摘要:
This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
摘要:
Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl, R2 is lower alkyl; R3 is hydroxy or protected hydroxy; X is O or S; and -A- is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective
摘要翻译:具有由式(I)表示的腺苷脱氨酶抑制活性的咪唑化合物:其中R 1是任选取代的芳基或任选取代的杂芳基,R 2是低级烷基; R 3是羟基或被保护的羟基; X是O或S; 和-A-是低级亚烷基,其前药或其盐。 该化合物可用于治疗和/或预防腺苷有效的疾病
摘要:
Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino, R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino, R.sup.3 is hydrogen or an organic group, R.sup.4 is hydrogen or lower alkyl, R.sup.8 is hydrogen or lower alkyl, and --Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
摘要:
wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 R is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
摘要:
Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I): wherein R1 is optionally substituted aryl or optionally substituted heteroaryl, R2 is lower alkyl; R3 is hydroxy or protected hydroxy; X is O or S; and -A- is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
摘要翻译:具有由式(I)表示的腺苷脱氨酶抑制活性的咪唑化合物:其中R 1是任选取代的芳基或任选取代的杂芳基,R 2是低级烷基; R 3是羟基或被保护的羟基; X是O或S; 和-A-是低级亚烷基,其前药或其盐。 该化合物可用于治疗和/或预防腺苷有效的疾病。
摘要:
A compound of the formula (1): wherein R1 is cyano, and the like; R2 is hydroxy, and the like; R3 is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译:式(1)的化合物:其中R 1是氰基等; R 2是羟基等; R 3是(低级)烷氧基等; X和Y各自为CH或N; 或其药学上可接受的盐,其可用作药物。
摘要:
A compound of the formula (I): wherein R1 is hydrogen, halogen, carbamoyl, cyano, formyl, or lower alkyl optionally substituted with halogen, amino or a protected amino; R2 is hydrogen, halogen, cyano or lower alkoxy; R3 is phenyl or pyridyl, each of which is substituted with lower alkoxy; and R4 is lower alkoxy; provided that either R1 or R2 is hydrogen, then the other is other than hydrogen, or its salts, which are useful as a medicament.
摘要翻译:式(I)的化合物:其中R 1是氢,卤素,氨基甲酰基,氰基,甲酰基或任选被卤素,氨基或被保护的氨基取代的低级烷基; R 2是氢,卤素,氰基或低级烷氧基; R 3是苯基或吡啶基,各自被低级烷氧基取代; R 4是低级烷氧基; 条件是R 1或R 2 2都是氢,则另一个不是用作药物的氢或其盐。
摘要:
A compound of the formula (I): wherein R1 is lower alkyl which is optionally substituted with halogen, cyano, N,N-di(lower)alkylcarbamoyl, phenyl optionally substituted with halogen, or heterocyclic group, cyclo(lower)alkyl, lower alkynyl, or N,N-di(lower)alkylcarbamoyl; R2 is lower alkyl, lower alkoxy, cyano, or 1H-pyrrol-1-yl; R3 is lower alkyl, lower alkoxy, or cyano; X is O, S, SO or SO2; Y and Z are each CH or N; and m is 0 or 1; or salts thereof, which are useful as a medicament.
摘要翻译:氰基,N,N-二(低级)烷基氨基甲酰基,任选被卤素取代的苯基或杂环基的式(I)化合物:其中R 1是任选被卤素, ,低级(低级)烷基,低级炔基或N,N-二(低级)烷基氨基甲酰基; R 2是低级烷基,低级烷氧基,氰基或1H-吡咯-1-基; R 3是低级烷基,低级烷氧基或氰基; X是O,S,SO或SO 2; Y和Z各自为CH或N; m为0或1; 或其盐,其可用作药物。
摘要:
Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1 is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s); R2 is hydrogen or lower alkyl; R3 is hydroxy or protected hydroxy; R4 is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and —A— is —Q— or —O—Q—, wherein Q is single bond or lower alkylene, provided that when R2 is lower alkyl, then R1 is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.