Abstract: This invention relates to isolated polypeptides that are long acting analogs of human PYY. The disclosed PYY analog polypeptides have beneficial physicochemical properties relative to endogenous PYY and known synthetic PYY analog polypeptides, such as longer (i.e., “long-acting”) elimination half-lives (t1/2), and improved solubility and thermal stability. This invention also relates to methods of using presently disclosed PYY analog polypeptides in a variety of therapeutic indications, as well as methods of producing the same. The disclosed PYY analog polypeptides are particularly useful in methods of treating metabolic diseases or disorders, such as type 2 diabetes, treating obesity, and providing weight loss, and in methods of treating nonalcoholic fatty liver disease (NAFLD) and/or nonalcoholic steatohepatitis (NASH).

Abstract: Pharmaceutical compositions comprising PYY (e.g., PYY(3-36) and analogs and variants thereof), satiety peptides, satiety hormones, metabolic hormones, and methods of treating metabolic diseases with such compositions are provided. Aspects include methods of increasing a feeling of fullness in patients treated with pharmaceutical compositions comprising PYY, PYY(3-36), satiety peptides, satiety hormones, metabolic hormones, and analogs, receptor antagonists and variants thereof.

Abstract: The present application provides methods and compositions for AAV-mediated delivery of PYY and Glucagon-like Peptide 1 or an analog thereof (e.g., Exendin-4) to a subject (e.g., the saliva of a subject). In some embodiments, compositions and methods for topical delivery of Ex-4 and PYY peptides also are provided. Methods and compositions are useful to promote weight loss and/or altered lipid taste sensitivity, as well as for the treatment of diabetes.

Abstract: Cyclic peptide agonists toward human galanin receptor 2 (GalR2) and galanin receptor 3 (GalR3) based on hidden conformation of spexin solution structure for GalR2 and GalR3-related and spexin-deficient disorders are designed and synthesized. LH101, LH102, and LH101 (Ac) are potent spexin analogs with prolonged action, which can be used in the treatment of GalR2 and GalR3-related diseases and spexin-deficient disorders, such as obesity.

Abstract: The present disclosure relates to a lipid source for nutritional compositions, comprising an enriched lipid fraction which comprises structured fat globules. The enriched lipid fraction provides fat globules having a desired size and fatty acid composition and may be stabilized by components such as phospholipids, cholesterol, milk-fat globule membrane protein and combinations thereof. Additionally, the disclosure relates to methods of supporting lipid digestion in a pediatric subject by providing a nutritional composition comprising an enriched lipid fraction having structured fat globules that are more accessible to lipases. The chemical composition, size and structure of the fat globules may improve digestion. The disclosed nutritional compositions may provide additive and or/synergistic beneficial health effects.

Abstract: The present disclosure relates to a lipid source for nutritional compositions, comprising an enriched lipid fraction which comprises structured fat globules. The enriched lipid fraction provides fat globules having a desired size and fatty acid composition and may be stabilized by components such as phospholipids, cholesterol, milk-fat globule membrane protein and combinations thereof. Additionally, the disclosure relates to methods of supporting lipid digestion in a pediatric subject by providing a nutritional composition comprising an enriched lipid fraction having structured fat globules that are more accessible to lipases. The chemical composition, size and structure of the fat globules may improve digestion. The disclosed nutritional compositions may provide additive and or/synergistic beneficial health effects.

Abstract: The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).

Abstract: In alternative embodiments, the invention provides methods for treating, ameliorating or protecting (preventing) an individual or a patient against a disease, an infection or a condition responsive to an increased paracrine polypeptide level in vivo comprising: providing a paracrine polypeptide-encoding nucleic acid or gene operatively linked to a transcriptional regulatory sequence; or an expression vehicle, a vector, a recombinant virus, or equivalent, having contained therein a paracrine-encoding nucleic acid or gene, and the expression vehicle, vector, recombinant virus, or equivalent can express the paracrine-encoding nucleic acid or gene in a cell or in vivo; and administering or delivering the paracrine polypeptide-encoding nucleic acid or gene operatively linked to a transcriptional regulatory sequence, or the expression vehicle, vector, recombinant virus, or equivalent, to an individual or a patient in need thereof, thereby treating, ameliorating or protecting (preventing) the individual or patient a

Abstract: Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

Abstract: Methods are disclosed for decreasing calorie intake, food intake, and appetite in a subject. The methods include peripherally administering PYY or an agonist thereof and GLP-1 or an agonist thereof to the subject, simultaneously or sequentially, thereby decreasing the calorie intake of the subject.

