公开(公告)号：US20240293566A1

公开(公告)日：2024-09-05

申请号：US18572930

申请日：2022-06-21

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Frank DELFINO ,  Marcus KELLY ,  Jessica KIRSHNER ,  Thomas NITTOLI ,  Gavin THURSTON

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

CPC classification number: A61K47/68035 ,  A61K45/06 ,  A61K47/6849 ,  A61P35/00

Abstract: The present disclosure provides antibody-drug conjugates (ADCs) comprising antibodies that bind to the class III variant of EGFR (EGFRVIII) conjugated to tesirine, and methods of using the same. According to certain embodiments, the antibodies or antigen-binding fragments thereof, useful herein, bind human EGFRVIII with high affinity. The antibodies or antigen-binding fragments thereof, useful herein, may be fully human antibodies. The ADCs provided herein are useful for the treatment of various cancers.

公开(公告)号：US20160251442A1

公开(公告)日：2016-09-01

申请号：US15051580

申请日：2016-02-23

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Nicholas J. PAPADOPOULOS ,  Gavin THURSTON ,  Jessica R. KIRSHNER ,  Marcus P. KELLY ,  Thomas NITTOLI ,  Frank J. DELFINO

IPC: C07K16/28 ,  A61K47/48

CPC classification number: C07K16/2866 ,  A61K31/537 ,  A61K47/6803 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2869 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/52 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2317/92 ,  C07K2317/94

Abstract: The present invention provides antibodies that bind to prolactin receptor (PRLR) and methods of using the same. According to certain embodiments, the antibodies of the invention bind human PRLR with high affinity. In certain embodiments, the invention includes antibodies that bind PRLR and block prolactin-mediated cell signaling. In other embodiments, the invention includes antibodies that bind PRLR but do not block prolactin-mediated cell signaling. The antibodies of the invention may be fully human antibodies. The invention includes anti-PRLR 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 as well as other PRLR-related disorders. The present invention also includes antibody drug conjugates comprising an antibody or antigen-binding fragment thereof that specifically binds a class I cytokine receptor, wherein the antibody or antigen-binding fragment thereof is conjugated to a cytotoxic agent.

公开(公告)号：US20240101672A1

公开(公告)日：2024-03-28

申请号：US18482448

申请日：2023-10-06

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Frank KUHNERT ,  Michael VAN METER ,  Thomas NITTOLI

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

CPC classification number: C07K16/2809 ,  A61K47/6803 ,  A61K47/6849 ,  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：US20220259225A1

公开(公告)日：2022-08-18

申请号：US17528144

申请日：2021-11-16

Applicant: Regeneron Pharmaceuticals, Inc.

Inventor： Thomas NITTOLI

IPC: C07D498/18 ,  A61K47/68

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

公开(公告)号：US20180237456A1

公开(公告)日：2018-08-23

申请号：US15554813

申请日：2016-03-17

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI ,  Srinath Thirumalai RAJAN ,  Thomas P. MARKOTAN ,  Nareshkumar JAIN

IPC: C07D498/18 ,  C07D263/46

Abstract: Provided herein are compounds useful for appending amino acids to nucleophiles.

公开(公告)号：US20160354482A1

公开(公告)日：2016-12-08

申请号：US14913965

申请日：2014-08-26

Applicant: REGENERON PHARMACEUTICALS, INC.

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

IPC: A61K47/48 ,  C07D498/18 ,  A61K45/06 ,  A61K31/537

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

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.

Abstract translation: 本公开涉及包含大环内酯非对映异构体的组合物，其与包含非对映体混合物的相应组合物相比，在抑制细胞增殖的情况下表现出改善的治疗特征。 本公开进一步提供了使用大环内酯非对映异构体形成的药物 - 配体结合物。 本公开还提供了制备大环内酯非对映体及其治疗用途的新方法。

公开(公告)号：US20250041433A1

公开(公告)日：2025-02-06

申请号：US18580547

申请日：2022-07-28

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Thomas NITTOLI

IPC: A61K47/68 ,  A61K47/65 ,  A61P31/16

Abstract: Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with influenza, including VX-787 and derivatives thereof, and protein (e.g., antibody) drug conjugates thereof.

公开(公告)号：US20240189319A1

公开(公告)日：2024-06-13

申请号：US18552303

申请日：2022-03-25

Applicant: Regeneron Pharmaceuticals, Inc

Inventor： Thomas NITTOLI ,  Anna ZUMSTEG

IPC: A61K31/538 ,  A61K38/14 ,  A61P31/04

CPC classification number: A61K31/538 ,  A61K38/14 ,  A61P31/04

Abstract: The disclosure relates to rifamycin analog compounds in combination with vancomycin, and pharmaceutical compositions and dosage forms comprising same, capable of inhibiting bacterial growth (e.g., S. aureus growth) and treating bacterial infections (e.g., S. aureus infections). The disclosure further relates to methods of use thereof to inhibit bacterial growth, treat bacterial infections. and treat disease with rifamycin analog compounds in combination with vancomycin. The disclosure further relates to methods of enhancing efficacy of rifamycin analog compounds and/or vancomycin.

公开(公告)号：US20210330803A1

公开(公告)日：2021-10-28

申请号：US17156525

申请日：2021-01-23

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Alina BAUM ,  Thomas NITTOLI

IPC: A61K47/68 ,  A61K31/506 ,  A61K31/5383

Abstract: Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with influenza, including VX-787 and derivatives thereof, baloxavir and derivatives thereof, and baloxavir marboxil and derivatives thereof, and protein (e.g., antibody) drug conjugates thereof.

公开(公告)号：US20210147557A1

公开(公告)日：2021-05-20

申请号：US16918656

申请日：2020-07-01

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 ,  A61K47/68 ,  C07K16/30

Abstract: The present invention provides antibodies that bind to the class Ill 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.