公开(公告)号：WO2017023631A1

公开(公告)日：2017-02-09

申请号：PCT/US2016/044158

申请日：2016-07-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： FRENNESSON, David B. ,  HEWAWASAM, Piyasena ,  LOPEZ, Omar D. ,  NGUYEN, Van N. ,  SAULNIER, Mark G. ,  TU, Yong ,  WANG, Alan Xiangdong ,  WANG, Gan ,  XU, Ningning ,  NIMJE, Roshan Yadavrao ,  RAHAMAN, Hasibur ,  GUPTA, Samayamunthula Venkata Satya Arun Kumar ,  MEANWELL, Nicholas A. ,  BELEMA, Makonen

IPC: A61K45/06 ,  A61K38/21 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/7056 ,  A61P31/14

CPC classification number: A61K31/4184 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.

Abstract translation: 本公开通常涉及抗病毒化合物，更具体地涉及可以抑制丙型肝炎病毒（HCV）编码的NS5A蛋白的功能的化合物的组合，包含这些组合的组合物，以及用于抑制NS5A的功能的方法 蛋白。

公开(公告)号：WO2010030538A2

公开(公告)日：2010-03-18

申请号：PCT/US2009/055648

申请日：2009-09-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  PRACITTO, Richard ,  KADOW, John F. ,  BENDER, John A. ,  BENO, Brett R. ,  GRANT-YOUNG, Katharine A. ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  NICKEL, Andrew ,  PARCELLA, Kyle E. ,  YEUNG, Kap-Sun ,  CHUPAK, Louis S.

Inventor： PRACITTO, Richard ,  KADOW, John F. ,  BENDER, John A. ,  BENO, Brett R. ,  GRANT-YOUNG, Katharine A. ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  NICKEL, Andrew ,  PARCELLA, Kyle E. ,  YEUNG, Kap-Sun ,  CHUPAK, Louis S.

IPC: C07D209/42 ,  C07D333/68 ,  C07D471/04 ,  C07D491/048 ,  A61K31/4745 ,  A61K31/4741 ,  A61K31/381

CPC classification number: C07D471/04 ,  C07D209/42 ,  C07D333/68 ,  C07D491/048

Abstract: The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract translation: 本公开提供式I，II，III，IV和V的化合物，包括它们的盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：WO2008112851A1

公开(公告)日：2008-09-18

申请号：PCT/US2008/056789

申请日：2008-03-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  YEUNG, Kap-sun ,  BENDER, John A. ,  GENTLES, Robert G. ,  YANG, Zhong ,  DING, Min ,  TU, Yong ,  HEWAWASAM, Piyasena ,  HAN, Ying ,  KADOW, John F.

Inventor： YEUNG, Kap-sun ,  BENDER, John A. ,  GENTLES, Robert G. ,  YANG, Zhong ,  DING, Min ,  TU, Yong ,  HEWAWASAM, Piyasena ,  HAN, Ying ,  KADOW, John F.

IPC: C07D487/04 ,  A61K31/55 ,  A61P31/12 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract translation: 本发明包括式I的化合物，其药学上可接受的盐，组合物和使用该化合物的方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：WO2008111978A1

公开(公告)日：2008-09-18

申请号：PCT/US2007/063885

申请日：2007-03-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  MEANWELL, Nicholas, A. ,  GENTLES, Robert G. ,  DING, Min ,  BENDER, John A. ,  KADOW, John F. ,  HEWAWASAM, Piyasena ,  HUDYMA, Thomas W. ,  ZHENG, Xiaofan

Inventor： MEANWELL, Nicholas, A. ,  GENTLES, Robert G. ,  DING, Min ,  BENDER, John A. ,  KADOW, John F. ,  HEWAWASAM, Piyasena ,  HUDYMA, Thomas W. ,  ZHENG, Xiaofan

IPC: C07D487/04 ,  A61P31/12 ,  A61K31/55

CPC classification number: C07D487/04

Abstract: The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Formula (I).

Abstract translation: 本发明包括式I的化合物，其药学上可接受的盐，组合物和使用该化合物的方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。 式（I）。

公开(公告)号：WO2007140109A1

公开(公告)日：2007-12-06

申请号：PCT/US2007/068861

申请日：2007-05-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  GENTLES, Robert G. ,  HEWAWASAM, Piyasena ,  DING, Min ,  BERGSTROM, Carl P. ,  MARTIN, Scott W. ,  YEUNG, Kap-Sun ,  HUDYMA, Thomas W. ,  ZHENG, Xiaofan ,  BENDER, John A. ,  KADOW, John F.

Inventor： GENTLES, Robert G. ,  HEWAWASAM, Piyasena ,  DING, Min ,  BERGSTROM, Carl P. ,  MARTIN, Scott W. ,  YEUNG, Kap-Sun ,  HUDYMA, Thomas W. ,  ZHENG, Xiaofan ,  BENDER, John A. ,  KADOW, John F.

IPC: C07D487/04 ,  A61P31/12 ,  A61K31/55

CPC classification number: C07D487/04

Abstract: The invention encompasses compounds of formula (I) as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract translation: 本发明包括式（I）的化合物以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：WO2006020082A1

公开(公告)日：2006-02-23

申请号：PCT/US2005/025234

申请日：2005-07-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  HUDYMA, Thomas, W. ,  ZHENG, Xiaofan ,  HE, Feng ,  DING, Min ,  BERGSTROM, Carl, P. ,  HEWAWASAM, Piyasena ,  MARTIN, Scott, W. ,  GENTLES, Robert, G.

