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1. (WO1991007429) ANTI-AGGREGATORY PEPTIDES CONTAINING A MERCAPTAN OR SULFIDE MOIETY
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/007429 International Application No.: PCT/US1990/006514
Publication Date: 30.05.1991 International Filing Date: 02.11.1990
Chapter 2 Demand Filed: 07.06.1991
IPC:
A61K 38/00 (2006.01) ,C07K 7/06 (2006.01) ,C07K 14/78 (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
7
Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
04
Linear peptides containing only normal peptide links
06
having 5 to 11 amino acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
78
Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin (CIG)
Applicants:
SMITHKLINE BEECHAM CORPORATION [--/US]; One Franklin Plaza - P.O. Box 7929 Philadelphia, PA 19101, US (AllExceptUS)
ALI, Fadia, El-Fehail [US/US]; US (UsOnly)
SAMANEN, James [US/US]; US (UsOnly)
Inventors:
ALI, Fadia, El-Fehail; US
SAMANEN, James; US
Agent:
KINZIG, Charles, M. ; SmithKline Beecham Corp. Corporate Patents - U.S. One Franklin Plaza P.O. Box 7929 Philadelphia, PA 19101, US
Priority Data:
433,93309.11.1989US
Title (EN) ANTI-AGGREGATORY PEPTIDES CONTAINING A MERCAPTAN OR SULFIDE MOIETY
(FR) PEPTIDES ANTI-AGREGATION RENFERMANT UNE MOITIE DE MERCAPTAN OU DE SULFURE
Abstract:
(EN) This invention relates to compounds of the formula: X-(V-A-B-Gly-Asp-Q)n-(V'-A'-B'-Gly-Asp, Q')-P, wherein: V and V' are absent, Asn, Gln, Ala or Abu; A and A' are absent or a D- or L- amino acid chosen from Arg, HArg, NArg, (Me2)Arg, (Et2)Arg, Abu, Ala, Gly, His, Lys, or an $g(a)-R' substituted derivative thereof, Dtc, Tpr or Pro; B and B' are Arg, HArg, NArg, (Me2)Arg, (Et2)Arg, Orn, Lys, HLys or an $g(a)-R' substituted derivative thereof; Q and Q' are a D- or L- amino acid chosen from Tyr, (Alk)Tyr, Phe, (4'W)Phe, HPhe, Phg, Trp, His, Ser, (Alk)Ser, Thr, (Alk)Thr, Cys, (Alk)Cys, Pen, (Alk)Pen, Pcs, Ala, Val, Nva, Met, Leu, Ile, Nle or Nal; R' is Alk or PhCH2; (a), (b), (c) or (d); W is halogen or Alk; X is R4R5N or H; Y is H, CONR1R2 or CO2R2; R1 and R2 are H, Alk or (CH2)pAr; R4 is H or Alk; R5 is R11, R11CO, R11OCO, R11OCH(R11')CO, R11NHCH(R11')CO, R11SCH(R11')CO, R11SO2 or R11SO; R7 is H, Alk, OAlk, halogen or Y; R8 and R8' are H, Alk, (CH2)pPh, (CH2)pNph or taken together are -(CH2)4- or -(CH2)5-; R11 and R11' are H, C1-5alkyl, C3-7cycloalkyl, Ar, Ar-C1-5alkyl, Ar-C3-7cycloalkyl; Ar is phenyl or phenyl substituted by one or two C1-5alkyl, trifluoromethyl, hydroxy, C1-5alkoxy or halogen groups; n is 0 or 1; p is 0, 1, 2, or 3; and q is 1 or 2; or a pharmaceutically acceptable salt thereof; which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, a method for inhibiting platelet aggregation and clot formation in a mammal, and a method for inhibiting reocclusion of a blood vessel following fibrinolytic therapy.
(FR) Cette invention se rapporte à des composés de formule: X-(V-A-B-Gly-Asp-Q)n-(V'-A'-B'-Gly-Asp-Q')-p dans laquelle: V et V' sont absents, Asn, Gln, Ala ou Abu; A et A' sont absents ou un acide aminé D- ou L- choisi parmi Arg, HArg, NArg, (Me2)Arg, (Et2)Arg, Abu, Ala, Gly, His, Lys, ou un dérivé a-R' substitué de ceux-ci, Dtc, Tpr ou Pro; B et B' sont Arg, HArg, NArg, (Me2)Arg, (Et2)Arg, Orn, Lys, HLys, ou un dérivé $g(a)-R' substitué de ceux-ci; Q et Q' sont un acide aminé D- ou L- choisi parmi Tyr, (Alk)Tyr, Phe, (4'W)Phe, HPhe, Phg, Trp, His, Ser, (Alk)Ser, Thr, (Alk)Thr, Cys, (Alk)Cys, Pen, (Alk)Pen, Pcs, Ala, Val, Nva, MEt, Leu, Ile, Nle ou Nal; R' est Alk ou PhCH2; P est (I, II, III) ou (IV) W est halogène ou Alk; X est R4R5N ou H; Y est H, CONR1R2 ou CO2R2; R1 et R2 sont H, Alk ou (CH2)pAr; R4 est H ou Alk; R5 est R11, R11CO, R11OCO, R11OCH(R'11)CO, R11NHCH(R11')CO, R11SCH(R11')CO, R11SO2 ou R11SO; R7 est H, Alk, OAlk, halogène ou Y; R8 et R8' sont H, Alk, (CH2)pPH, (CH2)pNph ou pris ensemble sont -(CH2)4- ou -(CH2)5-; R11 et R11' sont H, C1-5alcoyle, C3-7cycloalcoyle, Ar, Ar-C1-5alcoyle, Ar-C3-7cycloalcoyle; Ar est phényle ou phényle substitué par un ou deux C1-5 alcoyle, trifluorométhyle, hydroxy, C1-5 alcoxy ou groupes d'halogène; n est 0 ou 1; p est 0, 1, 2 ou 3; et q est 1 ou 2; ou un sel pharmaceutiquement acceptable de ceux-ci; qui sont utilisables pour inhiber l'agrégation des plaquettes, des composés pharmaceutiques permettant d'effectuer une telle activité, une méthode d'inhibition de l'agrégation des plaquettes et la formation de caillots chez le mammifère, et une méthode d'inhibition de la réocclusion d'un vaisseau sanguin suite à une thérapie fibrinolytique.
Designated States: JP, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0505385