公开(公告)号：US10233192B2

公开(公告)日：2019-03-19

申请号：US15677959

申请日：2017-08-15

Applicant: WILLIAM MARSH RICE UNIVERSITY ,  BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Kyriacos C. Nicolaou ,  Min Lu ,  Debashis Mandal ,  Sanjeev Gangwar ,  Naidu S. Chowdari ,  Yam B. Poudel

IPC: C07D491/08 ,  A61K47/68

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

公开(公告)号：US09777013B2

公开(公告)日：2017-10-03

申请号：US14911881

申请日：2014-08-14

Applicant: WILLIAM MARSH RICE UNIVERSITY ,  BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Kyriacos C. Nicolaou ,  Min Lu ,  Debashis Mandal ,  Sanjeev Gangwar ,  Naidu S. Chowdari ,  Yam B. Poudel

IPC: C07D491/08 ,  A61K47/48

CPC classification number: C07D491/08 ,  A61K47/6803 ,  A61K47/6851

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin of formulae (I) and (II). The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates comprising the compounds of formulae (I) and (II).

公开(公告)号：US10889590B2

公开(公告)日：2021-01-12

申请号：US16357109

申请日：2019-03-18

Applicant: WILLIAM MARSH RICE UNIVERSITY ,  BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Kyriacos C. Nicolaou ,  Min Lu ,  Debashis Mandal ,  Sanjeev Gangwar ,  Naidu S. Chowdari ,  Yam B. Poudel

IPC: C07D491/08 ,  A61K47/68

Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

公开(公告)号：US10287291B2

公开(公告)日：2019-05-14

申请号：US15680424

申请日：2017-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Fukang Yang ,  Qian Zhang ,  Lawrence B. Snyder ,  Sanjeev Gangwar ,  Dale L. Boger

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/407 ,  A61K31/437 ,  A61K47/68 ,  A61P35/00 ,  A61K39/00

Abstract: seco-Cyclopropapyrroloindole compounds of formula (I) where Hal, R1, R2, and R3 are as defined in the application, are potent anti-cancer agents that can be used in antibody-drug conjugates.

公开(公告)号：US10696676B2

公开(公告)日：2020-06-30

申请号：US16583869

申请日：2019-09-26

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：US20190388553A1

公开(公告)日：2019-12-26

申请号：US16437047

申请日：2019-06-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: A61K47/68 ,  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：US10279049B2

公开(公告)日：2019-05-07

申请号：US15587927

申请日：2017-05-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qiang Cong ,  Sanjeev Gangwar ,  Vangipuram S. Rangan ,  Mei-Chen Sung

IPC: A61K39/395 ,  A61K47/68 ,  C07K16/28

Abstract: The drug component of an antibody-drug conjugate having a structure according to formula (II), where Ab, m, n, R1, R2, R3, R4, and R5 are as defined in the application, exhibits unexpectedly improved stability.

公开(公告)号：US20190055245A1

公开(公告)日：2019-02-21

申请号：US16103581

申请日：2018-08-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D473/18 ,  A61K47/68

Abstract: Compounds having a structure according to formula (I) where R1 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：US09186416B2

公开(公告)日：2015-11-17

申请号：US14471096

申请日：2014-08-28

Applicant: Bristol-Myers Squibb Company

Inventor： Qian Zhang ,  Sanjeev Gangwar ,  Chin Pan ,  Daniel W. Derwin

IPC: A61K47/48 ,  C07K5/06 ,  C07K5/10 ,  C07K5/08 ,  A61K31/404 ,  C07D403/06 ,  C07D403/14 ,  C07D209/60

CPC classification number: A61K47/48384 ,  A61K31/404 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6859 ,  A61K47/6863 ,  A61K47/6869 ,  C07D209/60 ,  C07D403/06 ,  C07D403/14 ,  C07K5/06 ,  C07K5/06034 ,  C07K5/06095 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/10

Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.

Abstract translation: 一种免疫偶联物，其中式（I）的磷酸酯前体化DNA小沟结合剂（其中X是可亲可取代的离去基团）与抗体或抗体的抗原结合片段缀合，以及可用于制备的化合物 这样的免疫缀合物，以及这种免疫缀合物的用途。

公开(公告)号：US20140364585A1

公开(公告)日：2014-12-11

申请号：US14471096

申请日：2014-08-28

Applicant: Bristol-Myers Squibb Company

Inventor： Qian ZHANG ,  Sanjeev Gangwar ,  Chin Pan ,  Daniel W. Derwin

IPC: A61K47/48 ,  A61K31/404 ,  C07K5/08 ,  C07K5/06 ,  C07K5/10

CPC classification number: A61K47/48384 ,  A61K31/404 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6857 ,  A61K47/6859 ,  A61K47/6863 ,  A61K47/6869 ,  C07D209/60 ,  C07D403/06 ,  C07D403/14 ,  C07K5/06 ,  C07K5/06034 ,  C07K5/06095 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/10

Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.

Abstract translation: 一种免疫偶联物，其中式（I）的磷酸酯前体化DNA小沟结合剂（其中X是可亲可取代的离去基团）与抗体或抗体的抗原结合片段缀合，以及可用于制备的化合物 这样的免疫缀合物，以及这种免疫缀合物的用途。