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

Abstract: The present invention relates to nociceptin peptide mimetics that have ?-helical structures and bind to and modulate the opioid receptor-like-1 (ORL-1) receptor. The peptide mimetics are constrained cyclic nociceptin analogs which have either agonist or antagonist activity. Pharmaceutical compositions comprising the nociceptin peptide mimetics and methods of treating or preventing a disease or condition ameliorated by modulating the ORL-1 receptor are also described.

Abstract: A method for treating hyperglycemia and/or diabetes in a subject is provided. In particular, the method is directed for the treatment of patients with type 2 diabetes mellitus who have a fasting blood glucose concentration greater than about 8 mM, wherein the patient is administered a formulation comprising a GLP-1 molecule and a diketopiperazine by pulmonary inhalation with a dry powder inhalation system.

Abstract: Peptide analogs of peptide YY (PYY), compositions comprising them, and methods of using those analogs or compositions for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as diabetes and obesity, and for reduction in appetite, reduction in food intake or reduction of calorie intake in a subject, are provided herein.

Abstract: The present invention relates to novel analogs of PYY that have an improved therapeutic profile when compared to native human PYY. These novel PYY analogs are useful in the treatment of obesity, diabetes, and other disorders.

Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.

Abstract: The present invention relates to novel Motoneuronotrophic Factors (MNTF) peptides and analogs thereof, including compositions capable of promoting the growth and viability of neurons. MNTF peptides between two and six amino acids in length are provided, as well as analogs of these MNTF peptides that are modified by covalent attachment to another moiety. Other embodiments are described herein.

Abstract: The present invention relates to drug fusions that have improved serum half lives. These fusions and conjugates comprise polypeptides, immunoglobulin (antibody) single variable domains and GLP and/or exendin molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates.

Abstract: This invention relates generally to neuropeptide Y (“NPY”) Y4 receptor agonists including pancreatic polypeptide (PP), analogs thereof, and peptide fragments of PP, e.g. PP(32-36), and analogs thereof, to pharmaceutical compositions containing such Y4 receptor agonists, and to methods for treatment of mammals using the same. The NPY Y4 receptor agonists may be administered to mammals either alone or in combination with NPY Y2 receptor agonists including peptide YY (PYY) (3-36), analogs thereof, and to peptide fragments of PYY(3-36), e.g. PYY(22-36) and PYY(25-36), and analogs thereof, such as to control food intake in mammals, blood pressure, cardiovascular response, libido, circadian rhythm, hyperlipidimia, chronic pancreatitis, and nonalcoholic fatty liver disease including nonalcoholic steatohepatitis.

Abstract: Methods and compositions are disclosed to treat metabolic disorders such as obesity, diabetes, and increased cardiovascular risk comprising administering a therapeutically effective amount of a PYY or a PYY agonist.

Abstract: Methods, uses, agents and compositions useful for the prevention, treatment and/or diagnosis of neuroinflammatory conditions such as multiple sclerosis and spinal cord injury based on the modulation of nerve injury-induced protein-1 (Ninjurin-1) are disclosed.

Abstract: Methods and compositions are generally provided for treating metabolic disorders, e.g., obesity. One aspect discloses methods and compositions for obtaining a biological sample from the subject, evaluating the sample for the presence or absence of a genetic indicator, wherein the genetic indicator is selected from a single nucleotide polymorphism and a level of gene expression, and performing a first metabolic procedure if the genetic indicator is present, or performing an alternative second metabolic procedure if the genetic indicator is absent. One aspect discloses methods and compositions for obtaining a sample including deoxyribonucleic acids (DNA) from the subject, evaluating the DNA for an absence or presence of one or more genetic indicators and performing a first metabolic procedure or an alternative second metabolic procedure based on the absence or presence of the genetic indicator(s). Other aspects are also disclosed.

