公开(公告)号：WO2012106188A1

公开(公告)日：2012-08-09

申请号：PCT/US2012/022847

申请日：2012-01-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  REGUEIRO-REN, Alicia ,  SWIDORSKI, Jacob ,  SIT, Sing-Yuen ,  CHEN, Yan ,  CHEN, Jie ,  MEANWELL, Nicholas A. ,  LIU, Zheng

Inventor： REGUEIRO-REN, Alicia ,  SWIDORSKI, Jacob ,  SIT, Sing-Yuen ,  CHEN, Yan ,  CHEN, Jie ,  MEANWELL, Nicholas A. ,  LIU, Zheng

IPC: C07J63/00 ,  A61K31/56 ,  A61P31/18

CPC classification number: C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS. In particular, the following compounds are provided herein, including pharmaceutically acceptable salts thereof: a compound of formula (I), a compound of formula (II), and a compound of formula (III).

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的C-3修饰的桦木酸衍生物的C-28胺被提供为HIV成熟抑制剂。 这些化合物可用于治疗艾滋病毒和艾滋病。 特别地，本文提供以下化合物，包括其药学上可接受的盐：式（I）化合物，式（II）化合物和式（III）化合物。

公开(公告)号：WO2012021591A1

公开(公告)日：2012-02-16

申请号：PCT/US2011/047211

申请日：2011-08-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BELEMA, Makonen ,  SRINIVASU, Pothukanuri ,  BENDER, John A. ,  LOPEZ, Omar D. ,  CHEN, Qi ,  RAMPULLA, Richard A. ,  GUPTA, Samayamunthula Venkata Satya Arun Kumar ,  MEANWELL, Nicholas A.

Inventor： BELEMA, Makonen ,  SRINIVASU, Pothukanuri ,  BENDER, John A. ,  LOPEZ, Omar D. ,  CHEN, Qi ,  RAMPULLA, Richard A. ,  GUPTA, Samayamunthula Venkata Satya Arun Kumar ,  MEANWELL, Nicholas A.

IPC: C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  A61K31/4178 ,  A61K31/433 ,  A61P31/12

CPC classification number: C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

公开(公告)号：WO2009102633A1

公开(公告)日：2009-08-20

申请号：PCT/US2009/033380

申请日：2009-02-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

Inventor： BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

IPC: C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/044 ,  C07D491/052 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61P31/14

CPC classification number: C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/044 ,  C07D491/052

Abstract: The present disclosure relates to compounds of structure (I), compositions and Methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract translation: 本公开涉及结构（I），治疗丙型肝炎病毒（HCV）感染的组合物和方法的化合物。 还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

公开(公告)号：WO2009102325A1

公开(公告)日：2009-08-20

申请号：PCT/US2008/053779

申请日：2008-02-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

Inventor： BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

IPC: C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  A61P31/00 ,  A61K31/41

CPC classification number: C07D403/14 ,  C07D405/14 ,  C07D417/14

Abstract: The present disclosure relates to compounds Formule (I), compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in. the treatment of HCV infection.

Abstract translation: 本公开涉及化合物（I），治疗丙型肝炎病毒（HCV）感染的组合物和方法。 还公开了含有这些化合物的药物组合物和在治疗HCV感染中使用这些化合物的方法。

公开(公告)号：WO2008021927A2

公开(公告)日：2008-02-21

申请号：PCT/US2007/075544

申请日：2007-08-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

Inventor： BACHAND, Carol ,  BELEMA, Makonen ,  DEON, Daniel H. ,  GOOD, Andrew C. ,  GOODRICH, Jason ,  JAMES, Clint A. ,  LAVOIE, Rico ,  LOPEZ, Omar D. ,  MARTEL, Alain ,  MEANWELL, Nicholas A. ,  NGUYEN, Van N. ,  ROMINE, Jeffrey Lee ,  RUEDIGER, Edward H. ,  SNYDER, Lawrence B. ,  ST. LAURENT, Denis R. ,  YANG, Fukang ,  LANGLEY, David R. ,  WANG, Gan ,  HAMANN, Lawrence G.

