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公开(公告)号：US4415562A
公开(公告)日：1983-11-15
申请号：US322901
申请日：1981-11-19
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D253/075 , C07D317/28 , C07D501/24
CPC分类号： C07D253/075 , C07D317/28
摘要： New cephalosporins of the general formula: ##STR1## in which R is alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic rings, R' is a hydrogen atom or a radical of the general formula: ##STR2## and R.degree. is hydrogen, alkyl, vinyl, cyanomethyl or a carboxyalkyl radical of the general formula: ##STR3## and also their salts, their preparation and the pharmaceutical compositions in which they are present.
摘要翻译： 新的头孢菌素，其通式如下：其中R是烷基，L-2-氨基-2-羧乙基，苯基或各种杂环，R'是氢原子或通式如下的基团： 图像（II）和R DEG是通式为（III）的氢，烷基，乙烯基，氰基甲基或羧基烷基，以及它们的盐，它们的制备方法及其存在的药物组合物。
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公开(公告)号：US4503220A
公开(公告)日：1985-03-05
申请号：US408674
申请日：1982-08-16
IPC分类号： C07D501/18 , C07F9/6561 , C07D501/14 , A61K31/545
CPC分类号： C07F9/65613
摘要： 3-Vinylcephalosporin derivatives of the formula: ##STR1## in which the symbols R.sub.1 are phenyl radicals or radicals --OZ.sub.1 (it being possible for Z.sub.1 to be alkyl, 2,2,2-trichloroethyl or optionally substituted phenyl or benzyl, or for the radicals Z.sub.1 to form an alkylene radical), R.sub.2 is a radical which can be removed by an enzymatic method, or a protecting radical, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or together form a saturated 5-membered or 6-membered heterocyclic ring optionally containing another hetero-atom, are new, crystallizable intermediates useful for the preparation of anti-bacterial cephalosporins.
摘要翻译： 其中符号R1是苯基或基团-OZ1（Z1可以是烷基，2,2,2-三氯乙基或任选取代的苯基或苄基）的下式的3-乙烯基头孢菌素衍生物： 或基团Z 1形成亚烷基），R 2为可通过酶法或保护基除去的基团，且R 3和R 4为任选取代的烷基或苯基，或一起形成饱和的5元环 或任选含有另一个杂原子的6元杂环是可用于制备抗菌头孢菌素的新的可结晶中间体。
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公开(公告)号：US4370478A
公开(公告)日：1983-01-25
申请号：US323112
申请日：1981-11-19
IPC分类号： A61K31/535 , A61P31/04 , C07D501/24 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00
摘要： New oxacephalosporins of the general formula: ##STR1## in which either R.sub.1 is hydrogen or a protective radical, R.sub.4 is hydrogen or substituted 2-(2-aminothiazol-4-yl)-acetyl or .alpha.-carboxyarylacetyl, of which the amine and acid groups are free or protected, and R" is hydrogen or methoxy in the 7.alpha.-position, or R.sub.1 is a protective radical, R.sub.4 is a radical which can easily be removed and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.2 is a radical --O SO.sub.2 --R.sub.3 or --O CO--R'.sub.3 (R.sub.3 and R'.sub.3 being substituted or unsubstituted alkyl radicals, or phenyl radicals) or a halogen atom, are useful as intermediates for the preparation of antimicrobial oxacephalosporins.
摘要翻译： 新的通式为：其中R 1为氢或保护基的式（Ⅰ）的化合物，R4为氢或取代的2-（2-氨基噻唑-4-基） - 乙酰基或α-羧基芳基乙酰基，其中 胺和酸基是游离的或被保护的，并且R“在7α-位中是氢或甲氧基，或者R1是保护基，R4是可以容易地除去的基团，R”是氢或甲氧基， 7个α位或7位β-中的氢，R2是-O-SO 2 -R 3或-OCO-R'3（R3和R'3是取代或未取代的烷基或苯基）或 卤素原子，可用作制备抗微生物头孢菌素的中间体。
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公开(公告)号：US4369314A
公开(公告)日：1983-01-18
申请号：US322951
申请日：1981-11-19
IPC分类号： A61K31/535 , A61P31/04 , C07D501/24 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00
摘要： New oxacephalosporin derivative of the general formula: ##STR1## in which R.sub.1 is a protective radical, R.sub.2 is either a radical of the general formula: ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an .alpha.-carboxyarylacetyl radical and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively R.sub.2 is a protective radical and R" is either hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, and R.sub.3 and R.sub.4 are optionally substituted alkyl, or phenyl, or form a heterocyclic ring with the nitrogen atom, their E and Z forms and mixtures thereof and also their preparation.These new products are useful as intermediates for the preparation of biologically active oxacephalosporins.
