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1. 发明授权

US5656607A Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：US5656607A
公开(公告)日：1997-08-12
申请号：US414503
申请日：1995-03-31
申请人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Odile Le Martret
发明人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Odile Le Martret
IPC分类号： C07H17/08 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07H17/00
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.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form ##STR2## and R'.sub.1 and R'.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S 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 1和R 2分别选自氢和至多24个碳原子的任选不饱和烃，任选地被至少一个选自以下的杂原子间隔的杂原子由氧，硫和氮组成并且任选地具有至少一个官能团或一起形成的基团组成，并且R'1和R'2分别选自氢和任选不饱和的烃，最多达23个碳原子任选地被至少一个选自氮，氧和硫并且任选具有至少一个官能团的杂原子中断，Z是氢或具有1至18个碳原子的有机羧酸的酰基，波浪线表示该10-甲基可具有R或S构型或R + S与其无毒的药学上可接受的具有抗生素的酸加成盐的混合物 tic属性。

2. 发明授权

US5561118A Erythromycin compounds 失效
标题翻译：红霉素化合物
公开(公告)号：US5561118A
公开(公告)日：1996-10-01
申请号：US220484
申请日：1994-03-31
申请人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Claude Fromentin , Odile Le Martret
发明人： Constantin Agouridas , Yannick Benedetti , Jean-Francois 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, or X is ##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, 11-0 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 A is ##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，或X是< R a和R b是氢或烃基或与氮一起形成杂环或与A一起形成9-N，11-0环，X'是氢，-Y和Y'具有与X相同的定义， X'，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 A是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，它们是无毒的，药学上可接受的酸加成盐，它们的制剂和用作抗生素的中间体。

3. 发明授权

US5760233A Propanal derivatives 失效
标题翻译：丙醛衍生物
公开(公告)号：US5760233A
公开(公告)日：1998-06-02
申请号：US805439
申请日：1997-02-25
申请人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Odile Le Martret
发明人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Odile Le Martret
IPC分类号： C07H17/08 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07H17/00 , C07D215/00 , C07C13/00 , C07D271/00 , C07D277/04
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.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form ##STR2## and R'.sub.1 and R'.sub.2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S 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 1和R 2分别选自氢和至多24个碳原子的任选不饱和烃，任选地被至少一个选自以下的杂原子间隔的杂原子由氧，硫和氮组成并且任选地具有至少一个官能团或一起形成的基团组成，并且R'1和R'2分别选自氢和任选不饱和的烃，最多达23个碳原子任选地被至少一个选自氮，氧和硫并且任选具有至少一个官能团的杂原子中断，Z是氢或具有1至18个碳原子的有机羧酸的酰基，波浪线表示该10-甲基可具有R或S构型或R + S与其无毒的药学上可接受的具有抗生素的酸加成盐的混合物 tic属性。

4. 发明授权

US5444051A Erythromycin compounds 失效
标题翻译：红霉素化合物
公开(公告)号：US5444051A
公开(公告)日：1995-08-22
申请号：US83636
申请日：1993-06-28
申请人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis , Claude Fromentin , Odile Le Martret
发明人： Constantin Agouridas , Yannick Benedetti , Jean-Francois 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,or X is ##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，或X是< R a和R b是氢或烃基或与氮一起形成杂环或与A一起形成9-N，11-O环，X'是氢，-Y和Y'具有与X相同的定义， X'，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，它们是无毒的，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。

5. 发明授权

US5439889A Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：US5439889A
公开(公告)日：1995-08-08
申请号：US207355
申请日：1994-03-07
申请人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis
发明人： Constantin Agouridas , Yannick Benedetti , Jean-Francois Chantot , Alexis Denis
IPC分类号： A61K31/445 , A61K31/443 , A61K31/4523 , A61P31/04 , C07D405/14 , C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： All possible stereoisomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein the substituents are as defined in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.
摘要翻译：式I化合物的所有可能的立体异构形式及其混合物，其中取代基如说明书中所定义，及其无毒的药学上可接受的具有抗生素性质的酸加成盐。

6. 发明授权

US5635485A Erythromycin compounds 失效
标题翻译：红霉素化合物
公开(公告)号：US5635485A
公开(公告)日：1997-06-03
申请号：US426067
申请日：1995-04-21
申请人： Constantin Agouridas , Jean-Francois Chantot , Alexis Denis , Solange G. D'Ambrieres , Odile L. Martret
发明人： Constantin Agouridas , Jean-Francois Chantot , Alexis Denis , Solange G. D'Ambrieres , Odile L. Martret
IPC分类号： C07D249/18 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07D209/08 , C07D215/02 , C07D215/12 , C07D217/14 , C07D233/61 , C07D233/64 , C07D235/08 , C07D257/04 , C07D277/64 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/00 , C07D473/04 , C07D495/04 , C07H17/00 , C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： An erythromycin compound of Formula I or its non-toxic acid addition salt having antibiotic activity.
摘要翻译：式I的红霉素化合物或其具有抗生素活性的无毒酸加成盐。

7. 发明授权

US6162793A Erythromycin derivatives, method for preparing same and use thereof as drugs 有权
标题翻译：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。

8. 发明授权

US6100404A Erythromycin compounds 失效
标题翻译：红霉素化合物
公开(公告)号：US6100404A
公开(公告)日：2000-08-08
申请号：US780861
申请日：1997-01-09
申请人： Constantin Agouridas , Jean-Francois Chantot , Alexis Denis , Solange Gouin D'Ambrieres , Odile Le Martret
发明人： Constantin Agouridas , Jean-Francois Chantot , Alexis Denis , Solange Gouin D'Ambrieres , Odile Le Martret
IPC分类号： C07D249/18 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07D209/08 , C07D215/02 , C07D215/12 , C07D217/14 , C07D233/61 , C07D233/64 , C07D235/08 , C07D257/04 , C07D277/64 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/00 , C07D473/04 , C07D495/04 , C07H17/00 , C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： Intermediates for the preparation of compounds selected from the group consisting of a compound of the formula ##STR1## wherein R is ##STR2## n is an integer from 3 to 5, Ar is an optionally substituted heterocyclic selected from the group consisting of
摘要翻译：用于制备选自下式化合物的化合物的中间体其中R为n为3至5的整数，Ar为任选取代的杂环基，其选自

9. 发明授权

US5614614A Eryhromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：US5614614A
公开(公告)日：1997-03-25
申请号：US391959
申请日：1995-02-21
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： Novel intermediates for the preparation of the compounds of Formula I wherein the substituents are as defined in the specification.
摘要翻译：用于制备式I化合物的新型中间体，其中取代基如说明书中所定义。

10. 发明授权

US5527780A Erythromycin derivatives 失效
标题翻译：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。

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