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1. (EP1219603) Tryptophan analogs in proteins, peptides and peptidic structures

Application Number: 01130523 Application Date: 21.12.2001
Publication Number: 1219603 Publication Date: 03.07.2002
Publication Kind : A3
IPC:
C 07D
C07D 495/04
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
20
substituted additionally by nitrogen atoms, e.g. tryptophane
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
CPC:
C07D 495/04
Applicants: MAX PLANCK GESELLSCHAFT
PROTEROS BIOSTRUCTURES GBMH
Inventors: HUBER ROBERT PROF DR
BUDISA NEDILJKO DR
MORODER LUIS PROF
ALEFELDER STEFAN DR
BAE JAE HYUN
KAISER JENS DR
FREYE-MINKS CAROLINE DR
NEUEFEIND TORSTEN DR
Priority Data: 10063992 21.12.2000 DE
Title: (DE) Tryptophan-Analoga in Proteinen, Peptiden und peptidischen Leitstrukturen
(EN) Tryptophan analogs in proteins, peptides and peptidic structures
(FR) Analogues du tryptophane dans des protéines, des peptides et des structures peptidiques
Abstract: front page image
(DE) Die Erfindung betrifft Proteine, Peptide und peptidische Leitstrukturen, die aufgrund des Einbaus von Tryptophan-Aminosäureanaloga, insbesondere von Chalkogen- und/oder Halogen-Analoga, neue kristallographische, spektrale und/oder pharmakologische Eigenschaften aufweisen. Ferner betrifft die Erfindung ein Verfahren zur Markierung von Proteinen, Peptiden und peptidischen Leitstrukturen, bei dem diese durch den Einbau von Aminosäure-Analoga mit neuen kristallographischen und/oder spektralen Eigenschaften versehen werden. Des Weiteren betrifft die Erfindung ein Verfahren zur Bestimmung der dreidimensionalen Struktur von Proteinen, Peptiden oder peptidischen Leitstrukturen mittels Kristallstrukturanalyse. Schließlich betrifft die Erfindung pharmazeutische Zusammensetzungen, die als Wirkstoff mindestens ein Tryptophan-Analogon umfassen, das in einen Träger, beispielsweise ein Protein, ein Peptid oder eine peptidische Leitstruktur, eingebaut ist.
(EN) Protein, peptide or peptidic lead structures (A) that include at least one chalcogen (sulfur, selenium or tellurium)-containing amino acid analog (I) of tryptophan (Trp) and/or at least one halogen (bromo or iodo)-containing amino acid analog (Ia) of Trp. Peptides that contain bromine-containing (Ia) are excluded. Independent claims are also included for: (1) a method for labeling a protein, peptide or peptidic lead structure (B) for crystallographic and/or spectroscopic examination by incorporating at least one (I) and/or (Ia); (2) method for determining the three-dimensional structure of (B) by crystal structure analysis after replacing a Trp residue by (I) or (Ia); and (3) pharmaceutical composition containing at least one (A) that contains (I).