摘要翻译： （I）其中R1是保护基团的新的类似于以下通式的式（II）的新的类鞘氨醇衍生物：R2是以下通式的基团：其中R 5是氢，烷基，乙烯基，保护基 羧基烷基或保护基，R 6为保护基]或α-羧基芳基乙酰基，R“为7位上的氢或甲氧基，或者R2为保护基，R”为氢或甲氧基 7个β-位中的7个α-位或氢，R3和R4是任选取代的烷基或苯基，或与氮原子，它们的E和Z形式及其混合物形成杂环，以及它们的制备。 这些新产品可用作制备生物活性的羟基头孢菌素的中间体。
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公开(公告)号：US4415735A
公开(公告)日：1983-11-15
申请号：US322963
申请日：1981-11-19
IPC分类号： C07D501/14 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60
CPC分类号： C07D501/24
摘要： The invention provides new cephalosporins of the general formula: ##STR1## in which n=0 or 1, R.sub.4 is an amine-protecting radical, R.sup.a.sub.5 and R.sup.b.sub.5, which are identical or different, are hydrogen atoms or alkyl radicals, or form an alkylene radical of 2 or 3 carbon atoms, R.sup.c.sub.5 is a hydrogen atom or an acid-protecting radical and R.sub.2 is an acid-protecting radical or a radical which can easily be removed by an enzymatic method. The compounds of formula (I) are in the form of a 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane if n=0, and in the form of a 3-oxoethylbicyclooct-2-ene or a 3-oxoethylidenebicyclooctane if n=1. They are useful as intermediates for the preparation of pharmaceutically active cephalosporins.
摘要翻译： 本发明提供了新的头孢菌素，其通式如下：其中n = 0或1，R4是胺保护基，Ra5和Rb5相同或不同，为氢原子或烷基，或 形成2或3个碳原子的亚烷基，Rc5是氢原子或酸保护基，R2是酸保护基或可以通过酶法容易地除去的基团。 如果n = 0，式（I）化合物是3-氧代乙基 - 双环辛烯-2-烯或二环辛烯-3-烯或3-氧代亚乙基双环辛烷的形式，并且为3-氧代乙基双环辛-2 如果n = 1，则为3-烯亚乙基双环辛烷。 它们可用作制备药学活性头孢菌素的中间体。
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公开(公告)号：US4399135A
公开(公告)日：1983-08-16
申请号：US322962
申请日：1981-11-19
IPC分类号： A61K31/535 , A61P31/04 , C07D501/24 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00
摘要： New oxacephalosporins of the general formula (I), in which R is optionally N-oxidised pyridyl, pyrimidin-2-yl, substituted pyridazin-3-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 4-position, substituted 1-alkyl-1,3,4-triazol-5-yl or 1,2,4-triazol-5-yl, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 1-position, 5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl substituted in the 2-position, substituted or unsubstituted 2-alkyl-2,5-dihydro-5-oxo-1,2,4-triazin-3-yl, 1-amino-1,2-dihydro-2-oxo-pyrimidin-4-yl, substituted 1,3,4-thiadiazol-5-yl or tetrazol-5-yl substituted in the 1-position, R' is a substituted 2-(2-aminothiazol-4-yl)-acetyl radical or an .alpha.-carboxyarylacetyl radical and R" is a hydrogen atom or a methoxy radical in the 7.alpha.-position, and also their salts, their preparation and the medicaments in which they are present. ##STR1##
