公开(公告)号：WO2017066227A1

公开(公告)日：2017-04-20

申请号：PCT/US2016/056504

申请日：2016-10-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： YEUNG, Kap-Sun ,  CONNOLLY, Timothy P. ,  FRENNESSON, David B. ,  GRANT-YOUNG, Katharine A. ,  HEWAWASAM, Piyasena ,  LANGLEY, David R. ,  MENG, Zhaoxing ,  MULL, Eric ,  PARCELLA, Kyle E. ,  SAULNIER, Mark George ,  SUN, Li-Qiang ,  WANG, Alan Xiangdong ,  XU, Ningning ,  ZHU, Juliang ,  SCOLA, Paul Michael

IPC: C07D403/12 ,  C07D401/14 ,  C07D213/71 ,  C07D213/85 ,  C07D401/12 ,  C07D455/02 ,  C07D207/12 ,  A61K31/4427 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D401/14 ,  A61K31/135 ,  A61K31/138 ,  A61K31/166 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07C215/20 ,  C07C235/46 ,  C07D205/04 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D213/71 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85 ,  C07D265/30 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D455/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/08

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases. The compounds have formula (I), wherein R2 is selected from (II) and (III).

Abstract translation: 本公开一般涉及可用作免疫调节剂的化合物。 本文提供化合物，包含此类化合物的组合物及其使用方法。 本公开还涉及包含至少一种根据本公开内容的化合物的药物组合物，其可用于治疗各种疾病，包括癌症和感染性疾病。 该化合物具有式（I），其中R2选自（II）和（III）。

公开(公告)号：WO2013106520A1

公开(公告)日：2013-07-18

申请号：PCT/US2013/020954

申请日：2013-01-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： HEWAWASAM, Piyasena ,  KADOW, John, F. ,  LOPEZ, Omar, D. ,  MEANWELL, Nicholas, A. ,  TU, Yong ,  WANG, Alan Xiangdong ,  XU, Ningning ,  BELEMA, Makonen ,  FRIDELL, Robert, A. ,  GAO, Min ,  LEMM, Julie, A. ,  O'BOYLE II, Donald, R. ,  SUN, Jin-Hua ,  WANG, Chunfu ,  WANG, Ying-Kai ,  GUPTA, Samayamunthula, Venkata, Satya, Arun, Kumar ,  SRINIVASU, Pothukanuri ,  KUMAR, Indasi, Gopi ,  KUMAR, Ponugupati Suresh

IPC: A61K31/4178 ,  A61P31/14 ,  A61K45/06

CPC classification number: A61K31/4178 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/21 ,  A61K38/212 ,  A61K38/217 ,  A61K45/06 ,  C07D403/14 ,  C07D491/113 ,  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：WO2012039717A1

公开(公告)日：2012-03-29

申请号：PCT/US2010/050138

申请日：2010-09-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BELEMA, Makonen ,  HEWAWASAM, Piyasena

Inventor： BELEMA, Makonen ,  HEWAWASAM, Piyasena

IPC: C07D403/14 ,  A61K31/4178

CPC classification number: 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。

公开(公告)号：WO2011112191A1

公开(公告)日：2011-09-15

申请号：PCT/US2010/026898

申请日：2010-03-11

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

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

IPC: C07D307/79 ,  C07D401/14 ,  C07D403/10 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4433 ,  A61P31/12 ,  A61K31/506 ,  A61K31/343 ,  A61K31/422 ,  A61K31/501

CPC classification number: C07D307/79 ,  C07D401/14 ,  C07D403/10 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

Abstract: The disclosure provides compounds of formula (I), 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）化合物，包括其盐，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：WO2007136982A1

公开(公告)日：2007-11-29

申请号：PCT/US2007/068209

申请日：2007-05-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BENDER, John A. ,  DING, Min ,  GENTLES, Robert G. ,  HEWAWASAM, Piyasena

Inventor： BENDER, John A. ,  DING, Min ,  GENTLES, Robert G. ,  HEWAWASAM, Piyasena

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

CPC classification number: C07D519/00

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。 这些化合物对丙型肝炎病毒（HCV）具有活性，可用于治疗感染HCV的患者。

公开(公告)号：WO1998004135A1

公开(公告)日：1998-02-05

申请号：PCT/US1997014352

申请日：1997-07-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： BRISTOL-MYERS SQUIBB COMPANY ,  ROMINE, Jeffrey, L. ,  MARTIN, Scott, W. ,  HEWAWASAM, Piyasena ,  MEANWELL, Nicholas, A. ,  GRIBKOFF, Valentin, K. ,  STARRETT, John, E., Jr.

