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11. 发明申请

WO0048466A3 PROTEASE INHIBITORS THAT OVERCOME DRUG RESISTANCE 审中-公开
标题翻译：蛋白酶抑制剂，可以克服药物耐药性
公开(公告)号：WO0048466A3
公开(公告)日：2000-12-28
申请号：PCT/US0004215
申请日：2000-02-18
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： TANG JORDAN J N , GHOSH ARUN K
IPC分类号： C07D307/20 , C07D307/22 , A61K31/351 , A61P31/18
CPC分类号： C07D307/20
摘要： HIV protease inhibitors are among the most powerful drugs in suppressing HIV in human patients. However, HIV developed resistance to all protease inhibitor drugs so far marketed or used in clinical trials. HIV generates resistance by mutating its protease. The strains of HIV containing mutant proteases less vulnerable to inhibitor drug are able to replicate better and maintain the infection. No effective principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr). A new inhibitor has been developed based on a new concept for designing resistance invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs. The new concept is, therefore, generally applicable for the design of other resistance invulnerable HIVPr inhibitor drugs.
摘要翻译：艾滋病毒蛋白酶抑制剂是抑制人类患者HIV最有效的药物。然而，HIV对所有迄今为止在市场上销售或用于临床试验的蛋白酶抑制剂药物都产生了抗药性。 HIV通过突变其蛋白酶产生抗性。含有突变蛋白酶的HIV株不易受抑制剂药物的影响，能够更好地复制并维持感染。设计耐药性HIV蛋白酶抑制剂（HIVPr）没有有效的原则。根据设计抗药性HIVPr抑制剂的新概念开发了一种新的抑制剂。体外数据显示，该抑制剂对许多已知的对其他HIVPr抑制剂药物耐药的HIVPr突变体有效。因此，这个新概念通常适用于其他抗药性HIVPr抑制剂药物的设计。

12. 发明公开

EP1448218A4 BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： β-分泌酶抑制剂和使用方法
公开(公告)号：EP1448218A4
公开(公告)日：2009-01-14
申请号：EP02793826
申请日：2002-10-23
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS , COMENTIS INC
发明人： GHOSH ARUN K , TANG JORDAN , BILCER GEOFFREY , CHANG WANPIN , HONG LIN , KOELSCH GERALD , LOY JEFF , TURNER ROBERT T III
IPC分类号： A61K38/00 , A61P25/28 , C07D207/16 , C07D213/30 , C07D213/40 , C07D215/14 , C07D215/36 , C07D215/54 , C07D307/14 , C07D307/16 , C07D307/20 , C07D307/93 , C07D493/04 , C07D521/00 , C07K5/03 , C07K7/02 , C07K14/00 , C07K14/47 , C07K5/10 , C07K7/06
CPC分类号： C07D307/93 , C07D207/16 , C07D213/30 , C07D213/40 , C07D215/14 , C07D215/36 , C07D215/54 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/14 , C07D307/16 , C07D307/20 , C07D493/04

13. 发明专利

AU2008229725B2 Beta-secretase inhibitors and methods of use 未知
公开(公告)号：AU2008229725B2
公开(公告)日：2010-12-09
申请号：AU2008229725
申请日：2008-10-01
申请人： COMENTIS INC , OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： CHANG WANPIN , DEVASAMUDRAM THIPPESWAMY , TURNER ROBERT T III , TANG JORDAN , KOELSCH GERALD , BILCER GEOFFREY , GHOSH ARUN K , HONG LIN , LOY JEFF
IPC分类号： A61K38/00 , C07D207/16 , A61K31/00 , A61P25/28 , C07D213/30 , C07D213/40 , C07D215/14 , C07D215/36 , C07D215/54 , C07D307/14 , C07D307/16 , C07D307/20 , C07D307/93 , C07D493/04 , C07D521/00 , C07K5/03 , C07K7/02 , C07K14/00 , C07K14/47
摘要： The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.

14. 发明专利

CA2735130A1 COMPOUNDS AND METHODS FOR TREATING RESPIRATORY DISEASES 未知
公开(公告)号：CA2735130A1
公开(公告)日：2010-02-25
申请号：CA2735130
申请日：2009-08-21
申请人： PURDUE RESEARCH FOUNDATION , UNIV ILLINOIS
发明人： GHOSH ARUN K , TAKAYAMA JUN , MESECAR ANDREW DAVID , JOHNSON MICHAEL E , RATIA KIIRA M , CHAUDHURI RIMA , MULHEARN DEBBIE C
IPC分类号： C07C233/65 , A61K31/165 , A61K31/277 , A61K31/44 , A61K31/47 , A61P11/00 , A61P31/12 , C07C235/60 , C07C237/20 , C07C255/57 , C07C323/42 , C07D213/56 , C07D215/12
摘要： Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).

