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    • 9. 发明公开
    • Polyhydroxybenzyloxypropanolamines
    • EP0373591A3
    • 1991-03-20
    • EP89122921.3
    • 1989-12-12
    • THE DU PONT MERCK PHARMACEUTICAL COMPANY
    • Patil, GhanshyamMatier, William L.Mai, Khuong H.X.
    • C07C217/28A61K31/135C07C233/16A61K31/16C07C233/62C07C233/78
    • C07C233/62C07C217/28C07C233/18C07C233/78
    • Compounds of the present invention, are represented by the general formula
      wherein R₁ group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R₂, R₃ and R₄ are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NHCOR₅, -NHCONR₅R₆, or -NHCOOR₅ wherein R₅ and R₆ may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, cycloalkyl of from 3 to about 8 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 6 carbon atoms, phenyl which may be unsubstituted or substituted with alkyl of 1 to 6 carbon atoms; furanyl, thiophenyl, imidazole, oxazole or indole, aralkyl wherein the alkyl group contains from 1 to about 6 carbon atoms and the aryl group represents phenyl unsubstituted or substituted with alkyl of from 1 to about 6 carbon atoms, or R₅ and R₆ may together with N form a pyrrolidine, piperidine, piperazine, morpholine or thiomorpholine ring and except that R₅ is not hydrogen when B is -NHCOOR₅; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment or prophylaxis of cardiac disorders or in the treatment of glaucoma.
    • 本发明化合物由下列通式表示:其中R 1基团可以是1至约6个碳原子的烷基,2至约6个碳原子的链烯基,2至约10个碳原子的炔基, 烷基含有1至约6个碳原子的卤素,乙酰氨基,氨基,硝基,1至约6个碳原子的烷基氨基,羟基,1至约6个碳原子的羟基烷基,氰基或芳基烷氧基,其中烷基含有 1至约6个碳原子,R 2,R 3和R 4是氢或羟基或氢或羟基的组合; W表示1至约10个碳原子的亚烷基; 和B代表-NHCOR 5,-NHCONR 5 R 6或-NHCOOR 5,其中R 5和R 6可以相同或不同,代表氢,1至约6个碳原子的烷基,烷氧基烷基,其中烷基可以相同或不同,并且含有 1至约6个碳原子的环烷基,3至约8个碳原子的环烷基,2至约6个碳原子的烯基,2至约6个碳原子的炔基,可以未被取代或被1至6个 碳原子; 呋喃基,噻吩基,咪唑,恶唑或吲哚,其中烷基含有1至约6个碳原子的芳烷基和芳基表示未被取代或被1至约6个碳原子的烷基取代的苯基,或者R 5和R 6可以与 N形成吡咯烷,哌啶,哌嗪,吗啉或硫代吗啉环,并且当B是-NHCOOR 5时R 5不是氢; 或其药学上可接受的盐。 该化合物可用于治疗或预防心脏疾病或治疗青光眼。