摘要:
The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C1-4-alkylene; L = a simple bond or C1-2-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R1 = possibly substituted aryl or heteroaryl; R2, R3 = H, C1-3-alkyl, C1-3-fluoralkyl or R2 et R3 forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R4 = H, C1-5-alkyl, C1-3-fluoralkyl, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-3-alkylene, C1-3-alkyl-O-C1-3-alkylene, HO-C1-3-alkylene, C1-3-alkyl-X-C1-3-alkylene, wherein X = S, SO or S02; or R4 = RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O-, aryl-O-C1-3-alkylene, aryl-C1-3-alkylene-O-C1-3-alkylene, heteroaryl or heteroaryl-C1-3-alkylene; R5 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3-alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R5 = RaRbN-, RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O- or heteroaryl; R6 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, -CN, RaRbN-, RaRbN-C1-3-alkylene, aryl or heteroaryl ; R7 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3--alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R7, = RaRbN-, RaRbN-C1-3--alkylene, ReRbNC(O)-, C1-3-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R8 = H, halogen, C1-5-alkyl, C1-5-alkoxy, C1-3-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.
摘要:
The invention provided a method of synthesizing β -L-5-fluoro-2´,3´-dideoxy-2´,3´-didehydrocytidine (β -L-FD4C). The method allows for large-scale production of β -L-FD4C in an efficient, cost-efficient, and environmentally sound manner.
摘要:
Pyrimidine derivatives represented by general formula (I) which have an excellent herbicidal activity and a selectivity on crops from weeds, and herbicides containing these pyrimidine derivatives as the active ingredient. In said formula, R1 represents hydrogen, alkyl, haloalkyl, etc.; R2 represents alkyl, optionally substituted phenyl, etc.; R3 represents hydrogen, alkyl, alkynyl, etc.; R7 represents hydrogen, halogeno, alkyl, etc.; R8 represents hydrogen, alkyl, etc.; W represents -C(=Q)Z- or -SO¿2?- (wherein Q represents O or S; and Z represents O, S, -C(R?4)R5-, NR6¿, etc. (wherein R?4 and R5¿ represent each hydrogen, alkyl, alkoxy, etc.; and R6 represents hydrogen or alkyl;)); and Ar represents optionally substituted phenyl, optionally substituted pyridyl, etc.
摘要:
A medicine containing a compound represented by general formula (I) or a salt thereof as the active ingredient, having an excellent activity of inhibiting neuron necrosis, and being useful as a remedy for cerebrovascular disorder, wherein R1 represents aryl or heteroaryl; R2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino or phenyl; R?3 and R4¿ represent each hydrogen or alkyl, or R?3 and R4¿ are combined with the adjacent nitrogen atom to represent a 5- to 7-membered cyclic amino group NR3R4; A represents C¿2?-C10 alkylene; W represents O, S or (CH)n (wherein CH may be substituted by alkyl, and n represents 0, 1 or 2); and X, Y and Z represent each independently CH (wherein H may be replaced by alkyl) or N, provided the case where all of X, Y and Z are CH at the same time is excepted.
摘要翻译:一种药物组合物,其包含以下通式Ⅺ或其盐的化合物。 其中R 1表示芳基或杂芳基。 R 2表示氢,烷基,烯基,环烷基,环烷基烷基,羟基烷基,卤代烷基,烷氧基,烷硫基,氨基,单烷基氨基,二烷基氨基或苯基。 R 3和R 4独立地表示氢或烷基或R 3和R 4与相邻的N原子一起表示5-至7-元环状氨基。 A表示C2-10亚烷基。 W表示O,S或(CH)n(其中CH可以被烷基取代; n是0,1或2的整数)。 X,Y和Z可以相同或不同,各自表示CH(其可以被烷基取代)或N.可以排除X,Y和Z同时表示CH的情况。 本发明化合物具有优异的神经元死亡抑制活性,可用作脑血管疾病的治疗药物。