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    New derivatives of echinocandine, their preparation process and their use as antifungals
    1.
    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。

    Derivatives of echinocandine, their preparation process and their use as antifungals
    2.
    发明授权
    Derivatives of echinocandine, their preparation process and their use as antifungals 失效
    棘皮棘酸衍生物，其制备方法及其作为抗真菌剂的用途

    公开(公告)号：US07192920B2

    公开(公告)日：2007-03-20

    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

    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与携带它们的氮一起形成具有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：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，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。

    Echinocandin derivatives, method for preparing same and application as antifungal agents
    3.
    发明授权
    Echinocandin derivatives, method for preparing same and application as antifungal agents 失效
    棘白菌素衍生物，其制备方法和作为抗真菌剂的应用

    公开(公告)号：US07022669B1

    公开(公告)日：2006-04-04

    申请号：US10018073

    申请日：2000-06-08

    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

    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与携带它们的氮一起形成具有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：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH， Z：H，CH 3。 式（I）的化合物具有抗真菌性质。

    Heterocyclic dicarboxylic acids
    9.
    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。

    9-Oxalysergic acid derivatives and uses thereof
    10.
    发明授权
    9-Oxalysergic acid derivatives and uses thereof 失效
    9-氧肉桂酸衍生物及其用途

    公开(公告)号：US4493836A

    公开(公告)日：1985-01-15

    申请号：US493355

    申请日：1983-05-10

    申请人： Lucien Nedelec ,  Andre Pierdet ,  Patrick Fauveau

    发明人： Lucien Nedelec ,  Andre Pierdet ,  Patrick Fauveau

    IPC分类号： A61K31/535 ,  A61P9/12 ,  A61P43/00 ,  C07D209/00 ,  C07D209/90 ,  C07D265/00 ,  C07D498/06 ,  C07D498/04

    CPC分类号： C07D209/90

    摘要： Novel derivatives of 9-oxalysergic acid of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of --CH.sub.2 OH, alkylthiomethyl with 1 to 4 alkyl carbon atoms, --CH.sub.2 CN, --COOH, --COOAlk and ##STR2## Alk is alkyl of 1 to 5 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.5 is alkyl of 1 to 5 carbon atoms or R.sub.4 and R.sub.5 together with the nitrogen form a saturated heterocycle optionally containing another heteroatom and their non-toxic, pharmaceutically acceptable acid addition salts having essentially dopaminergic agonist activity, inhibiting activity of prolactin secretion, serotoninergic activity and antihypertensive activity and their preparation.

    摘要翻译： 其中R选自氢和1至4个碳原子的烷基，其中R选自氢，氯和溴，R2选自下列化学式的9-氧代戊酸的新型衍生物：其中R选自氢， 由氢，1-4个碳原子的烷基，7-12个碳原子的芳烷基和4-7个碳原子的环烷基烷基组成的组中，R3选自-CH2OH，具有1-4个烷基碳原子的烷硫基甲基 ，-CH 2 CN，-COOH，-COOAlk和Alk是1至5个碳原子的烷基，R 4选自氢和1至5个碳原子的烷基，R 5是1至5个碳原子的烷基 或R 4和R 5与氮一起形成任选地含有另外的杂原子的饱和杂环及其无毒的药学上可接受的酸加成盐，其具有基本上多巴胺能激动剂活性，抑制催乳素分泌的活性，血清素能活性和抗高血压 随行活动及其准备。