Abstract: The present invention relates to methods for prevention and treatment of bone-related or nutrition-related disorders using a GLP molecule or GLP activator either alone or in combination with another therapeutic. The present invention also encompasses methods of diagnosing or monitoring the progression of a disorder. The invention also encompasses methods of monitoring the effectiveness of treatment of the invention.

Abstract: The present invention relates to peptides of RPL41 and their use in the treatment of cancer and microbial infections. It is contemplated that modified forms of RPL41, including substitutional variants and mimetics, will be used. Mono- and combination therapies with other cancer treatments are contemplated.

Abstract: A stimuli-responsive, hybrid hydrogel wherein the bulk of the polymer is made up of relatively inexpensive water soluble polymer strands crosslinked by protein domains. The responsiveness of the gel is controlled or modulated by the protein component. The physical and biological properties of the hydrogel are determined by specifically designed or engineered protein domains. The crosslinking of the protein domains to the water soluble polymers is by means of non-covalent bonding such as chelation or coordination bonding, biotin-avidin bonding, protein—protein interaction and protein-ligand interaction, or by means of covalent bonding. Methods of making and using the polymer-protein hydrogels are disclosed in this application.

Abstract: The present invention encompasses pharmaceutical formulations comprising a biphasic mixture which comprises a glucagon like peptide (GLP-1) compound in a solid phase and an insulin in a solution phase.

Abstract: The present invention concerns processes for the production of dry, partially amorphous products containing biologically active and in particular therapeutically active material which are macroscopically homogeneous substance mixtures, the substance mixtures being selected from at least one substance of each of the groups (i) carbohydrate or zwitterion with a polar residue and derivatives thereof, and (ii) zwitterion with an apolar residue and derivatives thereof, wherein a solution is prepared of the biologically or therapeutically active material and of substances (i) and (ii) and the solution is dried at a product temperature above the freezing point of the solution. In addition the invention concerns new substance mixtures which are obtained by the said process as well as the use thereof in diagnostic or therapeutic methods.

Abstract: The invention regards a process for the production of ramoplanin-like derivatives of formula (I): RAMO-NC—CO—R (I), wherein the radical R represents a hydrocarbon radical and the portion RAMO-NH— represents deacylated ramoplanin, any of its factors or ramoplanose. The compound of Formula (I) are obtained by reacting a carboxylic acid R—COOH with deacylated ramoplanin, any of its factors or ramoplanose protected on the ornitine amino groups. New compounds wherein the hydrocarbon radical R is different form those characaterizing the ramoplanin and ramoplanose natural products and their tetrahydro-derivatives are calimed. The new compounds have the same or better antinfective activity, lower haemolytic effect and better tolerability profile than ramoplanin.

Abstract: Disclosed is a cyclic peptide antibiotic in which an enzyme-sensitive bond is replaced by an enzyme-resistant bond.

Abstract: Novel modified hemoglobins comprising polyalkylene glycols and novel methods for making those hemoglobins are provided. One group of modified hemoglobins comprise polyalkylene glycols bonded to the hemoglobin with an amide linkage at Glu-43(?). Additional polyalkylene glycols can also be bonded to the Glu-22(?) and/or the Asp-47(?). These hemoglobins are made by a novel amidation procedure. A second group of modified hemoglobins comprise a polyalkylene glycol covalently bonded to the hemoglobin at the ?-amino of a Val-1(?) or a Val-1(?). Additional polyalkylene glycols can optionally be covalently bonded to a limited number of ?-amino groups. This second group of hemoglobins is made using a novel reductive alkylation procedure. A third group of modified hemoglobins comprise a polyalkylene glycol bonded to a thiol group of the hemoglobin through a phenylsuccinimido linkage, wherein no polyalkylene glycol is bonded to a Cys-93(?).

Abstract: The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy formula (I), wherein X represents OH, (C1-5)alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C1-5) alkoxy group, a (C1-5) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R3 and R4 independently represent H, OH, (C1 –C5) alkyl, or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; R5 represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; and wherein R0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.

Abstract: The present invention to novel nociceptin receptor agonists which are peptide derivatives represented by the following general formula (1): (in which A is alkylene, —CH2)nCO— or a group expressed by the following formula (2) or (3): wherein n represents an integer of 1 to 8; X and Y are same or different and each represents —CONH— or —CH2NH—; R1, R2 and R3 are same or different and each represents alkyl, aryl or heteroaryl; Z represents —CON(R4)R5 or —CH2N(R4)R5; R4 and R5 are same or different and each represents hydrogen, alkyl, aryl or heteroaryl) or a pharmaceutically acceptable salt thereof. A pharmaceutical composition according to the present invention is useful as a nociceptin receptor agonist.

Abstract: A compound of the formula where R1 is H, C1–C4 alkyl and OH; R2 in is H, C1–C4 alkyl and OH; R3 is H and C1–C4 alkyl; R4 is H and C1–C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2–C6 alkyl; and R6 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, transferrin, glucosylamine, amino saccharin, saccharin ester, lactylamine, leucine, tryptophan, amino glutamate and amino cholines.

Abstract: Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.

Abstract: A complex is provided for the treatment of neurogenic conditions having the formula: where R1 is M is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium(II) represents the preferred metal ion as magnesium is known to have neuroprotective effects.

Abstract: The present inventive subject matter relates to novel antibacterial compounds that are capable of inhibiting bacterial multiplication and killing living bacteria. The present inventive subject matter further relates to methods for treating Gram positive bacterial infections using the inventive compounds.

Abstract: The present invention encompasses compositions wherein a GLP-1 compound is complexed with a basic polypeptide. The compositions provide a prolonged duration of action and can be administered by the pulmonary route.

Abstract: A stabilized pharmaceutical composition in the form of a solution for parenteral administration of a parathyroid hormone is described wherein the therapeutically active ingredient is stabilized with a buffer and a polyol. Preferred preparations contain in an aqueous solution human PTH(1–34), mannitol, an acetate or tartrate buffering agent and m-cresol or benzyl alcohol as a preservative.

Abstract: The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

Abstract: Disclosed are peptides that bind to Ang-2. Also disclosed are peptibodies comprising the peptides, methods of making such peptides and peptibodies, and methods of treatment using such peptides and peptibodies.

Abstract: Cyclic peptides and compositions comprising such cyclic peptides are provided. The cyclic peptides comprise a classical cadherin cell adhesion recognition sequence HAV. Methods for using such peptides and compositions for inducing apoptosis in cadherin-expressing cells, such as cancer cells, are also provided.

Abstract: Retro-inverso peptides derived from interleukin-6 (IL-6) having between 17 and about 40 amino acids and including the sequence shown in SEQ ID NO: 1. These peptides have the same activity as native IL-6 and also have neurotrophic activity. Because of the D-amino acid linkage in the peptides, they are less susceptible to proteolytic degradation in vivo.