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    Cephalosporins
    4.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US06313305B1

    公开(公告)日：2001-11-06

    申请号：US08900366

    申请日：1997-07-21

    申请人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Patrick Fauveau ,  Solange Gouin d'Ambrieres ,  Daniel Humbert ,  Christophe Dini

    发明人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Patrick Fauveau ,  Solange Gouin d'Ambrieres ,  Daniel Humbert ,  Christophe Dini

    IPC分类号： C07D28508

    CPC分类号： C07D501/00 ,  C07C45/63 ,  C07C45/673 ,  C07C45/71 ,  C07C47/565 ,  C07C47/575 ,  C07C59/64 ,  C07C69/734 ,  C07C205/44 ,  C07C239/20 ,  C07C255/56 ,  C07C255/57 ,  Y02P20/55

    摘要： A compound having the formula selected from the group consisting of wherein either R3p and R4p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R2p is selected from the group consisting of —CN, —F, Br and I and R1p and R5p are hydrogen or R5p is —F and R1p and R2p are hydrogen or R1p and R2p are F and R5p is hydrogen, or R4p and R5p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R3p is selected from the group consisting of F and —CN and R1p and R2p are hydrogen, R8 is hydrogen or an amine protective group and R10 is the remainder in which the hydroxy or amino are protected wherein R′1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, —CN, carboxy and alkoxy carbonyl of 1 to 4 carbon atoms.

    摘要翻译： 具有选自R3p和R4p中的式的化合物是相同的，并且选自-OH，被保护的-OH和1至8个碳原子的酰氧基，R2p选自-CN， -F，Br和I，R1p和R5p是氢或R5p是-F，R1p和R2p是氢或R1p，R2p是F，R5p是氢，或R4p和R5p是相同的，选自-OH， 保护的-OH和1至8个碳原子的酰氧基，R3p选自F和-CN，R1p和R2p是氢，R8是氢或胺保护基，R10是其中羟基或氨基 被保护，其中R'1选自1至4个碳原子的烷基，-CN，羧基和1至4个碳原子的烷氧基羰基。

    New derivatives of echinocandine, their preparation process and their use as antifungals
    9.
    发明申请
    New derivatives of echinocandine, their preparation process and their use as antifungals 失效
    棘皮菌素的新衍生物，其制备方法及其作为抗真菌剂的用途

    公开(公告)号：US20060035820A1

    公开(公告)日：2006-02-16

    申请号：US11225627

    申请日：2005-09-13

    申请人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    发明人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

    IPC分类号： A61K38/12 ,  C07K5/12

    CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S930/27

    摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b—C≡N radical or R1 and R2 together with the nitrogen which carries-them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear,. branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.

    摘要翻译： 本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4， 氢或羟基R：代表线性。 支链或环状链T：氢，甲基，CH 2 CONH 2，CH 2C≡N，a（CH 2） / SUB 2）或（CH 2）2 N 2 O 2 N 2 O 2 N 2 N 2 O 2 X，卤素和烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH，Z：H，CH 3 。 式（I）化合物具有抗真菌性质。

    Heterocyclic dicarboxylic acids
    10.
    发明授权
    Heterocyclic dicarboxylic acids 失效
    杂环二羧酸

    公开(公告)号：US5141952A

    公开(公告)日：1992-08-25

    申请号：US716950

    申请日：1991-06-18

    申请人： Constantin Agouridas ,  Patrick Fauveau

    发明人： Constantin Agouridas ,  Patrick Fauveau

    IPC分类号： A61K31/35 ,  A61K31/351 ,  A61K31/445 ,  A61K39/39 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D211/18 ,  C07D211/60 ,  C07D211/78 ,  C07D309/08 ,  C07D309/10 ,  C07D309/28

    CPC分类号： C07D309/10 ,  C07D211/18 ,  C07D211/60

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of --OH, hydrogen, ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.

    摘要翻译： 选自下式的化合物的化合物，其中虚线表示可能的内端或外双键，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至8个碳原子的烯基和炔基，6至14个碳原子的芳基，7至18个碳原子的芳烷基和1至8个碳原子的烷基或6至14个碳原子的芳基， X是-O-或-NR-，R选自-OH，氢，IMA和-COOR'，R'是氢或1至8个碳原子的烷基，Y选自 由氢，1至8个碳原子的烷基和2至8个碳原子的烯基和炔基组成，全部任选被至少一个卤素或-OH取代，条件是如果Y是-OH，X不是-NH- 及其无毒，药学上可接受的具有抗菌和免疫学特性的酸或碱的加成盐。