Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.

Abstract: Described herein are compositions comprising a derivatized polyglucosamine and a small molecule, peptide, or protein and related methods of use, e.g., to deliver a small molecule, peptide, or protein to cells (e.g., cancer cells) or tissues (e.g., mucosal membrane and epithelial membrane), e.g., to treat a disease or condition in a subject.

Abstract: There are provided mutants prepared by changing a DNA base sequence and an amino acid sequence of an epidermal growth factor (EGF), in which a mutant EGF protein has excellent thermal stability and stability even in the state of an aqueous solution, and a gene encoding the protein are provided; a recombinant vector including the gene and a microorganism transformed by the recombinant vector are provided; a method of preparing the mutant EGF protein is provided; a cosmetic composition for accelerating the growth of skin cell and skin regeneration, including the protein, the gene, or the recombinant vector, is provided; and by preparing a product using the EGF mutant according to the present invention, it is possible to produce functional cosmetics, in which the activity thereof is maintained even during a distribution and storage process unlike the conventional wild-type EGF product.

Abstract: The present invention includes a novel class of allosteric modulators that target a protein having a juxtamembrane segment. In another embodiment, the allosteric modulator is a peptide mimetic that is capable of interacting with an ?-helix or a coiled coil domain of a protein. In one embodiment, the peptide mimetic binds to at least an ?-helix or a coiled coil domain of EGFR and modulates its activity.

Abstract: The invention provides methods and compositions for use of desmopressin in combination with a beta-3-adrenergic receptor agonist. The methods and compositions are useful in the treatment of nocturia and other urinary frequency disorders.

Abstract: The invention provides methods and compositions for use of desmopressin in combination with a 5-alpha reductase inhibitor. The methods and compositions are useful in the treatment of nocturia and other urinary frequency disorders.

Abstract: Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: R1-A1-A2-A3-A4-A5-R2??(I) wherein: A1 is Aib, Apc or Inp; A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A5 is Apc, Dab, Dap, Lys, Orn, or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2; and pharmaceutical compositions and methods of use thereof.

Abstract: The subject application relates to methods for treating a placental syndrome, wherein relaxin is administered during the late secretory/luteal (LS) phase of the menstrual cycle in women who have a propensity for developing the placental syndrome. In certain embodiments, administration of relaxin continues beyond the LS phase and into pregnancy.

Abstract: The present invention provides methods for preventing or treating purulent rhinosinusitis. These methods include administering a composition comprising thymosin alpha 1 to a subject.

Abstract: The present disclosure relates to a collection of novel muteins derived from human ?1m (or a1m) polypeptide or a functional homologue thereof. The disclosure further refers to a ?1m mutein capable of specifically binding to one or more targets other than a target to which wild-type ?1m binds. The disclosure also relates to a method for producing such collection of muteins and a method for isolating a mutein capable of binding one or more such non-natural targets of wild-type ?1m polypeptide. These aspects are made possible due to, e.g, the structural elucidation of ?1m disclosed herein by the present inventors, an appreciation of ligand-binding sights thereof and, hence, an understanding of which amino acid positions are most suitable for mutagenesis for re-engineering specificity and affinity for any given target while maintaining the secondary and/or tertiary structure of ?1m.

Abstract: This invention relates to collagen-binding synthetic peptidoglycans and engineered collagen matrices comprising a collagen matrix and a collagen-binding synthetic peptidoglycan where the collagen-binding synthetic peptidoglycan can be aberrant or can have amino acid homology with a portion of the amino acid sequence of a protein or a proteoglycan that regulates collagen fibrillogenesis. The invention also relates to kits, compounds, compositions, and engineered graft constructs comprising such collagen-binding synthetic peptidoglycans or engineered collagen matrices and methods for their preparation and use.

Abstract: A pharmaceutical composition comprising an effective amount of a mutant thrombomodulin is disclosed. The mutant thrombomodulin comprises an ammo acid sequence that is at least 80% identical to SEQ ID NO: 2 and has residues corresponding to Ala364 and Ala391 of SEQ ID NO: 2. The mutant thrombomodulin has little or no protein C activation activity, and is effective in promoting wound healing and accelerating closure of an open wound in a diabetic.

Abstract: A method for purification of complement Factor H from a complement Factor H containing source such as blood or blood plasma, in particular a caprylate precipitate of a Factor H containing source, which is e.g. obtained by addition of caprylate ions to fractions of blood or plasma, comprising the steps of: a) providing a Factor H containing source, in particular reconstitution of caprylate precipitate to provide a complement Factor H containing solution; b) performing a cation exchange chromatography in particular as first chromatographic step; c) performing an anion exchange chromatography; d) performing a hydroxyl apatite chromatography; e) followed by ultra/diafiltration to obtain a complement Factor H concentrate.

Abstract: The present invention relates to an inhibitor of the Rho guanine nucleotide exchange factor 12 (RhoGEF12) or an inhibitor of an activator of RhoGEF12 for use in the prevention and/or treatment of heart failure associated with cardiac hypertrophy and/or cardiac fibrosis and diseases associated therewith. Further, it relates also a method of treatment and methods for identifying inhibitors of Rho guanine nucleotide exchange factor 12 (RhoGEF12) or inhibitors of an activator of RhoGEF12.

Abstract: The present invention provides therapeutic modalities for the treatment of an ischemic event (e.g., stroke) that creates or embodies a risk of neurological damage in CNS sites by administration of a thrombopoietin receptor ligand.

