Abstract: The present invention relates to new malonic acid derivatives of the formula 1, 1

Abstract: The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.

Abstract: The useful cyclic peptides cyclo[Thr-Lys-Pro-Arg-Gly] and cyclo[Thr-Lys-Pro-Arg-Asp] are disclosed.

Abstract: The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X.sub.1 -YIR-X.sub.2, wherein X.sub.1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X.sub.2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are tyrosine, isoleucine and arginine, respectively, or peptidomimetic or organic structures that possess the same functional activity as Y, I and R, respectively. In addition, the present invention provides a compound having the structure A1-A2-(A3).sub.m --B, where m is 0 or 1. A compound of the invention can be linear or cyclic and can be about 2 and 43 residues in length. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a K.sub.i of .ltoreq.100 .mu.M, preferably .ltoreq.

Abstract: Linear and Cyclic Alpha-MSH fragment analogues of Ac-Nle.sup.4 -Glu.sup.5 -His.sup.6 -D-Phe.sup.7 -Arg.sup.8 -Try.sup.9 -Gly.sup.10 -NH.sub.2. The method of stimulating melanocytes by the transdermal application of these biologically-active analogues and compositions comprising these analogues for use in the method are disclosed.

Abstract: Cyclic Alpha-MSH fragment analogues of Ac-Nle.sup.4 -Glu.sup.5 -His.sup.6 -D-Phe.sup.7 -Arg.sup.8 -Try.sup.9 -Gly.sup.10 -NH.sub.2. The method of stimulating melanocytes by the transdermal application of these biologically-active analogues and compositions comprising these analogues for use in the method are disclosed.