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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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2.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：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：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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公开(公告)号：US4307230A
公开(公告)日：1981-12-22
申请号：US152084
申请日：1980-05-21
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/06 , C07D501/14 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60
CPC分类号： C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/24
摘要： Novel 3-vinyl-cephalosporins of the formula ##STR1## in which n is 0 or 1, R.sub.1 is hydrogen, a radical of the formula ##STR2## [in which R.sub.4 is hydrogen or a protective radical and R.sub.5 is hydrogen, alkyl, vinyl or cyanomethyl or is a protective radical], or a protective radical, and R.sub.2 is hydrogen, a protective radical or an enzymatically removable radical, or R.sub.1 is hydrogen or an acyl radical which may carry various substituents and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a radical of the general formula R'.sub.3 --SO.sub.2 --O-- or R".sub.3 --CO--O--, in which R'.sub.3 is alkyl, trifluoromethyl, trichloromethyl or phenyl which is substituted by a halogen atom or by an alkyl or nitro radical, and R".sub.3 is defined like R'.sub.3 or represents methyl which is substituted by acyl or alkoxycarbonyl, or represents ethyl or propyl substituted in the 2-position by acyl or alkoxycarbonyl. These compounds are useful as intermediates for the preparation of antibiotic 3-thiovinyl-cephalosporins.
摘要翻译： 式（I）的新型3-乙烯基头孢菌素其中n为0或1，R 1为氢，式（II）的基团[其中R 4为氢或保护基，R 5为 是氢，烷基，乙烯基或氰基甲基，或是保护基]或保护基，R2是氢，保护基或酶可除去的基团，或R 1是氢或可以带有各种取代基的酰基，R 2是 氢或保护基，R3是通式为R'3-SO2-O-或R'3-CO-O-的基团，其中R'3是烷基，三氟甲基，三氯甲基或被取代的苯基 卤素原子或烷基或硝基，R“3定义为R'3，或表示被酰基或烷氧基羰基取代的甲基，或代表在2-位被酰基或烷氧基羰基取代的乙基或丙基。 这些化合物可用作制备抗生素3-硫代乙烯基 - 头孢菌素的中间体。
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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：US4365062A
公开(公告)日：1982-12-21
申请号：US152153
申请日：1980-05-21
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/06 , C07D501/14 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60
CPC分类号： C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/24
摘要： New cephalosporins of the formula: ##STR1## in which n=0 or 1, R.sub.1 is a radical of the formula: ##STR2## [in which R.sub.4 is a protective radical and R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl or a protective radical], or R.sub.1 is a protective radical and R.sub.2 is a protective radical or an enzymatically removable radical, or R.sub.1 is an acyl radical which may be substituted in various ways and R.sub.2 is a protective radical, in the 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or 3-oxoethylidene-bicyclooctane form if n=0, and in the 3-oxoethyl-bicyclooct-2-ene or 3-oxoethylidene-bicyclooctane form if n=1, are useful as intermediates for the preparation of 3-thiovinyl-cephalosporins useful as antibacterial agents.
摘要翻译： 式（I）的新型头孢菌素，其中n = 0或1，R1是下式的基团：其中R 4是保护基，R 5是氢，烷基，乙烯基 ，氰基甲基或保护基]，或R 1是保护基，R 2是保护基或可酶还原的基团，或者R 1是可以以各种方式被取代的酰基，R 2是保护基， 如果n = 0，则为3-氧代乙基 - 双环辛-2-烯或双环辛-3-烯或3-氧亚乙基 - 双环辛烷，如果n = 1，则为3-氧代乙基 - 双环辛-2-烯或3-氧亚乙基 - 双环辛烷， 可用作制备用作抗菌剂的3-硫代乙烯基 - 头孢菌素的中间体。
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公开(公告)号：US4307233A
公开(公告)日：1981-12-22
申请号：US152085
申请日：1980-05-21
IPC分类号： A61K20060101 , A61K31/545 , A61K31/546 , A61P3/02 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/38 , C07D501/46 , C07D501/58 , C07D501/60
CPC分类号： C07D501/14
摘要： Novel 3-vinyl-cephalosporin derivates of the general formula ##STR1## in the bicyclooct-2-ene or bicyclooct-3-ene form, in which R.sub.1 is a protective radical or is a radical of the general formula ##STR2## in which R.sub.5 is hydrogen, alkyl, vinyl or cyanomethyl, or a protective radical, and R.sub.6 is hydrogen or a protective radical, and R.sub.2 is a protective radical or an enzymatically removable radical, or R.sub.1 is an acyl radical, which may carry various substituents, and R.sub.2 represents a protective radical, 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 form, together with the nitrogen atom, a saturated 5-membered or 6-membered heterocyclic ring optionally containing another hetero-atom, their E- and Z-forms and their mixtures, are useful as intermediates for the preparation of 3-thiovinyl cephalosporins useful as antibacterial agents.
