Abstract: There is provided a radiolabelled peptide-based compound for diagnostic imaging using positron emission tomography (PET). The compound may thus be used for diagnosis of malignant diseases. The compound is particularly useful for imaging of somatostatin overexpression in tumors, wherein the compound is capable of being imaged by PET when administered with a target dose in the range of 150-350 MBq, such as 150-250 MBq, preferable in the range of 191-210 MBq.

Abstract: A multifunctional chemical agents comprising functional agents Fn1, Fn2 and linkers, for the linchpin directed (LDM), protein directed (PDPM) modifications of proteins, and Fn1 accelerated kinetic labeling by Fn2.

Abstract: A process for the primary clarification of feeds, including chemically treated flocculated feeds, containing the target biomolecules of interest such as mAbs, mammalian cell cultures, or bacterial cell cultures, using a primary clarification depth filtration device without the use of a primary clarification centrifugation step or a primary clarification tangential flow microfiltration step. The primary clarification depth filtration device contains a porous depth filter having graded porous layers of varying pore ratings. The primary clarification depth filtration device filters fluid feeds, including chemically treated flocculated feeds containing flocculated cellular debris and colloidal particulates having a particle size distribution of approximately about 0.5 ?m to 200 ?m, at a flow rate of about 10 litres/m2/hr to about 100 litres/m2/hr. Kits and methods of using and making the same are also provided.

Abstract: Peptide aldehydes containing a ureido group are effective as stabilizers for protease in a detergent composition, and as stabilizers for a second enzyme in a liquid composition with a protease.

Abstract: There is provided a radiolabelled peptide-based compound for diagnostic imaging using positron emission tomography (PET). The compound may thus be used for diagnosis of malignant diseases. The compound is particularly useful for imaging of somatostatin overexpression in tumors, wherein the compound is capable of being imaged by PET when administered with a target dose in the range of 150-350 MBq, such as 150-250 MBq, preferable in the range of 191-210 MBq.

Abstract: The present invention describes methods of removing DNA from an RNA transcript during the mRNA production process. The method embodies procedures for obtaining an in vitro transcription product, and removing any DNA from the product. The DNA can be removed by adding either free DNase or a resin containing immobilized DNase to the product, and recovering the RNA transcript. Alternatively, the DNA template used in the in vitro transcription reaction is labeled. After transcription, the product is applied to a resin that is configured to bind the label, and the RNA transcript is recovered. To detect whether any residual impurities are left in the RNA transcript product, the product is subjected to nuclease digestion and subsequently to liquid chromatography-tandem mass spectrometry analysis to quantitate any residual DNA. The present invention demonstrates efficient and effective methods of isolating an RNA transcript from an in vitro transcription product.

Abstract: The present invention relates to novel somatostatin analogs, dimers thereof, and methods of using the same to treat various diseases. Naturally occurring somatostatins (SSTs), which are also known as somatotropin release-inhibiting factors (SRIFs), have diverse biological effects in many cells and organs 10 throughout the body. They are produced by normal endocrine, gastrointestinal, immune and neuronal cells, as well as by certain tumors (Patel, Y. C, Frontiers in Neuroendocrinology, 20(3): 157-198 (1999); Froidevaux, et al., Biopolymers, 66(3): 161-83 (2002)).

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Abstract: A subject afflicted with a cancer or precancerous condition is treated by administering an agent that increases expression of somatostatin receptors, and a cytotoxic recognition ligand. In an alternative embodiment, somatostatin analogs, which are radiolabeled are used to treat cancer or precancerous conditions.

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Abstract: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

Abstract: The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Abstract: Peptide derivatives, their stereoisomers, mixtures thereof and/or their pharmaceutically acceptable salts, a method of obtaining them, pharmaceutical compositions containing them and the use thereof for the treatment, prevention and/or diagnosis of those conditions, disorders and/or pathologies in which the sstr1, sstr2, sstr3, sstr4 and/or sstr5 somatostatin receptors are expressed.

Abstract: Cyclohexapeptides of formula (I): as defined herein. The cyclohexapeptides are non-selective functional analogs of somatostatin.

Abstract: Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.

Abstract: The present invention relates to a method of labelling biological molecules with 18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.

