公开(公告)号：US20160199510A1

公开(公告)日：2016-07-14

申请号：US14994378

申请日：2016-01-13

Applicant: Bristol-Myers Squibb Company

Inventor： Ivar M. MCDONALD ,  Naidu S. CHOWDARI ,  Walter Lewis Johnson ,  Yong Zhang ,  Robert M. BORZILLERI ,  Sanjeev Gangwar

IPC: A61K47/48 ,  C07K5/062 ,  C07D487/04

CPC classification number: C07D471/04 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07D487/04 ,  C07D519/00 ,  C07K5/06052

Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Abstract translation: 苯并二氮杂二聚体具有由其中X表示的结构，其包含杂芳族部分并且在本申请中进一步定义; R1和式（I），（Ia）和（Ib）中的其它变量如本申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。

公开(公告)号：US09109008B2

公开(公告)日：2015-08-18

申请号：US14177498

申请日：2014-02-11

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang Cong ,  Heng Cheng ,  Sanjeev Gangwar

IPC: A61K38/07 ,  C07K5/117 ,  A61K47/48 ,  C07K7/06 ,  C07K5/10 ,  C07K5/06 ,  C07K5/078 ,  C07K5/107

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/48246 ,  A61K47/48415 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6861 ,  A61K47/6863 ,  A61K47/6869 ,  C07K5/06 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06

Abstract: Tubulysin compounds of the formula (I) where R1, R2R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Abstract translation: 其中R 1，R 2 R 3 a，R 3b，R 4，R 5，W和n如本文所定义的式（I）的调蛋白素化合物是可用于治疗癌症的抗有丝分裂剂，特别是当与靶向部分缀合时 。

公开(公告)号：US20150132324A1

公开(公告)日：2015-05-14

申请号：US14605549

申请日：2015-01-26

Applicant: Bristol-Myers Squibb Company

Inventor： Qiang CONG ,  Heng Cheng ,  Sanjeev Gangwar

IPC: A61K47/48 ,  A61K38/05

CPC classification number: C07K5/1024 ,  A61K38/05 ,  A61K38/07 ,  A61K47/48246 ,  A61K47/48415 ,  A61K47/48569 ,  A61K47/48592 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48638 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6861 ,  A61K47/6863 ,  A61K47/6869 ,  C07K5/06 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/10 ,  C07K5/1016 ,  C07K7/06

Abstract: Tubulysin compounds of the formula (I) where R1, R2, R3a, R3b, R4, R5, W, and n are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.

Abstract translation: 其中R 1，R 2，R 3a，R 3b，R 4，R 5，W和n如本文所定义的式（I）的调节素化合物是可用于治疗癌症的抗有丝分裂剂，特别是当与 靶向部分。

公开(公告)号：US11020490B2

公开(公告)日：2021-06-01

申请号：US16437047

申请日：2019-06-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ian S. Young ,  Sha Lou ,  Sanjeev Gangwar

IPC: A61K47/00 ,  A61K47/68 ,  C07K5/10

Abstract: In antibody-drug conjugates having tubulysin analog as the warhead, according to formula (III) the acetate group in the Tuv subunit (dotted box) demonstrates improved stability against hydrolytic cleavage.

公开(公告)号：US10913741B2

公开(公告)日：2021-02-09

申请号：US17003385

申请日：2020-08-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Liqi He ,  Sanjeev Gangwar ,  Yam B. Poudel ,  Prasanna Sivaprakasam

IPC: A61K31/52 ,  A61K31/522 ,  C07D473/18 ,  C07D473/04 ,  A61P37/04 ,  A61K47/68

Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R1, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

公开(公告)号：US10898578B2

公开(公告)日：2021-01-26

申请号：US16425596

申请日：2019-05-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. Poudel ,  Sanjeev Gangwar

IPC: A61K47/65 ,  A61K47/64 ,  A61K47/68 ,  A61P35/00 ,  A61K45/06

Abstract: Compounds represented by formula (I) can be used to make antibody-drug conjugates. The conjugates so made are stable in both human and mouse serum, enabling the performance of pre-clinical studies using a mouse model.

公开(公告)号：US20200291028A1

公开(公告)日：2020-09-17

申请号：US16890765

申请日：2020-06-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. Poudel ,  Sanjeev Gangwar ,  Prasanna Sivaprakasam ,  Shoshana L. Posy

IPC: C07D473/18 ,  A61P37/04

Abstract: Compounds having a structure according to formula (I) where R1, R2, and R3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

公开(公告)号：US10711003B2

公开(公告)日：2020-07-14

申请号：US16659735

申请日：2019-10-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Liqi He ,  Sanjeev Gangwar ,  Shoshana L. Posy ,  Yam B. Poudel ,  Prasanna Sivaprakasam

IPC: A61K31/52 ,  C07D473/18 ,  A61P37/04 ,  A61K47/60 ,  A61K47/68

Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

公开(公告)号：US20200039986A1

公开(公告)日：2020-02-06

申请号：US16529457

申请日：2019-08-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. POUDEL ,  Sanjeev Gangwar ,  Liqi He ,  Prasanna Sivaprakasam

IPC: C07D487/04 ,  A61K39/395 ,  A61K31/519 ,  A61K47/60

Abstract: Compounds according to formula II are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

公开(公告)号：US10472361B2

公开(公告)日：2019-11-12

申请号：US16103210

申请日：2018-08-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. Poudel ,  Sanjeev Gangwar ,  Prasanna Sivaprakasam ,  Shoshana L. Posy

IPC: C07D473/18 ,  A61P37/04

Abstract: Compounds having a structure according to formula (I) where R1, R2, and R3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.