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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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22.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：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：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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26.发明授权2-benzoylimidazopyridine derivatives, preparation and therapeutic use thereof 失效2-苯甲酰基咪唑并吡啶衍生物，其制备和治疗用途公开(公告)号：US07902219B2
公开(公告)日：2011-03-08
申请号：US12336989
申请日：2008-12-17
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to a compound of formula (I) wherein R1, R2, R3, R4 and X are as defined herein, or an acid-addition salt thereof, its preparation and therapeutic use in the treatment or prevention of diseases involving the Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.
摘要翻译： 本发明涉及其中R 1，R 2，R 3，R 4和X如本文所定义的式（I）化合物或其酸加成盐，其在治疗或预防涉及 Nurr-1核受体，也称为NR4A2，NOT，TINUR，RNR-1和HZF3。
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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：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：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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