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    BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    46.
    发明授权
    BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权
    取代的苯并咪唑磺酰胺衍生物用作广谱HIV蛋白酶抑制剂

    公开(公告)号：EP1485358B1

    公开(公告)日：2011-02-02

    申请号：EP03714954.9

    申请日：2003-03-12

    申请人： Tibotec Pharmaceuticals

    发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  WIGERINCK, Piet, Tom, Bert, Paul ,  VOETS, Marieke, Christiane, Johanna ,  VENDEVILLE, Sandrine, Marie, Helene ,  DE KOCK, Herman, Augustinus ,  VERGOUWEN, Bernhard, Joanna, Bernard

    IPC分类号： C07D235/32 ,  A61K31/415 ,  C07D493/04 ,  C07D235/30 ,  C07D407/12 ,  C07D417/12 ,  C07D413/12 ,  C07D401/12 ,  A61P31/18

    CPC分类号： C07D401/12 ,  A61K31/415 ,  C07D235/30 ,  C07D235/32 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D493/04

    摘要： The present invention concerns the compounds having the formula (I), wherein N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aRl0b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6 alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6 alkyl, optionally substituted amino­-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6 alkyloxy­carbonylamino or amino; and in case _A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and _A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2, R12 , is H, - NH2, _NR5AR6, - C1-6alkyl or alkyl-W-R14 , wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl and R13 is H, C1-6-alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1-4alkyl.

    NOVEL BENZIMIDAZOLE (THIO) CARBAMATES WITH ANTIPARASITIC ACTIVITY AND THE SYNTHESIS THEREOF
    48.
    发明公开
    NOVEL BENZIMIDAZOLE (THIO) CARBAMATES WITH ANTIPARASITIC ACTIVITY AND THE SYNTHESIS THEREOF 有权
    具有抗寄生虫效应和综合新苯并咪唑（硫）氨基甲酸酯

    公开(公告)号：EP1913009A1

    公开(公告)日：2008-04-23

    申请号：EP06777837.3

    申请日：2006-07-18

    申请人： Intervet International BV

    发明人： CHASSAING, Christophe, Pierre, Alain

    IPC分类号： C07F9/572 ,  C07D235/32 ,  C07F9/553 ,  C07F9/165 ,  C07F9/141

    CPC分类号： C07F9/65068

    摘要： The present invention is concerned with novel benzimidazole (thio)carbamates with antiparasitic activity. The present invention provides compounds of the following general formula (I) wherein X1 and X2 are O or S, wherein at least one of X1 and X2 is O, Y1 and Y2 are O or S, wherein at least one of Y1 and Y2 is O, R1 is alkyl of 1-4 carbon atoms, R2, R3 and R4 are independently of each other hydrogen, or a cation, R5 and R6 may both independently be hydrogen or halogen or alkyl having from 1-8 carbon atoms, or -OR7, wherein R7 is alkyl having from 1-8 carbon atoms, or -SR8, wherein R8 may be alkyl having from 1-8 carbon atoms, or aryl, or -CO-R9, wherein R9 is alkyl having from 1-8 carbon atoms, cycloalkyl having from 3-6 carbon atoms, or R9 is aryl, or -OSO2-Ar, wherein Ar is aryl, or -S(O)R10, wherein R10 is alkyl having from 1-8 carbon atoms, or wherein R10 is aryl. The compounds of the invention are highly soluble and stable in water. Moreover, it has been found that the compounds according to the invention are stable for over 8 hours at pH 5 and at pH 9, which are the lower and upper pH limits at which compounds should be stable for over 8 hours in order to be suitable for drinking water application. The compounds of the present invention have excellent antiparasitic, and especially anthelmintic activity in vivo, which is comparable to the state of the art, water insoluble, benzimidazole carbamates such as albendazole and fenbendazole.