公开(公告)号：US06982251B2

公开(公告)日：2006-01-03

申请号：US10166942

申请日：2002-06-11

申请人： Anima Ghosal ,  Shmuel Zbaida ,  Swapan K. Chowdhury ,  Robert M. Iannucci ,  Wenqing Feng ,  Kevin B. Alton ,  James E. Patrick ,  Harry R. Davis

发明人： Anima Ghosal ,  Shmuel Zbaida ,  Swapan K. Chowdhury ,  Robert M. Iannucci ,  Wenqing Feng ,  Kevin B. Alton ,  James E. Patrick ,  Harry R. Davis

IPC分类号： A61K31/7056 ,  A61K31/397 ,  A61K31/675 ,  C07H17/02 ,  C07D25/08

CPC分类号： A61K31/70 ,  A61K45/06 ,  C07H15/26

摘要： Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

公开(公告)号：US07271174B2

公开(公告)日：2007-09-18

申请号：US10874556

申请日：2004-06-23

申请人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

发明人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

IPC分类号： C07D221/06 ,  A61K31/435

CPC分类号： C07D401/14

摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.

摘要翻译： 本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶 使用新型化合物。