摘要:
Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension, and atherosclerosis are compounds depicted in formulas (1), (2), and (3): ##STR1## wherein: n is 2 or 3;R.sub.1 is CH.sub.2 OH, CHO, CO.sub.2 R or CO.sub.2 H;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl having 5-10 carbon atoms, ##STR2## optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen,in whicha is 0, 1 or 2;b is 3-7;m is 1 or 2; andR is ##STR3## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms,and the pharmaceutically acceptable, non-toxic salts and esters thereof.
摘要:
The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.
摘要:
The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.
摘要:
Novel compounds of the general formula ##STR1## and the pharmaceutically acceptable esters and acid addition salts thereof, wherein:R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, N-optionally substituted alkylamido, except that when R.sup.1 is methyl, R.sup.4 is not methyl; orR.sup.2 and R.sup.3 together form --OCH.sub.2 O--;R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are each independently hydrogen, lower acyl, aminocarbonylmethyl, cyano, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, di-lower alkyl amino; orR.sup.6 and R.sup.7 together form --CH.dbd.CH--CH.dbd.CH--;R.sup.7 and R.sup.8 together form --OCH.sub.2 O--;R.sup.11 and R.sup.12 are each independently hydrogen or lower alkyl; andW is oxygen or sulfur.These cardioselective compounds have calcium entry blockade properties and therefore are useful in therapy in the treatment of cardiovascular diseases, including arrhythmias, variant and exercise induced angina and myocardial infarction.
摘要:
Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:n is an integer equal to 0, 1, 2 or 3;R.sup.1 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl lower alkyl;each R is independently hydrogen, lower alkyl, optionally substituted phenyl, or optionally substituted phenyl lower alkyl;are .alpha..sub.2 blockers, and, therefore, are useful in treating essential hypertension and depression, and in inhibiting platelet aggregation.
摘要翻译:式(I)的化合物及其药学上可接受的酸加成盐,其中:n为等于0,1,2或3的整数; R 1是氢,低级烷基,任选取代的苯基或任选取代的苯基低级烷基; 每个R独立地为氢,低级烷基,任选取代的苯基或任选取代的苯基低级烷基; 是α2受体阻滞剂,因此可用于治疗原发性高血压和抑郁症,以及抑制血小板聚集。
摘要:
2-(1,4-Benzodioxan-2-ylalkyl)imidazoles having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, alkyl, optionally substituted phenyl, and optionally substituted phenyl lower alkyl;R.sup.3 is hydrogen, alkyl, or optionally substituted phenyl lower alkyl;n is an integer equal to 0, 1 or 2;with the proviso that R.sup.1, R.sup.2 and R.sup.3 cannot all be hydrogen and/or alkyl; and the pharmaceutically acceptable acid addition salts thereof, are useful as antidepressants.