公开(公告)号：US20100298342A1

公开(公告)日：2010-11-25

申请号：US12310573

申请日：2007-09-04

申请人： Melissa S. Egbertson ,  Shaun R. Stauffer ,  Craig A. Coburn ,  James C. Barrow ,  Lou Anne Neilson ,  Jenny M. Wai ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Melissa S. Egbertson ,  Shaun R. Stauffer ,  Craig A. Coburn ,  James C. Barrow ,  Lou Anne Neilson ,  Jenny M. Wai ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D471/10 ,  A61K31/497 ,  A61P25/28

CPC分类号： C07D471/10 ,  C07D498/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

摘要翻译： 本发明涉及式（I）的螺哌啶化合物及其互变异构体，其是β-分泌酶的抑制剂，并且其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US06391305B1

公开(公告)日：2002-05-21

申请号：US09254892

申请日：1999-06-28

申请人： Dong-Mei Feng ,  Victor M. Garsky ,  Raymond E. Jones ,  Allen I. Oliff ,  Jenny M. Wai

发明人： Dong-Mei Feng ,  Victor M. Garsky ,  Raymond E. Jones ,  Allen I. Oliff ,  Jenny M. Wai

IPC分类号： A61K3814

CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/1016

摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).

摘要翻译： 公开了包含具有由游离前列腺特异性抗原（PSA）选择性蛋白水解切割的氨基酸序列，亲水寡肽封闭基团和已知的细胞毒性剂的寡肽的化学共轭物。 这种缀合物可用于治疗前列腺癌和良性前列腺肥大（BPH）。

公开(公告)号：US5998362A

公开(公告)日：1999-12-07

申请号：US926412

申请日：1997-09-09

申请人： Dong-Mei Feng ,  Victor M. Garsky ,  Raymond E. Jones ,  Jenny M. Wai

发明人： Dong-Mei Feng ,  Victor M. Garsky ,  Raymond E. Jones ,  Jenny M. Wai

IPC分类号： A61K38/00 ,  A61P35/00 ,  C07K9/00 ,  A61K38/14 ,  C07K4/00

CPC分类号： C07K9/005 ,  A61K38/00

摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).