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1. WO2012055509 - DIKETOPIPERAZINE FORMING DIPEPTIDYL LINKER

Publication Number WO/2012/055509
Publication Date 03.05.2012
International Application No. PCT/EP2011/005280
International Filing Date 20.10.2011
Chapter 2 Demand Filed 15.02.2012
IPC
C07K 1/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
04on carriers
C07K 14/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
005from viruses
08RNA viruses
15Retroviridae, e.g. bovine leukaemia virus, feline leukaemia virus, human T-cell leukaemia-lymphoma virus
155Lentiviridae, e.g. human immunodeficiency virus (HIV), visna-maedi virus, equine infectious anaemia virus
16HIV-1
C07K 5/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
C07K 17/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
17Carrier-bound or immobilised peptides; Preparation thereof
02Peptides being immobilised on, or in, an organic carrier
08the carrier being a synthetic polymer
CPC
C07K 1/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
04on carriers
C07K 1/062
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
061using protecting groups
062for alpha- or omega-carboxy functions
C07K 1/068
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
06using protecting groups or activating agents
061using protecting groups
068for heterocyclic side chains
C07K 5/06086
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06086with the first amino acid being basic
C08F 112/08
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
112Homopolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an aromatic carbocyclic ring
02Monomers containing only one unsaturated aliphatic radical
04containing one ring
06Hydrocarbons
08Styrene
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of bulk chemicals
55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • LONZA LTD [CH]/[CH] (AllExceptUS)
  • ALBERICIO, Fernando [ES]/[ES] (UsOnly)
  • CRISTAU, Michèle [FR]/[CH] (UsOnly)
  • GIRAUD, Matthieu [FR]/[CH] (UsOnly)
  • GONGORA BENITEZ, Miriam [ES]/[ES] (UsOnly)
  • TULLA-PUCHE, Judit [ES]/[ES] (UsOnly)
Inventors
  • ALBERICIO, Fernando
  • CRISTAU, Michèle
  • GIRAUD, Matthieu
  • GONGORA BENITEZ, Miriam
  • TULLA-PUCHE, Judit
Common Representative
  • LONZA LTD
Priority Data
10014114.229.10.2010EP
10015434.308.12.2010EP
10015436.808.12.2010EP
11001442.022.02.2011EP
11004819.614.06.2011EP
61/496,65514.06.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DIKETOPIPERAZINE FORMING DIPEPTIDYL LINKER
(FR) DICÉTOPIPÉRAZINE FORMANT UN PONT DIPEPTIDYLE
Abstract
(EN)
The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C- PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.
(FR)
La présente invention concerne un procédé de synthèse de peptide en phase solution homogène (HSPPS, Homogeneous Solution Phase Peptide Synthesis) d'un fragment peptidique N-terminal PEP-N et d'un fragment peptidique C-terminal C-PEP, C-PEP portant une dicétopipérazine (DKP) spécifique comprenant un groupement protecteur C-terminal, qui contient un groupement préhensile HG (Handle Group), HG étant connecté à l'extrémité C du fragment peptidique ; ainsi, cette DKP spécifique comprenant un groupement protecteur C-terminal peut être clivée sélectivement d'avec le peptide comme un groupement protecteur C-terminal classique. L'emploi de cette DKP et de HG comportant le groupement protecteur C-terminal permet d'éviter certaines étapes de la synthèse peptidique convergente basée sur une combinaison de HSPPS et de synthèse peptidique en phase solide (SPPS). La présente invention concerne en outre une méthode de synthèse d'un tel fragment spécifiquement protégé C-PEP par SPPS en utilisant un pont comprenant un dipeptide spécifique et HG pour la connexion de la chaîne peptidique en croissance à la résine, ledit pont formant ledit groupement DKP, lorsque le fragment peptidique C-PEP est clivé d'avec la résine de support ; ainsi que les intermédiaires de ladite méthode de synthèse.
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