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    • 4. 发明授权
    • Method of increasing intracellular accumulation of hydrophilic anionic
agents using gemfibrizol
    • 使用吉非贝隆增加亲水性阴离子剂的细胞内积累的方法
    • US5422372A
    • 1995-06-06
    • US77755
    • 1993-06-15
    • Samuel C. SilversteinHarold C. NeuCharles Cao
    • Samuel C. SilversteinHarold C. NeuCharles Cao
    • A61K31/19A61K31/43A61K31/495A61K31/545
    • A61K31/43A61K31/19A61K31/495A61K31/545
    • This invention provides an improved therapeutic method which comprises administering to a mammal a therapeutic agent and 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog thereof, in an amount effective to improve the efficacy of the therapeutic agent. Also provided by this invention is an improved therapeutic method which comprises administering to a mammal a therapeutic agent and 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog thereof, in an amount effective to improve the efficacy of the therapeutic agent. Further provided by this invention is a method of treating an intracellular bacterial infection which comprises contacting the infected cell with an effective amount of a therapeutic agent and with an effective amount of 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid, or a structural analog therof, effective to treat an intracellular bacterial infection. A pharmaceutical composition is further provided by this invention wherein the composition comprises a therapeutic agent and 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid, or a structural analog thereof, and a pharmaceutically acceptable carrier.
    • 本发明提供了一种改进的治疗方法,其包括以有效提高功效的量向哺乳动物施用治疗剂和5-(2,5-二甲基苯氧基)-2,2-二甲基 - 戊酸或其结构类似物 的治疗剂。 本发明还提供了一种改进的治疗方法,其包括向哺乳动物施用有效剂量的治疗剂和5-(2,5-二甲基苯氧基)-2,2-二甲基 - 戊酸或其结构类似物 提高治疗剂的疗效。 本发明进一步提供了一种治疗细胞内细菌感染的方法,其包括将感染的细胞与有效量的治疗剂和有效量的5-(2,5-二甲基苯氧基)-2,2-二甲基 - 戊酸或结构类似物,有效治疗细胞内细菌感染。 通过本发明进一步提供药物组合物,其中组合物包含治疗剂和5-(2,5-二甲基苯氧基)-2,2-二甲基戊酸或其结构类似物和药学上可接受的载体。
    • 8. 发明授权
    • Antimicrobial activity of gemfibrozil
    • 吉非贝齐的抗菌活性
    • US06713043B2
    • 2004-03-30
    • US08608712
    • 1996-02-29
    • Christina KabbashHoward A. ShumanSamuel C. SilversteinPhyllis Della-Latta
    • Christina KabbashHoward A. ShumanSamuel C. SilversteinPhyllis Della-Latta
    • A61K5100
    • A61K31/192Y02A50/478Y02A50/481
    • The present invention provides for a method for inhibiting growth of a bacterium which consists essentially of contacting the bacterium with a compound having the structure: wherein each of R1, R2, R3, R4, R5 and R6 may be independently H, F, Cl, Br, I, —OH, —OR7, —CN, —COR7, —SR7, —N(R7)2, —NR7COR8, —NO2, —(CH2)pOR7, —(CH2)pX(R7)2, —(CH2)pXR7COR8, a straight chain or branched, substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C3-C10 cycloalkenyl, thioalkyl, methylene thioalkyl, acyl, phenyl, substituted phenyl, or heteroaryl; wherein a linkage to the benzene ring may alternatively be —N—, —S-—, —O— or —C—; wherein R7 or R8 may be independently H, F, Cl, Br, I, —OH, —CN, —COH, —SH2, —NH2, —NHCOH, —(CH2)pOH, —(CH2)pX(CH2), —(CH2)pXCOH, a straight chain or branched, substituted or unsubstituted C1-C10 alkyl, thioalkyl, methylene thioalkyl, acyl, phenyl, substituted phenyl, or heteroaryl; wherein A may be —N2—, —NH—, —C═C═CH2—, —C≡C—C2HOH—, —C≡C—CH2—, —CH2—CH2—O—, —CH2—CH2—CH2—O—, —S—, —S(═O)2, —C═O—, —C═O—O—, —NH—C═O—, —C═O—NH—.
    • 本发明提供了一种抑制细菌生长的方法,其基本上使细菌与具有以下结构的化合物接触:其中R 1,R 2,R 3,R 4,R 5和R 6各自独立地为H,F,Cl, Br,I,-OH,-OR7,-CN,-COR7,-SR7,-N(R7)2,-NR7COR8,-NO2, - (CH2)pOR7, - (CH2)pX(R7)2, - ( CH2)pXR7COR8,直链或支链的取代或未取代的C1-C10烷基,C2-C10烯基,C2-C10炔基,C3-C10环烷基,C3-C10环烯基,硫代烷基,亚甲基硫代烷基,酰基,苯基,取代的苯基, 或杂芳基; 其中与苯环的连接可以是-N-,-S-,-O-或-C-; 其中R 7或R 8可以独立地是H,F,Cl,Br,I,-OH,-CN,-COH,-SH 2,-NH 2,-NHCOH, - (CH 2)p OH, - (CH 2)p X(CH 2) - (CH 2)pXCOH,直链或支链的取代或未取代的C 1 -C 10烷基,硫代烷基,亚甲硫基烷基,酰基,苯基,取代的苯基或杂芳基; 其中A可以是-N 2 - , - NH - , - C = C = CH 2 - , - C = C-C 2 HOH - , - C = C-CH 2 - , - CH 2 -CH 2 -O - , - CH 2 -CH 2 -CH -O - , - S - , - S(= O)2,-C = O - , - C = OO - , - NH-C = O - , - C = O-NH-。