公开(公告)号：US20100168180A1

公开(公告)日：2010-07-01

申请号：US12478587

申请日：2009-06-04

申请人： Gerard Andrew Potter ,  Philip Huxley

发明人： Gerard Andrew Potter ,  Philip Huxley

IPC分类号： A61K31/443 ,  C07D213/64 ,  A61K31/4418 ,  C07D405/10 ,  A61P35/00

CPC分类号： C07D213/64 ,  C07D405/04

摘要： A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein: R1, R2 and R3 are independently H or lower alkyl; R4, R5, R6, R7 and R8 are independently H, halo, lower alkyl or —O-lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R4 to R8, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR14R15)n—O—, where n is 1 or 2 and R14 and R15 are independently H or lower alkyl, and the remainder of R4 to R8 are independently H, halo, lower alkyl or —O-lower alkyl; and R9, R10, R11, R12 and R13 are independently H, halo, lower alkyl or —O— lower alkyl, provided that at least one is —O-lower alkyl; or at least one pair of R9 to R13, the members of which pair are adjacent to one another on the ring, are conjoined to form —O—(CR16R17)m—O—, where m is 1 or 2 and R16 and R17 are independently H or lower alkyl, and the remainder of R9 to R13 are independently H, halo, lower alkyl or —O-lower alkyl.

摘要翻译： 一种用于治疗增殖性疾病如癌症的化合物，具有下式：其中：R1，R2和R3独立地为H或低级烷基; R 4，R 5，R 6，R 7和R 8独立地为H，卤素，低级烷基或-O-低级烷基，条件是至少一个为-O-低级烷基; 或至少一对R4至R8（其成对在环上彼此相邻）被结合形成-O-（CR14R15）n-O-，其中n为1或2，R14和R15为 独立地是H或低级烷基，R4至R8的其余部分独立地为H，卤素，低级烷基或-O-低级烷基; 并且R 9，R 10，R 11，R 12和R 13独立地为H，卤素，低级烷基或-O-低级烷基，条件是至少一个为-O-低级烷基; 或至少有一对R 9至R 13（其成对在环上彼此相邻）结合形成-O-（CR 16 R 17）m -O-，其中m为1或2，R 16和R 17为 独立地是H或低级烷基，R 9至R 13的其余部分独立地为H，卤素，低级烷基或-O-低级烷基。

公开(公告)号：US07112698B2

公开(公告)日：2006-09-26

申请号：US10491614

申请日：2002-09-30

申请人： Gerard Andrew Potter ,  Taeeba Ijaz

发明人： Gerard Andrew Potter ,  Taeeba Ijaz

IPC分类号： C07C49/76 ,  A61K31/12

CPC分类号： C07C49/84 ,  A61K31/12 ,  C07C45/29 ,  C07C45/71 ,  C07C45/74 ,  C07C47/575

摘要： The present invention pertains to compounds of the following formula: (1) wherein: RALK is primary or secondary aliphatic saturated C2-6alkyl; 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 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： 本发明涉及下式的化合物：（1）其中：R ALK是伯或仲脂族饱和C 2-6烷基; 每个R B2，B3，B3和Z5各自独立地是-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个芳基; R 3是-H，-OH，-OC（-O）R E，-OS（-O）2 OH，或 - OP（-O）（OH）2 < R e是：-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：US06465522B1

公开(公告)日：2002-10-15

申请号：US09868956

申请日：2001-11-07

申请人： Gerard Andrew Potter ,  Laurence Hylton Patterson ,  Paul Teesdale-Spittle ,  Zennia Paniwynk

发明人： Gerard Andrew Potter ,  Laurence Hylton Patterson ,  Paul Teesdale-Spittle ,  Zennia Paniwynk

IPC分类号： A61K31135

CPC分类号： A61K47/55 ,  A61K47/54

摘要： A molecule of formula (I); wherein: X is a halogen, or a substituted sulfonate group; m=1-5; n=1-5; R1, R2=H, C1-4 lower alkyl or C1-4 lower alkyl chain having additional functionality; and the amino group −NR1R2 linked to the anthraquinone is primary, secondary or tertiary or is a tertiary group in the N-oxide form having the formula —N(O)R1R2.

摘要翻译： 式（I）的分子;其中：X是卤素或取代的磺酸酯基; m = 1-5; n = 1-5; R 1，R 2 = H，C 1-4低级烷基或C 1-4低级烷基 链具有附加功能; 与蒽醌连接的氨基-NR1R2是伯，仲或叔或是具有式-N（O）R 1 R 2的N-氧化物形式的叔基。

公开(公告)号：US06441178B2

公开(公告)日：2002-08-27

申请号：US09487071

申请日：2000-01-19

申请人： Hooshang Shahriari Zavareh ,  Gerard Andrew Potter

发明人： Hooshang Shahriari Zavareh ,  Gerard Andrew Potter

IPC分类号： C07D21132

CPC分类号： C07D211/34

摘要： A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral acid or base, using a chiral resolving agent. The resolved salt can be esterified, to give the therapeutic agent d-threo-methylphenidate.

摘要翻译： 一种制备对映体富集形式的苏氨酸的方法，其包括使用手性拆分剂拆分酸的盐的对映异构体的混合物，所述盐与非手性酸或碱形成。 分解的盐可以酯化，得到治疗剂d-苏 - 哌甲酯。