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    • 16. 发明授权
    • Epoxy substituted cephalosporin derivatives
    • 环氧取代头孢菌素衍生物
    • US4137312A
    • 1979-01-30
    • US838830
    • 1977-10-03
    • Barry C. RossBraham Shroot
    • Barry C. RossBraham Shroot
    • A61K31/545C07D501/24C07D501/34C07D501/46
    • C07D501/20C07D501/24
    • A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-methyl-1,2,3,4-tetrazol-5-ylthiomethyl)-.alpha..sup.3 -cephem-4-carboxylic acid and 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalosporanic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.
    • 已经制备了一系列新颖的7-(D-α-酰基氨基芳基乙酰氨基)-TATA 3-头孢烯衍生物,其中酰基部分含有紧邻羰基碳原子的环氧基。 这些化合物可用作抗菌剂,用于治疗由革兰氏阴性菌和革兰氏阳性菌引起的疾病。 优选的成员包括7- [D-α - (顺式-2-羧基环氧乙烷-3-甲酰氨基)苯基乙酰氨基] -3-(1-甲基-1,2,3,4-四唑-5-基硫甲基)-α3-头孢烯 -4-羧酸和7- [D-α-(顺式-2-羧基环氧乙烷-3-甲酰氨基)苯基乙酰胺基]头孢烷酸。 为这些化合物提供了替代的制备方法,并详细描述了主要合成路线。
    • 17. 发明授权
    • 7[(Carboxyoxiran-3-carboxamido)phenylacetamido]cephalosporin derivatives
    • 7 {8(羧基氧环己烷-3-甲酰氨基)苯乙酰氨基{9头孢菌素衍生物
    • US4064241A
    • 1977-12-20
    • US628543
    • 1975-11-03
    • Barry Clive RossBraham Shroot
    • Barry Clive RossBraham Shroot
    • C07D303/48C07D501/20C07D501/24C07D501/36A61K31/545
    • C07D501/20C07D303/48C07D501/24
    • A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-methyl-1,2,3,4-tetrazol-5-ylthiomethyl)-.DELTA..sup.3 -cephem-4-carboxylic acid and 7-[D.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalosporanic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.
    • 已经制备了一系列新颖的7-(D-α-酰基氨基芳基乙酰氨基)-TATA 3-头孢烯衍生物,其中酰基部分含有紧邻羰基碳原子的环氧基。 这些化合物可用作抗菌剂,用于治疗由革兰氏阴性菌和革兰氏阳性菌引起的疾病。 优选的成员包括7- [D-α - (顺式-2-羧基环氧乙烷-3-甲酰胺基)苯基乙酰胺基] -3-(1-甲基-1,2,3,4-四唑-5-基硫甲基)-TATA 3 - 头孢烯 -4-羧酸和7- [Dα-(顺式-2-羧基环氧乙烷-3-甲酰氨基)苯基乙酰胺基]头孢烷酸。 为这些化合物提供了替代的制备方法,并详细描述了主要合成路线。
    • 20. 发明授权
    • Bi-aromatic esters, a process for their preparation and their use in
human or veterinary medicine and in cosmetic compositions
    • 双芳香酯,其制备方法及其在人体或兽医学和化妆品组合物中的用途
    • US5200550A
    • 1993-04-06
    • US553087
    • 1990-07-17
    • Braham ShrootJean-Michel Bernardon
    • Braham ShrootJean-Michel Bernardon
    • A61K31/235A61K8/00A61K8/30A61K8/33A61K8/37A61K8/40A61K8/41A61K8/42A61K8/46A61K8/49A61P11/00A61P17/00A61P27/02A61P29/00A61P35/00A61Q5/00A61Q19/00C07C67/14C07C69/00C07C69/76C07C69/773C07C69/78C07C69/88C07C69/94C07C309/42C07C309/58C07C311/29C07C317/22C07C317/44C07C323/62
