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1.再颁专利2-halogenated derivatives of 5-0 desosaminyl-erythronolide a, their preparation process and their antibiotic use 有权5-0脱氨基 - 赤藓酮苷a的2-卤代衍生物，其制备方法及其抗生素用途公开(公告)号：USRE39743E1
公开(公告)日：2007-07-24
申请号：US10302324
申请日：2002-11-21
IPC分类号： A61K31/55 , A61K31/42 , A61P31/04 , C07D243/00 , C07D498/00
CPC分类号： C07H17/08
摘要： Novel compounds of the formula wherein the substituents are defined as in the application having antibiotic properties.
摘要翻译： 新的下式化合物，其中取代基如本申请中所定义，具有抗生素性质。
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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
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。
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公开(公告)号：US5141952A
公开(公告)日：1992-08-25
申请号：US716950
申请日：1991-06-18
IPC分类号： A61K31/35 , A61K31/351 , A61K31/445 , A61K39/39 , A61P31/04 , A61P35/00 , A61P37/00 , A61P43/00 , C07D211/18 , C07D211/60 , C07D211/78 , C07D309/08 , C07D309/10 , C07D309/28
CPC分类号： C07D309/10 , C07D211/18 , C07D211/60
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of --OH, hydrogen, ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.
摘要翻译： 选自下式的化合物的化合物，其中虚线表示可能的内端或外双键，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至8个碳原子的烯基和炔基，6至14个碳原子的芳基，7至18个碳原子的芳烷基和1至8个碳原子的烷基或6至14个碳原子的芳基， X是-O-或-NR-，R选自-OH，氢，IMA和-COOR'，R'是氢或1至8个碳原子的烷基，Y选自 由氢，1至8个碳原子的烷基和2至8个碳原子的烯基和炔基组成，全部任选被至少一个卤素或-OH取代，条件是如果Y是-OH，X不是-NH- 及其无毒，药学上可接受的具有抗菌和免疫学特性的酸或碱的加成盐。
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公开(公告)号：US5747467A
公开(公告)日：1998-05-05
申请号：US767954
申请日：1996-12-19
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , A61P31/12 , A61P31/16 , C07H17/00 , C07H17/08
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
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公开(公告)号：US5439890A
公开(公告)日：1995-08-08
申请号：US340026
申请日：1994-11-14
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： A compound of the formula ##STR1## wherein A and B are both hydrogen or A is hydrogen and B is --OH or A and B form a carbon-carbon double bond and Z is hydrogen or acyl of an organic carboxylic acid of 1 to 6 carbon atoms and their nontoxic, pharmaceutically acceptable acid addition salts having antibiotic activity.
摘要翻译： 式Ⅰ化合物，其中A和B均为氢或A为氢，B为-OH或A和B形成碳 - 碳双键，Z为氢或有机羧酸的酰基为1〜 6个碳原子及其无毒的药学上可接受的具有抗生素活性的酸加成盐。
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公开(公告)号：US5089476A
公开(公告)日：1992-02-18
申请号：US161163
申请日：1988-02-26
IPC分类号： C07K1/113 , A61K31/195 , A61K31/22 , A61K38/00 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/22 , C07K5/02 , C07K5/06
CPC分类号： C07K5/06026
摘要： All isomeric forms and mixtures of isomers of glutamic acid compounds of the formula ##STR1## wherein the glutamic aid is of D- or L- configuration, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, an amino acid, a peptide of 2 to 4 amino acids and an amino acid or a peptide of 2 to 4 amino acids in which the amine is esterified with an optionally unsaturated aliphatic carboxylic acid of 6 to 24 carbon atoms or R.sub.1 is selected from the group consisting of a residue of a C.sub.6 -C.sub.24 optionally unsaturated aliphatic acid. R.sub.5 is selected from the group consisting of hydrogen or an alkyl radical of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydroxy, alkoxy of 1 to 5 carbon atoms, an amino acid with the amine optionally substituted with alkyl of 1 to 5 carbon atoms, Z is ##STR2## R.sub.2 is selected from the group consisting of hydrogen, an amino acid and a peptide of 2 to 4 amino acids, R.sub.4 is selected from the group consisting of hydroxy, alkoxy 1 to 5 carbon atoms and an amino acid optionally substituted on the amine with alkyl of 1 to 5 carbon atoms, U is selected from the group consisting of ##STR3## --CH.dbd.CH--CH.sub.2 -- (E or Z isomer), --CH.sub.2 --CH.dbd.CH-- (E or Z isomer) and ##STR4## or U and Y together are .dbd.CH--CH.sub.2 --CH.sub.2 -- (E or Z isomer) and X is hydrogen and their salts with non-toxic, pharmaceutically acceptable acid or bases having immunomodulatory properties.
