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1. 发明申请

WO1995013084A1 CATHEPSIN D IS AN AMYLOIDOGENIC PROTEASE IN ALZHEIMER'S DISEASE 审中-公开
标题翻译： CATHEPSIN D是阿尔茨海默病中的氨基酸分泌蛋白
公开(公告)号：WO1995013084A1
公开(公告)日：1995-05-18
申请号：PCT/US1994007043
申请日：1994-06-21
申请人： MILES INC. , TAMBURINI, Paul, Perry , BENZ, Günter, Hans, Heinz, Herbert , HÄBICH, Dieter , DREYER, Robert, Norman , KOENIG, Gerhard
发明人： MILES INC.
IPC分类号： A61K37/64
CPC分类号： C12N9/6478 , A61K38/00 , C07K14/4711 , C07K14/8142 , C07K16/18 , G01N33/6896 , G01N2333/4709 , G01N2333/8142 , G01N2333/96472
摘要： Deposition of the neurotoxic beta-amyloid peptide is a pathologic process that takes place in the brains of Alzheimer's disease patients. Disclosed are methods for treating a patient with a therapeutic compound that functions by blocking the formation of beta-amyloid from the amyloid precursor protein (APP). We have identified the aspartic protease cathepsin D as a protease responsible for amyloidogenic processing of APP. Non-toxic compounds are disclosed that block both the in vitro activity of human cathepsin D, and the release of beta-amyloid by human cells. Such aspartic protease inhibitors thus have utility as therapeutics for Alzheimer's disease by blocking the pathologic accumulation of beta-amyloid.
摘要翻译：神经毒性β-淀粉样蛋白肽的沉积是在阿尔茨海默病患者的大脑中发生的病理过程。公开了用于通过阻断淀粉样蛋白前体蛋白（APP）形成β-淀粉样蛋白而起作用的治疗化合物治疗患者的方法。我们已经鉴定出天冬氨酸蛋白酶组织蛋白酶D作为负责APP淀粉样生长加工的蛋白酶。公开了阻止人组织蛋白酶D的体外活性和人细胞释放β-淀粉样蛋白的无毒化合物。因此，这种天冬氨酸蛋白酶抑制剂因此通过阻断β-淀粉样蛋白的病理性积累而用作阿尔茨海默病的治疗剂。

2. 发明申请

WO99067254A2 MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND ASSOCIATED METHODS 审中-公开
标题翻译：多药耐药性退行性蛋白酶抑制剂及相关方法
公开(公告)号：WO99067254A2
公开(公告)日：1999-12-29
申请号：PCT/US1999/014120
申请日：1999-06-23
IPC分类号： G01N33/15 , A61K31/34 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37 , C07D493/00
CPC分类号： A61K31/4525 , A61K31/34 , C07D493/04 , C12Q1/025 , C12Q1/37 , G01N2333/16 , G01N2333/8142
摘要： 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.
摘要翻译：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。

3. 发明申请

WO1994013319A1 CATHEPSIN D IS AN AMYLOIDOGENIC PROTEASE IN ALZHEIMER'S DISEASE 审中-公开
标题翻译： CATHEPSIN D是阿尔茨海默病中的氨基酸分泌蛋白
公开(公告)号：WO1994013319A1
公开(公告)日：1994-06-23
申请号：PCT/US1993010889
申请日：1993-11-12
申请人： MILES INC. , TAMBURINI, Paul, Perry , BENZ, Günter, Hans, Heinz, Herbert , HÄBICH, Dieter , DREYER, Robert, Norman
发明人： MILES INC.
IPC分类号： A61K37/64
CPC分类号： C12N9/6478 , A61K38/55 , C07K14/4711 , C12Q1/37 , G01N33/6896 , G01N2333/4709 , G01N2333/8142 , G01N2333/96472 , G01N2800/2821
摘要： Disclosed are methods for regulating formation of beta-amyloid protein with inhibitors of proteases specific for the Precursor to the Alzheimer's Disease beta-amyloid protein, such as inhibitors of aspartic protease, cathepsin D, and a chymotryptic-like serine protease; a method for detecting in vitro protease activity for molecules which possess specificity necessary for the degradation of the Amyloid Precursor Protein; assays for identifying inhibitors of proteases specific for the Amyloid Precursor Protein; and identified inhibitors and their use as therapeutics for the treatment of Alzheimer's Disease.
摘要翻译：公开了调节β-淀粉样蛋白形成的方法，其具有对阿尔茨海默氏病前体β-淀粉样蛋白前体特异性蛋白酶的抑制剂，例如天冬氨酸蛋白酶，组织蛋白酶D和糜蛋白酶样丝氨酸蛋白酶的抑制剂; 用于检测具有淀粉样蛋白前体蛋白降解所必需的特异性的分子的体外蛋白酶活性的方法; 用于鉴定淀粉样前体蛋白特异性蛋白酶抑制剂的测定法; 并鉴定了抑制剂及其作为治疗阿尔茨海默病的治疗剂的用途。

