Abstract: The present invention relates to 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives having pharmacological activity formula (I) to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of a cognitive disorder.

Abstract: The present invention relates to 1-[1-(benzoyl )-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives having pharmacological activity formula (I) to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of a cognitive disorder.

Abstract: The present invention relates to 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives having pharmacological activity to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of a cognitive disorder.

Abstract: The peptides of formula (I) where: R1 is the group attached to the N-terminal of the first amino acid of the sequence P, optionally via the ligand X, and is selected from H, CH3C(?O)—, and maleimide; X is a biradical selected from —NH—(CH2)r—C(?O)—, —C(?O)—(CH2)r—C(?O)—, —S(CH2)r—, —S—(CH2)r—C(?O)—, —O—(CH2)r—, —S—CH—CH(NH2)—C(?O)—, —O—(CH2)r—C(?O)—, —(CH2)r—C(?O)—, —NH—O—CH2—C(?O)—NH—(CH2)r—CH(NH2)—C(?O)—, —(CH2)r—C(?O)—NH—(CH2)r—CH(NH2)—C(?O)—, and —NH—(CH2)r—CH(NHC(?O)CH2NH2)—C(?O)—; r is 1-5; P is a biradical of an amino acid sequence comprising the sequence D-Pro-D-Trp-D-Val-D-Pro-D-Ser-D-Trp-D-Met-D-Pro-D-Pro-D-Arg-D-His-D-Thr (SEQ ID NO: 1); Y is the group attached to the C-terminal of the last amino acid of the sequence P, and is selected from —NH2, —OH, —OR2 and —NHR2; R2 is a radical selected from (C1-C6)-alkyl and (CH2)2—NH—C(?O)—CH2—O—NH2; k is 0-2; m is 0-1; with the proviso that when the biradical X is —C(?O)(CH2)r—C(?O)—, then R1 is H; when the N of the amino acid of the sequence P to which is

Abstract: The present invention relates to 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives having pharmacological activity to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of a cognitive disorder.

Abstract: The peptides of formula (I) R1—(X)K—P—Y, where: R1 is the group attached to the N-terminal of the first amino acid of the sequence P, optionally via the ligand X, and is selected from H, CH3C(?O)—, and maleimide; X is a biradical selected from —NH—(CH2)r—C(?O)—, —C(?O)—(CH2)r—C(?O)—, —S(CH2)r—, —S—(CH2)r—C(?O)—, —O—(CH2)r—, —S—CH2—CH(NH2)—C(?O)—, —O—(CH2)r—C(?O)—, —(CH2)r—C(?O)—, —NH—O—CH2—C(?O)—NH—(CH2)r—CH(NH2)—C(?O)—, —(CH2)r—C(?O)—NH—(CH2)r—CH(NH2)—C(?O)—, and —NH—(CH2)r—CH(NHC(?O)CH2NH2)—C(?O)—; r is 1-5; P is a biradical of an amino acid sequence comprising the sequence D-Pro-D-Trp-D-Val-D-Pro-D-Ser-D-Trp-D-Met-D-Pro-D-Pro-D-Arg-D-His-D-Thr (SEQ ID NO: 1); Y is the group attached to the C-terminal of the last amino acid of the sequence P, and is selected from —NH2, —OH, —OR2 and —NHR2; R2 is a radical selected from (C1-C6)-alkyl and (CH2)2—NH—C(?O)—CH2—O—NH2; k is 0-2; m is 0-1; with the proviso that when the biradical X is —C(?O)(CH2)rC(?O)—, then R1 is H; when the N of the amino acid of the sequence P

Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.

Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.

Abstract: Trunkamide A and other cycloheptapeptides can be made by solid phase synthesis of a linear precursor.

Abstract: Compounds of formula (I) or their pharmaceutically or biologically acceptable salts are useful as cell penetrating carriers. According to formula (I), below, Val is L-Val or D-Val; Arg is L-Arg, D-Arg or L-(N-methyl)Arg; Pro is L-Pro or D-Pro; Leu is L-Leu or D-Leu; x is an integer from 1 to 20, preferably 3; L1 and L2 are chemical linkers; M1 and M2 are pharmacologically and/or biologically active moieties; and the bond between L1 and M1 and the bond between L2 and M2 are of the known chemical natures, including covalent and ionic. Compared with other previously described carrier peptides, this new family presents several advantages including its non-viral origin, its amphipathic character, its solubility in water and the absence of a cytotoxic effect at high concentrations.

Abstract: The present application relates to new peptide polymers comprising monomeric units derived from the residues of glutamic acid, aspartic acid and lysine, or their protected derivatives, and which are functionalized through the introduction of side chains containing thiol groups or protected thiol groups. The new peptide polymers can be crosslinked in aqueous medium, and the resulting polymer matrices have the capacity to entrap drugs and, subsequently, release them in a controlled way when introduced into a physiological medium. This enables new pharmaceutical compositions to be developed for the controlled release of drugs, especially peptide- and protein-based ones.