公开(公告)号：US08680139B2

公开(公告)日：2014-03-25

申请号：US13262422

申请日：2010-03-31

Applicant: Ping Cao ,  Joseph Weinstock ,  William D. Kingsbury ,  Craig A. Leach ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

Inventor： Ping Cao ,  Joseph Weinstock ,  William D. Kingsbury ,  Craig A. Leach ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

IPC: A61K31/381 ,  C07D333/18

CPC classification number: C07D409/12

Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.

Abstract translation: 公开了可用作治疗剂的新化合物，特别是在抗肿瘤治疗和涉及半胱氨酸蛋白酶抑制的其它治疗方案中。

公开(公告)号：US20110143958A1

公开(公告)日：2011-06-16

申请号：US13055042

申请日：2009-07-23

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

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

IPC: C40B30/04 ,  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：US07276530B2

公开(公告)日：2007-10-02

申请号：US11118260

申请日：2005-04-29

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

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

IPC: A61K31/407 ,  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：US07879892B2

公开(公告)日：2011-02-01

申请号：US12124909

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: A61K31/42 ,  C07D277/02

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：US07112581B2

公开(公告)日：2006-09-26

申请号：US10673036

申请日：2003-09-25

Applicant: Scott C. Mitchell ,  Benjamin Nicholson

Inventor： Scott C. Mitchell ,  Benjamin Nicholson

IPC: A61K31/395 ,  A61K35/02 ,  A61P35/00 ,  C07D225/02

CPC classification number: C07D225/02

Abstract: Compounds represented by the following structure (I), acid-addition salts and pro-drugs are disclosed: wherein the ring structure includes no substitutions, one substitution, or more than one substitution; and wherein n is equal to an integer grater than 1, preferably 2, 3, or 4; m is equal to a positive integer, preferably 1, 2 or 3, and each separate Xn and X are each separately selected from a nucleophilic residue, preferably —H, —OH, —O—CO-alkyl, —O-alkyl, —NH2, a halogen and the like; and wherein the dashed line represents a C—C bond or a C—H bond, and the dashed and solid line represents either a carbon-carbon single bond or a carbon-carbon double bond.

Abstract translation: 公开了由以下结构（I）表示的化合物，酸加成盐和前药：其中环结构不包括取代，一个取代或多于一个取代; 并且其中n等于1，优选2,3或4的整数倍; m等于正整数，优选1,2或3，并且每个单独的X n和X各自独立地选自亲核残基，优选-H，-OH，-O-CO- 烷基，-O-烷基，-NH 2，卤素等; 并且其中虚线表示C-C键或C-H键，虚线和实线表示碳 - 碳单键或碳 - 碳双键。

公开(公告)号：US20120114765A1

公开(公告)日：2012-05-10

申请号：US13262422

申请日：2010-03-31

Applicant: Ping Cao ,  Joseph Weinstock ,  William D. Kingsbury ,  Craig A. Leach ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

Inventor： Ping Cao ,  Joseph Weinstock ,  William D. Kingsbury ,  Craig A. Leach ,  Suresh Kumar Kizhakkethil-George ,  Benjamin Nicholson

IPC: A61K33/24 ,  A61K31/381 ,  C07D417/12 ,  A61K31/427 ,  C07D409/12 ,  A61K31/4178 ,  A61K31/4436 ,  A61K31/498 ,  C07D413/14 ,  A61K31/5377 ,  C07D409/14 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/704 ,  A61K38/14 ,  A61K31/7048 ,  A61K31/675 ,  A61K31/475 ,  A61K31/4745 ,  A61K31/415 ,  A61P35/00 ,  A61P35/02 ,  A61N5/10 ,  C07D333/42

CPC classification number: C07D409/12

Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.

Abstract translation: 公开了可用作治疗剂的新化合物，特别是在抗肿瘤治疗和涉及半胱氨酸蛋白酶抑制的其它治疗方案中。

公开(公告)号：US07544814B2

公开(公告)日：2009-06-09

申请号：US11865704

申请日：2007-10-01

Applicant: Barbara Christine Potts ,  Venkat Macherla ,  Scott Sherman Mitchell ,  Ram Rao Manam ,  Katherine A. McArthur ,  Kin Sing Lam ,  Saskia Neuteboom ,  Ta-Hsiang Chao ,  Benjamin Nicholson ,  Cheryl L. Billstrom

Inventor： Barbara Christine Potts ,  Venkat Macherla ,  Scott Sherman Mitchell ,  Ram Rao Manam ,  Katherine A. McArthur ,  Kin Sing Lam ,  Saskia Neuteboom ,  Ta-Hsiang Chao ,  Benjamin Nicholson ,  Cheryl L. Billstrom

IPC: A61K31/407 ,  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：US20080221183A1

公开(公告)日：2008-09-11

申请号：US12124909

申请日：2008-05-21

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

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

IPC: A61K31/421 ,  A61K31/19 ,  A61P31/04

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.

公开(公告)号：US07378530B2

公开(公告)日：2008-05-27

申请号：US11358961

申请日：2006-02-21

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

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

IPC: C07D277/02 ,  C07D263/04 ,  C07D233/02

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：US20050288352A1

公开(公告)日：2005-12-29

申请号：US11118260

申请日：2005-04-29

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 ,  C07D207/28 ,  C07D491/02 ,  C07D491/04

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。