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    • 2. 发明授权
    • Antihypertensive 2-phenyl Hantzsch dihydropyridines
    • 抗高血压2-苯基汉坦二氢吡啶类
    • US4607041A
    • 1986-08-19
    • US601389
    • 1984-04-17
    • Andrew J. G. BaxterJohn DixonThomas McInallyAlan C. Tinker
    • Andrew J. G. BaxterJohn DixonThomas McInallyAlan C. Tinker
    • C07C17/093C07C45/00C07C47/55C07C205/56C07D205/04C07D211/78C07D211/90C07D305/08C07D309/12C07D401/04C07D405/04C07D413/04C07D521/00A61K31/445C07D413/14
    • C07D231/12C07C17/093C07C205/56C07C45/00C07C47/55C07D205/04C07D211/78C07D211/90C07D233/56C07D249/08C07D305/08C07D309/12C07D401/04C07D405/04C07D413/04
    • There are described compounds of formula I, ##STR1## in which R.sub.1 represents benzofurazanyl, pyridyl or phenyl, the pyridyl or phenyl being substituted by one or more of the groups halogen, nitro, --CN, --OR.sub.9, --S(O).sub.p R.sub.9, or alkyl C1 to 6 optionally substituted by halogen,p is 0, 1 or 2,R.sub.2 and R.sub.3, which may be the same or different, each represent hydrogen; alkyl C1 to 6 optionally substituted by one or more of the groups halogen, cyano, --XR.sub.4, --NR.sub.5 R.sub.6 or phenyl; cycloalkyl C3 to 8 optionally substituted by alkyl C1 to 6; a 4, 5 or 6 membered oxygen or nitrogen containing heterocyclic ring which is optionally substituted by alkyl C1 to 6 the alkyl in turn optionally being substituted by one or more phenyl groups;R.sub.5 and R.sub.6, which may be the same or different, each represent alkyl C1 to 6 optionally substituted by phenyl,Y and Z together form a bond, and additionally, when R.sub.8 is an electron withdrawing group Y may be hydrogen and Z may be hydroxy,one of R.sub.7 and R.sub.8 represents alkyl C1 to 6 and the other represents phenyl,or R.sub.7 and R.sub.8 may be the same or different and each represents phenyl optionally substituted by one or more of alkyl C1 to 6, halogen, alkoxy C1 to 6 or nitro; amino; alkyl C1 to 6 substituted by halogen; --CN; --CH.sub.2 OH; --CHO or --CH(OR.sub.9).sub.2,X is O or S,R.sub.4 is alkyl C1 to 6 or phenyl,R.sub.9 is alkyl C1 to 6, with certain provisons.There are also described processes for making the compounds, and their formulation and use as pharmaceuticals for treatment of hypertension, angina, or congestive heart failure.
    • 描述式Ⅰ化合物,其中R1代表苯并呋喃基,吡啶基或苯基,吡啶基或苯基被一个或多个卤素,硝基,-CN,-OR9,-S(O) pR9或任选被卤素取代的C 1-6的烷基,p为0,1或2,R 2和R 3可以相同或不同,各自表示氢; 任选被一个或多个卤素,氰基,-XR 4,-NR 5 R 6或苯基基团取代的C 1-6烷基; 任选被C1至6的烷基取代的环烷基C3至8; 任选被烷基C1至6取代的4,5或6元含氧或含氮杂环,所述烷基依次可选地被一个或多个苯基取代; R 5和R 6可以相同或不同,各自表示任选被苯基取代的烷基C1至6,Y和Z一起形成键,另外,当R8是吸电子基团时,Y可以是氢,Z可以是羟基 R 7和R 8中的一个表示烷基C1至6,另一个表示苯基,或者R 7和R 8可以相同或不同,表示任选被一个或多个烷基C1至6,卤素,烷氧基C1至6或 硝基 氨基; 由卤素取代的C1至6烷基; -CN; -CH 2 OH; -CHO或-CH(OR 9)2,X为O或S,R 4为C 1-6烷基或苯基,R 9为烷基C 1-6,具有一定条件。 还描述了制备化合物的方法及其制剂和用作治疗高血压,心绞痛或充血性心力衰竭的药物。