IPC: A01N43/653

CPC classification number: C07D263/58 ,  C07D233/64 ,  C07D233/70 ,  C07D233/76 ,  C07D235/12 ,  C07D249/12 ,  C07D249/14 ,  C07D271/113 ,  C07D413/10

Abstract: Novel compounds of formula (1) are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels, wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R , R and R each are independently selected from hydrogen, halogen, OH, CF3, NO2, or (a); provided R is not hydrogen; and when R and R are hydrogen, R may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; R and R each are independently selected form hydrogen, halogen, CF3, NO2 or imidazol-1-yl; m, n and p each are independently selected from an integer of 0 or 1; and R and R each are independently hydrogen; C1-4 alkyl; or R and R , taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.

Abstract translation: 式（1）的新型化合物可用于治疗对大电导钙激活钾通道的开放物起反应的病症，其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; R a，R b和R c各自独立地选自氢，卤素，OH，CF 3，NO 2或（a）; 条件是R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶-2-基的杂环部分， 基; R d和R e各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自0或1的整数; 和R f和R g各自独立地为氢; C 1-4烷基; 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。

公开(公告)号：WO2018044963A1

公开(公告)日：2018-03-08

申请号：PCT/US2017/049252

申请日：2017-08-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： YEUNG, Kap-Sun ,  GRANT-YOUNG, Katharine A. ,  ZHU, Juliang ,  SAULNIER, Mark G. ,  FRENNESSON, David B. ,  LANGLEY, David R. ,  HEWAWASAM, Piyasena ,  WANG, Tao ,  ZHANG, Zhongxing ,  MENG, Zhaoxing ,  SUN, Li-Qiang ,  MULL, Eric ,  SCOLA, Paul Michael

IPC: C07D403/12 ,  C07D401/12 ,  C07D207/12 ,  C07C211/08 ,  C07D211/22 ,  C07D213/38 ,  C07C211/06 ,  C07C237/08 ,  C07D211/46 ,  C07D211/58 ,  C07D211/60 ,  C07D211/66 ,  C07D213/85 ,  C07C211/26 ,  C07C211/35 ,  C07D405/12 ,  C07D205/04 ,  C07D213/42 ,  C07D401/14 ,  C07C211/29 ,  C07D207/14 ,  C07D213/55 ,  C07D231/12 ,  C07D401/04 ,  C07D239/26 ,  C07D405/06 ,  C07C235/74 ,  C07D277/28 ,  C07D417/12 ,  A61K31/496 ,  A61K31/4025 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/4155 ,  A61K31/4409 ,  A61K31/4178 ,  A61K31/397 ,  A61K31/415 ,  A61K31/505 ,  A61K31/426 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02 ,  A61P37/04

Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

Abstract translation: 本公开一般涉及可用作免疫调节剂的化合物。 本文提供化合物，包含此类化合物的组合物及其使用方法。 本公开还涉及药物组合物，其包含至少一种根据本公开的化合物，其用于治疗各种疾病，包括癌症和传染性疾病。

公开(公告)号：WO2015005901A1

公开(公告)日：2015-01-15

申请号：PCT/US2013/049633

申请日：2013-07-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： HEWAWASAM, Piyasena ,  LOPEZ, Omar D. ,  TU, Yong ,  WANG, Alan Xiangdong ,  XU, Ningning ,  KADOW, John F. ,  MEANWELL, Nicholas A. ,  GUPTA, Samayamunthula Venkata Satya Arun Kumar ,  KUMAR, Indasi J. Gopi ,  PUNUGUPATI, Suresh Kumar ,  BELEMA, Makonen

IPC: A61K45/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61P31/14

CPC classification number: A61K31/4178 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/695 ,  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：WO2009067481A1

公开(公告)日：2009-05-28

申请号：PCT/US2008/083978

申请日：2008-11-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  HEWAWASAM, Piyasena ,  TU, Yong ,  BENDER, John A. ,  YANG, Zhong

Inventor： HEWAWASAM, Piyasena ,  TU, Yong ,  BENDER, John A. ,  YANG, Zhong

IPC: C07D471/08 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D519/00

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：WO2008112473A1

公开(公告)日：2008-09-18

申请号：PCT/US2008/055893

申请日：2008-03-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  GENTLES, Robert G. ,  ZHENG, Xiaofan ,  DING, Min ,  TU, Yong ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  KADOW, John F. ,  BENDER, John A. ,  YEUNG, Kap-sun ,  GRANT-YOUNG, Katharine A. ,  HUDYMA, Thomas W.

Inventor： GENTLES, Robert G. ,  ZHENG, Xiaofan ,  DING, Min ,  TU, Yong ,  HAN, Ying ,  HEWAWASAM, Piyasena ,  KADOW, John F. ,  BENDER, John A. ,  YEUNG, Kap-sun ,  GRANT-YOUNG, Katharine A. ,  HUDYMA, Thomas W.

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

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using. these 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化合物，包括药学上可接受的盐，以及组合物和使用方法。 这些化合物。 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。