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1. WO2019050780 - COMPOUNDS FOR REDUCING THE VISCOSITY OF BIOLOGICAL FORMULATIONS

Publication Number WO/2019/050780
Publication Date 14.03.2019
International Application No. PCT/US2018/048995
International Filing Date 31.08.2018
IPC
A61K 39/395 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 38/03 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
03Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
A61K 47/22 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
CPC
A61K 39/39591
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies
39591Stabilisation, fragmentation
A61K 47/183
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
16containing nitrogen, ; e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
183Amino acids, e.g. glycine, EDTA or aspartame
A61K 47/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07C 229/36
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34the carbon skeleton containing six-membered aromatic rings
36with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
Applicants
  • MERCK SHARP & DOHME CORP. [US]/[US]
  • CHU, Lin [US]/[US] (US)
  • TOUSSAINT, Nathalie, Y. [US]/[US] (US)
  • XIAO, Dong [US]/[US] (US)
  • VACHAL, Petr [US]/[US] (US)
  • KASHI, Ramesh, S. [US]/[US] (US)
  • BAK, Annette [US]/[SE] (US)
Inventors
  • CHU, Lin
  • TOUSSAINT, Nathalie, Y.
  • XIAO, Dong
  • VACHAL, Petr
  • KASHI, Ramesh, S.
  • BAK, Annette
Common Representative
  • MERCK SHARP & DOHME CORP.
Priority Data
62/554,13405.09.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS FOR REDUCING THE VISCOSITY OF BIOLOGICAL FORMULATIONS
(FR) COMPOSÉS POUR LA RÉDUCTION DE LA VISCOSITÉ DE FORMULATIONS BIOLOGIQUES
Abstract
(EN)
The present invention relates to pegylated amino acid compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3A, R3B and n are as defined herein. The present invention also relates to compositions which comprise a pegylated amino acid compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, in combination with a high concentration of an active biological ingredient (ABI). In embodiments of the invention, the ABI is an anti-PD-1 antibody or antigen binding fragment thereof that specifically binds human programmed death receptor 1 (PD-1). The invention further relates to methods for lowering the viscosity of an aqueous solution of a pharmaceutical composition comprising adding a compound of the invention to the solution. The invention also provides methods for treating a pathological disease or condition, such as cancer, by administering to a subject in need of such treatment a therapeutically effective amount of a pharmaceutical composition of the invention.
(FR)
La présente invention concerne des composés acides aminés pégylés de formule (I) et des sels pharmaceutiquement acceptables de ceux-ci, où X, R1, R2, R3A, R3B et n sont tels que définis dans la présente invention. La présente invention concerne également des compositions qui comprennent un composé acide aminé pégylé selon l'invention, ou un sel pharmaceutiquement acceptable de celui-ci, et un support pharmaceutiquement acceptable, en association avec une concentration élevée d'un principe actif biologique (ABI). Dans des modes de réalisation de l'invention, l'ABI est un anticorps anti-PD-1 ou un fragment de liaison à l'antigène de celui-ci qui se lie spécifiquement au récepteur-1 de mort cellulaire programmée (PD-1) humain. L'invention concerne en outre des procédés pour l'abaissement de la viscosité d'une solution aqueuse d'une composition pharmaceutique comprenant l'ajout d'un composé selon l'invention à la solution. L'invention concerne également des méthodes de traitement d'une maladie ou d'un état pathologique, tels que le cancer, par l'administration à un sujet qui a besoin d'un tel traitement d'une quantité thérapeutiquement efficace d'une composition pharmaceutique selon l'invention.
Also published as
JP2020512875
MXMX/a/2020/002429
RU2020112302
Latest bibliographic data on file with the International Bureau