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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：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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5.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：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：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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9.发明授权.beta.,.beta.-distributed derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A 失效9-脱氧-9a-N-乙烯基-9a-氮杂-9a-高红霉素A的β，β分布衍生物
公开(公告)号：US6071886A
公开(公告)日：2000-06-06
申请号：US223978
申请日：1998-12-31
申请人： Nedjeljko Kujundzic , Dina Pavlovic , Gabrijela Kobrehel , Gorjana Lazarevski , Zeljko Kelneric
发明人： Nedjeljko Kujundzic , Dina Pavlovic , Gabrijela Kobrehel , Gorjana Lazarevski , Zeljko Kelneric
IPC分类号： C07H17/00 , A61K31/00 , A61K31/04 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61P31/00 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to .beta.,.beta.-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are mutually the same or different and represent nitrile, carboxy group of the formula COOR.sup.3, wherein R.sup.3 represents C.sub.1 -C.sub.4 alkyl group, or keto group of the formula COR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for the preparation thereof, to a process for the preparation of pharmaceutical compositions, as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.
摘要翻译： 本发明涉及9-脱氧-9a-N-乙烯基-9a-氮杂-9a-高红霉素A的β，β-二取代衍生物，通式（I）的大环内酯类的新的半合成抗生素，其中R1和R2相互 表示腈，式COOR 3的羧基，其中R 3表示C 1 -C 4烷基，或式COR 4的酮基（其中R 4表示C 1 -C 4烷基）与其药学上可接受的加成盐与无机或 有机酸，其制备方法，制备药物组合物的方法，以及所用药物组合物在细菌感染治疗中的用途。
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10.发明授权9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin a 9a,11-cyclic carbamates 失效9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素a 9a,11-环状氨基甲酸酯
公开(公告)号：US5434140A
公开(公告)日：1995-07-18
申请号：US178559
申请日：1994-01-07
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61P31/04 , C07H17/00 , C07H17/08
摘要： The invention relates to 9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin A 9a,11-cyclic carbamates, novel semisynthetic macrolide antibiotics from the genus of azalides, of the formula (I) ##STR1## whereinR.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3, (IA)R.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.CH.sub.3, R.sup.4 .dbd.H, (IB)R.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.R.sup.4 .dbd.H, (IC)R.sup.1 .dbd.R.sup.2 .dbd.H, R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3,(ID)R.sup.1 .dbd.R.sup.2 .dbd.R.sup.4 .dbd.H, R.sup.3 .dbd.CH.sub.3,(IE)R.sup.1 .dbd.R.sup.2 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.H, (IF)R.sup.1 .dbd.H, R.sup.2 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3,(IG)R.sup.1 .dbd.R.sup.4 .dbd.H, R.sup.2 .dbd.R.sup.3 .dbd.CH.sub.3,(IH)R.sup.1 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.H, R.sup.2 .dbd.CH.sub.3,(IJ)to pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to intermediates and to processes for the preparation thereof, to a process for preparing pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in treatment of bacterial infections.
摘要翻译： 本发明涉及9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素A 9a,11-环状氨基甲酸酯，由式（I）的化合物制备的新的半合成大环内酯类抗生素，其中R1 = R2 = CO 2 CH 2 C 6 H 5，R 3 = R 4 = CH 3，（IA）R 1 = R 2 = CO 2 CH 2 C 6 H 5，R 3 = CH 3，R 4 = H，（IB）R 1 = R 2 = CO 2 CH 2 C 6 H 5， R3 = R4 = CH3，（ID）R1 = R2 = R4 = H，R3 = CH3，（IE）R1 = R2 = R3 = R4 = H，（IF）R1 = H，R2 = R3 = R4 = CH3，（ IG）R1 = R4 = H，R2 = R3 = CH3，（1H）R1 = R3 = R4 = H，R2 = CH3，（IJ）与其与无机或有机酸的药学上可接受的加成盐， 制备药物组合物的方法以及所获得的药物组合物在细菌感染治疗中的用途。
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