公开(公告)号：US20150152089A1

公开(公告)日：2015-06-04

申请号：US14616008

申请日：2015-02-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: C07D403/12 ,  C07D401/14 ,  C07D491/048 ,  C07D413/14 ,  C07D491/052 ,  C07D403/14 ,  C07D491/08

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

公开(公告)号：US11970511B2

公开(公告)日：2024-04-30

申请号：US17251964

申请日：2019-06-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Li Xu ,  David S. Yoon ,  Alicia Regueiro-Ren ,  Prasada Rao Jalagam ,  Manoranjan Panda ,  Satheesh Kesavan Nair

IPC: C07H17/04 ,  A61P13/12

CPC classification number: C07H17/04 ,  A61P13/12

Abstract: The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.

公开(公告)号：US20210323991A1

公开(公告)日：2021-10-21

申请号：US17251964

申请日：2019-06-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Li Xu ,  David S. Yoon ,  Alicia Regueiro-Ren ,  Prasada Rao Jalagam ,  Manoranjan Panda ,  Satheesh Kesavan Nair

IPC: C07H17/04 ,  A61P13/12

Abstract: The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.

公开(公告)号：US20150336975A1

公开(公告)日：2015-11-26

申请号：US14816405

申请日：2015-08-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: C07D491/113 ,  C07D403/14 ,  C07D491/048 ,  C07D491/08 ,  C07D413/14 ,  C07D491/052 ,  C07D403/12 ,  C07D401/14

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 本公开提供了一系列式（I）的化合物，其调节和淀粉样蛋白肽（＆bgr; -AP）产生，并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽（＆bgr; -AP）生产。

公开(公告)号：US20150291655A1

公开(公告)日：2015-10-15

申请号：US14682179

申请日：2015-04-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07J63/00 ,  C07F5/04 ,  C07C309/65

CPC classification number: A61K31/58 ,  A61K45/06 ,  C07C309/65 ,  C07C2601/16 ,  C07F5/025 ,  C07F5/04 ,  C07J63/008

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from 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 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C1-6 alkyl-halo. 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作为HIV成熟抑制剂提供，如式I化合物所示：X选自C 4-8环烷基，C 4-8环烯基，C 4-9螺环烷基，C 4-9螺环烯基，C 4 - 8个氧杂环烷基，C4-8二氧杂环烷基，C6-8氧杂环烯基，C6-8二氧杂环烯基，C6环二烯基，C6氧杂环辛烯基，C6-9氧杂螺环烷基和C6-9氧杂环烯烯基环，使得X被A取代，其中A是-C1-6 烷基卤 这些化合物可用于治疗艾滋病毒和艾滋病。

公开(公告)号：US20130178462A1

公开(公告)日：2013-07-11

申请号：US13785171

申请日：2013-03-05

Applicant: Bristol-Myers Squibb Company

Inventor： Kenneth M. Boy ,  Jason M. Guernon ,  John E. Macor ,  Richard E. Olson ,  Jianliang Shi ,  Lorin A. Thompson, III ,  Yong-Jin Wu ,  Li Xu ,  Yunhui Zhang ,  Dmitry S. Zuev

IPC: C07D239/70 ,  C07D491/08 ,  C07D471/04 ,  C07D403/14 ,  C07D491/107 ,  C07D403/12

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113

Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.

Abstract translation: 本公开提供了一系列调节β-淀粉样肽（β-AP）产生的式（I）化合物，并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽（β-AP）产生影响的病症 。

公开(公告)号：US09249180B2

公开(公告)日：2016-02-02

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 ,  Zheng Liu ,  Richard A. Hartz ,  Li Xu

IPC: A61K31/56 ,  A61K31/58 ,  C07J53/00 ,  C07J63/00 ,  A61K31/568

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 The 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化合物该化合物可用于治疗HIV和AIDS。