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    • 2. 发明授权
    • Benzimidazoles, and pharmaceutical preparations containing these
compounds
    • 苯并咪唑和含有这些化合物的药物制剂
    • US4957920A
    • 1990-09-18
    • US168273
    • 1988-03-15
    • Peter MorsdorfHelmut SchickanederRolf HerterVolker PfahlertHeidrun EnglerKurt H. Ahrens
    • Peter MorsdorfHelmut SchickanederRolf HerterVolker PfahlertHeidrun EnglerKurt H. Ahrens
    • A61K31/505A61P9/06C07D403/04C07D403/14
    • C07D403/04
    • New benzimidazoles corresponding to the general formula I ##STR1## are described, in which the pyridazinone ring is attached in the 5- or 6- position of the benzimidazole ring and R.sup.1 denotes a hydrogen atom or a straight chained or branched C.sub.1 to C.sub.4 alkyl group, R.sup.2 denotes a hydrogen atom, a straight chained or branched C.sub.1 to C.sub.4 alkyl group, a C.sub.1 to C.sub.4 alkoxy group, a hydroxy group, a halogen atom, an amino group or a nitro group, A denotes a hydrogen atom, a group of the formula ##STR2## wherein R.sup.3 denotes a hydrogen atom, an optionally substituted C.sub.1 to C.sub.4 alkyl group or a C.sub.1 to C.sub.4 alkoxy group and B denotes a cyano group, a benzoyl group or a phenylsulphonyl group, or A denotes a group of the formula ##STR3## in which m has the value of 2 or 3 and n represents an integer from 1 to 6, and the physiologically acceptable salts thereof as well as processes for their preparation and pharmaceutical preparations containing these compounds. These compounds are new, effective, positive inotropic substances which do not act by the mechanism of phosphodiesterase inhibition.
    • 描述了对应于通式I(I)的新的苯并咪唑,其中哒嗪酮环连接在苯并咪唑环的5-或6-位,R1表示氢原子或直链或支链C1至 C4烷基,R2表示氢原子,直链或支链C1〜C4烷基,C1〜C4烷氧基,羟基,卤素原子,氨基或硝基,A表示氢原子, 式中,R 3表示氢原子,可以具有取代基的C1〜C4烷基或C1〜C4烷氧基,B表示氰基,苯甲酰基或苯基磺酰基,A表示基团 其中m具有2或3的数值,n表示1至6的整数,以及其生理上可接受的盐以及其制备方法和含有这些化合物的药物制剂。 这些化合物是新的,有效的正性肌力物质,不受磷酸二酯酶抑制机制的作用。
    • 8. 发明授权
    • Benzothiazole derivatives, processes for their preparation and
pharmaceutical compositions containing these compounds
    • 苯并噻唑衍生物,其制备方法和含有这些化合物的药物组合物
    • US4732986A
    • 1988-03-22
    • US51214
    • 1987-05-12
    • Kay BruneHeidrun EnglerIstvan SzelenyiPeter MorsdorfHelmut SchickanederKurt H. Ahrens
    • Kay BruneHeidrun EnglerIstvan SzelenyiPeter MorsdorfHelmut SchickanederKurt H. Ahrens
    • A61K31/425A61K31/428A61P11/00A61P29/00A61P37/08A61P43/00C07D277/82C12N9/99
    • C07D277/82
    • Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup.13 represent, independently of one another, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group or R.sup.6 and R.sup.7 represent the group ##STR6## wherein R.sup.14 denotes a linear C.sub.1 -C.sub.3 -alkyl group, as well as the physiologically acceptable salts thereof, a process for the preparation of these compounds, and a pharmaceutical preparation containing them, are described.
    • 对应于通式I(I)的苯并噻唑衍生物,其中R 1,R 2,R 3和R 4彼此独立地表示氢原子,卤素原子,直链C 1 -C 3 - 烷基或直链C 1 -C 3 - C 3 - 烷氧基,R 5表示氢原子或直链C 1 -C 3 - 烷基,R 6表示氢原子,R 7表示甲酰基,式◎的烷氧基,其中,R 8表示直链或支链 或者它表示下式的酰基,其中R 9表示直链C 1 -C 3 - 烷基,或者R 6和R 7一起表示基团,其中R 10和R 11独立地表示 另一方面,氢原子或直链C 1 -C 6 - 烷基或R 6和R 7表示基团,其中R 12和R 13彼此独立地表示直链C 1 -C 3 - 烷基或直链C 1 -C 3 - 烷氧基或R6和R7表示基团,其中R14表示直链C1-C3-烷基,以及生理记录 描述了其可接受的盐,制备这些化合物的方法和含有它们的药物制剂。