Abstract: [Problem] To provide a glycosylated polypeptide having an affinity to somatostatin receptors, and, compared to somatostatins, having improved in-blood stability. [Solution] The glycosylated polypeptide is characterized by at least one amino acid in a somatostatin or an analog thereof being replaced with a glycosylated amino acid.

Abstract: The present invention provides a constant release copolymer composition adapted for use in a controlled release formulation for a bioactive agent, such as a formulation adapted for implantation within a patient's body tissues as a depot to release the agent over a period of time, wherein the copolymer provides a substantially constant rate of release of the bioactive agent over the time period for which the depot persists in the body tissues. The copolymer includes a PLG copolymer and a PLG oligomer of about 5-10 kDa average molecular weight, which can lack free carboxylic acid groups. When the PLG copolymer is a low burst copolymer, the constant release copolymer composition is a low burst, constant release copolymer composition adapted for implantation in the body tissues of a mammal, wherein a substantially constant rate of release of the bioactive agent is achieved.

Abstract: The invention relate to the new conjugated somatostatin analogs of formula (I), wherein A- is H or TAG-B—, wherein —B— is 0 or a spacer, wherein TAG is a chelating agent (e.g. DOTA), a fluorescent dye, (e.g. Bodipy-B derivative, a Rho-damine-B derivative, a Fluorescein-B derivative, a Cyanine-B derivative, a Porphyrin-B derivative), a bimodal agent, or a cytotoxic agent (e.g. a doxorubicin derivative) wherein R1 is CI-C4 alkynyl radical when R2 is CI-C4 azido radical and viceversa and methods for preparing same, pharmaceutical compositions comprising them and their use in imaging and the treatment of cancer.

Abstract: The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.

Abstract: The invention relates to peptides for modulate IGF-1 activity, a pharmaceutical composition comprising them as well as their applications as medicinal products and cell proliferation modulating agents in vitro.

Abstract: The subject-matter of the present invention are nanocomplexes of polyanions and cationic peptides which are, e.g., suitable for the transport of drugs into cells and their controlled release in the organism, as well as a complex material in which the nanocomplexes are bonded to a biologically active unit for the selective recognition of tissues, cells or organelles.

Abstract: 89Zr radiolabeled somatostatin receptors and other receptors, methods of their making, and method of their using for imaging and treatment of somatostatin receptor bearing tumors and other receptor bearing tumors.

Abstract: Tin-117m somatoostatin analogues or antagonist are used to treat tumors and symptoms associated with these tumors which express somatostatin receptors, such as gastroenteropancreatic neuroendocrine tumors. The tin-117m somatostatin receptor binding compounds can be administered at a dosage which is effectively apoptotic and not necrotic. Also, if desired, it can be administered at a dose that is necrotic and/or induces necrosis, but only to cells within 290 microns of the tin-117m atom. A novel somatostatin analogue is also disclosed, as well as novel methods to produce the tin labeled analogues and antagonists.

Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

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

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: Disclosed are Drug Delivery Molecules (DDMs) which both facilitate functional imaging, as by PET, MRI or SPECT, and create a biological effect and methods of their use. These DDMs which are variously designed to target specific receptors, internalized and then function biologically, as for purposes of cell destruction or therapy.

Abstract: Neuropeptide analogs and compositions including neuropeptide analogs are described herein. Also provided are methods of producing and using the neuropeptide analogs and compositions including one or more neuropeptide analogs.

Abstract: Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

Abstract: The present invention is directed to the use of the peptide compound D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-L-threoninol as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-L-threoninol optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

Abstract: Disclosed are compositions and methods related to improving pharmacological properties of bioactive compounds targeting nervous system.

Abstract: The present invention aims at providing a peptide fragment capable of improving biostability of a bioactive substance while maintaining the activity of the bioactive substance, and a bioactive substance to which the peptide fragment is added. The present invention relates to a partial peptide of a GA module having 5 to 25 amino acids, including a partial sequence of a GA module (SEQ ID NO: 1) and the amino acid sequence Ile-Asp-Glu-Ile-Leu (SEQ ID NO: 2), and a bioactive complex in which the partial peptide of the GA module is bound to a bioactive substance. The bioactive substance includes GLP-1, GLP-2, GIP, VIP, somatostatin, amylin, ghrelin, derivatives thereof, and the like.