摘要翻译： 通式（I）的新型硫代氨基甲酸酯，其中R为任选的N-氧化吡啶基，嘧啶-2-基，取代的哒嗪-3-基，5,6-二氧代-1,4,5,6-四氢-1 在4-取代的1-烷基-1,3,4-三唑-5-基或1,2,4-三唑-5-基中取代的2,4-三嗪-3-基， 在1-位上取代的二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，5,6-二氧代-1,4,5,6-四氢-1,2， 2-取代或未取代的2-烷基-2,5-二氢-5-氧代-1,2,4-三嗪-3-基，1-氨基-1,2 - 二氢-2-氧代 - 嘧啶-4-基，在1-位取代的取代的1,3,4-噻二唑-5-基或四唑-5-基是取代的2-（2-氨基噻唑-5-基） 4-基） - 乙酰基或α-羧基芳基乙酰基，R“是7α-位中的氢原子或甲氧基，以及它们的盐，它们的制备方法及其存在的药物。 （一）
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公开(公告)号：US4385181A
公开(公告)日：1983-05-24
申请号：US233109
申请日：1981-02-10
IPC分类号： C07D253/075 , C07D277/22 , C07D277/38 , C07D501/24 , C07D277/46 , C07D417/12 , C07D487/04
CPC分类号： C07D253/075 , C07D501/24
摘要： New thioloesters of the formula: ##STR1## wherein R.degree. represents hydrogen, alkyl, vinyl, cyanomethyl or a protecting radical, R' represents hydrogen or a protecting radical, R represents alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic radicals, and their syn and anti isomers and mixtures thereof, and metal salts thereof and addition salts thereof with tertiary nitrogen-containing bases, are intermediates useful in the preparation of cephalosporins having anti-bacterial properties.
摘要翻译： 新的硫代酯，其结构式如下：其中R DEG表示氢，烷基，乙烯基，氰基甲基或保护基，R'表示氢或保护基，R表示烷基，L-2-氨基-2-羧乙基，苯基或 各种杂环基以及它们的顺式和反式异构体及其混合物及其金属盐及其与叔氮基的加成盐是可用于制备具有抗细菌特性的头孢菌素的中间体。
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公开(公告)号：US4423214A
公开(公告)日：1983-12-27
申请号：US322949
申请日：1981-11-19
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24 , C07D501/60
CPC分类号： C07D501/24
摘要： New 3-vinylcephalosporin derivatives of the general formula: ##STR1## in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R.sub.5.sup.a and R.sub.5.sup.b are hydrogen atoms or alkyl radicals, or together form an alkyl radical containing 2 or 3 carbon atoms, R.sub.5.sup.c is an acid-protecting radical, R.sub.1 is an amino-protecting radical, R.sub.2 is an acid-protecting radical or a radical which can be removed by an enzymatic method, and R.sub.3 and R.sub.4, which are identical or different, represent alkyl (optionally substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino) or phenyl, or together form, with the nitrogen atom, a saturated heterocyclic ring of 5 or 6 members, optionally containing another hetero-atom, their E and Z forms, and their syn and anti forms, and mixtures thereof, and also their preparation. These new compounds are useful as intermediates for the preparation of biologically active cephalosporins.
