摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. Their formula is (I) where the meaning of the various symbols is provided in the description.
摘要:
Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.
摘要:
Analyse servant à dépister le venin de serpent pour la présence ou l'absence d'inhibiteurs de l'agrégation des plaquettes (PAIs) à base de liaison de récepteur spécifique. Grâce à cette analyse, l'identification et la caractérisation de PAIs dans un grand nombre d'échantillons de venin de serpent a été accompli. Le PAI isolé et purifié provenant de plusieurs de ces venins de serpent actifs est décrit et caractérisé. D'autre part, les PAI n'ayant pas la séquence d'adhésion Arg-Gly-Asp (RGD) mais contenant K*-(G/Sar)-D où K* est un résidu de lysyle modifié de la formule R12 N(CH2)4CHNHCO- où chaque R1 est indépendamment H, alkyle (1-6) ou tout au plus un R1 est R2-C=NR3 où R2 est H, alkyle (1-6C), phényle ou benzyle, ou est NR42 dans lequel chaque R4 est indépendamment H ou alkyle (1-6C) et R3 est H, alkyle (1-6C), phényle ou benzyle, ou R2-C=NR3 est un radical sélectionné parmi le groupe qui est constitué de (a), (b), (c) et (d) où m est un nombre entier de 2-3, et chaque R5 est indépendamment H ou alkyle (1-6C); et où un ou deux (CH2) peuvent être remplacés par O ou S à condition que lesdits O ou S ne soient pas contigus à un autre hétéroatome, sont préparés et leur action inhibitrice de la liaison du fibrinogène ou du Facteur von Willebrand au GP IIb-IIIa est démontrée.
摘要:
Novel compounds of general formula I, including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivative having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
摘要:
The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.
摘要:
Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an α2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.
摘要:
Defined constructs of modified human platelet-derived growth factor receptor polypeptides are provided. Extracellular region domain structures are identified and modifications and combinatorial rearrangements of the receptor segments are provided. Both cell bound and soluble forms of modified segments are made available, as are methods for assays using them, allowing for screening or ligand analogues.
摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders and have formula (I).