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    • 4. 发明授权
    • Polyaryl antitumor agents
    • 聚芳基抗肿瘤剂
    • US6046229A
    • 2000-04-04
    • US3317
    • 1998-01-06
    • Ching Te ChangYuh-Lin Yang
    • Ching Te ChangYuh-Lin Yang
    • C07D333/16C07D333/20C07D333/22A01N43/10C07D333/32C07D333/36C07D49/10
    • C07D333/20C07D333/16C07D333/22
    • A compound of the formula:Ar.sub.1 --B--Ar.sub.2wherein Ar.sub.1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, hydroxyalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; B is, --CH.dbd.CH--, or --C C--, in which R is H, alkyl, hydroxyl, alkoxy, ester, aldehyde, hydroxyalkyl, aminoalkyl, carboxyl, --CH(OR.sub.1).sub.2, or NR.sub.2 R.sub.3, where each R.sub.1, independently, is H, alkyl, or acyl; and each of R.sub.2 and R.sub.3, independently, is H, alkyl, hydroxyalkyl, or aminoalkyl; and Ar.sub.2 is substituted phenyl, substituted thienyl, substituted furanyl, or substituted pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; or a salt thereof. Also disclosed is a composition which contains a pharmaceutical acceptable carrier and an effective amount of a compound of the above formula.
    • 式中Ar1-B-Ar2的化合物是未取代或取代的苯基,噻吩基,呋喃基或吡咯基,其中取代的苯基,取代的噻吩基,取代的呋喃基和取代的吡咯基的各取代基独立地为醛,酰基 ,酯,羧基,酰氨基,腈,硝基,氰基,缩醛,缩酮,氧代烷基,氨基烷基,羟基烷基,卤代烷基,亚氨基烷基,酰卤,氨基烷基氨基烷基,氨基烷基氨基烷基氨基,羟基烷基氨基烷基或羟烷基氨基烷基氨基烷基。 B是-CH = CH-或-C≡C,其中R是H,烷基,羟基,烷氧基,酯,醛,羟基烷基,氨基烷基,羧基,-CH(OR 1)2或NR 2 R 3, 独立地是H,烷基或酰基; R 2和R 3各自独立地为H,烷基,羟基烷基或氨基烷基; 并且Ar 2是取代的苯基,取代的噻吩基,取代的呋喃基或取代的吡咯基,其中取代的苯基,取代的噻吩基,取代的呋喃基和取代的吡咯基的各取代基独立地是酰氨基,腈,硝基,氰基,缩醛,缩酮, 氧代烷基,氨基烷基,卤代烷基,亚氨基烷基,酰卤,氨基烷基氨基烷基,氨基烷基氨基烷基氨基,羟基烷基氨基烷基或羟烷基氨基烷基氨基烷基; 或其盐。 还公开了含有药学上可接受的载体和有效量的上式化合物的组合物。
    • 7. 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。
    • 9. 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。
    • 10. 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。