Abstract:
본 발명은 하기 일반식(I)의 화합물 또는 그의 약학적으로 허용가능한 염, 그의 제조방법 및 상기 화합물 또는 그의 염을 포함하는 약학적 조성물을 제공한다.
상기식에서, A는 직쇄, 분지쇄 또는 시클릭 C 1 -C 6 알킬 또는 OR 1 (여기에서, R 1 은 H 또는 직쇄, 분지쇄 또는 시클릭 C 1 -C 6 알킬임)이고, B는 할로겐, CF 3 또는 CF 2 CF 3 이며, X는 N 또는 N-옥사이드이고, Y는 -CH 2 -, -CH(OR 1 )- 또는 -C(=O)- 이며, Z는 H, 직쇄, 분지쇄 또는 시클릭 C 1 -C 6 알킬, 알케닐 또는 알키닐이다.
Abstract:
The cpd. of formula (I-a) is prepd. by (a) reacting ketone derivatives of formula (II) with trifluorosulfonic acid anhydride and ter-amine, or making the ketone derivatives (II) to enolate with a base and then reacting N-phenyl trifluoromethane sulfonimide to convert to the vinyl triflate derivs. of formula (III); and (b) reacting the derivs. (III) with pyridyl trialkyline derivs. of formula (IV) in the presence of palladium catalyst and chloride. In the formulas, R1 is -CN, -NO2, -OCX1X2X3, -NH2, -NHSO2Ra etc; X1, X2, and X3 are F, Cl or H; R3 is H or C1-6 alkyl or phenyl; R4 is C1-4 alkyl.
Abstract:
Novel benzopyran derivatives of formula (I) are prepared by O- nitration at C-3 hydroxy group of cromakalim of formula (II) in the anhydride acetic acid or C.H2SO4. In the formula (I), R1 R2=H, NO2, nitryl; R3= 2-oxo-1-pyrrolidinyl. Compound (I) are useful as antihypertensive and vasodilating agents.
Abstract:
Indane derivs. of formula (I) are new. In (I), R1= nitro, nitrile, halogen, amino, CF3, -(C=NH)-OMe, -NHCOCS3, -NHCSCX3, - COR4, -OCX3 OR -CSR4; X=H or halogen; R4=H, amino, lower alkyl or alkoxy, or opt. substd. phenyl; R2=-NO5R6, a gp. of formula (II), a gp. of formula (III), a gp. of formula (IV), etc.; R5 and R6 each=H, lower alkyl, cyclopropyl, cyclopropyl methyl or benzyl; n = 1 or 2; Y=CH2, O, S or -NR4; R3=H, OH, nitrooxy, formyloxy, alkanoyloxy, haloalkanoyloxy, alkoxycarbonyl, aroyloxy or carbamoyloxy. The cpds. (2) may be used in the treatment of hypertension.
Abstract:
5-[4-[5-[3-(4-Fluorophenyl) isoxazolidyl phenyl -(1H)tetrazole of formula (I) is new. Also claimed is the prepn. of (I) which comprises (a) reacting an aldehyde deriv. of formula (II) with a hydroxy amine cpd. to obtain an oxime deriv. of formula (III), (b) halogenating (III) and reacting the obtd. halogenated oxime deriv. with a styrene cpd. of formula (IV), and (c) reacting the obtd. cpd. with an azide cpd. to form (I). The cpd. (I) has an effect on blood pressure and on the contractility of the cardiac muscle.