Compounds for the treatment of metabolic disorders
    3.
    发明授权
    Compounds for the treatment of metabolic disorders 有权
    用于治疗代谢紊乱的化合物

    公开(公告)号:US08022249B2

    公开(公告)日:2011-09-20

    申请号:US11909120

    申请日:2006-03-31

    CPC classification number: C07C259/06 C07C235/34

    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3, 4 or 5; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 is hydrogen or —(CH2)gOH wherein g is 0, 1 or 2; R4 is hydrogen, methyl or ethyl; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; or a pharmaceutically acceptable salt of the compound.

    Abstract translation: 公开了可用于治疗各种代谢紊乱(例如胰岛素抵抗综合征,糖尿病,高脂血症,脂肪肝疾病,恶病质,肥胖症,动脉粥样硬化和动脉硬化)的化合物。 其中n为1或2; m为0,1,2,3,4或5; q为0或1; t为0或1; R1是具有1至3个碳原子的烷基; R2是氢,卤素,具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基; R3是氢或 - (CH2)gOH,其中g是0,1或2; R4是氢,甲基或乙基; A是未取代的或被1或2个选自:卤素,具有1或2个碳原子的烷基,全氟甲基,具有1或2个碳原子的烷氧基和全氟甲氧基取代的苯基; 或具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳独立地被甲基或乙基单取代; 或具有1或2个选自N,S和O的环杂原子的5或6元杂芳环,杂芳环通过环碳与式I化合物的其余部分共价结合; 或该化合物的药学上可接受的盐。

    Bacterial enzyme inhibitors
    8.
    发明授权
    Bacterial enzyme inhibitors 失效
    细菌酶抑制剂

    公开(公告)号:US07241921B2

    公开(公告)日:2007-07-10

    申请号:US10497494

    申请日:2002-11-27

    CPC classification number: C07D213/40 C07C275/24 C07C2601/08 C07D295/215

    Abstract: Compounds of formula (I) are antibacterial agents: wherein: Z is —N(OH)CH(═O) or —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula —N(OH)CH(═O), a hydroxy, halo or amino group; R2, R3 and R4 independently represents hydrogen or a group R10—(D)n—(ALK)m— wherein R10, D, n, m and ALK are as defined in the claims; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which R4 and R5 are attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen

    Abstract translation: 式(I)化合物是抗菌剂:其中:Z是-N(OH)CH(-O)或-C(-O)NH(OH); 除了当Z是式-N(OH)CH(-O),羟基,卤素或氨基基团时,R 1表示氢,甲基或三氟甲基。 R 2,R 3和R 4独立地表示氢或基团R 10 - (D)

    Histone deacetylase inhibitors
    10.
    发明授权
    Histone deacetylase inhibitors 失效
    组蛋白脱乙酰酶抑制剂

    公开(公告)号:US07154002B1

    公开(公告)日:2006-12-26

    申请号:US10681049

    申请日:2003-10-07

    CPC classification number: C07C259/06 C07D231/16 C07D239/38 C07D241/44

    Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3–12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.

    Abstract translation: 提供组蛋白脱乙酰酶抑制剂及其用途,其具有以下通式:其中R 1,R 2,R 3和R 4, / SUB>各自独立地选自氢,取代或未取代的直链C 1-12烷基,C 2-12-12氨基烷基或C 1 -C 12烷基, 2-12个氧杂烷基,以及取代和未取代的3,4,5,6,7或8元环,条件是R 3和R 4 不是氢; R 5选自羰基,取代或未取代的C 1-3烷基,取代或未取代的C 1-3烷基, 烷基-C(O),取代或未取代的-C(O)-C 1-3烷基和取代或未取代的-C(O)C(O)C 1-3烷基; M是能与蛋白质金属离子络合的取代基; L是包含连接M取代基与L取代基的α原子的3-12个原子的链的取代基。

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