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    Bi-aromatic esters, a process for their preparation and their use in human or veterinary medicine and in cosmetic compositions
    61.
    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。

    Method of producing A 2,4'-dihydroxydiphenylsulfone
    67.
    发明授权
    Method of producing A 2,4'-dihydroxydiphenylsulfone 失效
    制备A 2,4'-二羟基二苯砜的方法

    公开(公告)号：US5399772A

    公开(公告)日：1995-03-21

    申请号：US164855

    申请日：1993-12-10

    申请人： Masaaki Hosoda ,  Mikihiko Kurose ,  Yoshihiro Sasada ,  Hajime Saito ,  Masahiro Makino

    发明人： Masaaki Hosoda ,  Mikihiko Kurose ,  Yoshihiro Sasada ,  Hajime Saito ,  Masahiro Makino

    IPC分类号： C07C315/00 ,  C07C317/22 ,  C07C315/06

    CPC分类号： C07C315/00

    摘要： High purity 2,4'-dihydroxydiphenylsulfones useful as developers for thermal recording paper can be produced efficiently and with high selectivity by reacting one or more phenols and sulfuric acid in the presence as of at least one of phosphonic acid, phosphinic acid and salts thereof, in the absence of a solvent or in the presence of an aromatic hydrocarbon solvent having a boiling point at atmospheric pressure of 130.degree. to 200.degree. C., and then purifying the thus-produced crude 2,4'-dihydroxydiphenylsulfones using a mixed solvent containing (1) 5 to 20 weight % of at least one lower aliphatic alcohol and 95 to 80 weight % of at least one aromatic hydrocarbon which does not contain halogen, (2) 10 to 40 weight % of at least one ketone and 90 to 60 weight % of at least one aromatic hydrocarbon which does not contain halogen or (3) 10 to 40 weight % of at least one ester of acetic acid and 90 to 60 weight % of at least one aromatic hydrocarbon which does not contain halogen.

    摘要翻译： 作为热记录纸的显影剂的高纯度2,4'-二羟基二苯基砜可以通过一种或多种酚和硫酸在至少一种膦酸，次膦酸及其盐的存在下反应而高效选择性地制备， 在不存在溶剂的情况下，或在沸点在常压130〜200℃的芳烃溶剂存在下，使用含有以下物质的混合溶剂，纯化如此制得的粗2,4'-二羟基二苯基砜 （1）5至20重量％的至少一种低级脂族醇和95至80重量％的至少一种不含卤素的芳族烃，（2）10至40重量％的至少一种酮和90至60 至少一种不含卤素的芳族烃的重量％，或（3）10至40重量％的至少一种乙酸酯和90至60重量％的至少一种不含卤素的芳族烃。

    Substituted benzoic acids, inhibitors of phospholipases A.sub.2
    70.
    发明授权
    Substituted benzoic acids, inhibitors of phospholipases A.sub.2 失效
    取代的苯甲酸，磷脂酶A2的抑制剂

    公开(公告)号：US5374772A

    公开(公告)日：1994-12-20

    申请号：US141309

    申请日：1993-10-22

    申请人： Mathew Carson ,  Ru-Jen L. Han ,  Ronald LeMahieu ,  Vincent S. Madison

    发明人： Mathew Carson ,  Ru-Jen L. Han ,  Ronald LeMahieu ,  Vincent S. Madison

    IPC分类号： A61K31/135 ,  A61K31/235 ,  A61P1/04 ,  A61P11/00 ,  A61P17/00 ,  A61P19/06 ,  A61P37/08 ,  A61P43/00 ,  C07C43/225 ,  C07C65/21 ,  C07C65/24 ,  C07C69/86 ,  C07C69/88 ,  C07C69/92 ,  C07C219/14 ,  C07C315/04 ,  C07C317/22 ,  C07C65/00

    CPC分类号： C07C317/22 ,  C07C43/225 ,  C07C65/24 ,  C07C69/92

    摘要： The invention relates to compounds of the formula ##STR1## R is hydrogen, lower alkyl, --(CH.sub.2).sub.2 N(R.sub.3).sub.2 or --CH.sub.2 OOCR.sub.3 wherein R.sub.3 is lower alkyl;R.sub.1 is CH.sub.3 (CH.sub.2).sub.n --, wherein n is 0-17, or R.sub.4 (CH.sub.2).sub.p --, wherein p is 2-18 and R.sub.4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl;R.sub.2 is R.sub.4 (CH.sub.2).sub.p --, 1-adamantyl--CO-- or diphenylmethyl--CO--, and, when R is hydrogen, pharmaceutically acceptable salts with bases.The compounds of formula I are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.

    摘要翻译： 本发明涉及下式的化合物：其中R 3为低级烷基; R 1为氢，低级烷基， - （CH 2）2 N（R 3）2或-CH 2 O R1是CH3（CH2）n-，其中n是0-17，或R4（CH2）p-，其中p是2-18，R4是1-或2-萘氧基，2,3-或3,4-二羟基苯基 苯基，苯氧基或取代的苯基或苯氧基，其中取代基选自羟基，苄氧基，甲基亚磺酰基，甲基磺酰基或苯基; R2是R4（CH2）p-，1-金刚烷基-CO-或二苯基甲基-CO-，当R是氢时，是与碱的药学上可接受的盐。 式I化合物是磷脂酶A2（PLA2's）的有效抑制剂，因此可用于治疗诸如牛皮癣，炎性肠病，哮喘，过敏，关节炎，皮炎，痛风，肺部疾病，心肌缺血和创伤等疾病 引起炎症，如脊髓损伤。