    • C07C323/62C07C69/94C07C2103/74
    • Bi-aromatic esters have the formula ##STR1## wherein R.sub.1 represents H, OH, --CH.sub.3, --CH.sub.2 OH, --CH(OH)CH.sub.3, --COOR.sub.9, ##STR2## or SO.sub.2 R.sub.10 ; R.sub.9 represents H, C.sub.1 -C.sub.6 alkyl or monoor polyhydroxyalkyl; R.sub.10 represents OH, C.sub.1 -C.sub.6 alkyl or ##STR3## r' and r" represent H, C.sub.1 -C.sub.6 alkyl, aryl, aralkyl, mono or polyhydroxyalkyl, or r' and r" taken together form a heterocycle; R.sub.2 represents H, C.sub.1 -C.sub.6 alkyl, OR.sub.9, F or --CF.sub.3 ; R.sub.3, R.sub.4 and R.sub.5 represent H, F, OH, --CH.sub.3, --OCH.sub.3, --CF.sub.3, --COOH or --CH.sub.2 OH; R.sub.6 and R.sub.8 represent H, .alpha.-substituted C.sub.3 -C.sub.15 alkyl, .alpha.,.alpha.'-disubstituted C.sub.4 -C.sub.12 alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.12 mono or polycyclic cycloalkyl whose linking carbon is trisubstituted, --SR.sub.11, --SO.sub.2 R.sub.11 or --SOR.sub.11 ; R.sub.11 represents C.sub.1 -C.sub.6 alkyl or cycloalkyl; R.sub.6 and R.sub.8 cannot simultaneously represent H; R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl, alkenyl, alkenyloxy, OR.sub.12 or SR.sub.13 ; R.sub.12 represents H, C.sub.1 -C.sub.6 alkyl or alkenyl; R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl; with the proviso that when R.sub.1 represents ##STR4## and R.sub.2 represents H then: (i) either R.sub.3 and R.sub.4 are other than H or --CH.sub.3, (ii) or R.sub.7 is other than OR.sub.12 and R.sub.6 or R.sub.8 is cycloalkyl having more than 7 carbon atoms, (iii) or R.sub.7 is OR.sub.12 but R.sub.6 and R.sub.8 are other than H, (iv) or R.sub.7 is OR.sub.12 but R.sub.5 is other than H.The bi-aromatic esters are employed in human and veterinary medicine and in cosmetic compositions.
    • 双芳族酯具有式(I)其中R 1表示H,OH,-CH 3,-CH 2 OH,-CH(OH)CH 3,-COOR 9,或SO 2 R 10; R9表示H,C1-C6烷基或单或多羟基烷基; R 10表示OH,C 1 -C 6烷基或R 3',R“表示H,C 1 -C 6烷基,芳基,芳烷基,单或多羟基烷基,或r'和r”一起形成杂环; R 2表示H,C 1 -C 6烷基,OR 9,F或-CF 3; R3,R4和R5表示H,F,OH,-CH3,-OCH3,-CF3,-COOH或-CH2OH; R 6和R 8表示H,α-取代的C 3 -C 15烷基,α,α'-二取代的C 4 -C 12烷基,C 3 -C 12环烷基,连接碳是三取代的C 5 -C 12单环或多环环烷基,-SR 11,-SO 2 R 11或 - SOR11; R11表示C1-C6烷基或环烷基; R6和R8不能同时代表H; R7表示H,C1-C6烷基,烯基,烯氧基,OR12或SR13; R12表示H,C1-C6烷基或烯基; R3表示H,C1-C6烷基或芳烷基; 条件是当R1表示且R2表示H时:(i)R3和R4不是H或-CH3,(ii)或R7不是OR12,R6或R8是大于7的环烷基 碳原子,(iii)或R7是OR12,但R6和R8不是H,(iv)或R7是OR12,但R5不是H.双芳族酯用于人类和兽医学和化妆品组合物中。