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21.再颁专利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：USRE38520E1
公开(公告)日：2004-05-18
申请号：US09838628
申请日：2001-04-19
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： A subject of the invention is the compounds of formula (I): in which: X represents a CH2 or SO2 radical or an oxygen atom, Y represents a (CH2)m—(CH═CH)n(CH2)o radical, with m+n+o≦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.
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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：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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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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公开(公告)号：US5108990A
公开(公告)日：1992-04-28
申请号：US396631
申请日：1989-08-21
IPC分类号： C07C237/22 , C07K5/06
CPC分类号： C07K5/06026 , C07C237/22
摘要： All isomeric forms and mixtures of isomers of glutamic acid compounds of the formula ##STR1## wherein the glutamic acid 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 or U and X together are .dbd.CH--CH.sub.2 --CH.sub.2 -- (E or Z isomer) and Y 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D-或L-构型的谷氨酸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酯化，其选自： 的C 6 -C 24任选不饱和脂肪酸的残基，R 5选自氢或1至5个碳原子的烷基，R 3选自羟基，1至5个碳原子的烷氧基 ，任选被1至5个碳原子的烷基取代的胺的氨基酸，Z是R 2选自氢，氨基酸和2至4个氨基酸的肽，R 4选自 由羟基，烷氧基组成的组 1至5个碳原子的氨基酸和任选地在胺上与1至5个碳原子的烷基取代的氨基酸，U选自由下列组成的组：-CH = CH-CH 2 - （E或Z异构体），-CH 2 -CH = CH-（E或Z异构体）和或者U和Y一起是= CH-CH 2 -CH 2 - （E或Z异构体），X是氢或U和X一起是= CH-CH 2 -CH 2 - （E或Z异构体），Y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。
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公开(公告)号：US5296501A
公开(公告)日：1994-03-22
申请号：US53464
申请日：1993-04-27
IPC分类号： C07C229/30 , C07C271/22 , C07F7/08 , A61K31/195 , A61K31/24 , C07C229/00
CPC分类号： C07C271/22 , C07C229/30 , C07F7/0818
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines indicate an optionally endo or exo double bond, Y is selected from the group consisting of alkyl, alkenyl and alkynyl of 2 to 18 carbon atoms and alkyl of 1 to 18 carbon atoms substituted with at least one halogen, X, X' and X.sub.1 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, acyl of a fatty acid and acyl of an .alpha. or .omega.-amino acid, n and/or n.sub.1 is 1 and R and/or R.sub.1 is the remainder of an amine or an .alpha. or .omega.-amino acid or n and/or n.sub.1 is 2 and R and R.sub.1 are selected from the group consisting of hydrogen, alkyl of 1 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 and their non-toxic, pharmaceutically acceptable salts with acids or bases having antibacterial properties.
摘要翻译： 选自下式的化合物的化合物其中虚线表示任选的内部或外部双键，Y选自2至18个碳原子的烷基，烯基和炔基，以及 被至少一个卤素取代的1至18个碳原子的烷基，X，X'和X 1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，7至18个碳原子的芳烷基，脂肪酸的酰基和α或ω-氨基酸的酰基，n和/或n1是1，R和/或R1是胺的剩余部分，或 α或ω-氨基酸或n和/或n1为2，R和R1选自氢，1至8个碳原子的烷基，6至14个碳原子的芳基，7至18个碳原子的芳烷基 原子和R 2是具有1至8个碳原子的烷基或6至14个碳原子的芳基及其无毒的药学上可接受的 与具有抗菌性能的酸或碱形成的盐。
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公开(公告)号：US5081135A
公开(公告)日：1992-01-14
申请号：US580213
申请日：1990-09-10
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 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选自氢和-COOR'，R'是氢或1至8个碳原子的烷基，Y选自氢， 1至8个碳原子的烷基和2至8个碳原子的烯基和炔基，全部任选被至少一个卤素或-OH取代，条件是如果Y是-OH，则X不是-NH-， 具有抗菌和免疫学特性的酸或碱的药学上可接受的加成盐。
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公开(公告)号：US4831043A
公开(公告)日：1989-05-16
申请号：US155303
申请日：1988-02-12
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61P1/04 , A61P1/08 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D211/26 , C07D401/04
CPC分类号： C07D401/04 , C07D211/26
摘要： Novel benzimidazol-2-ones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 5 carbon atoms with the multiple bond not between the carbons .alpha.- and .beta.- to the nitrogen and aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, --OH, alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic, antiulcerous, and antihypertensive and vasodilatatory activity.
摘要翻译： 式Ⅰ的新型苯并咪唑-2-酮其中R选自氢，1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，3至5个碳原子的链烯基和炔基， 选择不是碳原子的碳原子和碳原子之间的碳原子数为7〜12个碳原子的碳原子和碳原子数为1〜5的烷基和烷氧基中的至少一个成员所取代的碳原子和R1之间的多重键， 由氢，-OH，1至5个碳原子的烷氧基，7至9个碳原子的苯氧基和苯基烷氧基组成的组，以及它们具有多巴胺能，抗溃疡和抗高血压和血管扩张活性的无毒的药学上可接受的酸加成盐。
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