摘要翻译： 式（I）的谷氨酸化合物的异构体的所有异构体形式和异构体的混合物，其中谷氨酸助剂为D-或L-构型，R1选自氢，1至5个碳原子的烷基， 氨基酸，2至4个氨基酸的肽和2至4个氨基酸的氨基酸或肽，其中胺与任选不饱和的6至24个碳原子的脂族羧酸或R1进行酯化，其选自 由C 6 -C 24任选不饱和脂族酸的残基组成。 R5选自氢或1至5个碳原子的烷基，R3选自羟基，1至5个碳原子的烷氧基，氨基酸与胺任选被1的烷基取代 至5个碳原子，Z为R 2选自氢，氨基酸和2至4个氨基酸的肽，R 4选自羟基，1至5个碳原子的烷氧基和 在胺上任选被1至5个碳原子的烷基取代的氨基酸，U选自
-CH = CH-CH 2 - （E或Z异构体），-CH 2 -CH = CH-（ E或Z异构体）和U和Y一起是= CH-CH 2 -CH 2 - （E或Z异构体），X是氢，它们与具有免疫调节特性的无毒，药学上可接受的酸或碱的盐。 -
公开(公告)号：US5030715A
公开(公告)日：1991-07-09
申请号：US267190
申请日：1988-11-03
IPC分类号： A61K38/00 , A61K31/195 , A61K31/22 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/04 , C07C67/00 , C07C227/00 , C07C227/04 , C07C227/16 , C07C227/18 , C07C227/20 , C07C229/24 , C07C229/30 , C07C231/00 , C07C237/12 , C07K1/02 , C07K1/08 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K14/52 , C07K14/525 , C07K14/54 , C07K14/545
CPC分类号： C07K1/08
摘要： A) Compounds selected from the group consisting of a compound of the formula ##STR1## wherein U is ##STR2## m and n are individually 1 or 2 of one, the dotted lines is a single double bond optionally of cis or trans configuration, a is selected from the group consisting of hydrogen, methyl and methylene, Y is selected from the group consisting of hydrogen, residue of an amino acid with an .alpha.-or .omega.-carboxyl and a peptide or 2,3 or 4 amino acids with the amine optionally acylated with an optionally unsaturated aliphatic carboxylic acid of 6 to 24 carbon atoms or alkylated with alkyl of 1 to 8 carbon atoms, R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon, alkenyl and alkynyl of 2 to 8 carbon atoms optionally substituted with at least one halogen with the proviso that if Y is hydrogen, alanine or proline and if a is hydrogen, U contains a double bond; and B) their non-toxic, pharmaceutically acceptable salts with bases or acids, the alkyl esters of 1 to 6 carbon atoms and their primary and secondary amides having remarkable immunomodulatric properties and anti-bacterial activity.
摘要翻译： A）选自下式的化合物的化合物其中U是m和n分别是1或2个，虚线是任选具有顺式或反式构型的单双键， a选自氢，甲基和亚甲基，Y选自氢，氨基酸与α或ω-羧基的残基和肽或2,3或4个氨基酸，其中 任选地用6至24个碳原子的任选不饱和的脂族羧酸酰化或用1-8个碳原子的烷基烷基化的胺，R选自氢，1至8个碳的烷基，烯基和炔基2至 8个碳原子，任选被至少一个卤素取代，条件是如果Y是氢，丙氨酸或脯氨酸，如果a是氢，则U含有双键; 和B）其与碱或酸的无毒的药学上可接受的盐，具有1-6个碳原子的烷基酯及其伯和仲酰胺具有显着的免疫组织学特性和抗细菌活性。
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8.发明申请2-Halogenated derivatives of 5-O-desosaminyl-erythronolide a, their preparation process and their antibiotic use 有权5-O-去酰氨基 - 赤藓酮苷a的2-卤代衍生物，其制备方法及其抗生素使用公开(公告)号：US20050065101A1
公开(公告)日：2005-03-24
申请号：US10987402
申请日：2004-11-12
IPC分类号： A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07H17/08 , A61K31/7052
CPC分类号： C07H17/08
摘要： A subject of the invention is a process for the preparation of the compounds of formula (I): Wherein the substituents are defined as in the application. The compounds of this invention exhibit antibiotic properties.
摘要翻译： 本发明的主题是制备式（I）化合物的方法：其中取代基如本申请中所定义。 本发明化合物具有抗生素特性。
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9.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：US6096714A
公开(公告)日：2000-08-01
申请号：US125959
申请日：1998-10-09
IPC分类号： A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/00 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： A subject of the invention is the compounds of formula (I): ##STR1## in which: X represents a CH.sub.2 or SO.sub.2 radical or an oxygen atom, Y represents a (CH.sub.2).sub.m --(CH.dbd.CH).sub.n (CH.sub.2).sub.o radical, with m+n+o.ltoreq.8, n=0 or 1, Ar represents an aryl radical,W represents a hydrogen atom, or the remainder of a carbamate function.The compounds of formula (I) have useful antibiotic properties.
摘要翻译： PCT No.PCT / FR97 / 00351 Sec。 371日期：1998年10月9日 102（e）日期1998年10月9日PCT 1997年2月27日PCT公布。 第WO97 / 31929号公报 日本公开日1997年9月4日本发明的目的是式（I）的化合物：其中：X表示CH 2或SO 2基或氧原子，Y表示（CH 2）m - （CH = CH）n ）o基团，其中m + n + o = 8，n = 0或1，Ar表示芳基，W表示氢原子或氨基甲酸酯官能团的其余部分。 式（I）化合物具有有用的抗生素性质。
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公开(公告)号：US5786339A
公开(公告)日：1998-07-28
申请号：US565252
申请日：1995-11-30
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
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。
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