THIOLACTONE ANTIBIOTICS
    1.
    发明申请
    THIOLACTONE ANTIBIOTICS 审中-公开
    噻吗酮抗生素

    公开(公告)号:WO2012135027A3

    公开(公告)日:2013-01-03

    申请号:PCT/US2012030354

    申请日:2012-03-23

    摘要: This invention provides a compound having the structure (I) wherein R1 is H, (II) or (III), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), (VIII), or (IX), wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or (X); and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or (XI), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), or (VIII); and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, and when R2 is H or CH3 then R1 is other than H, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明提供具有式(I)的化合物,其中R 1为H,(II)或(III),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII),(VIII)或(IX)所示的化合物,其中m为0至8的整数; 或者(X); R 3是具有或不具有取代基,支链或非支链的氨基,烷基,芳基,杂芳基,二醇,哌嗪,吗啉,哌啶,三唑,叠氮化物或联苯。 R 4是烷基,芳基或杂芳基,各自具有或不具有取代,支链或非支链,R2是H,CH3或烷基,芳基,杂芳基,吡咯,二唑或三唑,各自具有或不具有取代,支链或非支链, 或(XI),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII)或(VIII)存在的情况; 并且当R 1为H时,R 6为叠氮基,甲氧基,三氟甲基,联苯基,取代的苯基,取代的三唑或烷基,芳基或杂芳基,具有或不具有取代,分支或未分支,则R2不是H或CH3, H或CH 3,然后R 1不是H,或其药学上可接受的盐。

    DIPHENYL ETHER ANTIMICROBIAL COMPOUNDS
    2.
    发明申请
    DIPHENYL ETHER ANTIMICROBIAL COMPOUNDS 审中-公开
    二苯醚类抗微生物化合物

    公开(公告)号:WO2006137840A2

    公开(公告)日:2006-12-28

    申请号:PCT/US2005/030011

    申请日:2005-08-23

    IPC分类号: A61K31/075 C07C43/23

    摘要: The present invention is directed to compounds having the formula: wherein A 1 , A 3 , A 6 , and A 8 independently represent CH or N; A 2 represents N or C-­X 1 a - R 1 ; A 4 represents N or C-X 2 b -R 2 ; R 1 and R 2 independently represent H, or a hydrocarbon containing a minimum of one carbon atom and a maximum of twenty six carbon atoms, wherein the hydrocarbon is unsubstituted, or is substituted with one or more of -OH, -NH 2 , -SH, halo, or -COOH; X 1 and X 2 independently represent -O-, - S-, -NH-, -C(O)O-, -C(O)-, -C(O)NH-, or -SO 2 NH-; a and b independently represent 0 or 1, provided that when a and b are both 0, then R 1 and R 2 are not both H; when a is 1, then R 1 is not H; and when b is 1, then R 2 is not H; A 5 and A 9 independently represent CR 3 or N; R 3 represents H, methyl, ethyl, or halo; A7 represents CR 4 or N; R 4 represents H, methyl, ethyl, halo, nitro, hydroxy, amino, amido, or a methyl or ethyl group substituted with halo, nitro, hydroxy, amino, or amido; provided that A 2 and A 4 are not both N; and not more than three of A 5 , A 6 , A 7 , A 8 , and A 9 are N. The invention is also directed to pharmaceutical compositions comprising a compound according to (1) and a pharmaceutically acceptable carrier. The invention is also directed to methods of inhibiting the growth of a bacterium containing an enoyl reductase enzyme encoded by a fabI gene, a fabK gene, a fabL gene, or a combination thereof, in a mammal in need thereof, the method comprising administering to the mammal an effective amount of a compound according to formula (1).

    摘要翻译: 本发明涉及具有下式的化合物:其中A 1,A 3,A 6和A 8, SUP>独立代表CH或N; A 2表示N或C-X 1

    THIOLACTONE ANTIBIOTICS
    3.
    发明申请
    THIOLACTONE ANTIBIOTICS 审中-公开
    噻吗酮抗生素

    公开(公告)号:WO2012135027A2

    公开(公告)日:2012-10-04

    申请号:PCT/US2012/030354

    申请日:2012-03-23

    摘要: This invention provides a compound having the structure (I) wherein R 1 is H, (II) or (III), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), (VIII), or (IX), wherein m is an integer from 0 to 8; R 3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or (X); and R 4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R 2 is H, CH 3 , or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or (XI), wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is (IV), (V), (VI), (VII), or (VIII); and R 6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R 1 is H then R 2 is other than H or CH 3 , and when R 2 is H or CH 3 then R 1 is other than H, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明提供具有式(I)的化合物,其中R 1为H,(II)或(III),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII),(VIII)或(IX)所示的化合物,其中m为0至8的整数; 或者(X); R 3是具有或不具有取代基,支链或非支链的氨基,烷基,芳基,杂芳基,二醇,哌嗪,吗啉,哌啶,三唑,叠氮化物或联苯。 R 4是烷基,芳基或杂芳基,各自具有或不具有取代,支链或非支链,R2是H,CH3或烷基,芳基,杂芳基,吡咯,二唑或三唑,各自具有或不具有取代,支链或非支链, 或(XI),其中n和q独立地为0至8的整数; (IV),(V),(VI),(VII)或(VIII)存在的情况; 并且当R 1为H时,R 6为叠氮基,甲氧基,三氟甲基,联苯基,取代的苯基,取代的三唑或烷基,芳基或杂芳基,具有或不具有取代,分支或未分支,则R2不是H或CH3, H或CH 3,然后R 1不是H,或其药学上可接受的盐。

    VOLTAGE TRANSFORMATION CIRCUIT
    4.
    发明申请
    VOLTAGE TRANSFORMATION CIRCUIT 审中-公开
    电压变换电路

    公开(公告)号:WO2009020566A1

    公开(公告)日:2009-02-12

    申请号:PCT/US2008/009332

    申请日:2008-08-01

    IPC分类号: G01R19/00

    摘要: A voltage transformation circuit comprising a first input (2), a second input (6), a first output (18), first and second impedances (8, 14) and a current mirror (12) having master (10) and slave (16) terminals, wherein the first impedance is connected between the first input and the master terminal of the current mirror, the second impedance is connected between the second input and the slave terminal of the current mirror, and the first output is connected to the slave terminal of the current mirror.

    摘要翻译: 一种电压变换电路,包括第一输入(2),第二输入(6),第一输出(18),第一和第二阻抗(8,14)以及具有主器件(10)和从器件(10)的电流镜 16)端子,其中第一阻抗连接在电流镜的第一输入端和主端子之间,第二阻抗连接在电流镜的第二输入端和从端之间,第一输出端连接到从设备 终端的电流镜。