-
公开(公告)号:US4382084A
公开(公告)日:1983-05-03
申请号:US129188
申请日:1980-03-10
IPC分类号: C07D503/06 , A61K31/42 , A61K31/424 , A61K31/43 , A61K31/545 , A61P31/04 , C07D503/00 , C07D503/22 , A61K35/00
CPC分类号: A61K31/545 , A61K31/43 , C07D503/00
摘要: The compounds of the formula (II): ##STR1## and salts and esters theereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.
摘要翻译: 式(II)的化合物:其中R 1为至多14个碳原子的惰性有机基团,R 2为至多16个碳原子的惰性有机基团,其中R 1为NR 1 R 2 含有多达22个碳原子的抗菌剂是能够增强青霉素和头孢菌素对某些β-内酰胺酶生产菌的有效性的抗菌剂。
-
公开(公告)号:US4297345A
公开(公告)日:1981-10-27
申请号:US87030
申请日:1979-10-22
申请人: Thomas T. Howarth
发明人: Thomas T. Howarth
IPC分类号: A61K31/43 , A61K31/545 , C07D503/00 , A61K35/00
CPC分类号: A61K31/545 , A61K31/43 , C07D503/00
摘要: The compounds of the formula: ##STR1## and salts and esters thereof are useful agents for the treatment of bacterial infections either alone or in combination with a penicillin or cephalosporin derivative. The preceding compounds may be prepared by the hydrogenation of a compound of the formula: ##STR2## wherein R is a hydrogen atom or an acyl group or a salt or ester thereof.
摘要翻译: 下式的化合物及其盐和酯是单独或与青霉素或头孢菌素衍生物组合治疗细菌感染的有用试剂。 前述化合物可以通过下式化合物氢化制备:其中R是氢原子或酰基或其盐或酯。
-
公开(公告)号:US4256638A
公开(公告)日:1981-03-17
申请号:US942156
申请日:1978-09-14
IPC分类号: C07D503/06 , A61K31/42 , A61K31/424 , A61K31/43 , A61K31/545 , A61P31/04 , C07D503/00 , C07D503/22 , C07D498/04 , C07B29/00
CPC分类号: A61K31/545 , A61K31/43 , C07D503/00
摘要: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.
摘要翻译: 式(II)化合物:其中R 1为至多14个碳原子的惰性有机基团,R 2为至多16个碳原子的惰性有机基团,NR1R2基团 含有多达22个碳原子的抗菌剂是能够增强青霉素和头孢菌素对某些β-内酰胺酶生产菌的有效性的抗菌剂。
-
公开(公告)号:US4232005A
公开(公告)日:1980-11-04
申请号:US857112
申请日:1977-12-05
申请人: Thomas T. Howarth
发明人: Thomas T. Howarth
IPC分类号: A61K31/43 , A61K31/545 , C07D503/00
CPC分类号: A61K31/545 , A61K31/43 , C07D503/00
摘要: The compounds of the formula: ##STR1## and salts and esters thereof are useful agents for the treatment of bacterial infections either alone or in combination with a penicillin or cephalosporin derivative.The preceding compounds may be prepared by the hydrogenation of a compound of the formula: ##STR2## wherein R is a hydrogen atom or an acyl group or a salt or ester thereof.
-
公开(公告)号:US4138403A
公开(公告)日:1979-02-06
申请号:US708343
申请日:1976-07-26
IPC分类号: A61K31/42 , A61P31/04 , C07D205/08 , C07D205/09 , C07D263/16 , C07D503/00 , C07F7/18 , C07D498/04
CPC分类号: C07D263/16 , C07D205/08 , C07D205/09 , C07D503/00 , C07F7/1852
摘要: Compounds of the formula ##STR1## and salts and esters thereof wherein R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, phenyl, alkenyl of 2 to 4 carbon atoms, alkynyl of 2 to 4 carbon atoms, acyl of 1 to 4 carbon atoms, a carboxylic acid group or ester thereof of 1 to 7 carbon atoms, or alkyl of 1 to 4 carbon atoms substituted by 1 or 2 halogen atoms, hydroxyl, substituted hydroxyl, amino, protected amino, substituted thio of 1 to 7 carbon atoms, substituted sulphinyl of 1 to 7 carbon atoms, substituted sulphonyl of 1 to 7 carbon atoms, or by a carboxylic acid group or ester thereof of 1 to 7 carbon atoms;R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms, or is joined to R.sub.1 to form a cycloalkyl group of 3 to 6 carbon atoms;R.sub.3 is hydrogen, chlorine or bromine; andR.sub.4 is hydrogen, halogen, azido or amino; provided that when R.sub.4 is azido, R.sub.3 is hydrogen and R.sub.1 is methyl,R.sub.2 is not methyl, and that when R.sub.2 R.sub.3 and R.sub.4 are hydrogen andR.sub.1 is hydroxyethyl or an acyl derivative thereof, the compound does not have the (2R, 3S, 5R) stereochemistry; inhibit certain .beta.-lactamate enzymes and are useful in antiseptic and disinfectant solutions.
