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    Derivatives . . . use as medicaments
    2.
    发明授权
    Derivatives . . . use as medicaments 有权
    衍生品。 。 。 用作药物

    公开(公告)号：US06455505B2

    公开(公告)日：2002-09-24

    申请号：US09433146

    申请日：1999-11-03

    申请人： Constantin Agouridas ,  Alexis Denis ,  Claude Fromentin

    发明人： Constantin Agouridas ,  Alexis Denis ,  Claude Fromentin

    IPC分类号： A61K3170

    CPC分类号： C07D233/64 ,  C07H17/08

    摘要： A subject of the invention is, as new chemical products, the compounds of formula (I) in which X represents a hydrogen atom or a halogen atom and Z represents a hydrogen atom or the remainder of an acid as well as their addition salts with acids. The compounds of formula (I) have antibiotic properties.

    摘要翻译： 本发明的主题是作为新的化学产品，其中X表示氢原子或卤素原子，Z表示氢原子或酸的其余部分的式（I）化合物及其与酸的加成盐 。 式（I）化合物具有抗生素特性。

    Derivatives of erythromycin, their preparation process and their use as medicaments
    3.
    发明授权
    Derivatives of erythromycin, their preparation process and their use as medicaments 有权
    红霉素的衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US06440941B1

    公开(公告)日：2002-08-27

    申请号：US09442681

    申请日：1999-11-18

    申请人： Alexis Denis

    发明人： Alexis Denis

    IPC分类号： A61K3170

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07H17/08

    摘要： A subject of the invention is the compounds of formula (I) in which Y represents a hydrogen atom or a fluorine atom, n represents an integer comprised between 1 and 8, Z represents a hydrogen atom or the remainder of a carboxylic acid, optionally substituted on the heterocycle by one or more alkyl, alkenyl, alkynyl, O-alkyl, O-alkenyl, O-alkynyl, S-alkyl, S-alkenyl, S-alkynyl radicals containing up to 8 carbon atoms, one or more OH, NH2, C═N, NO2, CF3 radicals or one or more aryl radicals containing up to 14 carbon atoms or heteroaryl radicals containing one or more nitrogen oxygen or sulphur atoms, the aryl or heteroaryl radicals themselves being able to be substituted as well as their addition salts with acids, The products of formula (I) have antibiotic properties.

    摘要翻译： 本发明的主题是式（I）的化合物，其中Y代表氢原子或氟原子，n表示1至8之间的整数，Z表示氢原子或羧酸的其余部分，任选在 通过一个或多个烷基，烯基，炔基，O-烷基，O-链烯基，O-炔基，S-烷基，S-烯基，含有至多8个碳原子的S-炔基，一个或多个OH，NH 2， C = N，NO 2，CF 3基团或含有至多14个碳原子的一个或多个芳基或含有一个或多个氮氧原子或硫原子的杂芳基，芳基或杂芳基自身能够被取代，以及它们的加成盐 与酸，式（I）的产物具有抗生素特性。

    Erythromycin derivatives, a process for their preparation and their use as medicaments
    4.
    发明授权
    Erythromycin derivatives, a process for their preparation and their use as medicaments 有权
    红霉素衍生物，其制备方法及其用作药物

    公开(公告)号：US06433151B1

    公开(公告)日：2002-08-13

    申请号：US09350224

    申请日：1999-07-08

    申请人： Alexis Denis ,  Giuseppe Gigliotti

    发明人： Alexis Denis ,  Giuseppe Gigliotti

    IPC分类号： C07H1708

    CPC分类号： C07H17/08

    摘要： The invention relates to compounds of the formula (I) in which R represents a radical (CH2)mOn(X)YAr  in which m represents the number 0 or 1, n represents the number 0 or 1, X represents a radical (NH)a, CH2 or SO2, where a represents the number 0 or 1, Y represents a radical (CH2)b—(CH═CH)c—(CH2)d, where c=0 or 1 and b+c+d ≦8, Z represents a hydrogen or halogen atom, Ar represents an optionally substituted aryl or heteroaryl radical and W represents a hydrogen atom or an acyl radical, and their acid addition salts. The compounds of the formula (1) have antibiotic properties.

