公开(公告)号：US20050197344A1

公开(公告)日：2005-09-08

申请号：US11051268

申请日：2005-02-04

Applicant: Michael Palladino ,  George Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

Inventor： Michael Palladino ,  George Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

IPC: A61K31/496

CPC classification number: A61K31/496

Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1′, R1″, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

Abstract translation: 公开了由以下结构（I）表示的化合物：制备这种化合物的方法，其中所述方法包括使二酰基二酮哌嗪与第一醛反应以产生中间体化合物; 并使所述中间体化合物与第二醛反应以产生一类具有通式结构的化合物，其中第一种醛和第二种醛选自恶唑烷羧醛，咪唑甲醛，苯甲醛，咪唑甲醛衍生物和苯甲醛衍生物， 从而形成上述化合物，其中R 1，R 1，R 1，R 2，R 2，R 2， R 3，R 4，R 5和R 6，X 1和R 3， X 2，Y，Z，Z 1，Z 2，Z 3和Z 4 可以以与所附描述一致的方式分别定义。 还公开了治疗血管增生的组合物和方法。

公开(公告)号：US07935704B2

公开(公告)日：2011-05-03

申请号：US11051268

申请日：2005-02-04

Applicant: Michael A. Palladino ,  George Kenneth Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

Inventor： Michael A. Palladino ,  George Kenneth Lloyd ,  Yoshio Hayashi ,  Benjamin Nicholson

IPC: A61K31/497

CPC classification number: A61K31/496

Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1′, R1″, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

Abstract translation: 公开了由以下结构（I）表示的化合物：制备这种化合物的方法，其中所述方法包括使二酰基二酮哌嗪与第一醛反应以产生中间体化合物; 并使所述中间体化合物与第二醛反应以产生一类具有通式结构的化合物，其中第一种醛和第二种醛选自恶唑烷羧醛，咪唑甲醛，苯甲醛，咪唑甲醛衍生物和苯甲醛衍生物， 从而形成上述化合物，其中R1，R1'，R1“，R2，R3，R4，R5和R6，X1和X2，Y，Z，Z1，Z2，Z3和Z4各自可以以一致的方式分别定义 附带说明。 还公开了治疗血管增生的组合物和方法。

公开(公告)号：US20080070969A1

公开(公告)日：2008-03-20

申请号：US11865704

申请日：2007-10-01

Applicant: Barbara Potts ,  Venkat Macherla ,  Scott Mitchell ,  Ram Manam ,  Katherine Reed ,  Kin Lam ,  Saskia Neuteboom ,  Ta-Hsiang Chao ,  Benjamin Nicholson ,  Cheryl Billstrom

Inventor： Barbara Potts ,  Venkat Macherla ,  Scott Mitchell ,  Ram Manam ,  Katherine Reed ,  Kin Lam ,  Saskia Neuteboom ,  Ta-Hsiang Chao ,  Benjamin Nicholson ,  Cheryl Billstrom

IPC: A61K31/407 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  C07D491/044

CPC classification number: C07D491/04 ,  C07D207/28 ,  C07F5/025

Abstract: Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

Abstract translation: 具有抗癌，抗炎和抗微生物性质的式I-VI及其衍生物的化合物和包含一种或多种具有抗癌，抗炎和抗微生物的化合物及其衍生物或类似物的组合物 属性被公开。 还公开了包含这些化合物的药物组合物和用所公开的化合物或所公开的药物组合物治疗癌症，炎性病症和微生物感染的方法。

公开(公告)号：US20060205799A1

公开(公告)日：2006-09-14

申请号：US11358961

申请日：2006-02-21

Applicant: Venkata Macherla ,  Benjamin Nicholson ,  Kin Lam

Inventor： Venkata Macherla ,  Benjamin Nicholson ,  Kin Lam

IPC: C07D263/38 ,  C07C249/02 ,  A61K31/421

CPC classification number: C07D263/40 ,  C07C257/06 ,  C12P17/14

Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

Abstract translation: 本文公开了各种新的恶唑烷酮，咪唑啉酮和噻唑烷酮类似物以及使用这些类似物治疗癌症和/或微生物感染的方法。 特定的4-恶唑烷酮化合物显示具有抗癌和抗微生物活性。

公开(公告)号：US20100021941A1

公开(公告)日：2010-01-28

申请号：US12508128

申请日：2009-07-23

Applicant: Jeffrey Gordon Marblestone ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

Inventor： Jeffrey Gordon Marblestone ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

IPC: G01N33/53

CPC classification number: C12Q1/25 ,  G01N33/573 ,  G01N2333/9015

Abstract: Methods for identifying ubiquitin ligases and ubiquitin ligase modulators are disclosed. The methods comprise combining the components of a ubiquitylation reaction and using proteins that contain motifs that recognize ubiquitylated sites in the detection of ubiquitylation.

Abstract translation: 公开了用于鉴定泛素连接酶和泛素连接酶调节剂的方法。 所述方法包括组合泛素化反应的组分并使用含有在泛素化检测中识别泛素化位点的基序的蛋白质。

公开(公告)号：US20080221182A1

公开(公告)日：2008-09-11

申请号：US12124896

申请日：2008-05-21

Applicant: Venkata Rami Reddy Macherla ,  Benjamin Nicholson ,  Kin Sing Lam

Inventor： Venkata Rami Reddy Macherla ,  Benjamin Nicholson ,  Kin Sing Lam

IPC: A61K31/421 ,  C07D263/38 ,  C07C229/30 ,  A61K31/195

CPC classification number: C07D263/40 ,  C07C257/06 ,  C12P17/14

Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

Abstract translation: 本文公开了各种新的恶唑烷酮，咪唑啉酮和噻唑烷酮类似物以及使用这些类似物治疗癌症和/或微生物感染的方法。 特定的4-恶唑烷酮化合物显示具有抗癌和抗微生物活性。