-
公开(公告)号：US5527791A
公开(公告)日：1996-06-18
申请号：US123998
申请日：1993-09-21
IPC分类号： A61K31/40 , A61K31/397 , A61P31/04 , C07D205/08 , C07D207/16 , C07D403/12 , C07D409/12 , C07D409/14 , C07D477/00 , C07D477/20 , C07F9/568 , C07D487/04
CPC分类号： C07D477/20 , C07D207/16 , C07D403/12 , C07D409/12 , C07D409/14 , C07F9/5683
摘要： The present invention provides a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:A is a group of the formula (IA) or (IB): ##STR2## R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are the same or different and are a variety of substituents X is alkanediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x (wherein x is zero, one or two), --CONR.sup.5 -- or --NR.sup.5 -- or wherein R.sup.5 is hydrogen or C.sub.1-4 alkyl;or X is alkenediyl containing 1-6 carbon atoms optionally interrupted by O, S(O).sub.x or --NR.sup.5 --.
摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐或体内可水解的酯，其中：A为式（IA）或（IB）的基团： （IB）R1是1-羟乙基，1-氟乙基或羟甲基; R2是氢或C1-4烷基; R 3和R 4相同或不同，并且是各种取代基，X为任选被O，S（O）x（其中x为0或1或2）间隔的含1-6个碳原子的烷二基，-CONR 5 - 或-NR 5 - 或其中R5是氢或C1-4烷基; 或X是任选被O，S（O）x或-NR 5 - 中断的含有1-6个碳原子的烯二基。
-
公开(公告)号：US4504478A
公开(公告)日：1985-03-12
申请号：US415541
申请日：1982-09-07
申请人： Frederic H. Jung , Gareth M. Davies
发明人： Frederic H. Jung , Gareth M. Davies
IPC分类号： C07D501/16 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/18
CPC分类号： C07D501/18
摘要： An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen, 1-6C alkoxy or 1-6C alkylthio; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.5 ; R.sup.4 and R.sup.5 are a variety of radicals described in the specification; --A-- is of the formula II or III: ##STR2## in which R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.
摘要翻译： 一种式I的抗菌头孢菌素衍生物：其中X1是亚磺酰基; R1是本领域已知的来自抗菌活性头孢菌素的C-3取代基中的任何一个; R2是本领域已知的来自抗菌活性头孢菌素的C-4取代基中的任何一个; R3是氢，1-6C烷氧基或1-6C烷硫基; X2是氮或基团N（+）R5; R4和R5是说明书中描述的各种基团; -A-具有式II或III的化合物：其中R 6，R 7，R 8，R 9，R 10和R 11是说明书中描述的各种取代基; 和其药学上可接受的酸和碱加成盐。 还描述了药物组合物和制备方法。
-
公开(公告)号：US4492692A
公开(公告)日：1985-01-08
申请号：US333570
申请日：1981-12-22
申请人： Frederic H. Jung , Gareth M. Davies
发明人： Frederic H. Jung , Gareth M. Davies
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D207/34 , C07D209/48 , C07D463/00 , C07D487/04 , C07D501/16 , C07D501/18 , C07D505/00 , C07D501/56
CPC分类号： C07D209/48 , C07D207/34 , C07D463/20 , C07D463/22 , C07D487/04 , C07D505/00
摘要： A cephalosporin derivative of the formula: ##STR1## in which R.sup.0 is a hydrogen atom or a methyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is a hydrogen atom or a 1-6C alkoxy or 1-6C alkylthio radical; X.sup.1 is a sulphur or oxygen atom, a CH.sub.2 radical or a radical of the formula NR.sup.7 in which R.sup.7 is a hydrogen atom, a 1-6C alkyl, formyl or benzyl radical; X.sup.2 is a nitrogen atom or a radical of the formula N.sup..sym. -R.sup.7 ; R.sup.4 and R.sup.7, and R.sup.5 and R.sup.6 are a variety of substituents which are described in the specification; and the pharmaceutically-acceptable acid- or base-addition salts thereof. Pharmaceutical compositions, manufacturing processes and intermediates are also described.