15. 发明专利

AU2004202058A1 Inhibitors of memapsin 2 and use thereof 未知
公开(公告)号：AU2004202058A1
公开(公告)日：2004-06-10
申请号：AU2004202058
申请日：2004-05-14
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： GHOSH ARUN K , HONG LING , TANG JORDAN J N
IPC分类号： C07K14/00

16. 发明专利

CA2433446A1 INHIBITORS OF MEMAPSIN 2 AND USE THEREOF 未知
公开(公告)号：CA2433446A1
公开(公告)日：2002-07-11
申请号：CA2433446
申请日：2001-12-28
申请人： OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： KOELSCH GERALD , GHOSH ARUN K , TANG JORDAN J N
IPC分类号： A61K38/00 , A61K45/00 , A61P25/28 , A61P43/00 , C07K5/02 , C07K14/81 , C12N9/64 , C12Q1/37 , G01N33/68 , C07K5/03 , A61K38/55
摘要： Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined by a method which determine s the initial hydrolysis rate of the substrate by using MALDI-TOF/MS. Alternatively, the subsite specificity of mepapsin can be determined by probing a library of inhibitors with memapsin 2 and subsequently detecting t he bound memapsin 2 with an antibody raised to memapsin 2 and an alkaline phosphatase conjugated secondary antibody. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin2. The substra te analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least on e analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of substrate analogues including isoteres at the sites of the critical amino acid residues were developed and the more than seventy substrate analogues were synthetized, among which MMI-005, MMI-012, MMI-017, MMI-018, MMI-025, MMI-026, MMI-037, MMI-039, MMI-040, MMI-066, MMI- 070, and MMI-071 have inhibitionconstants in the range of 1.4-61.4 x 109 M against recombinant pro-memapsin 2. These inhibitors are useful in diagnosti cs and for the treatment and/or prevention of Alzheimer's disease.

17. 发明专利

ES2604662T3 Ensayo de acondicionamiento físico y métodos para reducir la resistencia del VIH a la terapia 未知
公开(公告)号：ES2604662T3
公开(公告)日：2017-03-08
申请号：ES10179052
申请日：1999-06-23
申请人： THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES , THE BOARD OF TRUSTEES OF THE UNIV ILLINOIS
发明人： ERICKSON JOHN W , GULNIK SERGEI V , MITSUYA HIROAKI , GHOSH ARUN K
IPC分类号： C07D493/04 , G01N33/15 , A61K31/34 , A61K31/445 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D491/04 , C07D495/04 , C12Q1/02 , C12Q1/37
摘要： Una cantidad eficaz inhibidora de la resistencia de un compuesto de fórmula: **Fórmula** en el que: (i) A es **Fórmula** R3 es fenilo, R5 es isobutilo, y Ar es fenilo sustituido con un grupo m-hidroxilo, un grupo m- o p-hidroximetilo, o un grupo p-aminometilo; o (ii) A es**Fórmula** R3 es R5 es isobutilo, y Ar es p-metoxifenilo; (iii) A es **Fórmula** R3 es fenilo, R5 es **Fórmula** y Ar es m-metoxifenilo; o (iv) A es **Fórmula** R3 es fenilo, R5 es isobutilo, y Ar es p-aminofenilo para su uso en el tratamiento de un mamífero infectado por el VIH que está infectado con un VIH mutante, en combinación con un agente antiviral seleccionado del grupo que consiste en ritonavir, indinavir y saquinavir en un vehículo farmacéuticamente aceptable, en el que dicho tratamiento previene la aparición de resistencia a los medicamentos debido a mutaciones adicionales.

18. 发明专利

CA2478731C CARBAMATES AS HIV PROTEASE INHIBITORS 未知
公开(公告)号：CA2478731C
公开(公告)日：2013-01-08
申请号：CA2478731
申请日：2003-03-07
申请人： UNIV ILLINOIS
发明人： GHOSH ARUN K , BILCER GEOFFREY M , DEVASAMUDRAM THIPPESWAMY
IPC分类号： C07D493/04 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/36 , A61K31/397 , A61K31/4025 , A61K31/403 , A61K31/4427 , A61K31/4525 , A61K31/4725 , A61K31/513 , A61K31/5377 , A61K31/635 , A61K45/06 , A61P31/18 , C07C311/29 , C07C311/41 , C07D207/26 , C07D209/96 , C07D213/70 , C07D307/20 , C07D307/935 , C07D307/94 , C07D317/44 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D419/12 , C07D491/10 , C07D519/00
摘要： The present invention relates to compounds having the general formula (I) depicted below, useful for inhibiting HIV protease. The present invention also relates methods of making such compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV. (see formula I)

19. 发明专利

AU2007203321C1 Method of treating HIV infections 未知
公开(公告)号：AU2007203321C1
公开(公告)日：2011-12-08
申请号：AU2007203321
申请日：2007-07-17
申请人： UNIV ILLINOIS , THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRETARY DEPARTMENT OF HEALTH AND HUMAN SERVICES
发明人： GHOSH ARUN K , GULNIK SERGEI V , ERICKSON JOHN W , HIROAKI MITSUYA
IPC分类号： A61K31/335 , A61P31/18 , C12Q1/00
摘要： The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity 5 relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of-thes emergence of drug resistance in therapy.

20. 发明专利

AU2008229725A1 Beta-secretase inhibitors and methods of use 未知
公开(公告)号：AU2008229725A1
公开(公告)日：2008-10-30
申请号：AU2008229725
申请日：2008-10-01
申请人： COMENTIS INC , OKLAHOMA MED RES FOUND , UNIV ILLINOIS
发明人： CHANG WAUPIN , TURNER ROBERT T III , TANG JORDAN , KOELSCH GERALD , BILCER GEOFFREY , GHOSH ARUN K , HONG LIU , LOY JEFF
IPC分类号： A61K38/00 , A61K31/00 , A61P25/28 , C07D207/16 , C07D213/30 , C07D213/40 , C07D215/14 , C07D215/36 , C07D215/54 , C07D307/14 , C07D307/16 , C07D307/20 , C07D307/93 , C07D493/04 , C07D521/00 , C07K5/03 , C07K7/02 , C07K14/00 , C07K14/47
摘要： The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.

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