Other

Asta Medica, Aktiengesellschaft

Medical Research Council Technology

Ardana Bioscience Limited

Romano Deghenghi

Francois Boutignon

Antonio Argiolas

A fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. Also, lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Sustained release of microcrystalline peptide suspensions

The invention relates to a method of preventing gel formation of a hydrophobic peptides by contacting the hydrophobic peptide with a counter-ion in an amount and at a molar ratio with the peptide that are sufficient to provide a fluid, milky microcrystalline aqueous suspension of the peptide without formation of a gel. The invention also relates to a fluid, milky microcrystalline aqueous suspension of a hydrophobic peptide and a counter-ion in water, wherein the peptide and counter-ion are present in amounts and at a molar ratio sufficient to form, upon mixing, the suspension without formation of a gel.

The present invention relates to novel growth hormone releasing pseudopeptides capable of stimulating the release of growth hormone from the pituitary and of promoting growth in mammals. The invention also provides pharmaceutical compositions comprising the pseudopeptides growth hormone secretagogues and a method for promoting the release of growth hormone in mammals. If continuously administered, the present pseudopeptides may also inhibit the release of growth hormone by down-regulating the growth response. An exemplary pseudopeptide compound of this invention is Aib-D-Trp-D-Trp&#x3c8;[CH&#x2014;NH&#x2014;O]Gly-NH:

Pseudopeptides growth hormone secretagogues

The present invention relates to small peptides that cause penile erections in male animals when injected into the paraventricular nucleus of the hypothalamus or when given systemically (intravenously or subcutaneously) to such animals. These peptides are useful in the treatment of erectile dysfunction.

Peptides for treatment of erectile dysfunction

A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.; aseptically extruding the dried mixture at a temperature between about 70 and 110.degree. C.; and aseptically cutting a cylindrical rod from the extruded mixture to form the pharmaceutical implant.

Implants containing bioactive peptides

Process to manufacture implants containing bioactive peptides

The present invention relates a number of novel peptide sequences which include a spirolactam, bicyclic or tricyclic peptidomimetic unit. The peptides disclosed herein exhibit binding to cardiac tissue and normalize cardiac pressure after administration, as well as diagnostic and therapeutic properties for certain neoplastic tissues. Importantly, these peptides do not release pituitary hormones such as corticotropin (ACTH) and growth hormone (GH), and are therefore devoid of certain unwanted side-effects. These peptides preferably have at least one lysine unit and at least one D-2-alkyl-trptophan unit.

Diazaspiro, azepino and azabicyclo therapeutic peptides

Somatostatin-analogous cyclic peptides with inhibitory activity on

Peptides containing in its amino acid chain a D-2-alkylTryptophan residue wherein the alkyl group has between one and three carbon atoms and having pharmacological activity equal to or greater than that of analogous peptides containing natural unsubstituted D-Tryptophan residues in place of the D-2-alkylTryptophan. These peptides are more resistant to oxidative degradation which usually takes place, for example, in the presence of reactive radicals or during high energy sterilization than unsubstituted Tryptophan containing peptides.

Peptides containing D-2-alkyl-Tryptophan

A process for manufacturing a pharmaceutical composition for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This process includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.; aseptically extruding the dried mixture at a temperature between about 70 and 110.degree. C.; and aseptically cutting cylindrical rods of about 1 to 2 mm diameter and between about 10 and 25 mm in length from the extruded mixture to form the pharmaceutical implants.

The present invention relates a number of different lysine containing peptides which can be administered to a mammal to normalize cardiac pressure for treatment of heart disease conditions such as myocardial ischemia. These peptides include certain known peptides, some of which are capable of liberating growth hormone to various degrees when administered to a mammal. Other peptides useful in the invention are novel peptide sequences which include a spirolactam, bicyclic or tricyclic peptidomimetic unit. The peptides disclosed herein exhibit binding to cardiac tissue and normalize cardiac pressure after administration, thus imparting cardiac protecting activity by a mechanism which at the present is unknown. One common feature of the peptides of this invention is that at least one lysine unit is present.

Lysine containing peptides for treatment of heart disease

Peptides containing D-2-Alkyl-Tryptophan

Oligopeptide compounds containing D-2-alkyltryptophan capable of

Novel peptides comprising D-2-alkyltryptophan, useful for promoting growth hormone release, compositions comprising such peptides and methods of using such compositions are described. In a preferred embodiment of the invention, the D-2-alkyl tryptophan is D-2-methyltryptophan.

Growing community of inventors

St. Cergue, Switzerland

Romano Deghenghi