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    • 1. 发明授权
    • Hydroxymethyl-polythiophene derivatives
    • 羟甲基 - 聚噻吩衍生物
    • US5596014A
    • 1997-01-21
    • US461176
    • 1995-06-05
    • Ching-Te ChangRong-Tsun Wu
    • Ching-Te ChangRong-Tsun Wu
    • C07D333/16C07D333/18C07D333/22A61K31/38C07D409/14
    • C07D333/16C07D333/18C07D333/22
    • A pharmaceutical composition containing a compound and an excipient, the compound having the formula: ##STR1## in which n is 2, 3 or 4; R is H, --CH(R.sup.1).cndot.OR.sup.2, --CH(O--Z).sub.2, or --COR.sup.3 ; R.sup.1 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, OH, C.sub.1-6 hydroxyalkyl, or COOH; R.sup.2 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, tetrahydropyranyl, phenyl, benzoyl, C.sub.1-6 acyl, tosyl, or --CO--Y--COOH; and R.sup.3 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, OH, C.sub.1-6 hydroxyalkyl, or COOH; wherein Z is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, or C.sub.1-6 acyl; and Y is C.sub.1-6 alkylidene, C.sub.2-6 alkenylidene, phenylene, or deleted; or an ester or a salt thereof.
    • 含有化合物和赋形剂的药物组合物,具有下式的化合物:其中n为2,3或4; R为H,-CH(R 1),OR 2,-CH(O-Z)2或-COR 3; R1是H,C1-6烷基,C2-6烯基,OH,C1-6羟基烷基或COOH; R2是H,C1-6烷基,C2-6烯基,四氢吡喃基,苯基,苯甲酰基,C1-6酰基,甲苯磺酰基或-CO-Y-COOH; 和R 3是H,C 1-6烷基,C 2-6烯基,OH,C 1-6羟基烷基或COOH; 其中Z为C 1-6烷基,C 2-6烯基或C 1-6酰基; Y为C1-6亚烷基,C2-6亚烯基,亚苯基或缺失; 或其酯或其盐。
    • 2. 发明授权
    • Medicinal thiophene compounds
    • 药用噻吩化合物
    • US5753692A
    • 1998-05-19
    • US468522
    • 1995-06-06
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • A61K31/38
    • A61K31/38
    • A method of augmenting the immune system including administering to a subject an effective amount of a compound of the following formula: ##STR1## wherein m is 1-4; and each of A and B, independently, is H, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, (CH.sub.2).sub.n CHO, (CH.sub.2).sub.o COOH, C.sub.1-7 alkoxy, C.sub.2-7 alkoxyalkyl, C.sub.1-7 hydroxyalkyl, CN, NO.sub.2, halogen, CH(OR.sup.1).sub.2, CO.R.sup.1, NR.sup.2 R.sup.3 or its acid salt, CO.NR.sup.2 R.sup.3, CHR.sup.1 NR.sup.2 R.sup.3 or its acid salt, CH.dbd.NR.sup.2, C.tbd.CR.sup.4, CR.sup.1 .dbd.CR.sup.5 R.sup.6, CO.CH.dbd.CHR.sup.7, CH.dbd.CHR.sup.8, or COOR.sup.9 ; in which each of n and o, independently, is 0-4; R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 acyl; each of R.sup.2 and R.sup.3, independently, is H, C.sub.1-4 alkyl, or C.sub.1-4 hydroxyalkyl; R.sup.4 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, COR.sup.2, COOR.sup.10, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 dihydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 halogenated alkyl; OR.sup.1, or NHR.sup.7 ; each of R.sup.5 and R.sup.6, independently, is H, CHO, COR.sup.1, COOH, COOR.sup.9, CN, or halogen; R.sup.7 is H, C.sub.1-4 alkyl, 2-thienyl, phenyl, mono-substituted phenyl, or di-substituted phenyl; R.sup.8 is COOR.sup.2, CO.CHO, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether; and R.sup.9 is H, C.sub.1-4 alkyl, phenyl, mono-substituted phenyl, di-substituted phenyl, or 2-thienyl.