Abstract: The present invention relates to novel Pancreatic Polypeptide Family (“PPF”) polypeptides. The PPF polypeptides of the invention generally include at least two PPF motif, have at least 50% sequence identity to PYY (3-36) over its length and will generally retain, at least in part, a biological activity of a PP, PYY or NPY. Preferred PPF polypeptides of the invention are those having a potency in one of the assays described herein (preferably food intake, gastric emptying, pancreatic secretion, or weight reduction assays) which is greater than the potency of PP, NPY, PYY, or PYY(3-36) in that same assay. In one aspect, the PPF polypeptides of the invention include novel PYY analog polypeptides. In another aspect, the PPF polypeptides of the invention include PPF chimeric polypeptides including a fragment of a PP family polypeptide linked to a second PP family polypeptide, wherein each of the first and second fragments includes a PPF motif.

Abstract: The present invention provides novel Pancreatic Polypeptide Family (“PPF”) polypeptides and methods for their use.

Abstract: Peptide analogues of PYY, compositions comprising said analogues, and methods of using said analogues for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as diabetes and obesity, and for reduction in appetite, reduction in food intake or reduction of calorie intake in a subject, are provided herein.

Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).

Abstract: The present invention relates to nociceptin peptide mimetics that have ?-helical structures and bind to and modulate the opioid receptor-like-1 (ORL-1) receptor. The peptide mimetics are constrained cyclic nociceptin analogues which have either agonist or antagonist activity. Pharmaceutical compositions comprising the nociceptin peptide mimetics and methods of treating or preventing a disease or condition ameliorated by modulating the ORL-1 receptor are also described.

Abstract: Neurturin polypeptides which possess reduced heparin and heparan sulfate binding affinity but retain neurotrophic activity, nucleic acids which encode the neurturin variants and vectors and host cells which express the enhanced neurturin polypeptides. Use of the enhanced neurturin polypeptides, nucleic acids and host cells in the treatment or prevention of disease.

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

Abstract: Methods of treatment using Fzd8 extracellular domains (ECDs), Fzd8 ECD fusion molecules, and/or antibodies that bind Fzd8 are provided. Such methods include, but are not limited to, methods of treating obesity and obesity-related conditions. Fzd8 ECDs and Fzd8 ECD fusion molecules are also provided. Polypeptide and polynucleotide sequences, vectors, host cells, and compositions comprising or encoding such molecules are provided. Methods of making and using Fzd8 ECDs, Fzd8 ECD fusion molecules, and antibodies that bind Fzd8 are also provided.

Abstract: The present invention provides novel Pancreatic Polypeptide Family (“PPF”) polypeptides and methods for their use.

Abstract: The present invention relates to PYY derivatives comprising a serum albumin binding side chain, wherein said derivative has a half-life of at least 7 hours as determined by Assay (IV) described herein as well as compositions comprising said derivative and its use in therapy.

Abstract: Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

Abstract: The invention is based on the discovery of a novel neuroprotective peptide. In addition, the invention rests on the discovery that the NAP peptide enhances the association of tau and the brain-specific beta tubulin subunit. In addition, NAP modifies microtubule assembly and dynamics, in part, by affecting the tyrosination of microtubule proteins. The invention provides compositions and methods for treatment and prevention of neuronal disorders, including NAP-binding and tau-binding agents, tau peptide mimetics, NAP-like and NAP-like tau peptide mimetics.

Abstract: Combinations of one or more anti-obesity drugs with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight comprised of a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA comprise about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition for the reduction of body weight in cardiovascular disease patients (CVD) and diabetics.

