公开(公告)号：US07304092B1

公开(公告)日：2007-12-04

申请号：US10705483

申请日：2003-11-11

申请人： David J. Austin ,  Viet-Ahn A. Nguyen ,  Doris Pupowicz ,  Albert Deisseroth ,  Tao Wang ,  Enrica Lerma

发明人： David J. Austin ,  Viet-Ahn A. Nguyen ,  Doris Pupowicz ,  Albert Deisseroth ,  Tao Wang ,  Enrica Lerma

IPC分类号： A61K31/215

CPC分类号： C07D307/68 ,  C07C233/09 ,  C07C2601/14 ,  C07D493/08

摘要： The present invention relates to novel compounds, pharmaceutical compositions and methods for treating tumors, cancer and hyperproliferative diseases including psoriasis, genital warts and hyperproliferative cell growth diseases, including hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus. These compounds are described according to the chemical structure: where R1 is H, OH, F, Cl, Br, I, a C1-C6 optionally substituted alkyl or alkenyl group, an optionally substituted aryl group or a  group; Ra is a H, OH, C1-C10, optionally substituted alkyl or alkenyl group, an optionally substituted O—(C1-C7 alkyl group) or O-aryl group, an amine group which is optionally substituted with at least one C1-C10 alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group; R2 is a  group; Rb is a H, OH, C1-C10, optionally substituted alkyl or alkenyl group, an optionally substituted O—(C1-C7 alkyl group) or O-aryl group, an amine group which is optionally substituted with at least one C1-C10 alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group; R3 and R6 are each independently selected from H, OH, F, Cl, Br, I, a C1-C6 optionally substituted alkyl or alkenyl group, an optionally substituted aryl group, a carbamate, alkylene carbamate, urethane or alkylene urethane; R4 is a  group, wherein Rb is as described above; and R5 is a  group, wherein Rb is as described above, with the proviso that at least one of R1 and R2 or R4 and R5 contains an Ra or Rb group which is an amine group which is optionally substituted with at least one C1-C10 alkyl group which may be optionally substituted, or a single optionally substituted aryl group, biphenyl group, (C1-C6) alkylenearyl group, (C1-C6) alkylenebiphenyl group, heteroaryl group, heterocyclic group, (C1-C6) alkylene heteroaryl group or (C1-C6) alkylene heterocyclic group; or a stereoisomer, pharmaceutically acceptable salt, solvate, and polymorph thereof.

摘要翻译： 本发明涉及用于治疗肿瘤的新型化合物，药物组合物和方法，包括牛皮癣，生殖器疣和过度增殖细胞生长疾病的癌症和过度增殖性疾病，包括过度增生性角化细胞疾病如角化过度，鱼鳞病，角化病或扁平苔藓。 这些化合物根据化学结构进行了描述：