公开(公告)号：US20060241106A1

公开(公告)日：2006-10-26

申请号：US10544443

申请日：2004-02-09

申请人： Martin Drysdale ,  Brian Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen James ,  Kwai Cheung ,  Thomas Matthews

发明人： Martin Drysdale ,  Brian Dymock ,  Harry Finch ,  Paul Webb ,  Edward McDonald ,  Karen James ,  Kwai Cheung ,  Thomas Matthews

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/42

CPC分类号： A61K31/541 ,  A61K31/42 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D261/08 ,  C07D261/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D495/04

摘要： Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.

公开(公告)号：USD449414S1

公开(公告)日：2001-10-16

申请号：US29134144

申请日：2000-12-14

申请人： Kenneth R. James ,  Karen James

设计人： Kenneth R. James ,  Karen James

公开(公告)号：US20050256058A1

公开(公告)日：2005-11-17

申请号：US11062017

申请日：2005-02-18

申请人： James Powers ,  Juliana Asgian ,  Ozlem Ekici ,  Marion Gotz ,  Karen James ,  Zhao Li ,  Brian Rukamp

发明人： James Powers ,  Juliana Asgian ,  Ozlem Ekici ,  Marion Gotz ,  Karen James ,  Zhao Li ,  Brian Rukamp

IPC分类号： A61K38/05 ,  A61K38/06 ,  C07D249/16 ,  C07K5/02 ,  C07K5/06 ,  C07K5/072 ,  C07K5/083 ,  C07K5/093

CPC分类号： A61K38/05 ,  A61K38/06 ,  C07K5/02 ,  C07K5/06026 ,  C07K5/06104 ,  C07K5/0808 ,  C07K5/0819

摘要： The present disclosure provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the disclosure include a peptidyl propenoyl hydrazide compositions that inhibit proteases, for example cysteine proteases, either in vivo or in vitro.

摘要翻译： 本公开提供了用于抑制蛋白酶的组合物，用于合成组合物的方法以及使用所公开的蛋白酶抑制剂的方法。 本公开的方面包括在体内或体外抑制蛋白酶例如半胱氨酸蛋白酶的肽基丙烯酰肼组合物。