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    Amides as inhibitors of human secreted phospholipase A2
    3.
    发明授权
    Amides as inhibitors of human secreted phospholipase A2 有权
    酰胺作为人体分泌的磷脂酶A2的抑制剂

    公开(公告)号：US08759392B2

    公开(公告)日：2014-06-24

    申请号：US12994136

    申请日：2009-07-21

    申请人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou ,  Samuel David

    发明人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou ,  Samuel David

    IPC分类号： A61K31/225

    CPC分类号： A61K31/165 ,  C07C233/51

    摘要： Methods and compounds useful for inhibiting a phoshpolipase A2 are provided, the methods comprising contacting the phoshpolipase A2 with a compound having the structure A, or pharmaceutically acceptable salts thereof: wherein R1 is H, F, NH2, or COOH; R2 is, H, linear saturated or unsaturated alkyl, alkenyl, or alkynyl; each of R3 and R4 is independently H, linear saturated or unsaturated alkyl, alkenyl, alkynyl, phenyl, or substituted phenyl; R5 is H, (C1-C6) alkyl such as methyl or ethyl; X is aryl or substituted aryl, such as phenyl or a substituted phenyl; and Y is O or S.

    摘要翻译： 提供了可用于抑制磷脂酶A2的方法和化合物，所述方法包括使磷脂酶A2与具有结构A的化合物或其药学上可接受的盐接触：其中R1是H，F，NH2或COOH; R2是H，直链饱和或不饱和的烷基，烯基或炔基; R 3和R 4各自独立地为H，直链饱和或不饱和的烷基，烯基，炔基，苯基或取代的苯基; R5是H，（C1-C6）烷基如甲基或乙基; X是芳基或取代的芳基，例如苯基或取代的苯基; Y是O或S.

    2-oxamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudopeptides
    4.
    发明授权
    2-oxamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudopeptides 有权
    基于二肽和假肽的磷脂酶A2活性的2-氧化物抑制剂和细胞花生四烯酸盐释放

    公开(公告)号：US08580852B2

    公开(公告)日：2013-11-12

    申请号：US13262618

    申请日：2010-04-19

    申请人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou

    发明人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou

    IPC分类号： A61K31/22 ,  A61K31/195 ,  A61P29/00

    CPC分类号： A61K31/22 ,  C07B2200/07 ,  C07C235/74 ,  C07C237/22

    摘要： The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA 2 and GVIA 1PLA 2) and one human secretory phospholipase A2 (GV sPLA 2) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA 2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA 2. The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA 2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 μM.

    摘要翻译： 本公开提供了一系列基于二肽和假二肽的2-氧代酰胺，其被合成并且对两种人细胞内磷脂酶A2（GIVA CPLA 2和GVIA 1PLA 2）和一种人分泌型磷脂酶A2（GV sPLA 2）的活性进行了评估。 含有游离羧基的衍生物是选择性GIVA cPLA 2抑制剂。 基于醚假二肽的乙酯的衍生物是第一个2-氧代酰胺，其优先抑制GVIA iPLA 2.还研究了2-氧代酰胺对RAW 264.7巨噬细胞产生花生四烯酸的影响。 发现选择性GIVA cPLA 2抑制剂优先抑制细胞花生四烯酸释放; 其中一个假二肽产生2μM的IC 50值。

    2-OXAMIDE INHIBITORS OF PHOSPHOLIPASE A2 ACTIVITY AND CELLULAR ARACHIDONATE RELEASE BASED ON DIPEPTIDES AND PSEUDOPEPTIDES
    5.
    发明申请
    2-OXAMIDE INHIBITORS OF PHOSPHOLIPASE A2 ACTIVITY AND CELLULAR ARACHIDONATE RELEASE BASED ON DIPEPTIDES AND PSEUDOPEPTIDES 有权
    磷脂酰胆碱酯酶A2活性的2-氧化胺抑制剂和基于脯氨酸和胰蛋白酶的细胞培养基释放

    公开(公告)号：US20120095096A1

    公开(公告)日：2012-04-19

    申请号：US13262618

    申请日：2010-04-19

    申请人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou

    发明人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou

    IPC分类号： A61K31/22 ,  A61K31/195 ,  A61P29/00 ,  C07C229/24

    CPC分类号： A61K31/22 ,  C07B2200/07 ,  C07C235/74 ,  C07C237/22

    摘要： The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA2 and GVIA 1PLA2) and one human secretory phospholipase A2 (GVsPLA2) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA2. The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 μM.

