首页> 外国专利> BENZOPYRAN(4,3-c)PYRAZOLE OR BENZOTHIOPYRAN(4,3-c)PYRAZOLE DERIVATIVES, PROCESSES OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE COMPRISED

BENZOPYRAN(4,3-c)PYRAZOLE OR BENZOTHIOPYRAN(4,3-c)PYRAZOLE DERIVATIVES, PROCESSES OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE COMPRISED

机译:苯并吡喃(4,3-c)吡唑或苯并噻吩并(4,3-c)吡唑衍生物,其制备方法和组成中的药物成分

摘要

The invention relates to compounds having the general formula (I) CHEM wherein X represents an oxygen atom or a -S(O)n-group, wherein n is zero, 1 or 2; R1 represents C1-C6 alkyl, benzyl, pyridyl, or phenyl, the phenyl being unsubstituted or substituted by one or two substituents chosen independently from halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, nitro, amino, formylamino and C2-C8 alkanoylamino; each of R2 and R3 is independently: a) hydrogen, halogen or C1-C6 alkyl; b) hydrogen, C1-C6 alkoxy or C3-C4 alkenyloxy; or c) nitro, amino, formylamino or C2-C8 alkanoylamino; R4 represents hydrogen or C1-C6 alkyl; and Q represents hydrogen, carboxy, CONH2, C2-C7 alkoxycarbonyl CHEM wherein Ra represents hydrogen or C1-C20 alkyl and Rb represents C1-C20 alkyl or a -(CH2)m-R5 group, wherein m is zero, 1 or 2 and R5 is: a') C5-C8 cycloalkyl; b') pyridyl, unsubstituted or substituted by one or two substituents chosen independently from halogen, C1-C6 alkyl and C1-C6 alkoxy; or c') phenyl, unsubstituted or substituted by one or two substituents independently chosen from halogen, CF3, C1-C6 alkyl, C1-C6 alkoxy, amino, nitro, formylamino, C2-C8 alkanoylamino, di (C1-C6 alkyl) amino, hydroxy, formyloxy and C2-C8 alkanoyloxy, and the pharmaceutically acceptable salts thereof, which possess immunodulating activity and are useful e.g. in the treatment of neoplastic diseases and acute and chronic infections of both bacterial and viral origin in mammals.
机译:本发明涉及具有通式(I)的化合物,其中X代表氧原子或-S(O)n-基团,其中n为零,1或2; R1代表C1-C6烷基,苄基,吡啶基或苯基,该苯基未被取代或被一个或两个独立地选自卤素,三氟甲基,C1-C6烷基,C1-C6烷氧基,硝基,氨基,甲酰氨基和C2-的取代基取代C8烷酰基氨基; R2和R3各自独立地是:a)氢,卤素或C1-C6烷基; b)氢,C1-C6烷氧基或C3-C4烯氧基; c)硝基,氨基,甲酰基氨基或C2-C8烷酰基氨基;或R4代表氢或C1-C6烷基; Q表示氢,羧基,CONH 2,C 2 -C 7烷氧羰基,其中Ra表示氢或C 1 -C 20烷基,R b表示C 1 -C 20烷基或-(CH 2)m -R 5基团,其中m为零,1或2和R5为:a')C5-C8环烷基; b')未被取代或被一个或两个独立地选自卤素,C1-C6烷基和C1-C6烷氧基的取代基取代的吡啶基;或c')未被取代或被一个或两个独立地选自卤素,CF 3,C 1 -C 6烷基,C 1 -C 6烷氧基,氨基,硝基,甲酰基氨基,C 2 -C 8烷酰基氨基,二(C 1 -C 6烷基)氨基的取代基取代的苯基,羟基,甲氧基和C 2 -C 8烷酰氧基及其药学上可接受的盐,它们具有免疫调节活性,并且可用于例如在哺乳动物中治疗肿瘤性疾病以及细菌和病毒来源的急性和慢性感染。

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