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    • 6. 发明授权
    • Antiviral compounds and antihypertensive compounds
    • 抗病毒化合物和抗高血压化合物
    • US5175151A
    • 1992-12-29
    • US830958
    • 1992-02-05
    • Adriano AfonsoJay WeinsteinMargaret J. Gentles
    • Adriano AfonsoJay WeinsteinMargaret J. Gentles
    • C07D215/22C07D215/56C07D311/18C07F7/18
    • C07D215/22C07D215/56C07D311/18C07F7/1856
    • Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0.Also disclosed is a compound of Structure B ##STR2## useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B ##STR3## is reacted with an alkoxide R.sub.1 O.sup.- M.sup.+ in a solvent comprising the corresponding alcohol R.sub.1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.
    • 公开了可用作抗高血压剂的化合物或抗DNA病毒的抗病毒剂如疱疹病毒。 化合物由式1.0表示:其中药学上可接受的盐和溶剂合物。 公开了含有由式1.0表示的化合物的药物组合物。 还公开了使用由式1.0表示的化合物治疗高血压或病毒感染的方法。 还公开了可用作制备式1.0化合物的中间体的结构B B的化合物。 还公开了制备式1.0化合物的方法。 在该方法中,将结构B B的化合物与醇盐R 1 O-M +在包含醇盐的相应醇R 1 OH的溶剂中反应。 任选地,有机共溶剂可以与溶剂一起使用。
    • 7. 发明授权
    • Tricyclic compounds having activity as RAS-FPT inhibitors
    • 具有作为RAS-FPT抑制剂的活性的三环化合物
    • US6130229A
    • 2000-10-10
    • US946527
    • 1997-10-07
    • Adriano AfonsoJoseph M. KellyStuart B. RosenblumRonald L. WolinJay Weinstein
    • Adriano AfonsoJoseph M. KellyStuart B. RosenblumRonald L. WolinJay Weinstein
    • C07D491/04C07D495/04A61K31/445
    • C07D491/04C07D495/04
    • Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl;each X.sup.2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl;n is 1 or 2;Y is selected from the group consisting of S(O).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl;R.sup.1 and R.sup.2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR.sup.5 ;A . . . is C=, CH-- or N--;R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein:Z is O, =CH--CN, or =N--CN;one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ;R.sup.3 is aryl, heteroaryl or heterocycloalkyl, with the proviso that R.sup.3 can also be lower alkyl when Z is =N--CN;and their pharmaceutically acceptable acid addition salts; have activity as Ras-FPT inhibitors. They can be used, e.g., in pharmaceutical compositions, for inhibiting the abnormal growth of cells and for inhibiting proliferative diseases. Processes for their preparation, and useful intermediates, are also disclosed.
    • 式I化合物:其中:X 1是氢,卤素,CF 3,硝基,NH 2或低级烷基; 每个X 2独立地选自氢,卤素,低级烷氧基和低级烷基; n为1或2; Y选自S(O)p,O和NR5,其中p为0,1或2,R5为氢,烷基,芳基,环烷基,低级烷氧羰基,氨基羰基或酰基; R 1和R 2可以相同或不同,选自氢和低级烷基,或者当Y是NR 5时可以一起形成氧原子; 一个 。 。 。 是C =,CH-或N-; R为-CZ-Y1-Y2-R3,其中:Z为O,= CH-CN或= N-CN; Y1和Y2之一是键,-CO-,O,S或-NR4-,另一个是(CH2)m,其中m是0或1-4的整数,R4是H或烷基, 条件是当Z为O且m为0时,则Y1或Y2选自-CO-,O,S或-NR4; R3是芳基,杂芳基或杂环烷基,条件是当Z = N-CN时,R3也可以是低级烷基; 及其药学上可接受的酸加成盐; 具有作为Ras-FPT抑制剂的活性。 它们可以用于例如药物组合物中,用于抑制细胞异常生长和抑制增殖性疾病。 还公开了它们的制备方法和有用的中间体。