公开(公告)号：US11166959B2

公开(公告)日：2021-11-09

申请号：US16761449

申请日：2018-11-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Erika M. V. Araujo ,  Yan Chen ,  Bireshwar Dasgupta ,  Andrew P. Degnan ,  Matthew D. Hill ,  Godwin Kwame Kumi ,  Harold A. Mastalerz ,  Mark D. Wittman ,  Bradley C. Pearce ,  Guifen Zhang

IPC: A61K31/5377 ,  A61K31/506 ,  A61P35/00 ,  A61K45/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D453/02 ,  C07D491/048 ,  C07D498/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CH or N; Y is CR5 or N; and R1, R2, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds to modulate or inhibit the enzymatic activity of hematopoietic progenitor kinase 1 (HPK1), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

公开(公告)号：US20150005342A1

公开(公告)日：2015-01-01

申请号：US14477594

申请日：2014-09-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: C07D401/12 ,  A61K45/06

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract translation: 公开了具有以下通式的丙型肝炎病毒抑制剂：其中R1，R2，R3，R'，B，Y和X在说明书中描述。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

公开(公告)号：US08889871B2

公开(公告)日：2014-11-18

申请号：US14183247

申请日：2014-02-18

Applicant: Bristol-Myers Squibb Company

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: C07D217/24 ,  C07D401/12

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract translation: 公开了具有以下通式的丙型肝炎病毒抑制剂：其中R1，R2，R3，R'，B，Y和X在说明书中描述。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。

公开(公告)号：US08889854B2

公开(公告)日：2014-11-18

申请号：US13799479

申请日：2013-03-13

Applicant: Bristol-Myers Squibb Company

Inventor： Ny Sin ,  Zheng Liu ,  Jacob Swidorski ,  Sing-Yuen Sit ,  Jie Chen ,  Yan Chen ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren

IPC: C07J53/00 ,  C07D498/08 ,  C07D495/08 ,  C07D495/10 ,  C07D487/10 ,  C07J63/00 ,  C07D491/08 ,  C07D209/52 ,  C07D487/08

CPC classification number: C07D487/08 ,  C07D209/52 ,  C07D487/10 ,  C07D491/08 ,  C07D495/08 ,  C07D495/10 ,  C07D498/08 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: 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三萜类化合物的C-17二环胺作为HIV成熟抑制剂提供，如式I，II和III化合物所示：这些化合物可用于治疗HIV和AIDS。

公开(公告)号：US11718601B2

公开(公告)日：2023-08-08

申请号：US17713598

申请日：2022-04-05

Applicant: Bristol-Myers Squibb Company

Inventor： Yan Chen ,  Godwin Kwame Kumi ,  Audris Huang ,  Satheesh Kesavan Nair ,  Bharat Dinkar Shimpukade ,  Suresh Babu Vishwa Krishna Penmetsa ,  James Aaron Balog

IPC: C07D401/14 ,  A61P35/00

CPC classification number: C07D401/14 ,  A61P35/00

Abstract: Disclosed are compounds of Formula (I):




or a salt thereof, wherein R1, R2, R4, R6, m, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

公开(公告)号：US09636375B2

公开(公告)日：2017-05-02

申请号：US14936419

申请日：2015-11-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: A61K31/40 ,  A61K38/06 ,  C07D207/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/062 ,  C07K5/083 ,  C07K5/08 ,  C07D217/24 ,  A61K45/06 ,  A61K38/00

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

公开(公告)号：US20160151387A1

公开(公告)日：2016-06-02

申请号：US15015741

申请日：2016-02-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Alicia Regueiro-Ren ,  Zheng Liu ,  Jacob Swidorski ,  Ny Sin ,  Brian Lee Venables ,  Sing-Yuen Sit ,  Yan Chen ,  Jie Chen ,  Nicholas A. Meanwell

IPC: A61K31/565 ,  A61K31/58 ,  A61K31/704 ,  A61K45/06

CPC classification number: A61K31/565 ,  A61K31/56 ,  A61K31/58 ,  A61K31/704 ,  A61K45/06 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: 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-17和C-3修饰的三萜类化合物作为HIV成熟抑制剂提供，如式I，II和III化合物所示：这些化合物可用于治疗HIV和AIDS。

公开(公告)号：US20140243298A1

公开(公告)日：2014-08-28

申请号：US14186533

申请日：2014-02-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jacob Swidorski ,  Yan Chen ,  Sing-Yuen Sit ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren ,  Jie Chen

IPC: C07J53/00 ,  A61K31/568 ,  A61K31/58

CPC classification number: C07J53/002 ,  A61K31/568 ,  A61K31/58 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV:a compound of Formula I a compound of Formula II a compound of Formula III and a compound of Formula IV 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烷基和烯基C-3修饰的桦木酸衍生物作为HIV成熟抑制剂提供，如式I，II，III和IV化合物所示：式I化合物式IIa化合物 式III化合物和式IV化合物这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：US08710229B2

公开(公告)日：2014-04-29

申请号：US13901637

申请日：2013-05-24

Applicant: Bristol-Myers Squibb Company

Inventor： Alan Xiangdong Wang ,  Li-Qiang Sun ,  Sing-Yuen Sit ,  Ny Sin ,  Paul Michael Scola ,  Yan Chen

IPC: C07D215/38

CPC classification number: A61K38/06 ,  A61K31/40 ,  A61K38/00 ,  A61K38/005 ,  A61K45/06 ,  C07D207/16 ,  C07D217/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/0808 ,  C07K5/0827 ,  A61K2300/00

Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R′, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

公开(公告)号：US20130210787A1

公开(公告)日：2013-08-15

申请号：US13760726

申请日：2013-02-06

Applicant: Bristol-Myers Squibb Company

Inventor： Jacob Swidorski ,  Nicholas A. Meanwell ,  Alicia Regueiro-Ren ,  Sing-Yuen Sit ,  Jie Chen ,  Yan Chen

IPC: C07J53/00 ,  A61K45/06 ,  A61K31/58

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。