Use of natural products and related synthetic compounds for the
treatment of cardiovascular disease
    1.
    发明授权
    Use of natural products and related synthetic compounds for the treatment of cardiovascular disease 失效
    使用天然产物和相关合成化合物治疗心血管疾病

    公开(公告)号:US5859067A

    公开(公告)日:1999-01-12

    申请号:US969145

    申请日:1997-11-12

    摘要: Use of a compound of formula (I), wherein Ar is an aromatic ring system comprising one or more optionally substituted phenyl rings optionally linked to or fused with one or more other optionally substituted phenyl rings or one or more 5 or 6-membered, optionally substituted heterocyclic rings wherein the heteroatom is oxygen; and wherein the ring system comprises 1-4 phenyl rings and wherein Ar can be linked to another Ar via a group X wherein the Ar is independently selected; where X is optionally substituted C.sub.1-20 alkylene, C.sub.2-20 alkenylene or C.sub.2-20 alkynylene; R is hydrogen; C.sub.1-20 alkenyl, C.sub.2-20 alkynyl, C.sub.2-20 alkanoyl, C.sub.2-20 alkynoyl, each of which can be optionally substituted; R.sub.1 is independently selected and is hydrogen; optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl; --COOR'--NR'R', halogen, --OR', --COR', --CONR'R', .dbd.O, --SR', --SO.sub.3 R', --SO.sub.2 NR'R', --SOR', --SO.sub.2 R', --NO.sub.2, --CN, glycoside, silyl; where R' is independently hyrogen; alkyl, alkenyl or akynyl each optionally substituted; and where two groups R.sub.1 can be joined; wherein the optional substituents are one or more independently selected from C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl; --COOR"--NR"R", halogen, OR", --COR", --CONR"R", --SR", .dbd.O, --SO.sub.3 R", --SO.sub.2 NR"R", --SOR", --SO.sub.2 ", --NO.sub.2, --CN; wherein R" is independently hydrogen, alkyl, alkenyl, or alkynyl; n=1, 2 or 3; m=1, 2, 3 or 4; or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for inhibiting the action of Ca.sup.2+ -ATPase enzymes. Certain compounds of formula (I) and 8-lavandulyl flavone pharmaceutical formulations are new.

    摘要翻译: 使用式(I)化合物,其中Ar是包含一个或多个任选取代的苯环的芳环体系,其任选地与一个或多个其它任选取代的苯环或一个或多个5或6元任意连接或稠合,任选地 取代的杂环,其中杂原子是氧; 并且其中所述环系统包含1-4个苯环,并且其中Ar可以经由独立选择Ar的基团X连接到另一个Ar; 其中X是任选取代的C 1-20亚烷基,C 2-20亚烯基或C 2-20炔基; R是氢; C 1-20烯基,C 2-20炔基,C 2-20烷酰基,C 2-20炔酰基,其各自可以任选被取代; R1独立地选择并且是氢; 任选取代的C 1-12烷基,C 2-12烯基,C 2-12炔基; -COOR'-NR'R',卤素-OR',-COR',-CONR'R',= O,-SR',-SO3R',-SO2NR'R',-SOR',-SO2R' -NO 2,-CN,糖苷,甲硅烷基; 其中R'独立地是氢; 烷基,烯基或炔基,各自任选取代; 并且可以连接两个基团R1; 其中任选的取代基是一个或多个独立地选自C 1-10烷基,C 2-10烯基,C 2-10炔基; -COOR“ - NR''R”,卤素,OR“,-COR”,-CONR''R“,-SR”,= O,-SO3R“,-SO2NR''R' ,-SOR“,-SO 2”,-NO 2,-CN; 其中R“独立地是氢,烷基,烯基或炔基; n = 1,2或3; m = 1,2,3或4; 或其药学上可接受的衍生物在制备用于抑制Ca2 + -ATP酶的作用的药物中的用途。 某些式(I)化合物和8-大茴香黄酮药物制剂是新的。

    Medicinal uses of phenylaikanols and derivatives
    3.
    发明授权
    Medicinal uses of phenylaikanols and derivatives 失效
    苯烷醇和衍生物的药用

    公开(公告)号:US06518315B1

    公开(公告)日:2003-02-11

    申请号:US09509829

    申请日:2000-06-23

    IPC分类号: A01N3500

    摘要: A compound of formula (I), a pharmaceutically acceptable derivative thereof, wherein Ph is a phenyl radical R1 is H, OH, OC1-4alkyl, NO2; R2 is OH, OC1-4alkyl, OC═OC1-4alkyl or OC═OPh where the Ph can be optionally substituted by halogen, C1-3 alkyl or NO2; R1 and R2 along with the two carbon atoms of the phenyl ring to which they are attached can combine to form a 5 or 6 membered heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S or N; R3 is an optionally substituted hydroycarby radical; R4 is H, CH3, OH or ═O; when R4 is ═O, then the carbon to which R4 is attached is not bonded to H; W is C(═O)—CH2, CH═CH—, CH2CO, CH(OH)—CH2, C(CH3)(OH)CH2, CH2CH(OH), CH2C(CH3)OH, CO, CHOH, C(CH3)(OH), CH2, CH2CH2; X is —CH—OH, C(CH3)OH, CH2, CH(CH3) or —C═O; Y is —CH—OH, C(CH3)OH, CH2, CH(CH3) or —C═O; provided that one of W, X or Y has an OH group.

    摘要翻译: 式(I)化合物,其药学上可接受的衍生物,其中Ph是苯基R1是H,OH,OC1-4烷基,NO2; R 2是OH,OC 1-4烷基,OC = OC 1-4烷基或OC = OPh,其中Ph可以任选地被卤素,C 1-3烷基或NO 2取代; R1和R2与它们所连接的苯环的两个碳原子一起可以结合形成包含1或2个选自O,S或N的杂原子的5或6元杂环; R3是任选取代的环烃基; R4是H,CH3,OH或= O; 当R 4为= O时,R 4所连接的碳不与H键合; W是C(= O)-CH 2,CH = CH-,CH 2 CO,CH(OH)-CH 2,C(CH 3)(OH)CH 2,CH 2 CH(OH),CH 2 C(CH 3)OH,CO,CHOH,C( CH3)(OH),CH2,CH2CH2; X是-CH-OH,C(CH 3)OH,CH 2,CH(CH 3)或-C = O; Y是-CH-OH,C(CH 3)OH,CH 2,CH(CH 3)或-C = O; 条件是W,X或Y中的一个具有OH基团。