    摘要翻译： 本公开提供了一系列基于二肽和假二肽的2-氧代酰胺，其被合成并且对两种人细胞内磷脂酶A2（GIVA CPLA2和GVIA 1PLA2）和一种人分泌型磷脂酶A2（GVsPLA2）的活性进行了评估。 含有游离羧基的衍生物是选择性GIVA cPLA2抑制剂。 基于醚假二肽的乙酯的衍生物是优先抑制GVIA iPLA2的第一个2-氧代酰胺。 还研究了2-氧代酰胺对RAW 264.7巨噬细胞产生花生四烯酸的影响。 发现选择性GIVA cPLA2抑制剂优先抑制细胞花生四烯酸释放; 其中一个假性肽给出2μM的IC 50值。

    Amides as Inhibitors of Human Secreted Phospholipase A2
    6.
    发明申请
    Amides as Inhibitors of Human Secreted Phospholipase A2 有权
    酰胺作为人分泌磷脂酶A2的抑制剂

    公开(公告)号：US20110111478A1

    公开(公告)日：2011-05-12

    申请号：US12994136

    申请日：2009-07-21

    申请人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou ,  Samuel David

    发明人： Edward A. Dennis ,  George Kokotos ,  Violetta Constantinou-Kokotou ,  Samuel David

    IPC分类号： C12N9/99 ,  C07C229/34

    CPC分类号： A61K31/165 ,  C07C233/51

    摘要： Methods and compounds useful for inhibiting a phospholipase A2 are provided, the methods comprising contacting the phospholipase A2 with a compound having the structure A, or pharmaceutically acceptable salts thereof: wherein R1 is H, F, NH2, or COOH; R2 is, H, linear saturated or unsaturated alkyl, alkenyl, or alkynyl; each of R3 and R4 is independently H, linear saturated or unsaturated alkyl, alkenyl, alkynyl, phenyl, or substituted phenyl; R5 is H, (C1-C6) alkyl such as methyl or ethyl; X is aryl or substituted aryl, such as phenyl or a substituted phenyl; and Y is O or S.

    摘要翻译： 提供了可用于抑制磷脂酶A2的方法和化合物，所述方法包括使磷脂酶A2与具有结构A的化合物或其药学上可接受的盐接触：其中R1是H，F，NH2或COOH; R2是H，直链饱和或不饱和的烷基，烯基或炔基; R 3和R 4各自独立地为H，直链饱和或不饱和的烷基，烯基，炔基，苯基或取代的苯基; R5是H，（C1-C6）烷基如甲基或乙基; X是芳基或取代的芳基，例如苯基或取代的苯基; Y是O或S.

    Hydrolytic enzyme inhibitors/inactivators and methods for using same
    8.
    发明授权
    Hydrolytic enzyme inhibitors/inactivators and methods for using same 失效
    水解酶抑制剂/灭活剂及其使用方法

    公开(公告)号：US5308766A

    公开(公告)日：1994-05-03

    申请号：US713116

    申请日：1991-06-10

    申请人： Edward A. Dennis ,  William N. Washburn

    发明人： Edward A. Dennis ,  William N. Washburn

    IPC分类号： C07F9/10 ,  C12Q1/34 ,  C12N9/99 ,  C12N9/14

    CPC分类号： C12Q1/34 ,  C07F9/10 ,  C12Q2334/10 ,  G01N2333/918 ,  G01N2405/04

    摘要： The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.

    摘要翻译： 本发明提供了作为水解酶抑制剂（灭活剂）和底物起作用的化合物。 这些化合物可用于检测和测量水解酶活性水平的测定中，并且特别适用于涉及潜在的特异性水解酶的各种疾病状态和条件的治疗方案。 水解酶的实例包括但不限于磷脂酶，脂肪酶，酯酶，蛋白酶等