    • 一种增强免疫系统的方法,包括向受试者施用有效量的下式化合物:其中m为1-4; A和B各自独立地为H,C 1-7烷基,C 2-7烯基,C 2-7炔基,(CH 2)n CHO,(CH 2)o COOH,C 1-7烷氧基,C 2-7烷氧基烷基,C 1-7 羟基烷基,CN,NO 2,卤素,CH(OR 1)2,CO.R 1,NR 2 R 3或其酸式盐,CO.NR 2 R 3,CHRRNR 2 R 3或其酸式盐CH = NR 2,C 3 D 4 CR 4,CR 1 = CR 5 R 6,CO.CH = CHR7,CH = CHR8或COOR9; 其中n和o各自独立地为0-4; R1是C1-4烷基或C1-4酰基; R 2和R 3各自独立地是H,C 1-4烷基或C 1-4羟基烷基; R4是H,C1-4烷基,C2-4烯基,COR2,COOR10,C1-4羟烷基或其酸酯或2-四氢吡喃基醚,C1-4二羟基烷基或其酸酯或2-四氢吡喃基醚,C1-4卤代 烷基; OR1或NHR7; R 5和R 6各自独立地是H,CHO,COR1,COOH,COOR9,CN或卤素; R 7是H,C 1-4烷基,2-噻吩基,苯基,单取代的苯基或二取代的苯基; R8是COOR2,CO.CHO,C1-4羟烷基或其酸酯或2-四氢吡喃基醚; 且R 9为H,C 1-4烷基,苯基,单取代苯基,二取代苯基或2-噻吩基。
    • 3. 发明授权
    • Medicinal thiophene compounds
    • 药用噻吩化合物
    • US5747525A
    • 1998-05-05
    • US468253
    • 1995-06-06
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • A61K31/38
    • A61K31/38
    • A method of treating tumor including administering to a subject an effective amount of a compound of the following formula: ##STR1## wherein m is 1-4; and each of A and B, independently, is H, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, (CH.sub.2).sub.n CHO, (CH.sub.2).sub.o COOH, C.sub.1-7 alkoxy, C.sub.2-7 alkoxyalkyl, C.sub.1-7 hydroxyalkyl, CN, NO.sub.2, halogen, CH(OR.sup.1).sub.2, CO.R.sup.1, NR.sup.2 R.sup.3 or its acid salt, CO.NR.sup.2 R.sup.3, CHR.sup.1 NR.sup.2 R.sup.3 or its acid salt, CH.dbd.NR.sup.2, C.tbd.CR.sup.4, CR.sup.1 .dbd.CR.sup.5 R.sup.6, CO.CH.dbd.CHR.sup.7, CH.dbd.CHR.sup.8, or COOR.sup.9 ; in which each of n and o, independently, is 0-4; R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 acyl; each of R.sup.2 and R.sup.3, independently, is H, C.sub.1-4 alkyl, or C.sub.1-4 hydroxyalkyl; R.sup.4 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, COR.sup.2, COOR.sup.10, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 dihydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 halogenated alkyl; OR.sup.1, or NHR.sup.7 ; each of R.sup.5 and R.sup.6, independently, is H, CHO, COR.sup.1, COOH, COOR.sup.9, CN, or halogen; R.sup.7 is H, C.sub.1-4 alkyl, 2-thienyl, phenyl, mono-substituted phenyl, or di-substituted phenyl; R.sup.8 is COOR.sup.2, CO.CHO, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether; and R.sup.9 is H, C.sub.1-4 alkyl, phenyl, mono-substituted phenyl, di-substituted phenyl, or 2-thienyl.