Abstract: Methods and compositions are disclosed to treat metabolic disorders such as obesity, diabetes, and increased cardiovascular risk comprising administering a therapeutically effective amount of a PYY or a PYY agonist.

Abstract: Systems and methods are described providing therapeutic preparations of tachykinins, and more specifically sialokinins, for treating various types of abnormal cellular proliferation conditions in regions of tissue associated with the body of a patient. The sialokinins may be isolated and purified from natural or bioengineered sources, or may be synthesized, and may be combined into, with, or on an implant for local elution or otherwise as a powder mixed in a carrier vehicle for injection delivery. Tumors, warts, and restenosis are abnormal cellular proliferation conditions treated by therapeutic doses of sialokinin. Size of the tissue structure to be treated is used to determine the therapeutic dose of sialokinin. The sialokinins are either locally or systemically delivered at therapeutic doses for the desired effect. Implants such as stents are coated with sialokinins for local elution at the site of injury or tissue otherwise vulnerable to harmful conditions treated by the sialokinin.

Abstract: Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is —C(O)—O—R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, —C(O)—NH2, or C1-C6 alkyl substituted with hydroxy or C1-C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, —CH2—(C1-C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or —CH2—(C1—C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

Abstract: Provided herein are neuropeptide-2 receptor agonists of the formula (I): Y—R1—R2—X—R3—R4—R5—R6—R7—R8—R9—R10—R11—R12—R13—R14—NH2??(I) (SEQ ID NO: 1), as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.

Abstract: The present invention relates to compositions and methods for regulating body weight, and for treating conditions associated with obesity, particularly, obesity-related diabetes. The present invention is premised on the discovery that body weight can be effectively regulated by modulating the levels and/or activities of two gut hormones, PYY and ghrelin.

Abstract: Provided herein are neuropeptide-2 receptor agonists of the formula (I): as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. X is 4-oxo-6-(1-piperazinyl)-3(4H)-quinazoline-acetic acid (Pqa). These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.

Abstract: The invention provides a compound of formula (I): X-PYY* (3-36) (I) wherein X is selected from H, PYY1-2 (ie Tyr Pro) and D-Allo-Ue; PYY*(3-36) representing PYY (3-36) in which one or more residues is replaced by an acylated lysine group, the acyl group being selected from: CO—C1-20 alkyl, CO—C2-20 alkenyl, CO—C5-10 aryl and CO—C5-10 ar-C1-20 alkyl; a variant or derivative thereof; or a salt or solvate thereof. The compounds are effective in inducing satiety and suppressing appetite and they are thus useful in treating various diseases, including obesity.

Abstract: The present invention provides compositions and methods for inducing weight loss, preventing weight gain, and/or treating obesity-related conditions such as diabetes by inducing the production of brown adipose tissue in subjects by administering orexin or biologically active fragments thereof.

Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).

Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes and associated metabolic disorders. In particular, the invention provides novel acylated glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.

Abstract: Methods are disclosed for decreasing calorie intake, food intake, and appetite in a subject. The methods include peripherally administering a therapeutically effective amount of PYY or an agonist thereof to the subject, thereby decreasing the calorie intake of the subject.

Abstract: The present invention relates to compounds of formula (I); variants or derivatives thereof, or salts or solvates thereof. The present invention also relates to the use of such compounds to control appetite, feeding, food intake, energy expenditure and calorie intake, particularly in the treatment of obesity.

Abstract: Methods and compositions for treating cancer and other disorders by ?-endorphin therapy are disclosed.

Abstract: An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X? is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.

Abstract: An over-the-counter (OTC) regulated therapeutic composition for self-medication use for application to wounds having a potential pathogen load, in which the composition comprises a tissue penetration enhancer comprising a Class I pharmaceutical incipient; a pharmaceutical antibiotic agent in a dosing suitable for use in an OTC listing; a hygroscopic carrier agent comprising a Class I pharmaceutical incipient suitable for mixing in solution with the tissue penetration enhancer and the antibiotic agent; and wherein the activity/water (Aw) measurement of the composition is less than the Aw measurement for a target pathogen in a tissue wound.