公开(公告)号：US08637531B2

公开(公告)日：2014-01-28

申请号：US12519500

申请日：2007-12-24

Applicant: Steven S. Bondy ,  William J. Watkins ,  Lee S. Chong ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe

Inventor： Steven S. Bondy ,  William J. Watkins ,  Lee S. Chong ,  Piet Andre Maurits Maria Herdewijn ,  Steven Cesar Alfons De Jonghe

IPC: A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00

CPC classification number: C07D471/04

Abstract: This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R1 is amino, R4 is hydrogen, and R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.

Abstract translation: 本发明提供由结构式（I）表示的吡啶并（3,2-d）嘧啶衍生物，其中：R 1为氨基，R 4为氢，R 2和R 3一起提供特定取代模式，药学上可接受的加成盐，立体化学异构体 形式，N-氧化物，溶剂合物和其前体药物可用于治疗丙型肝炎。

公开(公告)号：US08536187B2

公开(公告)日：2013-09-17

申请号：US12996110

申请日：2009-07-01

Applicant: Eda Canales ,  Lee S. Chong ,  Michael O' Neil Hanrahan Clarke ,  Scott E. Lazerwith ,  Willard Lew ,  Qi Liu ,  Michael L. Mitchell ,  William J. Watkins ,  Jennifer R. Zhang

Inventor： Eda Canales ,  Lee S. Chong ,  Michael O' Neil Hanrahan Clarke ,  Scott E. Lazerwith ,  Willard Lew ,  Qi Liu ,  Michael L. Mitchell ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D471/04

Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, for use in the treatment of hepatitis C.

Abstract translation: 由结构式（Ia）表示的吡啶并（3,2-d）嘧啶衍生物：其中R1，R2和R3如本文所定义，药学上可接受的加成盐，立体化学异构形式，N-氧化物，溶剂化物和其前体药物， 用于治疗丙型肝炎。

公开(公告)号：US08501714B2

公开(公告)日：2013-08-06

申请号：US13392467

申请日：2010-09-07

Applicant: Aesop Cho ,  Lee S. Chong ,  Michael O'Neil Hanrahan Clarke ,  Edward Doerffler ,  Choung U. Kim ,  Qi Liu ,  William J. Watkins ,  Jennifer R. Zhang

Inventor： Aesop Cho ,  Lee S. Chong ,  Michael O'Neil Hanrahan Clarke ,  Edward Doerffler ,  Choung U. Kim ,  Qi Liu ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A61K31/67 ,  A61K31/675 ,  C07F9/6558 ,  C07F9/6553

CPC classification number: C07F9/655345 ,  A61K31/662 ,  A61K31/67 ,  A61K31/675 ,  A61K31/683 ,  A61K45/06 ,  C07F9/65586 ,  C07F9/6561 ,  C07F9/65681

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

公开(公告)号：US08435969B2

公开(公告)日：2013-05-07

申请号：US13070179

申请日：2011-03-23

Applicant: Adrian S. Ray ,  Daniel B. Tumas ,  Hans Reiser ,  William J. Watkins ,  William A. Lee ,  Lee S. Chong

Inventor： Adrian S. Ray ,  Daniel B. Tumas ,  Hans Reiser ,  William J. Watkins ,  William A. Lee ,  Lee S. Chong

IPC: A61K31/675 ,  C07F9/6561

CPC classification number: C07F9/65616

Abstract: A compound of formula 1 and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.

Abstract translation: 式1化合物和/或其盐，互变异构体或溶剂合物用于治疗血液恶性肿瘤。 在一个实施方案中，提供化合物1的有机酸盐，用于一般用于治疗赘生物，并且在另一个实施方案中，所述盐用碳水化合物稳定。

公开(公告)号：US08022083B2

公开(公告)日：2011-09-20

申请号：US12166076

申请日：2008-07-01

Applicant: Constantine G. Boojamra ,  Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Haolun Jin ,  Ralph F. Hirschmann ,  Alan X. Huang ,  Choung U. Kim ,  Thorsten Kirschberg ,  Christopher P. Lee ,  William A. Lee ,  Richard L. Mackman ,  David Y. Markevitch ,  David A. Oare ,  Vidya K. Prasad ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William J. Watkins ,  Jennifer R. Zhang

Inventor： Constantine G. Boojamra ,  Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Haolun Jin ,  Ralph F. Hirschmann ,  Alan X. Huang ,  Choung U. Kim ,  Thorsten Kirschberg ,  Christopher P. Lee ,  William A. Lee ,  Richard L. Mackman ,  David Y. Markevitch ,  David A. Oare ,  Vidya K. Prasad ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A61K31/44 ,  C07D487/00

CPC classification number: C07F9/65616 ,  A61K31/662 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/58 ,  C07F9/60 ,  C07F9/65031 ,  C07F9/650905 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561 ,  C07H15/00 ,  C07H17/00 ,  C07H19/056 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  Y02A50/393 ,  Y02A50/465

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US20110178058A1

公开(公告)日：2011-07-21

申请号：US13006761

申请日：2011-01-14

Applicant: Eda CANALES ,  Lee S. Chong ,  Michael O' Neil Hanrahan Clarke ,  Edward Doerffler ,  Scott E. Lazerwith ,  Willard Lew ,  Michael Mertzman ,  Philip A. Morganelli ,  William J. Watkins