    • 一种治疗肿瘤的方法,包括向受试者施用有效量的下式化合物:其中m为1-4; A和B各自独立地为H,C 1-7烷基,C 2-7烯基,C 2-7炔基,(CH 2)n CHO,(CH 2)o COOH,C 1-7烷氧基,C 2-7烷氧基烷基,C 1-7 羟基烷基,CN,NO 2,卤素,CH(OR 1)2,CO.R 1,NR 2 R 3或其酸式盐,CO.NR 2 R 3,CHRRNR 2 R 3或其酸式盐CH = NR 2,C 3 D 4 CR 4,CR 1 = CR 5 R 6,CO.CH = CHR7,CH = CHR8或COOR9; 其中n和o各自独立地为0-4; R1是C1-4烷基或C1-4酰基; R 2和R 3各自独立地是H,C 1-4烷基或C 1-4羟基烷基; R4是H,C1-4烷基,C2-4烯基,COR2,COOR10,C1-4羟烷基或其酸酯或2-四氢吡喃基醚,C1-4二羟基烷基或其酸酯或2-四氢吡喃基醚,C1-4卤代 烷基; OR1或NHR7; R 5和R 6各自独立地是H,CHO,COR1,COOH,COOR9,CN或卤素; R 7是H,C 1-4烷基,2-噻吩基,苯基,单取代的苯基或二取代的苯基; R8是COOR2,CO.CHO,C1-4羟烷基或其酸酯或2-四氢吡喃基醚; 且R 9为H,C 1-4烷基,苯基,单取代苯基,二取代苯基或2-噻吩基。
    • 4. 发明授权
    • Medicinal thiophene compounds
    • 药用噻吩化合物
    • US5602170A
    • 1997-02-11
    • US302278
    • 1994-09-08
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • Ching-Te ChangKuo-Mou ChenWann-Huang LiuFen-Lan LinRong-Tsun Wu
    • A61K31/38
    • A61K31/38
    • A method of treating inflammation including administering to a subject an effective amount of a compound of the following formula: ##STR1## wherein m is 1-4; and each of A and B, independently, is H, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, (CH.sub.2).sub.n CHO, (CH.sub.2).sub.o COOH, C.sub.1-7 alkoxy, C.sub.2-7 alkoxyalkyl, C.sub.1-7 hydroxyalkyl, CN, NO.sub.2, halogen, CH(OR.sup.1).sub.2, CO.R.sup.1, NR.sup.2 R.sup.3 or its acid salt, CO.NR.sup.2 R.sup.3, CHR.sup.1 NR.sup.2 R.sup.3 or its acid salt, CH=NR.sup.2, C.tbd.CR.sup.4, CR.sup.1 =CR.sup.5 R.sup.6, CO.CH.dbd.CHR.sup.7, CH.dbd.CHR.sup.8, or COOR.sup.9 ; in which each of n and o, independently, is 0-4; R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 acyl; each of R.sup.2 and R.sup.3, independently is H, C.sub.1-4 alkyl, or C.sub.1-4 hydroxyalkyl; R.sup.4 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, COR.sup.2, COOR.sup.10, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 dihydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.1-4 halogenated alkyl; OR.sup.1, NHR.sup.7 ; each of R.sup.5 R.sup.6, independently, is H, CHO, COR.sup.1, COOH, COOR.sup.9, CN, or halogen; R.sup.7 is H, C.sub.1-4 alkyl, 2-thienyl, phenyl, mono-substituted phenyl, or di-substituted phenyl; R.sup.8 is COOR.sup.2, CO.CHO, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether; and R.sup.9 is H, C.sub.1-4 alkyl, phenyl, mono-substituted phenyl, di-substituted phenyl, or 2 -thienyl.
    • 一种治疗炎症的方法,包括向受试者施用有效量的下式化合物:其中m为1-4; A和B各自独立地为H,C 1-7烷基,C 2-7烯基,C 2-7炔基,(CH 2)n CHO,(CH 2)o COOH,C 1-7烷氧基,C 2-7烷氧基烷基,C 1-7 羟基烷基,CN,NO 2,卤素,CH(OR 1)2,CO.R 1,NR 2 R 3或其酸式盐,CO.NR 2 R 3,CHRRNR 2 R 3或其酸式盐CH = NR 2,C 3 D 4 CR 4,CR 1 = CR 5 R 6,CO.CH = CHR7,CH = CHR8或COOR9; 其中n和o各自独立地为0-4; R1是C1-4烷基或C1-4酰基; R 2和R 3各自独立地是H,C 1-4烷基或C 1-4羟基烷基; R4是H,C1-4烷基,C2-4烯基,COR2,COOR10,C1-4羟烷基或其酸酯或2-四氢吡喃基醚,C1-4二羟基烷基或其酸酯或2-四氢吡喃基醚,C1-4卤代 烷基; OR1,NHR7; R5 R6各自独立地为H,CHO,COR1,COOH,COOR9,CN或卤素; R 7是H,C 1-4烷基,2-噻吩基,苯基,单取代的苯基或二取代的苯基; R8是COOR2,CO.CHO,C1-4羟烷基或其酸酯或2-四氢吡喃基醚; 且R 9为H,C 1-4烷基,苯基,单取代苯基,二取代苯基或2-噻吩基。