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    MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND USE THEREOF
    1.
    发明申请
    MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND USE THEREOF 审中-公开
    多种抗药性复性蛋白酶抑制剂及其用途

    公开(公告)号：WO9967254A3

    公开(公告)日：2000-02-10

    申请号：PCT/US9914120

    申请日：1999-06-23

    Applicant: US HEALTH ,  UNIV ILLINOIS ,  ERICKSON JOHN W ,  GULNIK SERGEI V ,  GHOSH ARUN K ,  HUSSAIN KHAJA A

    Inventor： ERICKSON JOHN W ,  GULNIK SERGEI V ,  GHOSH ARUN K ,  HUSSAIN KHAJA A

    IPC: G01N33/15 ,  A61K31/34 ,  A61K31/4525 ,  A61P31/18 ,  A61P37/04 ,  A61P43/00 ,  C07D493/04 ,  C12Q1/02 ,  C12Q1/37 ,  C07D491/04 ,  C07D495/04

    CPC classification number: A61K31/4525 ,  A61K31/34 ,  C07D493/04 ,  C12Q1/025 ,  C12Q1/37 ,  G01N2333/16 ,  G01N2333/8142

    Abstract: The present invention generally provides a retroviral protease-inhibiting compound represented by formula (I), or a pharmaceutically acceptable salt, a prodrug, or an ester thereof, wherein A is a group of formula (II), (III), (IV), or (V); R , R , R , R , or R is H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH2, O, S, SO, SO2, amino, amides, carbamates, ureas or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO2; m is from 0 to 6; R is OH, =O (keto), NH2, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO2; wherein the compound inhibits a multidrug-resistant retroviral protease. Optionally, R and R , together the N-W bond of formula (I), comprise a 12- to 18-membered ring. Also provided are pharmaceutical compositions for, and therapeutic methods of, treating a multidrug-resistant retroviral infection in a mammal.

    Abstract translation: 本发明通常提供由式（I）表示的逆转录病毒蛋白酶抑制化合物或其药学上可接受的盐，前药或酯，其中A为式（II），（III），（IV）， ，或（V）; R 1，R 2，R 3，R 5或R 6是H，或任选取代的和/或含杂原子的烷基，烯基，炔基或环状基团; Y和/或Z是任选被烷基，烯基或炔基取代的CH 2，O，S，SO，SO 2，氨基，酰胺，氨基甲酸酯，脲或硫代羰基衍生物; n为1〜5; X是一个键，任选取代的亚甲基或亚乙基，氨基，O或S; Q是C（O），C（S）或SO 2; m为0〜6; R 4是OH，= O（酮），NH 2或烷基氨基，包括酯，酰胺和其盐; W为C（O），C（S），S（O）或SO 2; 其中所述化合物抑制多药耐药逆转录病毒蛋白酶。 任选地，R 5和R 6一起形成式（I）的N-W键，包含12至18元环。 还提供了用于治疗哺乳动物多药耐药逆转录病毒感染的药物组合物和治疗方法。

    FITNESS ASSAY AND ASSOCIATED METHODS
    2.
    发明申请
    FITNESS ASSAY AND ASSOCIATED METHODS 审中-公开
    适应性测定及相关方法

    公开(公告)号：WO9967417A2

    公开(公告)日：1999-12-29

    申请号：PCT/US9914119

    申请日：1999-06-23

    Applicant: US HEALTH ,  ERICKSON JOHN W ,  GULNIK SERGEI V

    Inventor： ERICKSON JOHN W ,  GULNIK SERGEI V

    IPC: G01N33/15 ,  A61K31/34 ,  A61K31/4525 ,  A61P31/18 ,  A61P37/04 ,  A61P43/00 ,  C07D493/04 ,  C12Q1/02 ,  C12Q1/37 ,  C12Q1/00

    CPC classification number: A61K31/341 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/47 ,  A61K31/4725 ,  A61K31/496 ,  C12Q1/025 ,  C12Q1/37 ,  G01N2333/16 ,  G01N2333/8142

    Abstract: The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity 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 the emergence of drug resistance in therapy. The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of formulas (A), (B), (C) or (D); R , R , R , R or R is H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH2, O, S, SO, SO2, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO2; m is from 0 to 6; R is OH, =O (keto), NH2, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO2. Optionally, R and R , together with the N-W bond of formula (I), comprise a macrocyclic ring.

