公开(公告)号：US20040116361A1

公开(公告)日：2004-06-17

申请号：US10723672

申请日：2003-11-26

申请人： Board of Trustees of Michigan State University ,  The Regents of the University of California

发明人： Robert H. Cichewicz ,  Muraleedharan G. Nair ,  James H. McKerrow

IPC分类号： A61K031/12

CPC分类号： A61K31/70 ,  A61K31/21 ,  C07C50/38 ,  Y02A50/423

摘要： Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: 1 wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

公开(公告)号：US20030229032A1

公开(公告)日：2003-12-11

申请号：US10317906

申请日：2002-12-12

申请人： Board of Trustees of MICHIGAN STATE UNIVERSITY ,  The Regents of the University of California

发明人： Robert H. Cichewicz ,  Muraleedharan G. Nair ,  James H. McKerrow

IPC分类号： A61K031/704 ,  A61K031/12

CPC分类号： A61K31/70 ,  A61K31/21 ,  C07C50/38 ,  Y02A50/423

摘要： Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: 1 wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

摘要翻译： 描述了蒽醌类化合物，其具有抗耳毒性，特别是可用于抑制血吸虫病的组合物。 体外或体内。 优选的蒽醌具有下式：其中R 1，R 2，R 3和R 4各自为氢，羟基，卤素，烷基，取代的烷基，烯烃，取代的烯烃，炔，芳基，取代的芳基，环状，取代的环状，酸基，碳水化合物 或其组合，R是含有1至12个碳的基团，例如甲基，烷基，取代的烷基，醛，羟基，羟甲基，酸基，碳水化合物或其组合，卤素是I，F，Br或Cl 。

公开(公告)号：US20040014801A1

公开(公告)日：2004-01-22

申请号：US10431714

申请日：2003-05-08

申请人： The Regents of the University of California

发明人： Fred E. Cohen ,  Xiaohui Du ,  Chun Guo ,  James H. McKerrow

IPC分类号： A61K031/415 ,  A61K031/175 ,  C07D231/06 ,  C07C337/08 ,  C07C281/12

CPC分类号： C07D231/06 ,  C07C281/14 ,  C07C337/08 ,  C07D207/48 ,  C07D209/14 ,  C07D307/52 ,  C07D333/22 ,  C07D333/28 ,  C07D409/04

摘要： The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

摘要翻译： 本发明涉及半胱氨酸蛋白酶的硫代缩氨基脲和缩氨基脲抑制剂以及使用这些化合物来预防和治疗原生动物感染如锥虫病，疟疾和利什曼病的方法。 该化合物还可用于抑制与癌发生相关的半胱氨酸蛋白酶，包括组织蛋白酶B和L.

公开(公告)号：US20040152645A1

公开(公告)日：2004-08-05

申请号：US10761071

申请日：2004-01-20

申请人： Board of Trustees of Michigan State University ,  The Regents of the University of California

发明人： Robert H. Cichewicz ,  Muraleedharan G. Nair ,  James H. McKerrow

IPC分类号： A61K031/704 ,  A61K031/12

CPC分类号： A61K31/70 ,  A61K31/21 ,  C07C50/38 ,  Y02A50/423

摘要： Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: 1 wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

摘要翻译： 描述了蒽醌类化合物，其具有抗耳毒性，特别是可用于抑制血吸虫病的组合物。 体外或体内。 优选的蒽醌具有下式：其中R 1，R 2，R 3和R 4各自为氢，羟基，卤素，烷基，取代的烷基，烯烃，取代的烯烃，炔，芳基，取代的芳基，环状，取代的环状，酸基，碳水化合物 或其组合，R是含有1至12个碳的基团，例如甲基，烷基，取代的烷基，醛，羟基，羟甲基，酸基，碳水化合物或其组合，卤素是I，F，Br或Cl 。

公开(公告)号：US20040106686A1

公开(公告)日：2004-06-03

申请号：US10723671

申请日：2003-11-26

申请人： Board of Trustees of Michigan State University ,  The Regents of the University of California

发明人： Robert H. Cichewicz ,  Muraleedharan G. Nair ,  James H. McKerrow

IPC分类号： A61K031/12 ,  A01N035/00

CPC分类号： A61K31/70 ,  A61K31/21 ,  C07C50/38 ,  Y02A50/423

摘要： Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: 1 wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.