摘要翻译: 式(I)的化合物及其盐和酯,其中R 1是氢,1至4个碳原子的烷基,苯基,2至4个碳原子的烯基,2至4个碳原子的炔基,1至 4个碳原子,1至7个碳原子的羧酸基团或其酯,或被1或2个卤素原子取代的1至4个碳原子的烷基,羟基,取代的羟基,氨基,保护的氨基,取代的硫代1至7个 碳原子,1至7个碳原子的取代亚磺酰基,1至7个碳原子的取代磺酰基,或其1至7个碳原子的羧酸基或其酯; R2是氢或1〜4个碳原子的烷基,或者与R1连接,形成3〜6个碳原子的环烷基; R3是氢,氯或溴; R4是氢,卤素,叠氮基或氨基; 条件是当R 4是叠氮基时,R 3是氢,R 1是甲基,R 2不是甲基,当R 2 + L,R 3和R 4是氢并且R 1是羟乙基或其酰基衍生物时,该化合物不具有 ,3S,5R)立体化学; 抑制某些β-乳酸酶,并且可用于消毒和消毒溶液。
-
公开(公告)号:US4609495A
公开(公告)日:1986-09-02
申请号:US278564
申请日:1981-06-29
IPC分类号: A61K31/42 , A61K31/43 , A61K31/545 , C07D503/00 , C07D498/04
CPC分类号: A61K31/42 , A61K31/43 , A61K31/545 , C07D503/00
摘要: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert organic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.
摘要翻译: 式(II)的化合物:其中R是具有至多18个碳原子的惰性有机基团并能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此,当将式(II)化合物或其盐或酯与青霉素或头孢菌素一起使用时,可以显着提高该青霉素或头孢菌素的有效性。 这些新型协同增效剂可以通过使用克拉维酸的酯化来制备,如果需要,通过酯化作用。 新型增效剂也具有抗菌活性。
-
公开(公告)号:US4556559A
公开(公告)日:1985-12-03
申请号:US924174
申请日:1978-07-13
IPC分类号: A61K31/42 , A61K31/43 , A61P31/04 , C07D503/00 , C12N9/99 , C12P1/06 , C12P17/18 , C12P37/04 , A61K35/00
CPC分类号: C12P17/188 , A61K31/42 , A61K31/43 , C07D503/00
摘要: A new antibacterially active agent has been isolated from Streptomyces clvuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.
摘要翻译: 已经从Streptomyces clvuligerus中分离出新的抗菌活性剂。 这种被称为克拉维酸的新化合物具有式(I):(I)除了是广谱抗生素的中等效力之外,克拉维酸及其盐和酯还具有增强β - 针对许多β-内酰胺酶生产细菌的内酰胺抗生素。
-
公开(公告)号:US4548815A
公开(公告)日:1985-10-22
申请号:US538767
申请日:1983-10-03
IPC分类号: A61K31/42 , A61K31/43 , A61K31/545 , C07D503/00 , A61K35/00
CPC分类号: A61K31/42 , A61K31/43 , A61K31/545 , C07D503/00
摘要: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert ogranic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.
摘要翻译: 式(II)的化合物:其中R是具有至多18个碳原子的惰性极性基团并且能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此,当将式(II)化合物或其盐或酯与青霉素或头孢菌素一起使用时,可以显着提高该青霉素或头孢菌素的有效性。 这些新型协同增效剂可以通过使用克拉维酸的酯化来制备,如果需要,通过酯化作用。 新型增效剂也具有抗菌活性。
-
公开(公告)号:US4525352A
公开(公告)日:1985-06-25
申请号:US327253
申请日:1981-12-03
IPC分类号: A61K31/42 , A61K31/43 , A61P31/04 , C07D503/00 , C12N9/99 , C12P1/06 , C12P17/18 , C12P37/04 , A61K35/00
CPC分类号: C12P17/188 , A61K31/42 , A61K31/43 , C07D503/00
摘要: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta. lactam antibotics against many .beta.-lactamase producing bacteria.
摘要翻译: 已经从Streptomyces clavuligerus中分离出一种新的抗菌活性剂。 这种被称为克拉维酸的新化合物具有式(I):其中除了是广谱抗生素的中等效力外,克拉维酸及其盐和酯还具有提高β-内酰胺的有效性的能力 针对许多β-内酰胺酶生产细菌的抗生素。
-
公开(公告)号:US4427690A
公开(公告)日:1984-01-24
申请号:US726224
申请日:1976-09-24
IPC分类号: A61K31/42 , A61K31/43 , A61P31/04 , C07D503/00 , C12N9/99 , C12P1/06 , C12P17/18 , C12P37/04 , C07D498/04
CPC分类号: C12P17/188 , A61K31/42 , A61K31/43 , C07D503/00
摘要: A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): ##STR1## In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria.
摘要翻译: 已经从Streptomyces clavuligerus中分离出一种新的抗菌活性剂。 这种被称为克拉维酸的新化合物具有式(I):(I)除了是广谱抗生素的中等效力之外,克拉维酸及其盐和酯还具有增强β - 针对许多β-内酰胺酶生产细菌的内酰胺抗生素。
-
-
-
-
-
-
-
-
-