4. 发明申请

WO1996008580A1 IN VITRO METHOD FOR PREDICTING THE EVOLUTIONARY RESPONSE OF HIV PROTEASE TO A DRUG TARGETED THEREAGAINST 审中-公开
标题翻译：用于预测艾滋病病毒蛋白酶对药物靶向药物的演变反应的体外方法
公开(公告)号：WO1996008580A1
公开(公告)日：1996-03-21
申请号：PCT/US1995011860
申请日：1995-09-18
申请人： SEPRACOR INC. , MELNICK, Laurence, M. , HEEFNER, Donald, L.
发明人： SEPRACOR INC.
IPC分类号： C12Q01/37
CPC分类号： C12N9/506 , C12N15/1048 , C12Q1/37 , C12Q1/6811 , G01N2333/16 , G01N2333/8142 , Y10S435/974 , Y10S435/975
摘要： An in vitro method for identifying distinct, first generation, drug-resistant, biologically active, HIV protease mutants that may emerge in vivo in response to a drug targeted thereagainst comprising: (a) preparing, in the presence of the drug, a library of all first-generation mutants of the protease differing therefrom by one to three amino acid substitutions, each of the protease mutants being generated as part of a polyprotein with reverse transcriptase; (b) isolating drug-resistant, biologically-active mutant proteases by assaying for activity of the reverse transcriptase; and (c) identifying the distinct amino acid changes leading to the drug-resistance of the active, mutant proteases so isolated. An in vitro method for evaluating the efficacy of a drug against a biologically active mutant or wild-type form of HIV protease comprising combining the drug and a mutant polyprotein, comprising an inactive HIV protease, HIV reverse transcriptase, and one or more protease cleavage sites, adding biologically-active mutant or wild-type protease, assaying for release of active reverse transcriptase, whereby reverse transcriptase activity indicates that the drug is not efficacious against the mutant or wild-type form of HIV protease tested.
摘要翻译：一种体外方法，其用于鉴定可能在其靶向靶向药物的体内可能出现的不同的第一代，耐药性，生物活性的HIV蛋白酶突变体，其包括：（a）在所述药物存在下，制备所有蛋白酶突变体的所有第一代突变体通过一至三个氨基酸取代基与之不同，每个蛋白酶突变体作为具有逆转录酶的多聚蛋白的一部分产生; （b）通过测定逆转录酶的活性来分离耐药性，生物活性的突变型蛋白酶; 和（c）鉴定导致如此分离的活性突变蛋白酶的耐药性的不同氨基酸变化。一种用于评估药物对生物活性突变体或野生型形式的HIV蛋白酶的功效的体外方法，包括将药物和突变体多蛋白（包括无活性的HIV蛋白酶，HIV逆转录酶和一个或多个蛋白酶切割位点），添加生物活性突变体或野生型蛋白酶，测定活性逆转录酶的释放，由此逆转录酶活性表明该药物对于所测试的HIV蛋白的突变体或野生型形式是无效的。

5. 发明申请

WO2017139679A1 SYSTEMS AND COMPOSITIONS FOR DIAGNOSING PATHOGENIC FUNGAL INFECTION AND METHODS OF USING THE SAME 审中-公开
标题翻译：用于诊断致病性真菌感染的系统和组合物及使用该系统和组合物的方法
公开(公告)号：WO2017139679A1
公开(公告)日：2017-08-17
申请号：PCT/US2017/017526
申请日：2017-02-10
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： NOBILE, Clarissa , WINTER, Michael , CRAIK, Charles , JOHNSON, Alexander , O'DONOGHUE, Anthony
IPC分类号： C12Q1/37 , G01N33/569 , C07K14/40
CPC分类号： G01N33/56961 , C12N9/48 , C12N9/60 , C12Y304/23024 , G01N2333/40 , G01N2333/8142
摘要： The present disclosure relates generally to detection of contamination of a sample or diagnosis of subject based upon detection or quantification of amino acid sequences in a sample, specifically to the identification and use of molecular biomarkers for Candida albicans biofilm infections.
摘要翻译：本公开内容一般涉及基于样品中氨基酸序列的检测或定量来检测样品的污染或对象的诊断，具体涉及鉴定和使用白色念珠菌生物膜的分子生物标志物感染。

6. 发明申请

WO99067417A3 FITNESS ASSAY AND ASSOCIATED METHODS 审中-公开
标题翻译：适应性测定及相关方法
公开(公告)号：WO99067417A3
公开(公告)日：2000-09-28
申请号：PCT/US1999/014119
申请日：1999-06-23
IPC分类号： G01N33/15 , A61K31/34 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37 , C07D491/04 , C07D495/04 , A61K31/445
CPC分类号： 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 , Y02A50/411
摘要： 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.
摘要翻译：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。

7. 发明申请

WO9967254A3 MULTI-DRUG RESISTANT RETROVIRAL PROTEASE INHIBITORS AND USE THEREOF 审中-公开
标题翻译：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
申请人： US HEALTH , UNIV ILLINOIS , ERICKSON JOHN W , GULNIK SERGEI V , GHOSH ARUN K , HUSSAIN KHAJA A
发明人： ERICKSON JOHN W , GULNIK SERGEI V , GHOSH ARUN K , HUSSAIN KHAJA A
IPC分类号： G01N33/15 , A61K31/34 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37 , C07D491/04 , C07D495/04
CPC分类号： A61K31/4525 , A61K31/34 , C07D493/04 , C12Q1/025 , C12Q1/37 , G01N2333/16 , G01N2333/8142
摘要： 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.
摘要翻译：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。

8. 发明申请

WO9967417A2 FITNESS ASSAY AND ASSOCIATED METHODS 审中-公开
标题翻译：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
申请人： US HEALTH , ERICKSON JOHN W , GULNIK SERGEI V
发明人： ERICKSON JOHN W , GULNIK SERGEI V
IPC分类号： G01N33/15 , A61K31/34 , A61K31/4525 , A61P31/18 , A61P37/04 , A61P43/00 , C07D493/04 , C12Q1/02 , C12Q1/37 , C12Q1/00
CPC分类号： 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
摘要： 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.
摘要翻译：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。

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