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1. (WO1998049189) (3R)-3-AMINO-4-CARBOXYBUTYRALDEHYDE DERIVATIVES INHIBITING THE RELEASE OF INTERLEUKIN-1/BETA
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/049189 International Application No.: PCT/HU1998/000040
Publication Date: 05.11.1998 International Filing Date: 22.04.1998
Chapter 2 Demand Filed: 13.11.1998
IPC:
A61K 38/00 (2006.01) ,C07K 5/02 (2006.01) ,C07K 7/02 (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
02
containing at least one abnormal peptide link
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
7
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
02
Linear peptides containing at least one abnormal peptide link
Applicants:
GYÓGYSZERKUTATÓ INTÉZET KFT. [HU/HU]; Berlini utca 47-49 H-1045 Budapest, HU (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)
BAJUSZ, Sándor [HU/HU]; HU (UsOnly)
VÉGHELYI, Irén [HU/HU]; HU (UsOnly)
NÉMETH, Klára [HU/HU]; HU (UsOnly)
BARABÁS, Éva [HU/HU]; HU (UsOnly)
JUHÁSZ, Attila [HU/HU]; HU (UsOnly)
LANGÓ, József [HU/HU]; HU (UsOnly)
LAVICH, Emília [HU/HU]; HU (UsOnly)
MOHAI, Zsuzsanna [HU/HU]; HU (UsOnly)
MORAVCSIK, Imre [HU/HU]; HU (UsOnly)
TASCHLER, Zsuzsanna [HU/HU]; HU (UsOnly)
TÓTH, Gábor [HU/HU]; HU (UsOnly)
PATTHY, Miklós [HU/HU]; HU (UsOnly)
SALÁT, János [HU/HU]; HU (UsOnly)
SZEKER, Ágnes [HU/HU]; HU (UsOnly)
MAKK, Klára [HU/HU]; HU (UsOnly)
Inventors:
BAJUSZ, Sándor; HU
VÉGHELYI, Irén; HU
NÉMETH, Klára; HU
BARABÁS, Éva; HU
JUHÁSZ, Attila; HU
LANGÓ, József; HU
LAVICH, Emília; HU
MOHAI, Zsuzsanna; HU
MORAVCSIK, Imre; HU
TASCHLER, Zsuzsanna; HU
TÓTH, Gábor; HU
PATTHY, Miklós; HU
SALÁT, János; HU
SZEKER, Ágnes; HU
MAKK, Klára; HU
Agent:
DANUBIA; Bajcsy-Zsilinszky út 16 H-1051 Budapest, HU
Priority Data:
P 97 0081628.04.1997HU
Title (EN) (3R)-3-AMINO-4-CARBOXYBUTYRALDEHYDE DERIVATIVES INHIBITING THE RELEASE OF INTERLEUKIN-1/BETA
(FR) DERIVES DE (3R)-3-AMINO-4-CARBOXYBUTYRALDEHYDE INHIBANT LA LIBERATION D'INTERLEUKINE-1/BETA
Abstract:
(EN) The invention relates to new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula (I), wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n = 1, a tetrapeptide of general formula Y 4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n = 0, an $g(a)-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an $g(a)-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an $g(a)-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q2-Q4 represent an acyl group selected form the following $g(a)-hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1$g(b) converting enzyme.
(FR) L'invention concerne de nouveaux dérivés de (3R)-3-amino-4-carboxybutyraldehyde de formule générale (I), dans laquelle X représente un groupe alkyle oxycarbonyle C1-4, un groupe phényl-(alkyloxy C1-2)-carbonyle éventuellement substitué, un groupe alkylcarbonyle C1-4 ou bien un groupe phényl-(alkyl C1-3)-carbonyle éventuellement substitué, n vaut 1 ou 0, Y représente, dans le cas où n = 1, un tétrapeptide de formule générale Y4-Y3-Y2-Y1, un tripeptide de formule générale Y3-Y2-Y1 ou bien un dipeptide de formule générale Y 2-Y1 ou encore un résidu aminoacide de formule générale Y1, ou bien dans le cas où n = 0, un tripeptide d'$g(a)-hydroxyacyle de formule générale Q4-Y3-Y2-Y1, un dipeptide d'$g(a)-hydroxyacyle de formule générale Q3-Y2-Y1 ou bien un résidu $g(a)-hydroxyacyl-aminoacyle de formule générale Q2-Y1, où Y1-Y4 représentent un résidu choisi dans le groupe des acides aminés L ou D suivants: alanine, alloisoleucine, cyclohexyl-glycine, phényl-alanine, glutamine, histidine, isoleucine, leucine, lysine, méthionine, acide pipécolique, proline, tyrosine et valine, et Q2-Q4 représentent un groupe acyle choisi parmi les $g(a)-hydroxyacides de configuration R ou S suivants: acide 2-cycloheptyl-2-hydroxyacétique, acide 2-cyclohexyl-2-hydroxyacétique, acide 3-cyclohexyllactique, acide 3-phényllactique, acide 2-hydroxy-3-méthylbutyrique, acide 2-hydroxy-3-méthylvalérique, acide mandélique ou acide lactique, ainsi que leurs sels formés avec des bases organiques ou inorganiques, et des compositions pharmaceutiques les contenant. Les composés de formule générale (I) sont de précieux inhibiteurs de l'enzyme de conversion de l'interleukine-1$g(b).
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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:
ES2259812EP0979241US6593300CA2288332DE000069833646PT979241
AU1998072261DK0979241