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    • 21. 发明授权
    • Antihypertensive phosphate derivatives
    • 抗高血压磷酸盐衍生物
    • US4827011A
    • 1989-05-02
    • US679790
    • 1984-12-10
    • Allan WissnerRobert E. Schaub
    • Allan WissnerRobert E. Schaub
    • C07F9/10A61K31/685
    • C07F9/10
    • Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is a C.sub.1 -C.sub.24 branched or straight chain alkyl group; R is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl, with the proviso that at least one R group is not hydrogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR.sup.1).sub.p --, wherein p is an integer from 2 to 12 and the moiety --(CHR.sup.1).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.2 may be chain alkyl and q is an integer from 4 to 7; in either the racemic or in the optically active form.
    • 描述了具有下式的抗高血压磷酸酯衍生物:其中X是C 1 -C 24支链或直链烷基; R选自氢和C 1 -C 4烷基,条件是至少一个R基团不是氢; T选自氢和其中R 1选自氢,C 1 -C 4支链或直链烷基,C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基 ; Q是选自 - (CH 2)p - 和(CHR 1)p - 的二价基团,其中p是2至12的整数,并且 - (CHR 1)p - 部分代表被取代的亚烷基链 通过一个或多个C 1 -C 10烷基或苯基; Z选自,其中R 2可以是链烷基,q是4至7的整数; 以外消旋或旋光形式。
    • 24. 发明授权
    • Substituted 3-cyano quinolines
    • US6002008A
    • 1999-12-14
    • US49718
    • 1998-03-27
    • Allan WissnerBernard D. JohnsonMarvin F. ReichMiddleton B. Floyd, Jr.Douglas B. KitchenHwei-Ru Tsou
    • Allan WissnerBernard D. JohnsonMarvin F. ReichMiddleton B. Floyd, Jr.Douglas B. KitchenHwei-Ru Tsou
    • C07D215/54C07D215/56C07D401/04C07D401/12C07D409/12A01N43/42C07D215/16C07D215/38
    • C07D401/04C07D215/54C07D215/56C07D401/12C07D409/12
    • This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.5 is alkyl which may be optionally substituted, or phenyl which may be optionally substituted;R.sub.6 is hydrogen, alkyl, or alkenyl;R.sub.7 is chloro or bromoR.sub.8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl, alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl+, chloro, fluoro, or bromo;Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino, piperazino, N-alkylpiperazino, or pyrrolidino;m=1-4,q=1-3, and p=0-3;any of the substituents R.sub.1, R.sub.2, R.sub.3, or R.sub.4 that are located on contiguous carbon atoms can together be the divalent radical --O--C(R.sub.8).sub.2 --O--;or a pharmaceutically acceptable salt thereof with the proviso that when Y is --NH--, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen, and n is 0, X is not 2-methylphenyl, which are inhibitors of protein tyrosine kinase.