摘要翻译： 下式的头孢菌素衍生物：其中R 0是氢原子或甲基，R1是本领域已知的来自抗菌活性头孢菌素的任何一个C-3取代基; R2是本领域已知的来自抗菌活性头孢菌素的C-4取代基中的任何一个; R3是氢原子或1-6C烷氧基或1-6C烷硫基; X1是硫或氧原子，CH2基或式NR7的基团，其中R7是氢原子，1-6C烷基，甲酰基或苄基; X 2是氮原子或式N（+） - R 7的基团; R4和R7以及R5和R6是说明书中描述的各种取代基; 及其药学上可接受的酸或碱加成盐。 还描述了药物组合物，制造方法和中间体。
-
公开(公告)号：US4490382A
公开(公告)日：1984-12-25
申请号：US333567
申请日：1981-12-22
申请人： Frederic H. Jung , Gareth M. Davies
发明人： Frederic H. Jung , Gareth M. Davies
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/10 , C07D499/21 , C07D499/42 , C07D277/20 , A61K31/425
CPC分类号： C07D499/00
摘要： A penicillin derivative of the formula I: ##STR1## in which R.sup.1 is any one of the C-3 substituents from antibacterially-active penicillins known in the art;X is a nitrogen atom or a radical of the formula N.sup..sym. --R.sup.3 ;R.sup.2 and R.sup.3, which may be the same or different, are hydrogen atoms or 1-6C alkyl, 1-6C alkanoyl, hydroxy, 1-6C alkoxy, amino, 1-6C alkanoylamino, 1-6C alkylamino, 1-6C aminoalkyl, 1-6C hydroxyalkyl, 2-6C carboxyalkyl, 2-6C alkenyl, 3-6C alkoxyalkyl, 3-8C alkoxycarbonylalkyl, furylmethyl, phenyl or 7-11C phenylalkyl radicals, in the latter two of which the phenyl ring is optionally substituted by a halogen atom or by a methyl, methoxy, nitro, hydroxy, amino, carboxy or methoxy-carbonyl radical;A
摘要翻译： 式I的青霉素衍生物：其中R 1是本领域已知的来自抗菌活性青霉素的C-3取代基中的任何一个; X是氮原子或式N（+） - R 3的基团; R2和R3可以相同或不同，是氢原子或1-6C烷基，1-6C烷酰基，羟基，1-6C烷氧基，氨基，1-6C烷酰基氨基，1-6C烷基氨基，1-6C氨基烷基， 1-6C羟烷基，2-6C羧基烷基，2-6C烯基，3-6C烷氧基烷基，3-8C烷氧基羰基烷基，呋喃基甲基，苯基或7-11C苯基烷基，其中苯基环任选被卤素 甲基，甲氧基，硝基，羟基，氨基，羧基或甲氧基 - 羰基; A <是式II或III的基团：其中R 4，R 5，R 6，R 7，R 8和R 9如说明书中所述; 及其药学上可接受的酸或碱加成盐。 还描述了药物组合物和制备方法。
-
5.发明授权6-Fluoro-shikimic acid derivatives, pharmaceutical compositions and use as antibacterials and fungicides 失效6-氟尿酸衍生物，药物组合物，用作抗生素和杀真菌剂
公开(公告)号：US5164382A
公开(公告)日：1992-11-17
申请号：US509802
申请日：1990-04-17
IPC分类号： A01N37/10 , A01N37/40 , A01N41/06 , A01N57/12 , A01N57/14 , A61K31/19 , A61K31/215 , C07C51/00 , C07C51/363 , C07C51/367 , C07C62/04 , C07C62/10 , C07C62/32 , C07C67/00 , C07C69/757 , C07D303/38 , C07D303/40 , C07D493/04 , C07F9/117 , C07F9/12 , C07F9/655
CPC分类号： C07D493/04 , A01N37/40 , A01N57/14 , C07C62/32 , C07D303/40 , C07F9/117 , C07F9/65507
摘要： 6-Fluoroshikimic acid derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydroxy or a moiety biotransformable thereto and R.sup.2 is hydrogen or --P(O)(OH).sub.2 have antibacterial, antifungal, and herbicidal activity. Their preparation and use are described as are pharmaceutical compositions containing them.
-
公开(公告)号：US5478820A
公开(公告)日：1995-12-26
申请号：US129056
申请日：1993-10-04
IPC分类号： A61K31/397 , A61K31/40 , A61K31/407 , A61K31/41 , A61K38/40 , A61P31/04 , C07C233/00 , C07D205/00 , C07D207/00 , C07D207/16 , C07D403/12 , C07D477/00 , C07D477/20 , C07D487/04 , C07F9/568 , C07F9/572 , C07F9/6574 , A61K31/395
CPC分类号： C07D477/20 , A61K31/40 , A61K31/407 , A61K31/41 , C07D207/16 , C07D403/12 , C07F9/5683
摘要： The present invention relates to carbapenems and provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 are the same or different and are selected from hydrogen, halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, C.sub.1-4 alkylaminosulphonyl, di-C.sub.1-4 alkylaminosulphonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino, C.sub.1-4 alkanesulphonamido and C.sub.1-4 alkylS(O).sub.n -- wherein n is zero, one or two:with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the --NR.sup.2 --. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译： PCT No.PCT / GB93 / 00217 Sec。 371日期：1993年10月4日 102（e）日期1993年10月4日PCT提交1993年2月2日PCT公布。 公开号WO93 / 15078 本发明涉及碳青霉烯并提供式（I）的化合物：其中：R1是1-羟基乙基，1 - 氟乙基或羟甲基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，选自氢，卤素，氰基，C1-4烷基，硝基，羟基，羧基，C1-4烷氧基，C1-4烷氧基羰基，氨基磺酰基，C1-4烷基氨基磺酰基，二-C1-4烷基氨基磺酰基，氨基甲酰基， C 1-4烷基氨基甲酰基，二-C 1-4烷基氨基甲酰基，三氟甲基，磺酸，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，C 1-4烷酰基氨基，C 1-4烷酰基（N-C 1-4烷基）氨基，C 1-4烷基磺酰氨基和C 1-4烷基 （O）n - 其中n为0，一个或两个：条件是在-NR 2的邻位没有羟基或羧基取代基。 其制备方法，制备中的中间体，其作为治疗剂的用途和含有它们的药物组合物。
