公开(公告)号：US20070037813A1

公开(公告)日：2007-02-15

申请号：US11537482

申请日：2006-09-29

Applicant: Ignacio Aliagas-Martin ,  Dean Artis ,  Michael Dina ,  John Flygare ,  Richard Goldsmith ,  Regina Munroe ,  Alan Olivero ,  Richard Pastor ,  Thomas Rawson ,  Kirk Robarge ,  Daniel Sutherlin ,  Kenneth Weese ,  Aihe Zhou ,  Yan Zhu

Inventor： Ignacio Aliagas-Martin ,  Dean Artis ,  Michael Dina ,  John Flygare ,  Richard Goldsmith ,  Regina Munroe ,  Alan Olivero ,  Richard Pastor ,  Thomas Rawson ,  Kirk Robarge ,  Daniel Sutherlin ,  Kenneth Weese ,  Aihe Zhou ,  Yan Zhu

IPC: A61K31/50 ,  A61K31/44 ,  A61K31/165 ,  C07D237/02

CPC classification number: C07C257/18 ,  C07C311/05 ,  C07C311/08 ,  C07C311/13 ,  C07C311/18 ,  C07C311/29 ,  C07C311/51

Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Abstract translation: 具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。

公开(公告)号：US20060167066A1

公开(公告)日：2006-07-27

申请号：US11312063

申请日：2005-12-19

Applicant: Frederick Cohen ,  Vickie Tsui ,  Cuong Ly ,  John Flygare

Inventor： Frederick Cohen ,  Vickie Tsui ,  Cuong Ly ,  John Flygare

IPC: A61K31/427 ,  A61K31/422 ,  C07D417/02 ,  C07D413/02

CPC classification number: C07D471/04 ,  C07D417/04 ,  C07D417/14

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4′, R5, R6′ and R6′ are as described herein.

Abstract translation: 本发明提供新的IAP抑制剂，其可用作治疗恶性肿瘤的治疗剂，其中化合物具有通式I：其中A，Q，X 1，X 2， Y，R 1，R 2，R 3，R 4，R 4， R 5，R 6和R 6'如本文所述。

公开(公告)号：US20050261203A1

公开(公告)日：2005-11-24

申请号：US11088008

申请日：2005-03-22

Applicant: Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Keteltas ,  Vickie Tsui

Inventor： Frederick Cohen ,  Wayne Fairbrother ,  John Flygare ,  Stephen Keteltas ,  Vickie Tsui

IPC: A61K31/403 ,  A61K38/04 ,  C07D203/02 ,  C07D209/02 ,  C07D409/12 ,  C07K5/06 ,  C07K14/47

CPC classification number: C07K5/06026 ,  C07K14/4747

Abstract: The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: X1 and X2 are independently O or S; L is a bond or —C(X3)—, —C(X3)NR12, —C(X3)O— wherein X3 is O or S and R12 is H or R1; R1 is alkyl, a carbocycle, carbocycle-substituted alkyl, a heterocycle or heterocycle-substituted alkyl, wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, haloalkyl, alkoxy, alkylsulfonyl, amino, nitro, aryl and heteroaryl; R2 is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, a heterocycle or heterocyclylalkyl; R3 is H or alkyl; R4 and R4′ are independently H, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroaralkyl wherein each is optionally substituted with halogen, hydroxyl, mercapto, carboxyl, alkyl, alkoxy, amino and nitro; R5, and R5 are each independently H or alkyl; R6 is H or alkyl; and salts and solvates thereof.

Abstract translation: 本发明提供可用作治疗恶性肿瘤的治疗剂的IAP的新型抑制剂，其中化合物具有通式I：X 1和X 2独立地为O或S ; -C（X 3） - ， - C（X 3）NR 12，-C（X 3） 3其中X 3是O或S，R 12是H或R 1; R 1是烷基，碳环，碳环取代的烷基，杂环或杂环取代的烷基，其中各自任选被卤素，羟基，巯基，羧基，烷基，卤代烷基，烷氧基，烷基磺酰基， 氨基，硝基，芳基和杂芳基; R 2是烷基，环烷基，环烷基烷基，芳基，芳烷基，杂环或杂环基烷基; R 3是H或烷基; R 4和R 4'独立地为H，烷基，芳基，芳烷基，环烷基，环烷基烷基，杂芳基或杂芳烷基，其中各自任选被卤素，羟基，巯基， 羧基，烷基，烷氧基，氨基和硝基; R 5和R 5各自独立地为H或烷基; R 6是H或烷基; 及其盐和溶剂合物。