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1.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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公开(公告)号：US4526962A
公开(公告)日：1985-07-02
申请号：US408712
申请日：1982-08-16
IPC分类号： A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/24 , C07D505/00
CPC分类号： C07D505/00
摘要： New cephalosporin derivatives of the formula: ##STR1## in which R' represents a protected carboxyl radical, Hal represents a halogen atom, X.sub.1 represents a sulphur or oxygen atom or a sulphinyl radical and R represents an acyl radical or an amine-protecting radical, are useful as intermediates for the preparation of cephalosporins having antibacterial activity.
摘要翻译： 下式的新型头孢菌素衍生物：其中R'表示被保护的羧基，Hal表示卤素原子，X1表示硫或氧原子或亚磺酰基，R表示酰基或胺 - 保护基，可用作制备具有抗菌活性的头孢菌素的中间体。
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公开(公告)号：US4554350A
公开(公告)日：1985-11-19
申请号：US522261
申请日：1983-08-11
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24
CPC分类号： C07D501/24
摘要： New cephalosporin derivatives of the formula: ##STR1## in which R is an amino-protecting radical, R' is a protected carboxyl radical, Hal is a halogen atom, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or R.sub.a is a protected carboxyl radical and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms, or C.sub.1 -C.sub.4 alkyl radicals, or together form a C.sub.2 -C.sub.5 alkylene radical, and n=0 or 1, their isomeric forms and mixtures thereof, are useful for the preparation of cephalosporins which have antibacterial properties.
摘要翻译： 下式的新型头孢菌素衍生物：其中R为氨基保护基，R'为被保护的羧基，Hal为卤素原子，Ra，Rb和Rc为氢原子，或Ra为被保护的羧基 和相同或不同的R b和R c是氢原子或C 1 -C 4烷基，或一起形成C 2 -C 5亚烷基，n = 0或1，它们的异构形式及其混合物可用于 制备具有抗菌性能的头孢菌素。
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公开(公告)号：US4369315A
公开(公告)日：1983-01-18
申请号：US323113
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 R.sub.1 is a protective radical and (a) R.sub.4 is a substituted 2-(2-aminothiazol-4-yl)-acetyl radical of which the amine group is protected, or an .alpha.-carboxyarylacetyl radical, and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively(b) R.sub.4 is a protective radical and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, in the form of a bicyclooct-2-ene or bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane, are useful as intermediates for the preparation of pharmaceutically active oxacephalosporins.
摘要翻译： 其中R 1为保护基的通式为（IMA）（Ⅰ）的新型硫代吗啡，（a）R4为被保护的胺基的取代的2-（2-氨基噻唑-4-基） - 乙酰基，或 一个α-羧基芳基乙酰基，R“是7个α-位的氢或甲氧基，或者（b）R4是保护基，R”是7位中的氢或甲氧基或7位中的氢 以双环-2-烯或双环辛烯-3-烯或3-氧代亚乙基双环辛烷的形式的β-位可用作制备药学活性的硫氰酸头孢菌素的中间体。
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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：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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8.发明授权Cephalosporin derivatives, their preparation and compositions containing them 失效头孢菌素衍生物，它们的制备和含有它们的组合物
公开(公告)号：US4508717A
公开(公告)日：1985-04-02
申请号：US522359
申请日：1983-08-11
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/24 , C07D501/36
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.
摘要翻译： 下式的头孢菌素衍生物：其中A是单键或者连接到吡啶基的3-位或4-位的基团-CH 2 - ， - NH-或-NHCO-，R 是甲基，羧甲基，氨基甲酰基甲基，苄基或烯丙基，Ra，Rb和Rc是氢原子，或者Ra是羧基，Rb和Rc相同或不同，是氢原子或烷基，或一起形成亚烷基 自由基，n等于0或1，并且它们与酸，金属盐和与含氮碱的加成盐的加成盐也是具有广谱活性的抗菌剂。
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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：US4347359A
公开(公告)日：1982-08-31
申请号：US225446
申请日：1981-01-15
IPC分类号： C07D249/10 , C07D253/075 , C07D257/04 , C07D317/28 , C07D319/06 , C07D501/24 , C07D253/06
CPC分类号： C07D253/075 , C07D257/04 , C07D317/28 , C07D319/06
摘要： New thiols of the general formula: ##STR1## wherein A represents a 2-hydroxy-1-oxoethan-1-yl-2-ylidene or alkoxycarbonylmethyne radical or a nitrogen atom and R represents various substituted alkyl radicals, and their alkali metal and alkaline earth metal salts are useful as intermediates in the preparation of cephalosporins having anti-bacterial properties.
摘要翻译： 新的具有以下通式的硫醇：其中A代表2-羟基-1-氧代乙烷-1-基-2-亚基或烷氧基羰基甲炔基或氮原子，R代表各种取代的烷基，以及它们的碱金属和碱 地球金属盐可用作制备具有抗菌性质的头孢菌素的中间体。
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