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公开(公告)号：US20060154878A1
公开(公告)日：2006-07-13
申请号：US10527940
申请日：2003-09-26
IPC分类号： A61K31/7048 , C07H17/08
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.
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公开(公告)号：US07358367B2
公开(公告)日：2008-04-15
申请号：US10527940
申请日：2003-09-26
IPC分类号： C07D498/08
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections
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公开(公告)号：US06593360B1
公开(公告)日：2003-07-15
申请号：US09959204
申请日：2002-01-22
IPC分类号： C07H1708
CPC分类号： C07H17/08
摘要： The invention relates to novel 15-membered 8a- and 9a-lactams from the class of 6-O-methyl-erythromycin A of general formula (I) their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for their preparation, to a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to their hydrates, to a process for the preparation of pharmaceutical compositions as well as to a use of pharmaceutical compositions for the treatment of bacterial infections.
摘要翻译： 本发明涉及由通式（I）的6-O-甲基 - 红霉素A类别的与无机或有机酸及其水合物的药学上可接受的加成盐与其中间体的新型15-元8a-和9-内酰胺， 制备，其制备方法，其与无机或有机酸的药学上可接受的加成盐，其水合物，制备药物组合物的方法以及药物组合物用于治疗细菌感染的用途。
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公开(公告)号：US06369035B1
公开(公告)日：2002-04-09
申请号：US09529642
申请日：2000-04-17
IPC分类号： A61K3170
摘要： The invention relates to novel compounds from the class of macrolide antibiotics. Particularly, the invention relates to novel 3,6-heiketals from the class of 9a-azalides, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.
摘要翻译： 本发明涉及来自大环内酯类抗生素类的新化合物。 特别地，本发明涉及来自9-氮杂类的新型3,6-尾环，其与无机或有机酸的药学上可接受的加成盐，其制备方法及其作为抗生素或作为其用途的中间体 合成其他大环内酯类抗生素。
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公开(公告)号：US5250518A
公开(公告)日：1993-10-05
申请号：US731781
申请日：1991-07-18
IPC分类号： C07H17/00 , A61K31/00 , A61K31/70 , A61K31/7042 , A61P31/04 , C07D413/14 , C07H17/02 , C07H17/08
CPC分类号： C07H17/08
摘要： The invention relates to O-methyl derivatives of azithromycin A of the formula (I) ##STR1## wherein Ia R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =CH.sub.3, R.sup.4 =R.sup.5 =HIb R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.4 =CH.sub.3, R.sup.5 =HIc R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.5 =H, R.sup.4 =C.sub.3Id R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3Ie R.sup.1 =R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.3 =CH.sub.3If R.sup.1 =R.sup.2 =R.sup.5 =H, R.sup.3 =R.sup.4 =CH.sub.3Ig R.sup.1 =R.sup.2 =R.sup.3 =R.sup.5 =H, R.sup.4 =CH.sub.3Ih R.sup.1 =R.sup.2 =H, R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3Ii R.sup.1 =R.sup.4 =R.sup.5 =H, R.sup.2 =R.sup.3 =CH.sub.3Ij R.sup.1 =R.sup.5 =H, R.sup.2 =R.sup.3 =R.sup.4 =CH.sub.3Ik R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =R.sup.4 =CH.sub.3Il R.sup.1 =H, R.sup.2 =R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to their use in the obtaining of antibacterial pharmaceutical preparations.
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公开(公告)号：US06573367B1
公开(公告)日：2003-06-03
申请号：US09869606
申请日：2001-07-02
IPC分类号： C07H100
摘要： The invention relates to novel compounds from the class of the macrolide antibiotic oleandomycin of the general formula (I) wherein R1 has the individual meaning of —CH2CH3 group, of a fragment of the formula (II), together with R2 has the meaning of a fragment of the formula (III) or together with R4 has the meaning of a fragment of the formula (IV) or a fragment of the formula (V) R2 together with R3 has the meaning of a ketone or together with R1 has the meaning of a fragment of the formula (III), R3 has the individual meaning of OH group or together with R2 has the meaning of a ketone, R4 has the individual meaning of a methyl group, or together with R1 has the meaning of a fragment of the formula (IV) or of a fragment of the formula (V), R5 has the individual meaning of hydrogen or a benzyloxycarbonyl group, R6 has the individual meaning of hydrogen, a methyl group or a benzyloxycarbonyl group, to intermediates for the preparation thereof, to a process for preparing them as well as to pharmaceutically acceptable addition salts thereof with inorganic or organic acids.
摘要翻译： 本发明涉及通式（I）的大环内酯类抗生素素多霉素类别的新化合物，其中R 1具有-CH 2 CH 3基团的单独含义，式（II）的片段，以及R2具有片段的含义 式（III）或与R4一起具有式（Ⅳ）的片段或式（Ⅴ）的片段的含义R 2与R 3一起具有酮的含义或与R 1一起具有以下含义： 式（III）的片段，R3具有OH基团的单独含义或与R2一起具有酮的含义，R4具有甲基的单独含义，或与R 1一起具有式 （Ⅳ）或式（Ⅴ）的片段，R5具有氢或苄氧基羰基的独立含义，R 6具有氢，甲基或苄氧基羰基的单个含义，用于制备其中间体， 一个准备它们以及pha的过程 其药学上可接受的加成盐与无机或有机酸。
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7.发明授权Compounds of the secomacrolide and secoazalide class and a process for the preparation thereof 失效噻氯匹定类和次氯酸盐类的化合物及其制备方法
公开(公告)号：US5721346A
公开(公告)日：1998-02-24
申请号：US611781
申请日：1996-03-07
IPC分类号： C07D407/12 , A61K31/351 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H15/04 , C07H15/26 , C07H17/04 , C07H17/08 , C07H1/00 , C07H17/00
摘要： The present invention refers to the new compounds of the secomacrolide and secoazalide class, a process for the preparation thereof as well as to new intermediates for the preparation of these seco derivatives.