摘要翻译： 双环-2-烯或双环-3-烯形式的新颖的3-乙烯基 - 头孢菌素衍生物，其中R 1是保护基或是通式为“IMAGE”的基团， （II），其中R 5是氢，烷基，乙烯基或氰基甲基或保护基，R 6是氢或保护基，R 2是保护基或可酶解的基，或者R 1是酰基， 并且R 2表示保护基，R 3和R 4相同或不同，代表烷基（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， 任选地含有另一个杂原子的饱和5元或6元杂环，它们的E-和Z-形式及其混合物可用作制备用作抗菌剂的3-硫代乙烯基头孢菌素的中间体。
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公开(公告)号：US4307116A
公开(公告)日：1981-12-22
申请号：US152115
申请日：1980-05-21
IPC分类号： A61K20060101 , A61K31/545 , C07D20060101 , C07D277/38 , C07D417/12 , C07D501/00 , C07D501/24 , C07D501/36 , C07D501/46
CPC分类号： C07D501/24
摘要： Novel cephalosporins of the general formula (I); ##STR1## in which R is alkyl, L-2-amino-2-carboxy-ethyl, phenyl, pyridyl, pyridyl-N-oxide, 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, 1,3,4-triazol-5-yl or 2-alkoxycarbonyl-1,3,4-triazol-5-yl substituted in the 1-position, 1,4-dialkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 1-alkyl-5,6-dioxo-1,4,5,6-tetrahydro-1,2,4-triazin-3-yl, 2-alkyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl, triazol-5-yl, 1,3,4-thiadiazol-5-yl which is substituted or unsubstituted, 1,2,4-thiadiazol-5-yl which is substituted, 1,3,4-oxadiazol-5-yl which is substituted or unsubstituted, oxazol-2-yl which is substituted or unsubstituted or tetrazol-5-yl which is substituted or unsubstituted in the 1-position, R' is a hydrogen atom or a radical of the general formula (II); ##STR2## and R.sup.o is hydrogen, alkyl, vinyl or cyanomethyl, as well as their salts, are useful as anti-bacterial agents.
摘要翻译： 通式（I）的新型头孢菌素; （I）其中R是烷基，L-2-氨基-2-羧基 - 乙基，苯基，吡啶基，吡啶基-N-氧化物，嘧啶-2-基，取代的哒嗪-3-基，5,6 在4-位取代的1-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，1,3,4-三唑-5-基或2-烷氧基羰基-1,3 在1-位上取代的4-三唑-5-基，1,4-二烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，1 - 烷基-5,6-二氧代-1,4,5,6-四氢-1,2,4-三嗪-3-基，2-烷基-5,6-二氧代-1,2,5,6-四氢 -1,2,4-三嗪-3-基，三唑-5-基，取代或未取代的1,3,4-噻二唑-5-基，被取代的1,2,4-噻二唑-5-基 被取代或未取代的取代或未取代的1,3,4-恶二唑-5-基，在1位被取代或未取代的四唑-5-基，R'是氢 原子或通式（II）的基团; （II）和Ro是氢，烷基，乙烯基或氰基甲基，以及它们的盐可用作抗细菌剂。
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