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    Erythromycins
    2.
    发明授权
    Erythromycins 失效
    红霉素

    公开(公告)号：US5747467A

    公开(公告)日：1998-05-05

    申请号：US767954

    申请日：1996-12-19

    申请人： Constantin Agouridas ,  Fran.cedilla.ois Bretin ,  Jean-Fran.cedilla.ois Chantot

    发明人： Constantin Agouridas ,  Fran.cedilla.ois Bretin ,  Jean-Fran.cedilla.ois Chantot

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  A61P31/12 ,  A61P31/16 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein X is selected from the group consisting of --(NH).sub.a --, --CH.sub.2 --, --SO.sub.2 -- and --O--, a is 0 or 1, Y is --(CH.sub.2).sub.m - (CH.dbd.CH).sub.n --(CH.sub.2).sub.o -, m+n+o.ltoreq.8, n=o or 1, Ar is aryl optionally substituted with at least one member of the group consisting of --OH, halogen, --NO.sub.2, --CN, ##STR2## and alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, -N-alkyl, -N-alkenyl and N-alkynyl of up to 12 carbon atoms, R.sub.a and R.sub.b individually are hydrogen or alkyl of up to 12 carbon atoms, R.sub.3 is selected from the group consisting of alkyl of 1 to 12 carbon atoms, aryl, heteroaryl, carbocyclic aryl, aryloxy, arylthio and heterocyclic aryl, heterocyclic aryloxy and heterocyclic arylthio of 5 to 6 ring members containing at least one heteroatom, Hal is halogen, Z is hydrogen or acyl of an organic carboxylic acid and their non-toxic, pharmaceutically acceptable addition salts having antibacterial properties.

    摘要翻译： 选自下列化学式的化合物的化合物其中X选自 - （NH）a - ， - CH 2 - ， - SO 2 - 和-O-，a为0或1 ，Y是 - （CH 2）m - （CH = CH）n - （CH 2）o-，m + n + o = 8，n = 0或1，Ar是任选被至少一个 由-OH，卤素，-NO 2，-CN，和烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，烯硫基，炔硫基，-N-烷基，-N-链烯基和N-炔基组成的组 至多12个碳原子，R a和R b分别为氢或至多12个碳原子的烷基，R 3选自1至12个碳原子的烷基，芳基，杂芳基，碳环芳基，芳氧基，芳硫基和杂环芳基 ，含有至少一个杂原子的5至6个环成员的杂环芳氧基和杂环芳硫基，Hal是卤素，Z是氢或有机羧酸的酰基及其无毒的药学上可接受的加成盐，其具有抗菌性 关系

    Erythromycins
    3.
    发明授权
    Erythromycins 失效
    红霉素

    公开(公告)号：US5786339A

    公开(公告)日：1998-07-28

    申请号：US565252

    申请日：1995-11-30

    申请人： Constantin Agouridas ,  Jean-Fran.cedilla.ois Chantot

    发明人： Constantin Agouridas ,  Jean-Fran.cedilla.ois Chantot

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08 ,  A61K31/70

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R and R.sub.1 are --OH or --O-acyl of an organic carboxylic acid of 2 to 20 carbon atoms, R.sub.2 is hydrogen or methyl, R.sub.3 is --(CH.sub.2).sub.m --R.sub.4 or ##STR2## or --N--(CH.sub.2).sub.q --R.sub.4, m is an integer from 1 to 6, n, p and q are individually an integer from 0 to 6, A and B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 8 carbon atoms with the geometry of the double bond being E or Z or a mixture of E and Z or A and B form a triple bond, R.sub.4 is an optionally substituted mono- or polycyclic heterocycle and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

    摘要翻译： 选自下式的化合物的化合物其中R和R 1是具有2至20个碳原子的有机羧酸的-OH或-O-酰基，R 2是氢或甲基，R 3是 - （CH 2）m -R 4或者N-（CH 2）q -R 4，m是1至6的整数，n，p和q各自为0至6的整数，A和B各自独立地选择 由氢，卤素和1至8个碳原子的烷基组成的组，双键的几何形式为E或Z，或E和Z或A和B的混合物形成三键，R4为任选取代的单 - 或多环杂环及其无毒的药学上可接受的具有抗生素性质的酸加成盐。

    Erythromycin compounds
    4.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5770579A