-
7.发明授权Compounds useful as intermediates in the synthesis of shikimic acid derivatives 失效用作合成莽草酸衍生物的中间体的化合物
公开(公告)号：US5214165A
公开(公告)日：1993-05-25
申请号：US933827
申请日：1992-08-24
IPC分类号： A01N37/40 , A01N57/14 , C07C62/32 , C07D303/40 , C07D493/04 , C07F9/117 , C07F9/655
CPC分类号： C07D493/04 , A01N37/40 , A01N57/14 , C07C62/32 , C07D303/40 , C07F9/117 , C07F9/65507
摘要： 6-Fluoroshikimic acid derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydroxy or a moiety biotransformable thereto and R.sup.2 is hydrogen or --P(O)(OH).sub.2 have antibacterial, antifungal and herbicidal activity. Their preparation and use are described as are pharmaceutical compositions containing them.
摘要翻译： 式（I）的6-氟代缩水甘油酸衍生物：其中R 1是羟基或可生物转化的部分，R 2是氢或-P（O）（OH）2）具有抗菌，抗真菌和除草活性。 它们的制备和用途被描述为含有它们的药物组合物。
-
公开(公告)号：US5149803A
公开(公告)日：1992-09-22
申请号：US732478
申请日：1991-07-18
IPC分类号： C07D501/18 , C07D501/46
CPC分类号： C07D501/46
摘要： Cephalosporin antibiotics having a 3-position substituent of the formula:--CH.sub.2 NR.sup.1 --Y--A--Z--Qare described, wherein R.sup.1 is hydrogen or certain optionally substituted alkyl groups; Y is --CO-- or --SO.sub.2 --; A is optionally substituted phenylene or heterocyclylene; Z is a linking group and Q is a catechol or related ring system. Processes for their preparation and use are described.
摘要翻译： 描述了具有下式的-CH 2 NR1-Y-A-Z-Q的3-位取代基的头孢菌素抗生素，其中R 1是氢或某些任选取代的烷基; Y是-CO-或-SO 2 - ; A是任选取代的亚苯基或亚杂环基; Z是连接基团，Q是儿茶酚或相关环系。 描述了其制备和使用的方法。
-
公开(公告)号：US5055462A
公开(公告)日：1991-10-08
申请号：US349662
申请日：1989-05-10
IPC分类号： A01N43/90 , A61K31/545 , C07D501/18 , C07D501/38 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/52 , C07D501/54 , C07D501/56
CPC分类号： C07D501/46
摘要： Cephalosporin antibiotics having a 3-position substituent of the formula:--CH.sub.2 NR.sup.1 --Y--A--Z--Qare described, wherein R.sup.1 is hydrogen or certain optionally substituted alkyl groups; Y is --CO-- or --SO.sub.2 --; A is optionally substituted phenylene or heterocyclylene; Z is a linking group and Q is a catechol or related ring system. Processes for their preparation and use are described.
-
公开(公告)号：US4486426A
公开(公告)日：1984-12-04
申请号：US399875
申请日：1982-07-19
申请人： Frederich Jung , Gareth M. Davies
发明人： Frederich Jung , Gareth M. Davies
IPC分类号： C07D501/16 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/18 , C07D505/00 , A61K31/425
CPC分类号： C07D505/00
摘要： An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphur, oxygen, sulphinyl or sulphonyl; R.sup.1 is a variety of radicals defined in the specification; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen or methoxy; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.8 ; R.sup.4 and R.sup.8 are a variety of radicals described in the specification; --A-- is of the formula V or VI: ##STR2## in which R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.
摘要翻译： 式I的抗菌头孢菌素衍生物：其中X 1是硫，氧，亚磺酰基或磺酰基; R1是规范中定义的各种基团; R2是本领域已知的来自抗菌活性头孢菌素的C-4取代基中的任何一个; R3是氢或甲氧基; X 2是氮或基团N（+）R 8; R4和R8是说明书中描述的各种基团; -A-具有式V或VI：其中R 9，R 10，R 11，R 12，R 13和R 14是说明书中描述的各种取代基; 和其药学上可接受的酸和碱加成盐。 还描述了药物组合物和制备方法。
-
-
-
-
-
-
-
-
-
搜索结果
10 条记录 (耗时 0.025 秒)
