Inhibitors of dimethylarginine dimethylaminohydrolase
    1.
    发明授权
    Inhibitors of dimethylarginine dimethylaminohydrolase 有权
    二甲基精氨酸二甲氨基水解酶抑制剂

    公开(公告)号:US08921421B2

    公开(公告)日:2014-12-30

    申请号:US13133799

    申请日:2009-12-08

    摘要: The invention relates to an inhibitor of dimethylarginine dimethylaminohydrolase (DDAH) of general structural formula (I), wherein B is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; R1 is selected from the group of structures (i-vii), wherein R2, R3 and R4 are selected from the group consisting of hydrogen, an alkyl or aryl radical, R5 and R6 are selected from the group consisting of hydrogen, a hydrocarbon chain having a chain length of 1 to 8 and an aryl radical, R7, R8, R9 and R10 are selected from the group consisting of hydrogen, and alkyl or aryl radical; W is oxygen (O) or nitrogen (N); and X is a methylene group (CH2) or a secondary amino group (NH); Y is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; Z is hydrogen (H) or a methoxyl group; and the radical (B) carrying the amino group has no carboxyl group.

    摘要翻译: 本发明涉及一般结构式(I)的二甲基精氨酸二甲氨基水解酶(DDAH)抑制剂,其中B是链长为1-6的支链或非支链,取代或未取代的饱和或不饱和烃链和/或 具有3至6个环的取代或未取代的芳族体系; R1选自结构式(i-vii),其中R2,R3和R4选自氢,烷基或芳基,R5和R6选自氢,烃链 具有1至8个链长和芳基,R 7,R 8,R 9和R 10选自氢和烷基或芳基; W是氧(O)或氮(N); 并且X是亚甲基(CH 2)或仲氨基(NH); Y是链长为1至6的支链或非支链,取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; Z是氢(H)或甲氧基; 并且带有氨基的基团(B)没有羧基。

    Inhibitors of Dimethylarginine Dimethylaminohydrolase
    2.
    发明申请
    Inhibitors of Dimethylarginine Dimethylaminohydrolase 有权
    二甲基精氨酸二甲基氨基水解酶抑制剂

    公开(公告)号:US20110294878A1

    公开(公告)日:2011-12-01

    申请号:US13133799

    申请日:2009-12-08

    摘要: The invention relates to an inhibitor of dimethylarginine dimethylaminohydrolase (DDAH) of general structural formula (I), wherein B is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; R1 is selected from the group of structures (i-vii), wherein R2, R3 and R4 are selected from the group consisting of hydrogen, an alkyl or aryl radical, R5 and R6 are selected from the group consisting of hydrogen, a hydrocarbon chain having a chain length of 1 to 8 and an aryl radical, R7, R8, R9 and R10 are selected from the group consisting of hydrogen, and alkyl or aryl radical; W is oxygen (O) or nitrogen (N); and X is a methylene group (CH2) or a secondary amino group (NH); Y is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; Z is hydrogen (H) or a methoxyl group; and the radical (B) carrying the amino group has no carboxyl group.

    摘要翻译: 本发明涉及一般结构式(I)的二甲基精氨酸二甲氨基水解酶(DDAH)抑制剂,其中B是链长为1-6的支链或非支链,取代或未取代的饱和或不饱和烃链和/或 具有3至6个环的取代或未取代的芳族体系; R1选自结构式(i-vii),其中R2,R3和R4选自氢,烷基或芳基,R5和R6选自氢,烃链 具有1至8个链长和芳基,R 7,R 8,R 9和R 10选自氢和烷基或芳基; W是氧(O)或氮(N); 并且X是亚甲基(CH 2)或仲氨基(NH); Y是链长为1至6的支链或非支链,取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; Z是氢(H)或甲氧基; 并且带有氨基的基团(B)没有羧基。

    Amino acid derivatives used as pharmaceutical substances
    7.
    发明授权
    Amino acid derivatives used as pharmaceutical substances 失效
    用作药物的氨基酸衍生物

    公开(公告)号:US08658826B2

    公开(公告)日:2014-02-25

    申请号:US12847544

    申请日:2010-07-30

    IPC分类号: C07C257/00

    摘要: The invention relates to a method for improving bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.

    摘要翻译: 本发明涉及一种提高药物物质生物利用度和允许药物渗透血脑屏障的方法,具有至少一种或多种脒,胍,N-羟基脒(偕胺肟)或N-羟基胍功能的药物物质 。 本发明还涉及含有相应修饰的药物的药物。

    ANTIBACTERIAL AND ANTIFUNGAL SUBSTANCES BIPHENYLYL COMPOUNDS
    10.
    发明申请
    ANTIBACTERIAL AND ANTIFUNGAL SUBSTANCES BIPHENYLYL COMPOUNDS 审中-公开
    抗生素和抗真菌物质联苯化合物

    公开(公告)号:US20140323763A1

    公开(公告)日:2014-10-30

    申请号:US13995261

    申请日:2011-12-21

    摘要: The invention relates to the use of a substance of the general form (I) to produce an antibacterial and/or antifungal drug, wherein X is a methylene group or a carbonyl group; R1, R2, and R3 are each selected from the group comprising hydrogen, an alkyl group having a chain length of 1-4 carbon atoms, an alkoxy group having a chain length of 1-3 carbon atoms, and a halogen; R4 and R5 are each selected from the group comprising hydrogen and an alkyl group having a chain length of 1-4 carbon atoms; and n=3 to 6.

    摘要翻译: 本发明涉及一般形式(I)物质生产抗菌和/或抗真菌药物的用途,其中X为亚甲基或羰基; R1,R2和R3各自选自氢,链长为1-4个碳原子的烷基,链长为1-3个碳原子的烷氧基和卤素; R4和R5各自选自氢和链长为1-4个碳原子的烷基; n = 3〜6。