摘要翻译： 本发明涉及新型的次氯酸和次氯酸类化合物，其制备方法以及用于制备这些衍生物的新中间体。
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公开(公告)号：US6110965A
公开(公告)日：2000-08-29
申请号：US127764
申请日：1998-07-31
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/35 , C07D267/00
CPC分类号： C07H17/08
摘要： The present invention relates to the new 15-membered ketoazalides from the class of 6-O-methyl-8a-aza-8a-homo-and 6-O-methyl-9a-aza-9a-homoerythromycin A with the general formula (I) ##STR1## wherein A represents NH group and B at the same time represents C.dbd.O group, orA represents C.dbd.O group and B at the same time represents NH group,R.sup.1 represents OH group, L-cladinosyl group of the formula (II) ##STR2## or together with R.sup.2 represents ketone, R.sup.2 represents hydrogen or together with R.sup.1 represents ketone,R.sup.3 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group,to intermediates and a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions, as well as to the use of pharmaceutical compositions for treating bacterial infections.
摘要翻译： 本发明涉及一种具有通式（I）的6-O-甲基-8a-氮杂-8a-均聚物和6-O-甲基-9a-氮杂-9a-高红霉素A的新的15-元酮马来酸盐 ）其中A表示NH基团，B同时表示C = O基团，或A表示C = O基团，B同时表示NH基团，R1表示OH基团，式（II）所示L-赖壁糖苷酶基团， 或与R2一起表示酮，R 2表示氢或R 1表示酮，R 3表示氢或C 1 -C 4烷酰基，其中间体及其制备方法，其与无机或有机酸的药学上可接受的加成盐与该方法 用于制备药物组合物，以及用于治疗细菌感染的药物组合物。
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公开(公告)号：US07262172B2
公开(公告)日：2007-08-28
申请号：US10399426
申请日：2001-10-19
申请人： Suleman Alihodzic , Andrea Berdik , Francesca Cardullo , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Zorica Marusic-Istuk , Stjepan Mutak , Alfonso Pozzan , Marko Derek
发明人： Suleman Alihodzic , Andrea Berdik , Francesca Cardullo , Antun Hutinec , Gorjana Lazarevski , Sergio Lociuro , Zorica Marusic-Istuk , Stjepan Mutak , Alfonso Pozzan , Marko Derek
摘要： The invention relates to novel semi-synthetic macrolides of formula (I) having antibacterial activity. More particularly this invention relates to derivatives of 8a-aza-8a-homoerythromycin A, to processes for their preparation, to compositions containing them and to their use in medicine
摘要翻译： 本发明涉及具有抗菌活性的式（I）的新型半合成大环内酯类。 更具体地说，本发明涉及8a-氮杂-8a-高红霉素A的衍生物，其制备方法，含有它们的组合物及其在医药中的用途
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10.发明授权
公开(公告)号：US6077944A
公开(公告)日：2000-06-20
申请号：US38901
申请日：1998-03-12
摘要： The invention relates to novel secomacrolides from the class of erythromycin A, potential intermediates for preparation of novel macrolide antibiotics general formula ##STR1## and its pharmaceuticaly acceptable addition salts with inorganic or organic acids, wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl group, arylcarbonyl group and together with R.sub.2 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.2 represents hydrogen or together with R.sub.1 and carbon atoms to which they are bound, cyclic carbonyl or thiocarbonyl group, R.sub.3 represents hydrogen, C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,Z is hydrogen or L-cladinosyl group represented by formula (i) ##STR2## wherein R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group, W is hydrogen or D-desosaminyl group represented by formula (ii) ##STR3## wherein R.sub.5 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl or arylcarbonyl group,X and Y together represent a lactone, or X is CH.sub.2 OR.sub.6, wherein R.sub.6 represents hydrogen or C.sub.1 -C.sub.4 alkanoyl group and Y is hydroxyl group.
摘要翻译： 本发明涉及来自红霉素A类的新型次氯氰菊酯，用于制备新型大环内酯类抗生素通用型的潜在中间体及其与无机或有机酸的药学上可接受的加成盐，其中R1表示氢，C1-C4烷酰基，芳基羰基和一起 R 2和它们所连接的碳原子，环状羰基或硫代羰基，R 2表示氢或与它们所连接的R 1和碳原子一起，环状羰基或硫代羰基，R 3表示氢，C 1 -C 4烷酰基或芳基羰基 Z为氢或由式（ⅰ）表示的L-克拉糖糖基，其中R 4表示氢或C 1 -C 4烷酰基，W为氢或式（ⅱ）表示的D-脱氨基甲酰基，其中R 5表示氢或C 1 -C 4烷酰基或 芳基羰基，X和Y一起表示内酯，或X是CH 2 OR 6，其中R 6表示氢或C 1 -C 4烷酰基，Y是羟基。
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