公开(公告)号：US06787672B2

公开(公告)日：2004-09-07

申请号：US10239757

申请日：2002-09-26

申请人： Gerard Andrew Potter ,  Paul Crispin Butler ,  Elugba Wanogho

发明人： Gerard Andrew Potter ,  Paul Crispin Butler ,  Elugba Wanogho

IPC分类号： C07C49115

CPC分类号： G01N33/574 ,  A61K31/12 ,  A61K31/15 ,  A61K31/222 ,  C07C69/017 ,  C07C251/40 ,  C07C305/24 ,  C07F9/12 ,  G01N2333/90209

摘要： This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

摘要翻译： 本发明涉及具有治疗应用的取代的查尔酮，特异性取代的1-（4-甲氧基苯基）-3-（3,5-二甲氧基苯基）丙-1-烯-3-酮，例如作为有效的抗增殖剂和抗炎药 （O）2 OH或-OP（= O）（OH）2）的式（I）化合物，其中：X为-H，-OH，-OC（= O） Y是-H或C 1-4烷基; Z是-H或-OCH 3; R1是-H，C1-4烷基或C1-4氟烷基; R2是-H，C1-4烷基或C1-4氟烷基; 且R 3为-H，C 1-6烷基，C 3-20杂环基或C 5-20芳基; 和其药学上可接受的盐，酯和保护形式。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内用于诊断和治疗例如增生性疾病如癌症和炎性病症的用途。

公开(公告)号：US06677383B1

公开(公告)日：2004-01-13

申请号：US09633699

申请日：2000-08-07

申请人： Gerard Andrew Potter ,  Lawrence Hylton Patterson ,  Michael Danny Burke ,  Paul Crispin Butler

发明人： Gerard Andrew Potter ,  Lawrence Hylton Patterson ,  Michael Danny Burke ,  Paul Crispin Butler

IPC分类号： A61K3109

CPC分类号： C07C43/215 ,  C07C49/84 ,  C07C205/35 ,  C07C255/36 ,  C07C327/48 ,  C07C2602/10 ,  C07D213/57

摘要： The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

摘要翻译： 本发明涉及酶促芳族羟基化活化的前体药物，特别是抗肿瘤前体药物以及由CYP1B1酶的羟基化活性特异性活化的药物。

公开(公告)号：US20100028262A1

公开(公告)日：2010-02-04

申请号：US12574392

申请日：2009-10-06

申请人： Gerard Andrew Potter ,  Paul Crispin Butler

发明人： Gerard Andrew Potter ,  Paul Crispin Butler

IPC分类号： A61K49/00 ,  C07D307/87 ,  A61K31/343 ,  A61P35/00

CPC分类号： A61K31/357 ,  A61K47/54 ,  A61K47/555 ,  C07D317/54 ,  C07F9/65517

摘要： The present invention pertains to the use of a compounds for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula: wherein: each of RB2, RB3, RB4, and RB5 is independently —H, —OH, or —OMe; each of R1 and R2 is independently: —H, optionally substituted C1-4alkyl, or optionally substituted C5-20aryl; RA3 is —H, —OH, —OC(═O)RE, —OS(═O)2OH, or —OP(═O)(OH)2; RE is: —H, optionally substituted C1-6alkyl, optionally substituted C3-20heterocyclyl, or optionally substituted C5-20aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

摘要翻译： 本发明涉及化合物在制备用于治疗增殖性病症的药物中的用途，其中所述化合物具有下式：其中：RB2，RB3，RB4和RB5各自独立地为-H ，-OH或-OMe; R 1和R 2各自独立地为：-H，任选取代的C 1-4烷基，或任选取代的C 5-20芳基; RA 3是-H，-OH，-OC（-O）RE，-OS（-O）2 OH或-OP（-O）（OH）2） RE为：-H，任选取代的C 1-6烷基，任选取代的C 3-20杂环基，或任选取代的C 5-20芳基; 或其药学上可接受的盐，溶剂化物，酰胺，酯，醚，化学保护形式或前药。 本发明还涉及这样的化合物，包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内用于诊断和治疗例如增殖性疾病如癌症和炎症的用途 条件。