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    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    41.
    发明授权
    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions 失效
    双芳族酯，其制备方法及其在人或兽医学和化妆品组合物中的应用

    公开(公告)号：US5468897A

    公开(公告)日：1995-11-21

    申请号：US237991

    申请日：1994-05-04

    申请人： Braham Shroot ,  Jean-Michel Bernardon ,  William R. Pilgrim

    发明人： Braham Shroot ,  Jean-Michel Bernardon ,  William R. Pilgrim

    IPC分类号： A61K31/235 ,  A61K8/00 ,  A61K8/30 ,  A61K8/33 ,  A61K8/37 ,  A61K8/40 ,  A61K8/41 ,  A61K8/42 ,  A61K8/46 ,  A61K8/49 ,  A61P11/00 ,  A61P17/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61Q5/00 ,  A61Q19/00 ,  C07C67/14 ,  C07C69/00 ,  C07C69/76 ,  C07C69/773 ,  C07C69/78 ,  C07C69/88 ,  C07C69/94 ,  C07C309/42 ,  C07C309/58 ,  C07C311/29 ,  C07C317/22 ,  C07C317/44 ,  C07C323/62 ,  C07C321/00

    CPC分类号： C07C323/62 ,  C07C69/94 ,  C07C2103/74

    摘要： 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 mono or 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, C1-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.

    摘要翻译： 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。

    Epoxy substituted cephalosporin derivatives
    46.
    发明授权
    Epoxy substituted cephalosporin derivatives 失效
    环氧取代头孢菌素衍生物

    公开(公告)号：US4137312A

    公开(公告)日：1979-01-30

    申请号：US838830

    申请日：1977-10-03

    申请人： Barry C. Ross ,  Braham Shroot

    发明人： Barry C. Ross ,  Braham Shroot

    IPC分类号： A61K31/545 ,  C07D501/24 ,  C07D501/34 ,  C07D501/46

    CPC分类号： C07D501/20 ,  C07D501/24

    摘要： 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.

    摘要翻译： 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。

    7[(Carboxyoxiran-3-carboxamido)phenylacetamido]cephalosporin derivatives
    47.
    发明授权
    7[(Carboxyoxiran-3-carboxamido)phenylacetamido]cephalosporin derivatives 失效
    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

    公开(公告)号：US4064241A

    公开(公告)日：1977-12-20

    申请号：US628543

    申请日：1975-11-03

    申请人： Barry Clive Ross ,  Braham Shroot

    发明人： Barry Clive Ross ,  Braham Shroot

    IPC分类号： C07D303/48 ,  C07D501/20 ,  C07D501/24 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/20 ,  C07D303/48 ,  C07D501/24

    摘要： 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.

    摘要翻译： 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。

    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    49.
    发明授权
    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions 失效
    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

    公开(公告)号：US5200550A

    公开(公告)日：1993-04-06

    申请号：US553087

    申请日：1990-07-17

    申请人： Braham Shroot ,  Jean-Michel Bernardon

    发明人： Braham Shroot ,  Jean-Michel Bernardon

    IPC分类号： A61K31/235 ,  A61K8/00 ,  A61K8/30 ,  A61K8/33 ,  A61K8/37 ,  A61K8/40 ,  A61K8/41 ,  A61K8/42 ,  A61K8/46 ,  A61K8/49 ,  A61P11/00 ,  A61P17/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61Q5/00 ,  A61Q19/00 ,  C07C67/14 ,  C07C69/00 ,  C07C69/76 ,  C07C69/773 ,  C07C69/78 ,  C07C69/88 ,  C07C69/94 ,  C07C309/42 ,  C07C309/58 ,  C07C311/29 ,  C07C317/22 ,  C07C317/44 ,  C07C323/62

    CPC分类号： C07C323/62 ,  C07C69/94 ,  C07C2103/74

    摘要： 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.

    摘要翻译： 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。

    2-adamantyl-4-isothiazoline-3-ones, as bactericidal and fungicidal agents
    50.
    发明授权
    2-adamantyl-4-isothiazoline-3-ones, as bactericidal and fungicidal agents 失效
    2-金刚烷基-4-异噻唑啉-3-酮，作为杀菌剂和杀真菌剂

    公开(公告)号：US5153212A

    公开(公告)日：1992-10-06

    申请号：US709227

    申请日：1991-06-03

    申请人： Braham Shroot ,  Jean Maignan ,  Rainer Schmidt

    发明人： Braham Shroot ,  Jean Maignan ,  Rainer Schmidt

    IPC分类号： C07D213/81 ,  A01N43/80 ,  A61K8/00 ,  A61K8/49 ,  A61K31/425 ,  A61K31/435 ,  A61P31/04 ,  A61P31/10 ,  C07D275/02 ,  C07D275/03 ,  C07D275/04 ,  C07D513/04

    CPC分类号： C07D275/03 ,  C07D275/04 ,  C07D513/04

    摘要： 2-adamantyl-4-isothiazoline-3-one has the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently, represent hydrogen or halogen,or R.sub.1 and R.sub.2, taken together, form a polymethylene chain having 3-4 carbon atoms, optionally substituted by lower alkyl or halogen,or R.sub.1 and R.sub.2, taken together, form a pyridine ring with the double bond of the 4-isothiazoline-3-one ring andAda represents 1'-adamantyl, 2'-adamantyl or 1'-adamantyl methyl, and its mineral or organic acid salt.The compound is useful as an antibacteria, antialgae or antifungus agent in various industrial fields.

    摘要翻译： 2-金刚烷基-4-异噻唑啉-3-酮具有式（I）其中R 1和R 2各自独立地表示氢或卤素，或者R 1和R 2一起形成具有3-4个碳原子的聚亚甲​​基链 原子，任选被低级烷基或卤素取代，或者R 1和R 2一起形成具有4-异噻唑啉-3-酮环的双键的吡啶环，Ada代表1'-金刚烷基，2'-金刚烷基或1 ' - 金刚烷基甲基及其矿物或有机酸盐。 该化合物可用作各种工业领域的抗细菌，抗藻类或抗真菌剂。