首页> 外国专利> DERIVATIVES OF CONDENSED IMIDAZOLS AS MODULATORS OF RESISTANCE TO MULTIPLE DRUGS.

DERIVATIVES OF CONDENSED IMIDAZOLS AS MODULATORS OF RESISTANCE TO MULTIPLE DRUGS.

机译:缩合咪唑衍生物作为抗多种药物的调节剂。

摘要

THIS INVENTION REFERS TO THE FORMULA COMPOUNDS (I), THE N-OXIDE FORMS, THE PHARMACEUTICALLY ACCEPTABLE ADDITION SALTS AND THE STEREOCHEMICALLY ISOMERIC FORMS, IN WHICH THE LINE STITCHED IN AN OPTIONAL LINK; N ES 1 O 2; R1 IS HYDROGEN, HALOGEN, FORMULO, RENT C1 - C4 OPTIONALLY REPLACED WITH HYDROXY, OXIALQUIL C1-C4, OXIALQUIL C1-C4 CARBONYL, IMIDAZOLYL, TIAZOLYL OR OXAZOLYL OR A RADICAL-RX-R7 -COR10 IN WHICH -X- IS A DIRECT LINK, C1-C4 CANDYL OR C2-C6 RENT; R5 IS HYDROGEN, C1-C12 RENT, AR, HET, C1-C6 RENT REPLACED WITH C1-C4 OXIALQUIL, ARYL OR HETEROARILE; R6 AND R7 ARE EACH OF THEM INDEPENDENTLY HYDROGEN OR C1-C4 RENT; R2 IS HYDROGEN, HALOGEN, RENT C1-C 4, HYDROXIAL alkyl C1-C4, ALCOXI C1-C 4 CARBONYL, CARBOXYL, FORMIL OR PHENYL; R3 IS HYDROGEN, C1-C4 RENT OR OXIALQ C1-C4 UIL; R4 IS HYDROGEN, HALOGEN, C1-C 4 RENT, C1-C4 OXIALQUIL OR C1-C4 UILO HALOALQ; Z ES -CH2-, -CH2 - CH2 -, -CH = CH-, CHOH-CH2 -, -O-CH2 -, -C (= O) -CH2 O -C (= NOH) CH2 -; A-B IS A BIVALENT RADICAL; A 1 IS A DIRECT LINK, OPTIONALLY REPLACED C1-C6 CANDYL, C1-C6-OXI-C1-C6 CANDYL 6, CARBONYL, C1-C6 CARBONYL, C1-C6 OPTIONALLY OXIALCANDYL SUBSTITUTE; A 2 IS A DIRECT LINK OR C1-C6 CANDYL; AND Q IS ARILO. PROCEDURES ARE DESCRIBED FOR THE PREPARATION OF SUCH PRODUCTS, FORMULATIONS THAT INCLUDE THESE PRODUCTS AND THEIR USE AS A MEDICINAL PRODUCT, IN PARTICULAR TO INHIBIT REVERTIRLOS EFFECTS OF MULTIPHARMACO RESISTANCE.
机译:本发明涉及式(I),N-氧化物形式,可药用的附加盐和立体化学异构形式,其中线缝在任选的链节中; N ES 1 O 2; R1是氢,卤素,甲醛,租金C1-C4可选用氢,草酸C1-C4,草酸C1-C4羰基,咪唑基,噻唑基或恶唑或自由基-RX-R7 -COR10替代-D LINK,C1-C4芳基或C2-C6租金; R5是氢,C1-C12租金,AR,HET,C1-C6租金,替换为C1-C4乙氧基,芳基或杂芳烃; R6和R7各自独立地为氢或C1-C4租金; R2是氢,卤素,C1-C4租,羟基C1-C4烷基,C1-C4醇羰基,羧基,甲酰基或苯酚; R3是氢,C1-C4租金或OXIALQ C1-C4尿素; R4是氢,卤素,C1-C 4租金,C1-C4氧喹或C1-C4 UILO HALOALQ; Z ES -CH 2-,-CH 2 -CH 2-,-CH = CH-,CHOH-CH 2-,-O-CH 2-,-C(= O)-CH 2 O-C(= NOH)CH 2-; A-B是双自由基; A 1是直接连接的,可选地取代的C1-C6取代基,C1-C6-OXI-C1-C6取代基6,羰基,C1-C6取代基,C1-C6任选的氧代取代基; A 2是直接链接或C1-C6戊基; Q是ARILO。描述了用于制备这类产品,包括这些产品的配方以及将其用作药物产品的程序,尤其是对多药耐药性的抗逆转录作用有抑制作用。

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