IPC: C07D401/14 ,  C07D403/14 ,  A61P31/12 ,  A61K31/4025 ,  A61K31/4178

CPC classification number: C07D233/64 ,  A61K31/4178 ,  A61K45/06 ,  C07D207/16 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07F5/025 ,  C07F7/0812

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract translation: 本公开涉及用于治疗丙型肝炎病毒（HCV）感染的化合物，组合物和方法。 还公开了含有这些化合物的药物组合物和使用这些化合物治疗HCV感染的方法。

公开(公告)号：WO2016077572A1

公开(公告)日：2016-05-19

申请号：PCT/US2015/060360

申请日：2015-11-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： SIT, Sing-Yuen ,  CHEN, Jie ,  CHEN, Yan ,  SWIDORSKI, Jacob ,  REGUEIRO-REN, Alicia ,  MEANWELL, Nicholas A.

IPC: C07J63/00 ,  A61K31/575 ,  A61K31/56 ,  A61K31/58 ,  A61P31/18

CPC classification number: C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II:. These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的桦木酸衍生物作为HIV成熟抑制剂提供，如式I和II的化合物所示。 这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：WO2015195776A1

公开(公告)日：2015-12-23

申请号：PCT/US2015/036191

申请日：2015-06-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： REGUEIRO-REN, Alicia ,  GOSWAMI, Animesh ,  GUO, Zhiwei ,  TULLY, Thomas P. ,  SWIDORSKI, Jacob ,  LIU, Zheng ,  MEANWELL, Nicholas A.

IPC: C07D295/03 ,  C07D303/06 ,  C07J63/00 ,  A61K8/63 ,  A61K31/56 ,  A61K31/54 ,  A61P31/18

CPC classification number: C07J63/008 ,  C07J71/001 ,  C07J71/0026

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivaties that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: [Please insert chemical structure here]; [Please insert chemical structure here]; [Please insert chemical structure here]; These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的桦木酸衍生物作为HIV成熟抑制剂提供，如式I，II和III化合物所示：[请在此插入化学结构]; [请在此插入化学结构]; [请在此插入化学结构]; 这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：WO2014160692A1

公开(公告)日：2014-10-02

申请号：PCT/US2014/031697

申请日：2014-03-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： WANG, Tao ,  YIN, Zhiwei ,  ZHANG, Zhongxing ,  BENDER, John A. ,  JOHNSON, Barry L. ,  KADOW, John F. ,  MEANWELL, Nicholas A.

IPC: C07D471/04 ,  C07D519/00 ,  C07D401/06 ,  A61K31/404

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/55 ,  A61K45/06 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: I useful as HIV attachment inhibitors.

Abstract translation: 式I的化合物，包括其药学上可接受的盐：可用作HIV附着抑制剂。

公开(公告)号：WO2014025854A1

公开(公告)日：2014-02-13

申请号：PCT/US2013/053903

申请日：2013-08-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： WANG, Tao ,  ZHANG, Zhongxing ,  KADOW, John F. ,  MEANWELL, Nicholas A. ,  RUEDIGER, Edward H. ,  JAMES, Clint A. ,  DEON, Daniel H. ,  CARINI, David J. ,  JOHNSON, Barry L.

IPC: C07D401/06 ,  C07D471/04 ,  A61K31/454 ,  A61K31/437 ,  A61P31/18

CPC classification number: C07D471/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/06

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formule (I): wherein A is selected from the group consisting of:formule (II) and wherein Z is selected from the group consisting of: formule (III):,, and. are useful as HIV attachment inhibitors.

Abstract translation: 式I化合物，包括其药学上可接受的盐：结构（I）：其中A选自：结构（II），其中Z选自：构型（III）：和 可用作HIV附着抑制剂。

公开(公告)号：WO2013123019A1

公开(公告)日：2013-08-22

申请号：PCT/US2013/025897

申请日：2013-02-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： SWIDORSKI, Jacob ,  MEANWELL, Nicholas A. ,  REGUEIRO-REN, Alicia ,  SIT, Sing-Yuen ,  CHEN, Jie ,  CHEN, Yan

IPC: C07J63/00 ,  A61K31/58 ,  A61K31/575 ,  A61P31/18

CPC classification number: C07J53/002 ,  A61K31/58 ,  A61K45/06 ,  C07J63/008 ,  A61K2300/00

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.

Abstract translation: 阐述了具有药物和生物影响特性的化合物，其药物组合物和使用方法。 特别地，具有独特抗病毒活性的C-3环烯基三萜类化合物作为HIV成熟抑制剂提供，如式I，II，III和IV化合物所示：其中X可以是C 4-8环烷基，C 4-8环烯基，C 4 -9螺环烷基，C4-9螺环烯基，C4-8氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6-9氧杂螺环烷基或C6-9氧杂环烯烯基环。 这些化合物可用于治疗艾滋病毒和艾滋病。