公开(公告)号：US08841462B2

公开(公告)日：2014-09-23

申请号：US12999003

申请日：2009-07-01

Applicant: Robert A. Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

Inventor： Robert A. Heald ,  Philip Jackson ,  Joseph P. Lyssikatos ,  Stephen Price ,  Pascal Pierre Alexandre Savy

IPC: C07D275/04 ,  C07D231/56 ,  C07D513/04 ,  C07D471/04 ,  A61K31/437 ,  A61K31/428 ,  A61K31/416

CPC classification number: C07D231/56 ,  C07D275/04 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract translation: 本发明涉及式I和II的双环杂环，其具有抗癌和/或抗炎活性，更具体地涉及MEK激酶抑制活性。 本发明提供了可用于抑制异常细胞生长，治疗过度增殖性疾病或治疗哺乳动物炎性疾病的组合物和方法。 本发明还涉及将化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

公开(公告)号：US07115619B2

公开(公告)日：2006-10-03

申请号：US10398767

申请日：2001-10-12

Applicant: Malcolm F. G. Stevens ,  Lloyd R Kelland ,  Robert A Heald

Inventor： Malcolm F. G. Stevens ,  Lloyd R Kelland ,  Robert A Heald

IPC: A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/06

Abstract: The present invention pertains to certain N8,N13-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q−) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each RA is —H or a ring substituent; each RB is —H or a ring substituent; each RC is —H or a ring substituent; RN8 is a nitrogen substituent; RN13 is a nitrogen substituent; and, Q is an anion. 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, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

Abstract translation: 本发明涉及某些式（Q-O-SO 2）n N，N 13 - 二取代的喹啉并[4,3,2-k]吖啶鎓盐 >），其抑制端粒酶，其中：p为0至4的整数; q是0至3的整数; r为0〜4的整数; 每个R A A是-H或环取代基; 每个R B是-H或环取代基; 每个R O是-H或环取代基; R N8是氮取代基; R 13是氮取代基; 而Q是阴离子。 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的用途，以抑制端粒酶，调节细胞增殖以及治疗增殖性疾病如癌症。