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    • 2. 发明授权
    • Sulfonates of hydroxycoumarins
    • 羟基香豆素磺酸盐
    • US4618622A
    • 1986-10-21
    • US552787
    • 1983-11-17
    • Rainer SchleckerPeter SchmidtPeter C. ThiemeDieter LenkeHans-Jurgen TeschendorfMartin TrautClaus D. MuellerHans P. HofmannHorst Kreiskott
    • Rainer SchleckerPeter SchmidtPeter C. ThiemeDieter LenkeHans-Jurgen TeschendorfMartin TrautClaus D. MuellerHans P. HofmannHorst Kreiskott
    • A61K31/35A61K31/352A61K31/365A61P25/18A61P25/24A61P25/26A61P37/08A61P43/00C07D311/08C07D311/16C07D311/80A61K31/37
    • C07D311/80C07D311/16
    • Sulfonates of hydroxycoumarins of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, halogen or alkyl of 1 to 5 carbon atoms which can be substituted by --NR.sup.4 R.sup.5, --OR.sup.4 or --OC(O)R.sup.4, where R.sup.4 and R.sup.5 are identical or different and are each hydrogen or alkyl of 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 are each a carboxylic acid group --OC(O)R.sup.4 or a carboxamido radical, with the proviso that R.sup.1 is not methyl when R.sup.2 is hydrogen, or R.sup.1 and R.sup.2 together form a --(CH.sub.2).sub.n -- chain where n is 3-5, and R.sup.3 is a straight-chain or branched alkyl radical of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms, each of which can be substituted by halogen, --OR.sup.4, --NR.sup.4 R.sup.5, --CN or phenyl, or R.sup.3 is a straight-chain or branched alkenyl radical of 3 to 8 carbon atoms, an amino group -- NR.sup.4 R.sup.5, or phenyl or naphthyl, each of which is unsubstituted or monosubstituted or polysubstituted by --OR.sup.4, --NR.sup.4 R.sup.5, --NO.sub.2, halogen, --SR.sup.4, --S(O)R.sup.4, --OS(O)R.sup.4, --SCF.sub.3, --OS(O)CF.sub.3, --CN, --C(O)R.sup.4, --OC(O)R.sup.4, --NHC(O)R.sup.4, --CF.sub.3, C.sub.1 -C.sub.4 -alkyl or a combination of these substituents, a process for their preparation, drugs containing these compounds, and compounds of the formula I, in which R.sup.1 is methyl and R.sup.2 is hydrogen, for use as drugs.
    • 式I的羟基香豆素的磺酸盐其中R 1和R 2相同或不同,各自为氢,卤素或可被-NR 4 R 5,-OR 4或-OC(O)取代的1至5个碳原子的烷基 )R 4,其中R 4和R 5相同或不同并且各自为氢或1至4个碳原子的烷基,或者R 1和R 2各自为羧酸基-OC(O)R 4或甲酰胺基,条件是R 1 当R 2为氢时,R 1和R 2一起形成 - (CH 2)n - 链,其中n为3-5,R 3为1至8个碳原子的直链或支链烷基或3个环烷基 至8个碳原子,每个可以被卤素,-OR4,-NR4R5,-CN或苯基取代,或R3是3-8个碳原子的直链或支链烯基,氨基-NR4R5或 苯基或萘基,它们各自被-OR4,-NR4R5,-NO2,卤素,-SR4,-S(O)R4,-OS(O)R4,-SCF3,-OS(O)未取代或单取代或多取代, CF 3,-CN,-C(O)R 4,-OC(O)R 4, -NHC(O)R 4,-CF 3,C 1 -C 4烷基或这些取代基的组合,其制备方法,含有这些化合物的药物和式I化合物,其中R 1是甲基,R 2是氢, 用作药物。
    • 10. 发明授权
    • 3-substituted pyrido [3',4':4,5] Thieno [2,3-d] pyrimidine derivatives,
and production and use of the same
    • 3-取代的吡啶并[3',4':4,5]噻吩并[2,3-d]嘧啶衍生物及其制备和使用
    • US6159981A
    • 2000-12-12
    • US445178
    • 1999-12-08
    • Gerd SteinerUta DullweberDorothea StarckAlfred BachKarsten WickeHans-Jurgen TeschendorfFrancisco-Javier Garcia-LadonaFranz Emling
    • Gerd SteinerUta DullweberDorothea StarckAlfred BachKarsten WickeHans-Jurgen TeschendorfFrancisco-Javier Garcia-LadonaFranz Emling
    • A61K31/519A61P25/00A61P25/24A61P43/00C07D495/14A61K31/495A61K31/505
    • C07D495/14
    • 3-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl group, an acetyl group, a phenylalkyl C.sub.1 -C.sub.4 radical, the aromatic system being unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen,R.sup.2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms,A is NH or an oxygen atom,Y is CH.sub.2, CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --CH.sub.2 or CH.sub.2 --CH,Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond,and n is 2, 3 or 4, and the physiologically tolerated salts thereof.
    • PCT No.PCT / EP98 / 03231 Sec。 371 1999年12月8日第 102(e)日期1999年12月8日PCT提交1998年5月29日PCT公布。 第WO98 / 56793号公报 日期:19983年12月17日 - 取代式I的3,4,5,6,7,8-六氢吡啶并[3',4':4,5] - 噻吩并[2,3-d]嘧啶衍生物,其中R1是 一个氢原子,一个C 1 -C 4烷基,一个乙酰基,一个苯基烷基C 1 -C 4基团,该芳族体系是未被取代的或被卤素,C 1 -C 4烷基,三氟甲基,羟基,C 1 -C 4烷氧基,氨基 氰基或硝基,或者是苯基烷酮基,苯基可以被卤素取代,R2是苯基,吡啶基,嘧啶基或吡嗪基,其是未被取代的或被卤原子单取代或被C1- C4-烷基,三氟甲基,三氟甲氧基,羟基,C 1 -C 4 - 烷氧基,氨基,一甲基氨基,二甲基氨基,氰基或硝基,并且它们可以与苯核稠合,苯核可被未被取代或被卤素原子, C 4 - 烷基,羟基,三氟甲基,C 1 -C 4 - 烷氧基,氨基,氰基或硝基,并且可以含有1个氮原子,或可以含有5或6元环, 含有1-2个氧原子,A是NH或氧原子,Y是CH 2,CH 2 -CH 2,CH 2 -CH 2 -CH 2或CH 2 -CH,Z是氮原子,碳原子或CH,也可以是 Y与Z之间的连接为双键,n为2,3或4,以及其生理上耐受的盐。