摘要翻译： 新的3-乙烯基头孢菌素衍生物，其通式为：双环-2-烯或双环-3-烯的形式，其中式R5a和R5b为氢原子或烷基，或 一起形成含有2或3个碳原子的烷基，R5c是酸保护基，R1是氨基保护基，R2是可以通过酶法除去的酸保护基或基团，R3和 R 4相同或不同，表示烷基（任选被羟基，烷氧基，氨基，烷基氨基或二烷基氨基）或苯基取代，或与氮原子一起形成5或6个成员的饱和杂环，任选地含有另外的杂原子 原子，它们的E和Z形式，以及它们的顺式和反型形式及其混合物，以及它们的制备方法。 这些新化合物可用作制备生物活性头孢菌素的中间体。
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公开(公告)号：US4622393A
公开(公告)日：1986-11-11
申请号：US610175
申请日：1984-05-14
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D253/07 , C07D501/24
CPC分类号： C07D253/065 , C07D253/07
摘要： New 3-vinylcephalosporins of the general formula (I), ##STR1## in which n=0 or 1, R.sub.1 is a radical of the general formula (II), ##STR2## in which R.sub.4 is hydrogen or a protective radical and R.sub.5 represents a radical of the general formula (IIa) ##STR3## in which R.sup.a.sub.5 and R.sup.b.sub.5 are hydrogen or alkyl or together form an alkylene radical and R.sup.c.sub.5 is hydrogen or a protective radical, R.sub.2 is hydrogen, a protective radical or a radical which can easily be removed by an enzymatic method, and R.sub.3 is a halogen atom or a radical R'.sub.3 SO.sub.2 O-- or R".sub.3 CO--O--, in which radicals R'.sub.3 and R".sub.3 are substituted or unsubstituted alkyl or phenyl radicals, or alternatively R.sub.1 is a hydrogen atom or a radical of the general formula (II) in which R.sub.4 is defined as above and R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl or a protective radical, and R.sub.2 is defined as above, or R.sub.1 is hydrogen or a variously substituted acyl radical and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a halogen atom.These new products are useful as intermediates for the preparation of antibiotic cephalosporins.
摘要翻译： 通式（I）的新的3-乙酰头孢菌素，其中n = 0或1的其中R 1是通式（II）的基团，其中R 4是氢或 保护基，R 5表示通式（IIa）（IIa）的基团，其中Ra5和Rb5为氢或烷基或一起形成亚烷基，Rc5为氢或保护基，R2为氢， 保护基或可以通过酶法容易地除去的基团，R3是卤素原子或基团R'3SO2O-或R'3CO-O-，其中基团R'3和R'3被取代 或未取代的烷基或苯基，或者R 1是氢原子或通式（II）的基团，其中R 4如上定义，R 5是氢，烷基，乙烯基，氰基甲基或保护基，并且R 2被定义 如上所述，或R 1为氢或各种取代的酰基，R 2为氢或保护基，R 3为卤素原子。 这些新产品可用作制备抗生素头孢菌素的中间体。
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10.发明授权
公开(公告)号：US4496560A
公开(公告)日：1985-01-29
申请号：US408676
申请日：1982-08-16
IPC分类号： A61K31/535 , A61P31/04 , C07D501/20 , C07D501/24 , C07D505/00 , A61K31/545
CPC分类号： C07D505/00
摘要： New cephalosporin derivatives, of the formula: ##STR1## in which R.sub.1 is a heterocyclic, phenyl, p-hydroxyphenyl, phenoxy or dichlorophenylthio radical and R.sub.2 is a hydrogen atom, or R.sub.1 is phenyl or p-hydroxyphenyl and R.sub.2 is an amino radical, R.sub.3 is hydrogen, phenyl, substituted phenyl, alkylthio or substituted amino or a radical of the structure --A--R'.sub.3, which A is --CH.sub.2 --, --NH-- or --NHCO-- and R'.sub.3 is a substituted pyridinio radical, R is a carboxyl radical or a carboxylato radical if R.sub.3 is a --AR'.sub.3 radical and X is a sulphur or oxygen atom, the said alkyl moieties or radicals containing 1 to 4 carbon atoms each in their D, L and D,L forms, where these exist, and their salts are narrow-spectrum anti-bacterial agents which are active against gram-positive bacteria.
摘要翻译： 新的头孢菌素衍生物，其结构式如下：其中R1是杂环，苯基，对羟基苯基，苯氧基或二氯苯硫基，R2是氢原子，或R1是苯基或对羟基苯基，R2是 氨基，R3是氢，苯基，取代的苯基，烷硫基或取代的氨基或结构-A-R'3的基团，其中A是-CH 2 - ， - NH-或-NHCO-，R'3是取代的 吡啶基，R为羧基或羧基，如果R3为-AR'3基，X为硫或氧原子，则所述烷基部分或含有1至4个碳原子的基团各自为D，L和D L形式，其中存在这些盐，其盐是对革兰氏阳性细菌具有活性的窄谱抗菌剂。
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