Abstract: The present invention provides a process for the preparation of a compound of formula I in which a compound of formula II in which R is H or OR represents a protecting group for a carboxylic hydroxy group is reacted with a compound of formula III C6H13X ??III wherein X is a leaving group, in the presence of a base in the presence of an inert solvent at a temperature in the range ?25° C. to 150° C. and optionally, when OR represents a protecting group, removal of the protecting group.

Abstract: A compound selected from one or more of the following: a (1R,2S)-2-hydroxyindan-1-amine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an L-arginine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a tert-butylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino-2-oxoethoxyphenyl)propanoic acid; a choline salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; an adamantylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N-benzyl-2-phenylethanaminium salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; a N-benzyl-2-(benzylamino) ethanaminium salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid; or a tris(hydroxymethyl)methylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl(2-phenylethyl)amino]-2-oxoethoxy}phenyl)propanoic acid.

Abstract: The present invention provides the S enantiomer of a compound of formula I wherein R1 represents chloro, trifluoromethyl or trifluoromethoxy, R2 represents H or fluoro and R3 represents a C2-4alkyl group as well as pharmaceutically acceptable salts, solvates and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to a linear block polymer having a molecular weight of at least 104 Dalton, which linear block polymer is comprised of internally linearly connected sequences, which sequences may be described according to formula (1), wherein 1 to 100% of R1, which 1 to 100 % of R1 may be the same or different, comprise a functional group Z and each Z, which Z may be the same or different is a protected or unprotected functional group such as hydroxyl, amino, carboxyl, thiol, cyano, or nitro group; and, each R2, which R2 may be same or different, may be derived from a diisocyanate and comprises no, one or more ester groups; each R3, which R3 may be same or different, comprises no, one or more ester groups and may be derived from one or more of polyesterdiol, polyetherdiol or monodiol; method for preparation and fractional precipitation, implants, material for promotion of wound healing, pharmaceutical compositions, microencapsules, suspensions and emulsions.

Abstract: Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal .beta.-aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the .beta.-aminoalcohol Z is --NR--CH(Q)--CH.sub.2 OH, Q is (CH.sub.2).sub.n --NH--A is H or --C(.dbd.NH)NH.sub.2, and R is CH.sub.3 or C.sub.2 H.sub.5, and the moiety S wherein H is a D-aromatic .alpha.-aminoacid and Y is an aliphatic .alpha.-aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.

Abstract: The present invention relates to new vasotocin derivatives with prolonged activity compared to previous vasotocin derivatives. In particular, the vasotocin derivatives of the present invention are of the formula (I) ##STR1## wherein Hmp is a 2-hydroxy-3-mercaptopropionic acid residue, ##STR2## Z is Phe or Tyr, Y is Hgn or Hci, X is a residue of the formula ##STR3## wherein Q is H, alanyl or L-2-aminobutyryl and n is 1, 2 or 3. The present invention also relates to pharmaceutical compositions containing these vasotocin derivatives.