Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.

Abstract: Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.

Abstract: A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH2) or an amino-protecting group; aa1 is an amino acid residue having a side chain selected from formula (A) and (B)—(CO)a—(CH2)b-Dc-(CH2)d-E (A), —(CO)a—(CH2)b-Dc-Ce(E1)(E2)(E3) wherein E1, E2 and E3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E1, E2 and E3 is hydrogen and the other two are a said hydrocarbyl ring, E, E1, E2 and E3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R9 is a straight chain alkyl group interrupted by one or more ether linkages or R9 is —(CH2)mW and W is —OH or halogen.

Abstract: Salts of a pharmaceutically acceptable divalent metal and an organoboronic acid drug. Examples of such metals are calcium, magnesium and zinc. The organoboronic acid drug may be a boropeptide protease inhibitor. The salts may be formulated in oral dosage form.

Abstract: Salts of a pharmaceutically acceptable divalent metal and an organoboronic acid drug. Examples of such metals are calcium, magnesium and zinc. The organoboronic acid drug may be a boropeptide protease inhibitor. The salts may be formulated in oral dosage form.

Abstract: Salts of a peptide boronic acid drug, for example of Cbz—(R)—Phe—(S)—Pro—(R)—Mpg—B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.

Abstract: Dendroaspin, a polypeptide neurotoxin analogue is modified by recombinant DNA techniques, particularly “loop grafting” to provide a modified polypeptide. The modified polypeptide is constructed so as to retain dendroaspin activity, for example, platelet adhesion to fibrinogen, in addition to possessing one or more further biological or biochemical activities not native to dendroaspin, for example, platelet derived growth factor (PDGF) activity or hirudin activity.

Abstract: Novel peptide analogues of platelet-derived growth factor, for use in inhibiting or stimulating growth and/or chemotaxis of cells, for example, smooth muscle cells, are provided. Also provided are compositions of matter comprising those peptide analogues.

Abstract: Pharmaceutical compositions comprising compounds of the formula: in which X=H or is an N-protecting group; Y is 1-10 á-amino acids; Q1 and Q2 taken together represent the residue of a diol; R is C1-4alkyl; and the asymmetric carbon atom marked * may have the D- or L-configuration, are useful in therapeutic methods of inhibiting thrombin.

Abstract: This invention is directed to peptide inhibitors of serine proteases, espcecially thrombin, in which the P1-P2 natural amide linkage is replaced by another bond. Exemplary thrombin inhibitors have the formula: X-(aa.sup.3)-(aa.sup.2)-.psi.-(aa.sup.1)-Z wherein X is H or a substituent on the N-terminal amino group, aa.sup.3 is a hydrophobic amino acid, aa.sup.23 is Pro, aa.sup.1 is Arg or an Arg analgoue, Z is --COOH or a heteroatom acid group and .psi. is a non-amide linkage.

Abstract: Pharmaceutical compositions comprising compounds of the formula: ##STR1## in which X.dbd.H or is an N-protecting group; Y is 1-10 .alpha.-amino acids; Q1 and Q2 taken together represent the residue of a diol; R is C.sub.1-4, alkyl; and the asymmetric carbon atom marked * may have the D- or L-configuration, are useful in therapeutic methods of inhibiting thrombin.

Abstract: This invention relates to cyclic platelet-derived growth factor (PDGF) analogues and pharmaceutical compositions thereof.

Abstract: Novel peptide analogues of platelet-derived growth factor, for use in inhibiting or stimulating growth and/or chemotaxis of cells, e.g., smooth muscle cells, are provided. Also provided are compositions of matter comprising those peptide analogues.

Abstract: This invention provides peptides of the formula ##STR1## wherein X is H, CH.sub.3 or an N-protecting group;Y is(1) C.sub.3 -C.sub.9 alkyl optionally substituted by C.sub.1 -C.sub.4 alkoxy,(2) C.sub.5 -C.sub.10 aryl optionally substituted by C.sub.1 -C.sub.4 alkoxy,(3) C.sub.5 -C.sub.10 alkylaryl optionally substituted by C.sub.1 -C.sub.4 alkoxy,(4) (CH.sub.2).sub.n --Q or ##STR2## wherein Q is H, amino, amidino, imidizole, guanidino or isothioureido and n is 1-5;Z is COR.sub.1, ##STR3## wherein: R.sub.1 is H, OH, CH.sub.2 Cl, CH.sub.2 --CH.sub.2 --CO-pip, CF.sub.2 --CF.sub.2 --CO-pip, CH.sub.2 --CH(CH.sub.3)--CO-pip, CF.sub.2 --CF(CF.sub.3)--CO-pip, CH.sub.2 --CH.sub.2 --CO-Pro-NHEt, CF.sub.2 --CF.sub.2 --CO-Pro-NHEt or a chromophoric group,R.sub.2 and R.sub.3 may be the same or different and are selected from the group consisting of OH, OR.sub.6 and NR.sub.6 R.sub.7, wherein R.sub.6 and R.sub.7 may be the same or different and are selected from the group consisting of C.sub.1-10 alkyl, phenyl or C.sub.6 -C.

Abstract: Pharmaceutical compositions comprising compounds of the formula: ##STR1## in which X.dbd.H or is an N-protecting group; Y is 1-10 .alpha.-amino acids; Q1 and Q2 taken together represent the residue or a diol; R is C.sub.1-4 alkyl; and the asymmetric carbon atom marked * may have the D- or L-configuration, are useful in therapeutic methods of inhibiting thrombin.