Abstract: The invention features somatostatin antagonists having a D-amino acid at the second residue.

Abstract: Delivery systems based on liposomes functionalized with peptides and chelating agents, for therapy and imaging by selective targeting of tumour cells expressing the receptors GRP, BB1, BB2, BB3 e BB4 and any other receptor which recognizes the bombesin peptide or analogues thereof are described. In particular, the liposomes contain within them cytotoxic drugs, such as for example doxorubicin, for target-selective antitumour therapy, and, through the presence of the chelating agent, can contain radioactive or paramagnetic ions for the real time visualization of the tumour cells. The liposomes described in this invention thus act as a selective delivery system for drugs and/or contrast agents onto tumour cells expressing the receptors for the class of known peptides such as bombesin (endogenous sequence, analogous or peptidomimetic peptides, agonists or non agonists).

Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.

Abstract: The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.

Abstract: We describe preparation of compounds of an AT1 receptor antagonist(s) and Angiotensin (1-7), for example, Angiotensin-(1-7) losartanate and analogues thereof, and/or mixtures of these systems, pharmaceutical compositions thereof and use of their derivative products. Cyclodextrins and derivatives thereof may be used for the micro-encapsulation of compounds, for example, Angiotensin (1-7) losartanate, liposomes and biodegradable polymers and/or mixtures of these systems and/or derivative products for the obtainment of nano- or microparticles as controlled or sustained release devices of Ang-(1-7) losartanate and analogues and/or mixtures thereof. The compounds may be used as agents for treating or preventing hypertension, cardiovascular diseases, heart hypertrophy, heart failure, coronary diseases, such as angina pectoris, endothelial disorder or endothelial lesions, as a consequence, for example, of atherosclerosis processes or in association with diabetes mellitus.

Abstract: The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, including 1,2 diaza heterocyclic compounds, having a photolabile N—N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N—N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.

Abstract: The invention relates generally to optical agents for biomedical applications, including phototherapy. Provided are disulfide compounds having an acyclic S—S bond with at least one aromatic and/or heterocyclic aromatic group providing phototherapeutic agents, including Type 1 phototherapeutic agents. Optical agents of the invention enable a versatile phototherapy platform for treatment of a range of pathological conditions, including the treatment of cancers, stensosis and inflammation. The invention further provides preparations and formulations comprising the disulfide optical agents and related methods of making and using disulfide optical agents in an in vivo or ex vivo biomedical procedure.