公开(公告)号：US20230321109A1

公开(公告)日：2023-10-12

申请号：US18145811

申请日：2022-12-22

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI ,  Nareshkumar F. JAIN ,  Thomas Patrick MARKOTAN

IPC: A61K31/537 ,  A61K31/5365 ,  A61K47/68 ,  A61K45/06 ,  C07D498/18

CPC classification number: A61K31/537 ,  A61K31/5365 ,  A61K47/6803 ,  C07B2200/07 ,  A61K47/6851 ,  A61K45/06 ,  C07D498/18 ,  A61K47/6809

Abstract: The disclosure relates to compositions comprising diastereomer of a macrolide exhibiting improved therapeutic profile in the context of inhibiting cell proliferation compared to the corresponding compositions comprising mixture of diastereomers. The disclosure further provides drug-ligand conjugates formed using diastereomer of the macrolide. The disclosure also provides novel method of preparation of diastereomer of the macrolide and their therapeutic uses.

公开(公告)号：US20230116771A1

公开(公告)日：2023-04-13

申请号：US17889301

申请日：2022-08-16

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Thomas NITTOLI ,  Thomas P. MARKOTAN

IPC: A61K47/68 ,  A61K31/537 ,  C07D498/18 ,  C07K16/32 ,  C07K16/40

Abstract: Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.

公开(公告)号：US20210087272A1

公开(公告)日：2021-03-25

申请号：US17026132

申请日：2020-09-18

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Frank KUHNERT ,  Michael VAN METER ,  Thomas NITTOLI

IPC: C07K16/28 ,  A61K47/68 ,  A61P35/02

Abstract: The present disclosure provides antibody-drug conjugates comprising anti-PTCRA antibodies and methods of using the same. The ADCs of the disclosure are useful for the treatment of T-ALL and other disorders related to elevated expression of PTCRA.

公开(公告)号：US20200368361A1

公开(公告)日：2020-11-26

申请号：US16722958

申请日：2019-12-20

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Thomas NITTOLI ,  Seungyong Sean CHOI ,  Mrinmoy SAHA

IPC: A61K47/68 ,  C07D498/18

Abstract: The disclosure relates to rifamycin analog compounds, intermediates and precursors thereof, and pharmaceutical compositions capable of inhibiting bacterial growth (e.g., S. aureus growth) and treating bacterial infections (e.g., S. aureus infections). The disclosure further relates to antibody-drug conjugates of rifamycin analog compounds and antibodies, for example, antibodies specific for infectious disease-related targets such as membrane glycoprotein receptor (MSR1), wall teichoic acids (WTA) or Protein A, and methods of use thereof to inhibit bacterial growth and treat bacterial infections.

公开(公告)号：US20200277306A1

公开(公告)日：2020-09-03

申请号：US16740312

申请日：2020-01-10

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI

IPC: C07D507/00 ,  A61K47/68 ,  A61K31/5365

Abstract: The present disclosure relates to linker compounds that are useful in covalently linking biologically active molecules with Ligands. The disclosed compounds also relate to biologically active molecules and Ligand conjugates, wherein the biologically active molecule is linked to the Ligand through a linker. The disclosure further provides compositions comprising biologically active molecule-ligand conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.

公开(公告)号：US20180312597A1

公开(公告)日：2018-11-01

申请号：US15926998

申请日：2018-03-20

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI ,  Arthur KUNZ

IPC: C07K16/28 ,  A61K47/68 ,  C07K16/30 ,  A61K39/00

Abstract: The present disclosure relates to conjugates comprising biologically active molecules linked to a multimeric antigen-binding compound or a multimeric immunoglobulin via a linker. The disclosure further provides reagents and methods of manufacturing the conjugates and the linkers. The disclosure also provides compositions comprising the conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.

公开(公告)号：US20170121413A1

公开(公告)日：2017-05-04

申请号：US15314909

申请日：2015-06-01

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI ,  Arthur KUNZ

IPC: C07K16/28 ,  C07K16/30

CPC classification number: C07K16/2866 ,  A61K47/6801 ,  A61K47/6803 ,  A61K47/6813 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/2863 ,  C07K16/30 ,  C07K2317/34 ,  C07K2317/77 ,  C07K2317/92

Abstract: The present disclosure relates to conjugates comprising biologically active molecules linked to a multimeric antigen-binding compound or a multimeric immunoglobulin via a linker. The disclosure further provides reagents and methods of manufacturing the conjugates and the linkers. The disclosure also provides compositions comprising the conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.

公开(公告)号：US20160375147A1

公开(公告)日：2016-12-29

申请号：US15081759

申请日：2016-03-25

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Thomas NITTOLI

IPC: A61K47/48 ,  C07D498/18

CPC classification number: C07D498/18 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6889

Abstract: Provided herein are maytansinoid derivatives, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.

Abstract translation: 本文提供美登木素生物碱衍生物，其缀合物，以及用其治疗或预防增殖性疾病的方法。

公开(公告)号：US20160304615A1

公开(公告)日：2016-10-20

申请号：US15170628

申请日：2016-06-01

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Jessica R. KIRSHNER ,  Douglas MACDONALD ,  Gavin THURSTON ,  Joel H. MARTIN ,  Frank DELFINO ,  Thomas NITTOLI ,  Marcus KELLY

IPC: C07K16/28 ,  A61K39/395 ,  A61K45/06 ,  C07K16/30 ,  A61K47/48

CPC classification number: C07K16/2863 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/6803 ,  A61K47/6851 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/30 ,  C07K16/3015 ,  C07K16/3023 ,  C07K16/3069 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/565 ,  C07K2317/77 ,  C07K2317/92

Abstract: The present invention provides antibodies that bind to the class III variant of EGFR (EGFRvIII) and methods of using the same. According to certain embodiments, the antibodies of the invention bind human EGFRvIII with high affinity. The antibodies of the invention may be fully human antibodies. The invention includes anti-EGFRvIII antibodies conjugated to a cytotoxic agent, radionuclide, or other moiety detrimental to cell growth or proliferation. The antibodies of the invention are useful for the treatment of various cancers.

公开(公告)号：US20160030591A1

公开(公告)日：2016-02-04

申请号：US14776668

申请日：2014-03-14

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI

IPC: A61K47/48 ,  C07D507/00 ,  A61K31/5365

Abstract: The present disclosure relates to linker compounds that are useful in covalently linking biologically active molecules with Ligands. The disclosed compounds also relate to biologically active molecules and Ligand conjugates, wherein the biologically active molecule is linked to the Ligand through a linker. The disclosure further provides compositions comprising biologically active molecule-ligand conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.

Abstract translation: 本公开涉及可用于共价连接生物活性分子与配体的连接体化合物。 所公开的化合物还涉及生物活性分子和配体缀合物，其中生物活性分子通过连接体与配体连接。 本公开进一步提供包含生物活性分子 - 配体缀合物的组合物，修饰异常细胞生长的方法和使用缀合物或组合物的治疗方法。