Inventor： HUDYMA, Thomas, W. ,  ZHENG, Xiaofan ,  HE, Feng ,  DING, Min ,  BERGSTROM, Carl, P. ,  HEWAWASAM, Piyasena ,  MARTIN, Scott, W. ,  GENTLES, Robert, G.

IPC: C07D491/14 ,  C07D487/04 ,  C07D498/14 ,  C07D471/14 ,  C07D471/04 ,  C07D487/14 ,  C07D513/14 ,  A61K31/55 ,  A61P31/14

CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D513/14

Abstract: Indole compounds of Formula (I) are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.

Abstract translation: 描述了式（I）的吲哚化合物。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。 还描述了包含化合物的不同形式和组合物以及制备化合物的方法。

公开(公告)号：WO2002066036A1

公开(公告)日：2002-08-29

申请号：PCT/US2002/004305

申请日：2002-02-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： HEWAWASAM, Piyasena ,  DODD, Dharmpal, S. ,  WEAVER, Charles, D. ,  DEXTRAZE, Pierre ,  GRIBKOFF, Valentin, K. ,  KINNEY, Gene, G. ,  DWORETZKY, Steven, I.

IPC: A61K31/505

CPC classification number: C07D239/42 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12

Abstract: There is provided a method of treatment for disorders responsive to the modulation of KCNQ potassium channels by administering to a mammal in need thereof a therapeutically effective amount of a 2,4-disubstituted pyrimidine-5-carboxamide derivative of Formula (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description. The present invention also provides pharmaceutical compositions comprising openers or activators of the KCNQ potassium channels and especially to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine.

Abstract translation: 提供了通过向有需要的哺乳动物施用治疗有效量的式（I）的2,4-二取代嘧啶-5-甲酰胺衍生物，其中R 1，R 2， R 1，R 2，R 3，R 4和R 5如说明书中所定义。 本发明还提供包含KCNQ钾通道的开放剂或活化剂的药物组合物，特别是治疗对KCNQ钾通道开放活性敏感的疾病如偏头痛的方法。

公开(公告)号：WO1998016222A1

公开(公告)日：1998-04-23

申请号：PCT/US1997015323

申请日：1997-10-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： BRISTOL-MYERS SQUIBB COMPANY ,  PENDRI, Yadagiri, R. ,  MARTINEZ, Eduardo, J. ,  THOTTATHIL, John, K. ,  HEWAWASAM, Piyasena

IPC: A61K31/405

CPC classification number: C07C201/16 ,  C07C201/12 ,  C07C205/56 ,  C07C227/04 ,  C07C229/42 ,  C07D209/34 ,  Y02P20/55

Abstract: The present invention relates to novel itermediates of formula (1) wherein the wavy bond ( SIMILAR SIMILAR ) represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.

Abstract translation: 本发明涉及式（1）的新颖化合物，其中波状键（类似的）表示外消旋物，（R） - 对映异构体或（S） - 对映异构体; R为氢，羧基保护基或加成盐的阳离子; 或其溶剂合物; 以及在制备某些3-氟羟吲哚衍生物的方法中的用途。

公开(公告)号：WO2011112186A1

公开(公告)日：2011-09-15

申请号：PCT/US2010/026786

申请日：2010-03-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  PRACITTO, Richard ,  KADOW, John, F. ,  BENDER, John, A. ,  BENO, Brett, R. ,  GRANT-YOUNG, Katharine ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  NICKEL, Andrew ,  PARCELLA, Kyle, E. ,  YEUNG, Kap-Sun ,  CHUPAK, Louis, S.

Inventor： PRACITTO, Richard ,  KADOW, John, F. ,  BENDER, John, A. ,  BENO, Brett, R. ,  GRANT-YOUNG, Katharine ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  NICKEL, Andrew ,  PARCELLA, Kyle, E. ,  YEUNG, Kap-Sun ,  CHUPAK, Louis, S.

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: The disclosure provides ten specific compounds with a basic structure of pyrazolo [1, 5-a] pyridine, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract translation: 本公开提供了具有吡唑并[1,5-a]吡啶的基本结构的十种具体化合物，包括它们的盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：WO2010117635A1

公开(公告)日：2010-10-14

申请号：PCT/US2010/028456

申请日：2010-03-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BENDER, John A. ,  HEWAWASAM, Piyasena ,  KADOW, John F. ,  LOPEZ, Omar D. ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  WANG, Gan ,  XU, Ningning ,  BELEMA, Makonen

Inventor： BENDER, John A. ,  HEWAWASAM, Piyasena ,  KADOW, John F. ,  LOPEZ, Omar D. ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  WANG, Gan ,  XU, Ningning ,  BELEMA, Makonen

IPC: C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  A61K31/4178 ,  A61P31/14

CPC classification number: C07D403/04 ,  C07D403/14 ,  C07D405/14

Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.

Abstract translation: 本公开涉及如说明书中定义的式（I）新化合物和包含这些新化合物的组合物。 这些化合物是有用的抗病毒剂，特别是抑制由丙型肝炎病毒（HCV）编码的NS5A蛋白的功能。 因此，本公开还涉及通过使用这些新化合物或包含这些新化合物的组合物治疗HCV相关疾病或病症的方法。