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1. WO2019058367 - LIPOPHILIC PEPTIDE PRODRUGS

Publication Number WO/2019/058367
Publication Date 28.03.2019
International Application No. PCT/IL2018/051042
International Filing Date 17.09.2018
IPC
A61K 47/54 2017.1
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
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
CPC
A61K 38/31
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
31Somatostatins
A61K 47/18
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
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 47/542
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
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
542Carboxylic acids, e.g. a fatty acid or an amino acid
Applicants
  • YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. [IL]/[IL]
Inventors
  • HOFFMAN, Amnon
  • GILON, Chaim
  • FANOUS, Joseph
  • KLINGER, Adi
Agents
  • WEBB, Cynthia
  • BARZAM, Maty
  • BOGIN, Liora
  • BURSTEIN, Tal
  • FINAROV, Igal
  • GANOR, Sharon
  • HORNIK, Vered
  • NOAH, Eran
  • POTASH, Shay
  • SCHICKLER, Hedva
  • SCHVARTZ, Iris
  • SILVERMAN, Eran
  • TRAVITSKY, Nina
  • WEBB, Yael
  • ZIPOR, Gadi
Priority Data
62/560,21419.09.2017US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) LIPOPHILIC PEPTIDE PRODRUGS
(FR) PROMÉDICAMENTS LIPOPHILES À BASE DE PEPTIDES
Abstract
(EN) The present invention relates to methods of preparing peptide-based prodrugs having enhanced oral bioavailability and intestinal penetration. Said prodrugs are characterized in improved lipophilicity, reduced electric charge and tendency to undergo biotransformation through enzymatic reaction (e.g. in the blood stream) to form biologically active peptides.
(FR) La présente invention concerne des procédés de préparation de promédicaments à base de peptides ayant une biodisponibilité orale et une pénétration intestinale améliorées. Lesdits promédicaments sont caractérisés par une lipophilie améliorée, une charge électrique réduite et une tendance à subir une biotransformation par réaction enzymatique (par exemple dans le flux sanguin) pour former des peptides biologiquement actifs.
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