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1. (WO1998049197) OLIGOPEPTIDIC INHIBITORS OF ELASTASES AND METHODS OF PREPARATION THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/049197 International Application No.: PCT/CZ1998/000019
Publication Date: 05.11.1998 International Filing Date: 27.04.1998
Chapter 2 Demand Filed: 23.10.1998
IPC:
A61K 38/00 (2006.01) ,C07K 5/11 (2006.01) ,C07K 14/81 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
10
Tetrapeptides
11
the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
81
Protease inhibitors
Applicants:
VÚFB, A.S. [CZ/CZ]; Kour^¿imská 17 130 60 Praha 3, CZ (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
KASAFÍREK, Evzen [CZ/CZ]; CZ (UsOnly)
PIHERA, Pavel [CZ/CZ]; CZ (UsOnly)
S^¿TURC, Antonín [CZ/CZ]; CZ (UsOnly)
S^¿EDO, Aleksi [CZ/CZ]; CZ (UsOnly)
Inventors:
KASAFÍREK, Evzen; CZ
PIHERA, Pavel; CZ
S^¿TURC, Antonín; CZ
S^¿EDO, Aleksi; CZ
Agent:
GUTTMANN, Michal; Rott, Ruzic^¿ka & Guttmann P.O. Box 71 142 00 Praha 4, CZ
Priority Data:
PV 1315-9730.04.1997CZ
Title (EN) OLIGOPEPTIDIC INHIBITORS OF ELASTASES AND METHODS OF PREPARATION THEREOF
(FR) INHIBITEURS OLIGOPEPTIDIQUES D'ELASTASES ET PROCEDES DE PREPARATION DE CES INHIBITEURS
Abstract:
(EN) The invention relates to oligopeptidic inhibitors of elastases, with potent inhibition of leukocyte elastase. The inhibitors are isobutylamides of tetra- to pentapeptides which have substituted lysine incorporated in the N-terminal portion of the molecule. This dibasic aminoacid is alternatively substituted at both $g(a)- and $g(e)-aminogroups with higher saturated acids or with $g(v)-carboxylalkanoylic residues. In one type of these compounds the $g(e)-aminogroup is acylated with an acyl-alanine, where an acyl means a higher saturated acid. The compounds of this invention are the active components of medicinal preparations used mainly in dental practice.
(FR) Cette invention concerne des inhibiteurs oligopeptidiques d'élastases qui possèdent une grande puissance d'inhibition d'élastases de leucocyte. Ces inhibiteurs consistent en des isobutylamides de tetrapeptides ou de pentapeptides qui possèdent une lysine substituée incorporée dans la partie de la terminaison N de la molécule. Dans une autre variante, cet acide aminé dibasique peut être substitué aux deux groupes $g(a)-amino et $g(e)-amino par des acides saturés supérieurs ou par des résidus $g(v)-carboxyalcanoyles. Dans un type de ces composés, le groupe $g(e)-amino est acylé à l'aide d'une acyl-alanine, étant entendu qu'un acyle représente un acide saturé supérieur. Les composés décrits dans cette invention sont utilisés comme composants actifs dans des préparations médicales principalement à usage dentaire.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0979245JP2002511848 AU1998068197