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    HYPOPHOSPHOROUS ACID DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
    11.
    发明公开
    HYPOPHOSPHOROUS ACID DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS 审中-公开
    HYPO PHOSPHORIC衍生物及其治疗它们的应用

    公开(公告)号：EP1937699A2

    公开(公告)日：2008-07-02

    申请号：EP06842368.0

    申请日：2006-10-18

    申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

    发明人： ACHER, Francine ,  SELVAM, Chelliah ,  TRIBALLEAU, Nicolas ,  PIN, Jean-Philippe ,  BERTRAND, Hugues-Olivier

    IPC分类号： C07F9/30 ,  C07F9/38 ,  C07F9/6527 ,  C07F9/655 ,  C07F9/6553 ,  A61P25/00 ,  A61K31/662 ,  A61K31/663 ,  A61K31/665 ,  A61K31/67

    CPC分类号： C07F9/655345 ,  C07F9/301 ,  C07F9/302 ,  C07F9/306 ,  C07F9/3821 ,  C07F9/6527 ,  C07F9/65515 ,  Y02P20/55

    摘要： Hypophosphorous acid derivatives having Formula (I) wherein . M is a [C(R3,R4)]n1 - C(E,COOR1, N(H, Z)) group, or an optionally substituted Ar-CH(COOR1, N(H, Z)) group, or an a, ß, or a ß, g-cyclic aminoacid; . R1 is H or R, R being an hydroxy or a carboxy protecting group; . Z is H or an amino protecting group R', benzyl oxycarbonyl, benzyl or benzyl substituted; . E is H or a C1-C3 alkyl, aryl, an hydrophobic group; . R2 is selected in the group comprising: D-CH(R6)- C-(R7, R8), (R11,R12)CH- C(R9, R10), D - CH(OH), D- [C(R13, R14)]n3 -, C[(R15, R16, R17)]n4, D-CH2, (R18)CH = C(R19), D-(M1)n6-CO, Formula (II), PO(OH)2-CH2 or (PO(OH)2-CH2), (COOH-CH2)-CH2, with - D = H, OH, OR, (CH2)n2OH, (CH2)n1OR, COOH, COOR, (CH2)n2COOH, (CH2)n1COOR, SR, S(OR), SO2R, NO2, heteroaryl, C1-C3 alkyl, cycloalkyl, heterocycloalkyl, (CH2)n2-alkyl, (COOH, NH2)-(CH2)u1-cyclopropyl-(CH2)u2-, CO-NH-alkyl, Ar, (CH2)n2-Ar, CO-NH-Ar; - R3 to R19 being H, OH, OR, (CH2)n2OH, (CH2)n1OR, COOH, COOR, (CH2)n2COOH, (CH2)n1COOR, C1-C3 alkyl, cycloalkyl, (CH2)n1-alkyl, aryl, (CH2)n1-aryl, halogen, CF3, SO3H, (CH2)x PO3H2, with x = 0, 1 or 2, B(OH)2 , Formula (III), NO2 , SO2NH2 , SO2NHR; SR, S(O)R, SO2R, benzyl; - M1 is an alkylene or arylene group; - n1= 1, 2 or 3, n2= 1, 2 or 3, n3= 0, 1, 2 or 3 and n4= 1, 2 or 3, n5= 1,2 or 3, n6= 0 or 1, u1 and u2, identical or different = 0,1 or 2, with the proviso that Formula (I) does not represent the racemic (3R, S) and the enantiomeric form (3R) of 3 amino,3-carboxy-propyl-2'-carboxy-ethylphosphinic acid; 3 amino,3-carboxy-propyl- 4'carboxy,2'carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl- 2'carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl- 3'amino, 3'carboxy-propylylphosphinic acid; and 3 amino,3-carboxypropyl -7'amino-2', 7'-dicarboxyheptylphosphinic acid, said hypophosphorous acid derivatives being diasteroisomers or enantiomers. Application as drugs.