公开(公告)号：US08207183B2

公开(公告)日：2012-06-26

申请号：US13178946

申请日：2011-07-08

Applicant: Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanling Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

Inventor： Mark G. Palermo ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming Wang ,  Leigh Zawel ,  Yanling Zhang ,  Zhuoliang Chen ,  Yaping Wang ,  Fan Yang ,  Wojciech Wrona ,  Gang Liu ,  Mark G. Charest ,  Feng He

IPC: A61K31/427 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/435 ,  A61K31/40 ,  A61K31/506 ,  A61K31/41 ,  C07D277/20 ,  C07D271/06 ,  C07D263/30 ,  C07D401/02 ,  C07D239/02 ,  C07D403/02

CPC classification number: C07D207/16 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).

公开(公告)号：US20110009371A1

公开(公告)日：2011-01-13

申请号：US12778797

申请日：2010-05-12

Applicant: Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

Inventor： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC: A61K31/65 ,  C07D261/20 ,  C07C237/26 ,  C07C231/14 ,  C07D221/18 ,  A61K31/473 ,  A61P31/04

CPC classification number: C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Abstract translation: 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 所描述的四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前难以接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可以用作抗微生物剂或抗增殖剂来治疗人类或其他动物的疾病。

公开(公告)号：US08546336B2

公开(公告)日：2013-10-01

申请号：US13606676

申请日：2012-09-07

Applicant: Zhuoliang Chen ,  Mark G. Charest ,  Christine Hiu-Tung Chen ,  Miao Dai ,  Feng He ,  Huangshu Lei ,  Ly Luu Pham ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming David Wang ,  Fan Yang ,  Leigh Zawel

Inventor： Zhuoliang Chen ,  Mark G. Charest ,  Christine Hiu-Tung Chen ,  Miao Dai ,  Feng He ,  Huangshu Lei ,  Ly Luu Pham ,  Sushil Kumar Sharma ,  Christopher Sean Straub ,  Run-Ming David Wang ,  Fan Yang ,  Leigh Zawel

IPC: A61K38/00

CPC classification number: C07D417/04 ,  A61K31/427 ,  A61K45/06 ,  C07K5/06191

Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.

Abstract translation: 本发明涉及下式的化合物或其药学上可接受的盐，以及在哺乳动物中用于治疗增殖性疾病例如癌症的用途。

公开(公告)号：US06589962B1

公开(公告)日：2003-07-08

申请号：US10031513

申请日：2002-04-16

Applicant: James R Tata ,  Zhijian Lu ,  Subharekha Raghavan ,  Tracy T. Huening ,  Thomas A. Rano ,  Mark G. Charest

Inventor： James R Tata ,  Zhijian Lu ,  Subharekha Raghavan ,  Tracy T. Huening ,  Thomas A. Rano ,  Mark G. Charest

IPC: A01N4316

CPC classification number: C07D405/12 ,  A61K45/06 ,  C07D207/16 ,  C07D277/06 ,  C07D311/68 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04

Abstract: Certain &agr;-hydroxy-&ggr;-[[(carbocyclic- or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Abstract translation: 某些α-羟基-γ - [[（碳环或杂环取代的）氨基]羰基]烷酰胺衍生物被描述为HIV蛋白酶抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。 这些化合物对HIV病毒突变体有效，其对目前用于治疗AIDS和HIV感染的HIV蛋白酶抑制剂具有抗性。

公开(公告)号：US08598148B2

公开(公告)日：2013-12-03

申请号：US12778797

申请日：2010-05-12

Applicant: Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

Inventor： Andrew G. Myers ,  Mark G. Charest ,  Christian D. Lerner ,  Jason D. Brubaker ,  Dionicio R. Siegel

IPC: A61K31/65 ,  C07C237/26 ,  C07D221/18 ,  C07D235/02 ,  C07D239/70 ,  C07D307/77

CPC classification number: C07D261/20 ,  C07C231/10 ,  C07C237/26 ,  C07D209/56 ,  C07D209/58 ,  C07D213/56 ,  C07D221/18 ,  C07D235/02 ,  C07D237/26 ,  C07D239/70 ,  C07D241/38 ,  C07D263/52 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D307/77

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

Abstract translation: 四环素类抗生素在过去50年的传染病治疗中发挥了重要作用。 然而，四环素在人类和兽医药物中的使用量的增加已经导致了以前易受四环素抗生素影响的许多生物体之间的抵抗。 所描述的四环素和四环素类似物的模块合成为通过先前的四环素合成和半合成方法先前难以接近的各种四环素类似物和聚环状体提供了有效和对映选择性的途径。 这些类似物可以用作抗微生物剂或抗增殖剂来治疗人类或其他动物的疾病。

公开(公告)号：US08044209B2

公开(公告)日：2011-10-25

申请号：US12445435

申请日：2007-10-10

Applicant: Mark G. Charest ,  Christine Hiu-Tung Chen ,  Ming Chen ,  Zhuoliang Chen ,  Miao Dai ,  Feng He ,  Huangshu Lei ,  Christopher Sean Straub ,  Run-Ming David Wang ,  Leigh Zawel

Inventor： Mark G. Charest ,  Christine Hiu-Tung Chen ,  Ming Chen ,  Zhuoliang Chen ,  Miao Dai ,  Feng He ,  Huangshu Lei ,  Christopher Sean Straub ,  Run-Ming David Wang ,  Leigh Zawel

IPC: A61K31/4439 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07K5/06191

Abstract: The present invention relates to novel IAP inhibitor compounds of: Formula (I).

Abstract translation: 本发明涉及式（I）的新型IAP抑制剂化合物。

公开(公告)号：US20110065726A1

公开(公告)日：2011-03-17

申请号：US12376057

申请日：2007-07-31

Applicant: Zhuoliang CHEN ,  Sushil Kumar Sharma ,  Christopher Straub ,  Mark G. Charest ,  Feng He ,  Run-Ming David Wang ,  Leigh Zawel ,  Christine Hiu-Tung Chen ,  Miao Dai ,  Huangshu Lei ,  Ly Pham ,  Fan Yang

Inventor： Zhuoliang CHEN ,  Sushil Kumar Sharma ,  Christopher Straub ,  Mark G. Charest ,  Feng He ,  Run-Ming David Wang ,  Leigh Zawel ,  Christine Hiu-Tung Chen ,  Miao Dai ,  Huangshu Lei ,  Ly Pham ,  Fan Yang

IPC: C07D401/12 ,  A61P35/04 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/506 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D417/04 ,  A61K31/427 ,  A61K45/06 ,  C07K5/06191

Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.

Abstract translation: 本发明涉及下式的化合物或其药学上可接受的盐，以及在哺乳动物中用于治疗增殖性疾病例如癌症的用途。