Inventor： Eda CANALES ,  Lee S. Chong ,  Michael O' Neil Hanrahan Clarke ,  Edward Doerffler ,  Scott E. Lazerwith ,  Willard Lew ,  Michael Mertzman ,  Philip A. Morganelli ,  William J. Watkins

IPC: A61K31/381 ,  C07D409/14 ,  A61K31/4545 ,  C07D409/12 ,  A61K31/4025 ,  C07D493/04 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61P31/14

CPC classification number: C07D333/38 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/427 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D493/04

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

公开(公告)号：US20110020278A1

公开(公告)日：2011-01-27

申请号：US12838684

申请日：2010-07-19

Applicant: Eda Canales ,  Lee S. Chong ,  Michael O'Neil Hanrahan Clarke ,  Edward Doerffler ,  Scott E. Lazerwith ,  Willard Lew ,  Qi Liu ,  Michael Mertzman ,  Philip A. Morganelli ,  William J. Watkins ,  Hong Ye

Inventor： Eda Canales ,  Lee S. Chong ,  Michael O'Neil Hanrahan Clarke ,  Edward Doerffler ,  Scott E. Lazerwith ,  Willard Lew ,  Qi Liu ,  Michael Mertzman ,  Philip A. Morganelli ,  William J. Watkins ,  Hong Ye

IPC: A61K31/381 ,  C07D409/12 ,  A61K31/4436 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/41 ,  C07D417/14 ,  A61K31/427 ,  A61P31/14 ,  A61K38/21 ,  A61K31/7056

CPC classification number: A61K31/513 ,  A61K31/427 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  C07D333/68 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D493/04

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract translation: 提供式I的化合物及其药学上可接受的盐和酯。 所提供的化合物，组合物和方法可用于治疗黄病毒科感染，特别是丙型肝炎感染。

公开(公告)号：US20090275535A1

公开(公告)日：2009-11-05

申请号：US12166076

申请日：2008-07-01

Applicant: Constantine G. Boojamra ,  Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Haolun Jin ,  Ralph F. Hirschmann ,  Alan X. Huang ,  Choung U. Kim ,  Thorsten Kirschberg ,  Christopher P. Lee ,  William A. Lee ,  Richard L. Mackman ,  David Y. Markevitch ,  David A. Oare ,  Vidya K. Prasad ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William J. Watkins ,  Jennifer R. Zhang

Inventor： Constantine G. Boojamra ,  Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Haolun Jin ,  Ralph F. Hirschmann ,  Alan X. Huang ,  Choung U. Kim ,  Thorsten Kirschberg ,  Christopher P. Lee ,  William A. Lee ,  Richard L. Mackman ,  David Y. Markevitch ,  David A. Oare ,  Vidya K. Prasad ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  Rosemarie Sherlock ,  Sundaramoorthi Swaminathan ,  William J. Watkins ,  Jennifer R. Zhang

IPC: A61K31/675 ,  C07F9/6561 ,  A61P31/12

CPC classification number: C07F9/65616 ,  A61K31/662 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/548 ,  C07D205/04 ,  C07D211/58 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D475/00 ,  C07F9/4075 ,  C07F9/5728 ,  C07F9/58 ,  C07F9/60 ,  C07F9/65031 ,  C07F9/650905 ,  C07F9/653 ,  C07F9/6539 ,  C07F9/65515 ,  C07F9/655354 ,  C07F9/6561 ,  C07H15/00 ,  C07H17/00 ,  C07H19/056 ,  C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  Y02A50/393 ,  Y02A50/465

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有抗病毒活性的磷取代的化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US07470724B2

公开(公告)日：2008-12-30

申请号：US10833295

申请日：2004-04-26

Applicant: Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Manoj Desai ,  Maria Fardis ,  Alan X. Huang ,  Thorsten Kirschberg ,  Christopher P. Lee ,  Richard L. Mackman ,  Peter H. Nelson ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  William J. Watkins ,  Jennifer R. Zhang ,  Sundaramoorthi Swaminathan

Inventor： Carina Cannizzaro ,  James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Manoj Desai ,  Maria Fardis ,  Alan X. Huang ,  Thorsten Kirschberg ,  Christopher P. Lee ,  Richard L. Mackman ,  Peter H. Nelson ,  Hyung-Jung Pyun ,  Adrian S. Ray ,  William J. Watkins ,  Jennifer R. Zhang ,  Sundaramoorthi Swaminathan

IPC: A61K31/27

CPC classification number: A61K47/548 ,  A61K47/542

Abstract: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及具有免疫调节活性的膦酸酯取代的化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

公开(公告)号：US07427624B2

公开(公告)日：2008-09-23

申请号：US10832816

申请日：2004-04-26

Applicant: James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Thorsten Kirschberg ,  Adrian S. Ray ,  Sundaramoorthi Swaminathan ,  William J. Watkins

Inventor： James M. Chen ,  Xiaowu Chen ,  Aesop Cho ,  Lee S. Chong ,  Maria Fardis ,  Thorsten Kirschberg ,  Adrian S. Ray ,  Sundaramoorthi Swaminathan ,  William J. Watkins

IPC: A61K31/517 ,  C07D487/00

CPC classification number: A61K31/519 ,  A61K31/662 ,  A61K31/675 ,  A61K47/54 ,  A61K47/548

Abstract: The invention is related to phosphorus substituted purine nucleoside phosphorylase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明涉及磷取代的嘌呤核苷磷酸化酶抑制化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。