    Abstract translation: 本发明提供了一种用于确定突变体复制生物实体中生物化学物质相对于其前身的生物化学适应性的测定法。 本发明还提供了用于测量蛋白酶抑制剂的抗HIV蛋白酶活性的连续荧光测定法。 本发明还提供一种给药治疗化合物的方法，所述治疗化合物降低治疗中耐药性出现的可能性。 本发明还提供式（I）化合物或其药学上可接受的盐，前药，组合物或酯，其中A为式（A），（B），（C）或（D ）; R 1，R 2，R 3，R 5或R 6是H，或任选取代的和/或含杂原子的烷基，烯基，炔基或环状基团; Y和/或Z是任选被烷基，烯基或炔基取代的CH 2，O，S，SO，SO 2，氨基，酰胺，氨基甲酸酯，脲或硫代羰基衍生物; n为1〜5; X是一个键，任选取代的亚甲基或亚乙基，氨基，O或S; Q是C（O），C（S）或SO 2; m为0〜6; R 4是OH，= O（酮），NH 2或烷基氨基，包括酯，酰胺和其盐; W是C（O），C（S），S（O）或SO 2。 任选地，R 5和R 6与式（I）的N-W键一起包含大环。

    ANTI-FUSION ASSAY
    4.
    发明申请
    ANTI-FUSION ASSAY 审中-公开
    抗融合测定

    公开(公告)号：WO03027255A2

    公开(公告)日：2003-04-03

    申请号：PCT/US0230611

    申请日：2002-09-27

    Applicant: TIBOTEC PHARM LTD ,  XIE DONG ,  ERICKSON JOHN W ,  GRULICH PAUL

    Inventor： XIE DONG ,  ERICKSON JOHN W ,  GRULICH PAUL

    IPC: A61K45/00 ,  A61P31/18 ,  C07K7/00 ,  C07K14/47 ,  G01N27/447 ,  G01N33/15 ,  G01N33/48 ,  G01N33/50 ,  G01N33/561 ,  G01N33/569 ,  G01N33/68 ,  G06F19/00 ,  C12N

    CPC classification number: G01N33/56988 ,  G01N33/6803 ,  G01N2333/162 ,  G01N2500/02

    Abstract: Methods of identifying a fusion inhibitor and inhibitors of gp41-mediated membrane fusion are disclosed. The methods comprise, for example, providing a first helical polypeptide comprising a sequence of IQN17 (SEQ ID NO: 1); providing a second helical polypeptide of 34 or less than 34 amino acids comprising the amino acid sequence W-X1-X2-W-X3-X4-X5-I, wherein X1, X2, X3, X4, and X5 are each independently chosen from any amino acid except proline; measuring, by capillary zone electrophoresis, the degree of complex formation between these peptides; and comparing the measured degree of complex formation to the degree in the presence of a test composition.

    Abstract translation: 公开了鉴定融合抑制剂和gp41介导的膜融合抑制剂的方法。 所述方法包括例如提供包含IQN17（SEQ ID NO：1）序列的第一螺旋多肽; 提供包含氨基酸序列W-X1-X2-W-X3-X4-X5-I的34个或小于34个氨基酸的第二螺旋多肽，其中X1，X2，X3，X4和X5各自独立地选自 除脯氨酸以外的任何氨基酸; 通过毛细管区带电泳测量这些肽之间的复合物形成程度; 并将测量的复合物形成程度与存在测试组合物的程度进行比较。

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