Abstract: The present invention provides a method comprising administering to a patient suffering from an endocrine disorder characterized by partial endogenous growth hormone activity or signaling an amount of insulin-like growth factor-1 (IGF-1) and an amount of growth hormone (GH) that in combination are effective to improve growth or metabolism in the patient, where the patient receives IGF-1 in a single daily administration and receives GH in a single daily administration, and where the single administrations are administered to the patient substantially contemporaneously each day.

Abstract: The present invention relates to a method of increasing the bioavailability of a peptide. The method includes altering the lipophilicity of a peptide by the creation of fatty acid peptide salts of the peptide. The fatty acid peptide salts exhibit increased transdermal and transmucosal permeability.

Abstract: A solid phase method for synthesizing a peptide containing three or more amino acid residues utilizing both Boc and Fmoc protected amino acids and a chloromethylated polystyrene resin.

Abstract: Chimeric somatostatin-based polypeptides, polynucleotides used to encode the polypeptides, the methods for isolating and producing the polypeptides and the uses thereof are provided. In addition, low cost adjuvants for enhanced immunogenic response are provided. Vaccinations that include both chimeric somatostatin-based polypeptides and novel adjuvants are included, useful in facilitating farm animal productivity.

Abstract: Pharmaceutical compositions comprising a somastatin analogue in the form of a liquid formulation for parenteral administration are disclosed.

Abstract: The present invention is directed to fusion proteins that can be used to assay gene transfer and expression both in vitro and in vivo. The fusion proteins contain a reporter protein, e.g. a somatostatin receptor, fused to a second protein, which may be a protein fusion tag. Alternatively, a fusion protein may be fused to a leader sequence. A leader sequence may localize an expressed protein, e.g. localize a fusion protein to the cell membrane. The invention includes nucleic acids encoding the fusion proteins and methods of assaying for gene expression.

Abstract: The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R1—H which comprises a first functional moiety of formula F1 to a second functional moiety of formula F2 wherein X, X?, Y, R1, F1 and F2 are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.

Abstract: The present invention relates to the use of a compound comprising a moiety of formula (I) as a reagent for protecting a thiol group in a thiol compound wherein X, X? and Y are as defined herein. The protecting group methodology of the present invention allows straightforward and selective protection of thiol groups. Cleaving of the thiol group to regenerate the thiol functional group is also facile and controllable. The present invention further provides an analogous protecting group methodology directed to protection of disulfide groups.

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: Peptide derivatives, their stereoisomers, mixtures thereof and/or their pharmaceutically acceptable salts, a method of obtaining them, pharmaceutical compositions containing them and the use thereof for the treatment, prevention and/or diagnosis of those conditions, disorders and/or pathologies in which the sstr1, sstr2, sstr3, sstr4 and/or sstr5 somatostatin receptors are expressed.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.

Abstract: Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).

Abstract: The present invention provides methods and compositions for increasing the growth rates, alleviating the symptoms, or improving the metabolism of human patients having insulin-like growth factor-1 deficiency (IGFD). The invention relates to methods comprising administering insulin-like growth factor-I to a patient having a height which, at the time of treatment or prior to initial treatment with IGF-1, is at least about 2 standard deviations below normal for a subject of the same age and gender, a blood level of insulin-like growth factor-I that, and at the time of treatment or prior to initial treatment with IGF-1, is below normal mean levels, usually at least about 1 standard deviations below normal mean levels, for age and gender.

Abstract: An intracellular selection system allows screening for peptide bioactivity and stability. Randomized recombinant peptides are screened for bioactivity in a tightly regulated expression system, preferably derived from the wild-type lac operon. Bioactive peptides thus identified are inherently protease- and peptidase-resistant. Also provided are bioactive peptides stabilized by a stabilizing group at the N-terminus, the C-terminus, or both. The stabilizing group can be a small stable protein, such as the Rop protein, glutathione sulfotransferase, thioredoxin, maltose binding protein, or glutathione reductase, an ?-helical moiety, or one or more proline residues.

Abstract: The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.