D403/04 ,  C07D209/42 ,  C07D403/12

摘要： This invention is in the area of phenylindoles that are useful for the treatment of HIV infection, and, in particular, phenylindoles that exhibit significant activity against resistant strains of HIV. The phenylindoles have at least two substituents other than hydrogen on the benzo ring of the indole function, preferably at the 4′ and 5′, 5′ and 6′ or the 5′ and 7′ positions, optionally in combination with disubstitution at positions 3″ and 5″ on the phenyl ring of the compound, and carboxamide containing moieties at position-2 on the indole group of the compound. Methyl is a preferred group for substitution on the phenyl ring. Preferred substituents for the benzo ring of the indole function include but are not limited to chlorine, fluorine, bromine, iodine, CF3, methoxy, CN, and NO2.

摘要翻译： 本发明在可用于治疗HIV感染的苯基吲哚的区域中，特别是对抗HIV抗性菌株显示出显着活性的苯基吲哚。 苯吲哚在吲哚官能团的苯并环上具有至少两个除氢之外的取代基，优选在4'和5'，5'和6'或5'和7'位置，任选地与3位的取代基组合 “和5”，化合物的吲哚基上的位置-2的含羧酰胺的部分。 甲基是在苯环上取代的优选基团。 吲哚官能团的苯并环的优选取代基包括但不限于氯，氟，溴，碘，CF 3，甲氧基，CN和NO 2。