Hydroxystyrene compounds having tyrosine kinase inhibiting activity
    3.
    发明授权
    Hydroxystyrene compounds having tyrosine kinase inhibiting activity 失效
    具有酪氨酸激酶抑制活性的羟基苯乙烯化合物

    公开(公告)号:US5202341A

    公开(公告)日:1993-04-13

    申请号:US735581

    申请日:1991-07-25

    摘要: A hydroxystyrene derivative represented by the formula (I): ##STR1## wherein when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O- (R.sup.5 : H, a C.sub.1 to C.sub.5 alkyl group or benzyl group) and R.sup.2 : benzyl group or PhSCH.sub.2, R.sup.3 and R.sup.4 are taken together to represent --CONH--CS--S--, ##STR2## (X.sup.1 : H, a halogen, methyl group, ethyl group, R.sup.7 O-- (R.sup.7 : methyl or ethyl group), nitro group, aminosulfonyl group or amino group, m.sup.1 : 1 or 2), pyridyl group, furyl group or thienyl group, n.sup.1 : an integer of 0 to 3); when R.sup.1 and R.sup.2 : phenyl group, benzyl group or phenethyl group, or R.sup.1 : R.sup.5 O-- (R.sup.5 : as defined above) and R.sup.2 : benzyl group, R.sup.3 : cyano group and R.sup.4 : a carbamoyl group, or R.sup.3 and R.sup.4 are taken together to represent --CO--Y--CH.sub.2 CH.sub.2 -- (Y: O or --NH--) or ##STR3## and when R.sup.1 and R.sup.2 : a C.sub.1 to C.sub.3 alkyl group, R.sup.3 and R.sup.4 are taken together to represent ##STR4## (n.sup.1, R.sup.6 : as defined above), or a salt thereof. The hydroxystyrene derivative or a salt thereof is a compound which is useful as an active ingredient of an antiallergic agent, a 5-lipoxygenase inhibiting agent, an antibacterial agent, a tyrosine kinase inhibiting agent, an ultraviolet absorber or a reverse transcriptase inhibiting agent, and also is useful as an intermediate for preparing various organic compounds.

    摘要翻译: 由式(I)表示的羟基苯乙烯衍生物:其中当R1和R2:苯基,苄基或苯乙基或R1:R5O-(R5:H,C1-C5烷基或苄基 基团)和R 2:苄基或PhSCH 2,R 3和R 4一起表示-CONH-CS-S-,(X1:H,卤素,甲基,乙基,R7O-( R7:甲基或乙基),硝基,氨基磺酰基或氨基,m1:1或2),吡啶基,呋喃基或噻吩基,n1:0〜3的整数)。 当R1和R2:苯基,苄基或苯乙基或R1:R5O-(R5:如上定义)和R2:苄基,R3:氰基和R4:氨基甲酰基,或R3和R4合在一起 表示-CO-Y-CH 2 CH 2 - (Y:O或-NH-)或,并且当R 1和R 2为C 1至C 3烷基时,R 3和R 4一起表示(n1,R6 :如上所定义),或其盐。 羟基苯乙烯衍生物或其盐是可用作抗变应性剂的活性成分,5-脂氧合酶抑制剂,抗菌剂,酪氨酸激酶抑制剂,紫外线吸收剂或逆转录酶抑制剂的化合物,以及 也可用作制备各种有机化合物的中间体。

    Antibacterial compositions with synergistic effect, drugs and remedies for digestive diseases containing the same, process for the production thereof and preparations associated therewith
    9.
    发明授权
    Antibacterial compositions with synergistic effect, drugs and remedies for digestive diseases containing the same, process for the production thereof and preparations associated therewith 失效
    具有协同效应的抗菌组合物,含有其的消化疾病的药物和补救剂,其生产方法和与其相关的制剂

    公开(公告)号:US06362169B1

    公开(公告)日:2002-03-26

    申请号:US09622712

    申请日:2000-08-22

    IPC分类号: A61K3170

    摘要: Antibacterial compositions comprising (1) a rifamycin derivative represented by the formula (I) or its physiologically acceptable salt, and (2) a proton pump inhibitor (a) or a bismuth preparation (b) wherein the components (1) and (2) are used in such amounts as producing a synergistic effect against Helicobacter pylori, drugs and remedies for digestive organ diseases which contain the antibacterial compositions, process for producing them, and pharmaceutical preparations related to the antibacterial compositions. The compositions can be administered to patients with digestive diseases caused by infection of Helicobacter pylori in a smaller dose and at a lower administration frequency as compared with conventional remedies.

    摘要翻译: 抗菌组合物,其包含(1)由式(I)表示的利福霉素衍生物或其生理学上可接受的盐,和(2)质子泵抑制剂(a)或铋制剂(b),其中组分(1)和(2) 用于产生对幽门螺杆菌的协同效应,含有抗菌组合物的消化器官疾病的药物和补救剂,其制备方法和与抗菌组合物相关的药物制剂。 与常规治疗相比,组合物可以以较小的剂量和较低的施用频率施用于由幽门螺杆菌感染引起的消化系统疾病的患者。