    公开(公告)日：1998-06-23

    申请号：US378186

    申请日：1995-01-25

    申请人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Yannick Benedetti ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Claude Fromentin ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  C07H20060101 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Compounds of the formula ##STR1## wherein X and X' form C.dbd.O or C.dbd.NOR, R is selected from the group consisting of hydrogen, heterocycle, alkyl, alkenyl, alkynyl, all optionally substituted, ##STR2## R.sub.a and R.sub.b are hydrogen or a hydrocarbon group or form together with the nitrogen a heterocycle, or with A forms a 9-N, 11-O ring, and X' is hydrogen, --Y and Y' have the same definition as X and X', b is hydrogen or OR.sub.4, R.sub.4 is hydrogen or forms together with A a carbonate or a carbamate, A forms with C a double bond or A is OR'.sub.4, R'.sub.4 is hydrogen or forms together with B a carbonate or ##STR3## R.sub.2 is alkyl or --CONH.sub.2, --CONHCOR.sub.11 or --CONHSO.sub.2 R.sub.11, R.sub.11 is a hydrocarbon up to 18 carbon atoms, R.sub.3 is hydrogen, ##STR4## and Z is hydrogen or a carboxylic acid remainder and their non-toxic, pharmaceutically acceptable acid addition salts, their preparation and intermediates useful as antibiotics.

    摘要翻译： 式I的化合物其中X和X'形成C = O或C = NOR，R选自氢，杂环，烷基，烯基，炔基，全部被取代，R a和R b 是氢或烃基或与氮杂环的形式，或与A一起形成9-N，11-O环，X'为氢，-Y和Y'具有与X和X'相同的定义， b是氢或OR 4，R 4是氢或与A一起形成碳酸酯或氨基甲酸酯，A形式与C是双键或A是OR'4，R'4是氢或与B一起形成碳酸酯或 R 2是烷基或-CONH 2，-CONHCOR 11或-CONHSO 2 R 11，R 11是至多18个碳原子的烃，R 3是氢，Z是氢或羧酸残基及其无毒的药学上可接受的酸加成盐 ，它们的制备和中间体可用作抗生素。

    Erythromycin compounds
    5.
    发明授权
    Erythromycin compounds 失效
    红霉素化合物

    公开(公告)号：US5543400A

    公开(公告)日：1996-08-06

    申请号：US146695

    申请日：1993-11-01

    申请人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Fran.cedilla.ois Chantot ,  Alexis Denis ,  Odile Le Martret

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/706 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is ##STR2## m and n are individually integers from 0 to 6, A and B are individually a member selected from the group consisting of hydrogen, halogen and alkyl of 1 to 8 carbon atoms, the double bond geometry being E or Z or E+Z or A and B form a third bond between the carbon atoms to which they are attached, Ar is selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms optionally substituted with at least one member of the group consisting of free carboxy, alkoxycarbonyl, carboxy salified with a non-toxic, pharmaceutically acceptable base, amidified carboxy, --OH, halogen, --NO.sub.2, --CN, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio and alkynylthio of up to 12 carbon atoms, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms and cycloalkyl of 3 to 12 carbon atoms, all optionally substituted with at least one halogen and ##STR3## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms, carbocyclic aryl, aryloxy, arylthio, heterocyclic aryl and aryloxy and arylthio containing at least one heteroatom, all optionally substituted as above and b) heterocyclic aryl having at least one heteroatom optionally substituted with at least one of the above substituents, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.

    摘要翻译： 选自下列化合物的化合物其中R为M的化合物，其中R为0至6的整数，A和B分别为选自氢，卤素 1至8个碳原子的烷基，双键几何为E或Z或E + Z或A和B在它们所连接的碳原子之间形成第三键，Ar选自a）碳环 任选被至少一个由游离羧基，烷氧基羰基，无毒的药学上可接受的碱盐化的羧基，酰胺化的羧基，-OH，卤素，-NO 2，-CN， 烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，烯硫基和炔硫基，最多12个碳原子的N-烷基，N-烯基和N-炔基和3-12个碳原子的环烷基， 全部任选被至少一个卤素取代， nd R2各自独立地选自氢，1至12个碳原子的烷基，碳环芳基，芳氧基，芳硫基，杂环芳基和含有至少一个杂原子的芳氧基和芳硫基，全部如上所述被取代，和b）杂环芳基，其具有 至少一个任选被至少一个上述取代基取代的杂原子Z是氢或具有1至18个碳原子的有机羧酸的酰基及其无毒的药学上可接受的具有抗生素性质的酸加成盐。