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    MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND USE THEREOF
    2.
    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
    3.
    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。

    LONG ACTING BIOLOGICALLY ACTIVE CONJUGATES
    4.
    发明申请
    LONG ACTING BIOLOGICALLY ACTIVE CONJUGATES 审中-公开

    公开(公告)号：WO2004085505A3

    公开(公告)日：2004-10-07

    申请号：PCT/US2004/008847

    申请日：2004-03-24

    Applicant: SEQUOIA PHARMACEUTICALS, INC. ,  SILVA, Abelardo ,  ERICKSON, John, E. ,  EISSENSTAT, Michael ,  AFONINA, Elena ,  GULNIK, Sergei

    Inventor： SILVA, Abelardo ,  ERICKSON, John, E. ,  EISSENSTAT, Michael ,  AFONINA, Elena ,  GULNIK, Sergei

    IPC: A61K38/00

    Abstract: The invention provides biologically active compounds that may be reacted with macromolecules, such as albumin, to form covalent linked complexes wherein the resulting complexes exhibit a desired biological activity in vivo. More specifically, the complexes are isolated complexes comprising a biologically active moiety covalently bound to a linking group and a protein. The complexes are prepared by conjugating a biologically active moiety, for example, a renin inhibitor or a viral fusion inhibitor peptide, with purified and isolated protein. The complexes have extended lifetimes in the bloodstream as compared to the unconjugated molecule, and exhibit biological activity for extended periods of time as compared to the unconjugated molecule. The invention also provides anti-viral compounds that are inhibitors of viral infection and/or exhibit anti-fusiogenic properties. In particular, this invention provides compounds having inhibiting activity against viruses such as human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) and that have extended duration of action for the treatment of viral infections.

    LONG ACTING BIOLOGICALLY ACTIVE CONJUGATES
    9.
    发明申请
    LONG ACTING BIOLOGICALLY ACTIVE CONJUGATES 审中-公开
    长期生物活性结合

    公开(公告)号：WO2004085505A2

    公开(公告)日：2004-10-07

    申请号：PCT/US2004008847

    申请日：2004-03-24

    Applicant: SEQUOIA PHARMACEUTICALS INC ,  SILVA ABELARDO ,  ERICKSON JOHN E ,  EISSENSTAT MICHAEL ,  AFONINA ELENA ,  GULNIK SERGEI

    Inventor： SILVA ABELARDO ,  ERICKSON JOHN E ,  EISSENSTAT MICHAEL ,  AFONINA ELENA ,  GULNIK SERGEI

    IPC: A61K38/00 ,  C07K14/00 ,  C07K14/765 ,  C08G20060101 ,  C08G

    CPC classification number: C07K14/765 ,  A61K38/00 ,  A61K47/643

    Abstract: The invention provides biologically active compounds that may be reacted with macromolecules, such as albumin, to form covalent linked complexes wherein the resulting complexes exhibit a desired biological activity in vivo. More specifically, the complexes are isolated complexes comprising a biologically active moiety covalently bound to a linking group and a protein. The complexes are prepared by conjugating a biologically active moiety, for example, a renin inhibitor or a viral fusion inhibitor peptide, with purified and isolated protein. The complexes have extended lifetimes in the bloodstream as compared to the unconjugated molecule, and exhibit biological activity for extended periods of time as compared to the unconjugated molecule. The invention also provides anti-viral compounds that are inhibitors of viral infection and/or exhibit anti-fusiogenic properties. In particular, this invention provides compounds having inhibiting activity against viruses such as human immunodeficiency virus (HIV), respiratory syncytial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) and that have extended duration of action for the treatment of viral infections.

    Abstract translation: 本发明提供可与大分子如白蛋白反应的生物活性化合物以形成共价连接的络合物，其中所得的复合物在体内显示出所需的生物学活性。 更具体地，复合物是包含与连接基团和蛋白质共价结合的生物活性部分的分离的复合物。 通过将生物活性部分例如肾素抑制剂或病毒融合抑制剂肽与纯化和分离的蛋白质缀合来制备复合物。 与非共轭分子相比，复合物在血液中的寿命延长，与非共轭分子相比，延长的时间段具有生物活性。 本发明还提供了抗病毒化合物，其是病毒感染的抑制剂和/或表现出抗融合生物学特性。 特别地，本发明提供了对人体免疫缺陷病毒（HIV），呼吸道合胞病毒（RSV），人副流感病毒（HPV），麻疹病毒（MeV）和猿猴免疫缺陷病毒（SIV）等病毒具有抑制活性的化合物， 延长了治疗病毒感染的时间。

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