    摘要翻译： 本发明涉及式（I）化合物，其中R表示基团，其中m表示数字0或1，n表示数字0或1，X表示基团（NH）a，CH 2或SO 2，其中a表示 数字0或1，Y表示基团（CH 2）b - （CH = CH）c - （CH 2）d，其中c = 0或1，b + c + d <= 8，Z表示氢或卤素原子 ，Ar表示任选取代的芳基或杂芳基，W表示氢原子或酰基，以及它们的酸加成盐。式（1）化合物具有抗生素特性。

    Erythromycin derivatives, method for preparing same and use thereof as drugs
    6.
    发明授权
    Erythromycin derivatives, method for preparing same and use thereof as drugs 有权
    红霉素衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US6162793A

    公开(公告)日：2000-12-19

    申请号：US230126

    申请日：1999-02-11

    申请人： Constantin Agouridas ,  Jean-Francois Chantot ,  Alexis Denis ,  Jean-Marie Pejac

    发明人： Constantin Agouridas ,  Jean-Francois Chantot ,  Alexis Denis ,  Jean-Marie Pejac

    IPC分类号： A61K31/7048 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70 ,  C07D215/00

    CPC分类号： C07H17/08

    摘要： The compounds of formula (I): ##STR1## in which R is a hydrogen atom, an alkyl, optionally substituted by a halogen atom or a (CH.sub.2).sub.m Ar radical or a ##STR2## in which m represents an integer (1-8), n and p, identical or different, represent an integer (0-6), A and B, identical or different, represent a hydrogen or a halogen or an alkyl and Ar represents an aryl or heteroaryl, and Z represents a hydrogen or the remainder of a carboxylic acid, preparation process and use as medicaments.

    摘要翻译： PCT No.PCT / FR97 / 01372 Sec。 371日期1999年2月11日 102（e）1999年2月11日PCT PCT 1997年7月23日PCT公布。 第WO98 / 03530号公报 日期：1998年1月29日式（I）化合物：其中R为氢原子，任选被卤素原子或（CH 2）mAr基团取代的烷基，或其中m表示整数（1-8） ，n和p相同或不同，表示整数（0-6），A和B相同或不同，表示氢或卤素或烷基，Ar表示芳基或杂芳基，Z表示氢或 剩余的羧酸，制备方法和用作药物。

    Erythromycin compounds
    9.
    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。

    Erythromycin derivatives
    10.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号：US5527780A

    公开(公告)日：1996-06-18

    申请号：US146697

    申请日：1993-11-01

    申请人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    发明人： Constantin Agouridas ,  Alain Bonnefoy ,  Jean-Francois Chantot ,  Alexis Denis ,  Odile Le Martret

    IPC分类号： C07C211/27 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/00 ,  A61P31/04 ,  C07C217/62 ,  C07D239/20 ,  C07D333/10 ,  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 --(CH.sub.2).sub.n --Ar.sub.1 or --XAr.sub.2, n is an integer from 1 to 6, Ar.sub.1 and Ar.sub.2 are individually selected from the group consisting of a) carbocyclic aryl of up to 18 carbon atoms substituted by at least one member of the group consisting of free carboxy, alkoxy carbonyl and carboxyl salified with a pharmaceutically acceptable base, --OH, halogen, --NO.sub.2, --CN, ##STR2## and alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, N-alkyl, N-alkenyl and N-alkynyl of up to 12 carbon atoms optionally substituted with at least one halogen, R.sub.1 and R.sub.2 are individually hydrogen or alkyl of 1 to 12 carbon atoms, b) ##STR3## wherein R.sub.3 is selected from the group consisting of alkyl of 1 to 12 carbon atoms, optionally substituted carbocyclic aryl, aryloxy and arylthio, optionally substituted heterocyclic aryl, aryloxy and arylthio containing at least one heteroatom with the optional substituents being those of carbocyclic aryl above, X is an alkyl of 1 to 6 carbon atoms interrupted by a member of the group consisting of --O--, --S--, --SO--, --SO.sub.2, --CO--, ##STR4## Z is hydrogen or acyl of an organic carboxylic acid of up to 18 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity against gram positive and gram negative bacteria.

    摘要翻译： 选自下式的化合物的化合物其中R为 - （CH 2）n -Ar 1或-XAr 2，n为1至6的整数，Ar 1和Ar 2分别选自 a）由至少一个由游离羧基，烷氧基羰基和与药学上可接受的碱成盐的羧基取代的至多18个碳原子的碳环芳基，-OH，卤素，-NO 2，-CN， 烷基，环烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，烯硫基，炔硫基，任选被至少一个卤素取代的具有12个碳原子的N-烷基，N-烯基和N-炔基R1和R2 单独的氢或1至12个碳原子的烷基，b）其中R 3选自1至12个碳原子的烷基，任选取代的碳环芳基，芳氧基和芳硫基，任选取代的杂环芳基，芳氧基和芳硫基 含有至少一个杂原子 任选的取代基是上述碳环芳基的取代基，X是被-O - ， - S - ， - SO - ， - SO 2，-CO-， - CO-的成员间隔的1至6个碳原子的烷基， Z是具有至多18个碳原子的有机羧酸的氢或酰基，以及它们对革兰氏阳性和革兰氏阴性菌具有抗生素活性的无毒的药学上可接受的酸加成盐。