Abstract:
본 발명은 항종양제 내성의 저해 효과가 탁월하고 부작용이 없는 하기 일반식 (I)의 화합물 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 항종양제 내성 저해용 약학적 조성물에 관한 것이다.
이때, X는 CN, 카르복시, COOR 10 , SO 2 Ph 또는 SPh이고; k, l, m 및 n은 각각 독립적으로 0 내지 4의 정수이고; R 1 은 수소 또는 C 1-3 알킬이고; R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 및 R 9 는 각각 독립적으로 수소, 히드록시 또는 C 1-3 알콕시이고; R 10 은 C 1-2 알킬이다.
Abstract:
Ryridazinone derivatives of formula (I) are new. In formula (I), R1= methyl, hydroxymethyl, nitrosylmethyl, monohalomethyl, dihalomethyl or trihalomethyl; X,Y=H, nitro, cyano, -NHCOR3 or - NHSO2R4 (R3,R4= C1-6 alkyl, substituted phenyl or halogen-substd. alkyl); R2=H, C1-6 alkyl, branched alkyl, cyclic alkyl, alkene, alkyne or halogen-substd. alkyl, alkene, alkyne or phenyl-substd. alkyl, alkene, alkyne. Compounds (I) are useful as cardiotonics for enhancing contractile force of cardiac muscle and (I) have antihypertensive activities.
Abstract:
Benzopyran derivatives of formula (I) are prepd. by (a) reacting the epoxy cpd. of formula (II) with a nucleophilic agent contg. cpd. to prepare the alcohol dervs. of formula (III), in the presence of a base; (b) dehydration reacting the cpd. (III) in the presence of a base. In the formulas, R1 is -CN, -NO2, OCX1X2X3 or -SO2Rc; X1, X2 and X3 are eachly F, Cl or H; Rc is H, C1-6 alkyl or opt. satd. phenyl where satd. gp. is halogen, or straight or branched C1-3 alkyl. The obptd. benzopyran dervs. are useful for curing hypertension.