Abstract: The invention provides a chimeric antigen receptor (CAR) (a) an antigen binding domain of HN1 or SS, a transmembrane domain, and an intracellular T cell signaling domain, or (b) an antigen binding domain of SS1, a transmembrane domain, an intracellular T cell signaling domain, and a granulocyte-macrophage colony-stimulating factor (GM-CSF) receptor 2 leader. Nucleic acids, recombinant expression vectors, host cells, populations of cells, antibodies, or antigen binding portions thereof, and pharmaceutical compositions relating to the CARs are disclosed. Methods of detecting the presence of cancer in a mammal and methods of treating or preventing cancer in a mammal are also disclosed.

Abstract: This invention provides compositions and methods for treating cancer. More specifically this invention is directed to a targeted retroviral vector comprising a cytokine gene that can be administered either alone or in combination with a targeted retroviral vector comprising a cytocidal gene for treating cancer in a subject. Also provided are a kit or drug delivery system comprising the compositions for use in the methods described.

Abstract: A method of diagnosing metastatic potential of a breast cancer in an individual with breast cancer is described. The method comprises a step of assaying a breast cancer tumour sample from the patient for expression of ADAM22, wherein expression of ADAM22 correlates with increased potential for metastasis compared with a patient who is ADAM22 negative. The invention also describes an agent for use in the treatment of metastatic breast cancer in a patient, in which the agent is selected from LGI1 protein (SEQ ID NO:1) and an LGI1 peptide mimic capable of mimicking the ADAM22 binding activity of LGI1 by binding to the LGI1 binding domain of ADAM22 (SEQ ID NO: 4) and which is capable of inhibiting migration of endocrine resistant breast cancer cells.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

Abstract: Oral dosage compositions for drugs normally given intravenously such as Paclitaxel, containing a plant sterol to enhance solubility and a small intestine efflux inhibitor to prevent P-glycoprotein from being a barrier to absorption.

Abstract: An ophthalmic composition is described for the treatment of dry eye syndrome in a human or mammal. The composition comprises an aqueous solution including an effective amount of silk protein. The aqueous solution comprises from about 0.01% by weight to about 30% by weight of the silk protein. In one embodiment, the silk protein may be fibroin. A method of treating an eye having an ocular surface is also described. The method comprises providing an ophthalmic composition comprising an aqueous solution including an effective amount of silk protein, and administering the ophthalmic composition topically to the ocular surface.

Abstract: Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.

Abstract: The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.

Abstract: The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions.

Abstract: The bifunctional peptide is capable of activating collagen synthesis and inhibiting the production of matrix metallo-proteinases. The peptide has a sequence including three peptide parts A, B and C. The first peptide part A corresponds to a hexapeptide repeated at least three times, the part A being capable of bonding to a receptor elastin-binding protein in order to stimulate collagen synthesis. The second peptide part B corresponds to a tetrapeptide capable of acting as a competitive inhibitor of urokinase protease and of being cleaved by said protease. The third peptide part C corresponds to a tripeptide occupying at least one active site of the matrix metallo-proteinases in order to enable inhibition of the proteinases. The present invention further concerns a cosmetic and/or pharmaceutical composition incorporating the bifunctional peptide.

Abstract: The present invention provides, among other things, methods of treating Marfan Syndrome and/or a Marfan-related disorder including administering to a subject suffering from or susceptible to Marfan Syndrome and/or a Marfan-related disorder an angiotensin (1-7) peptide. In some embodiments, the angiotensin (1-7) peptide is administered at an effective dose periodically at an administration interval such that at least one symptom or feature of Marfan Syndrome and/or a Marfan-related disorder is reduced in intensity, severity, duration, or frequency or has delayed in onset.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.

Abstract: The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (IBAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.

Abstract: The present invention relates to a chemically modified heparin, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa. Also disclosed is a method of preparing the heparin and its medical use, including treatment of malaria.

Abstract: The present invention concerns the antidiabetic-activity of compounds type A, namely of 8-?-D-glucosylgenistein, which is not toxic to eukaryotic cells and has demonstrated to produce complete normalization of fasting hyperglycaemia, to reduce excessive postprandial glucose excursion, to increase glucose-induced insulin secretion and insulin sensitivity. An alternative synthesis for this molecular entity and its binding ability to ?-amyloid oligomers is also included in the present invention, which also comprises Genista tenera ethyl acetate extract for use as antihyperglycaemic, agent i.e. for lowering blood glucose levels in mammals that are pre-diabetic or have type 2 or type 1 diabetes. The inhibitory activity of ?-glucosidase by Genista tenera ethyl acetate and butanol extracts and that of glucose-6-phosphatase by these two extracts and the diethyl ether plant extract is also part of the present invention.

Abstract: It has been determined that co-administration of a rifamycin and a switch-region inhibitor 1) results in synergistic antibacterial effects, enabling efficacy at low, subtoxic doses, and/or 2) results in a low spontaneous resistance frequency, enabling treatment of high-titer infections without treatment failure due to spontaneous resistance. Accordingly, certain embodiments provide composition comprising a rifamycin and a switch region inhibitor, as well as methods of use thereof.

Abstract: Gene mutations are associated with the progression of acute myeloid leukemia (AML). The invention relates to methods and systems for evaluating the progression of AML based on these gene mutations. The present invention also relates to methods and compositions for treating AML patients by modulating the expression or activity of certain genes involved in AML progression and/or their encoded proteins. The invention further relates to methods and compositions for determining the responsiveness of an AML patient to induction chemotherapy therapy.

Abstract: The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof in combination with Decitabine or a salt thereof or the hydrate thereof for treating patients suffering from acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).

Abstract: The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof in combination with Azacitidine or a salt thereof or the hydrate thereof for treating patients suffering from acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).

Abstract: The invention provides novel amphiphilic drug-drug conjugates useful as cancer therapeutics, and compositions and methods thereof.

Abstract: Disclosed are nutritional compositions including human milk oligosaccharides that can be administered to preterm infants, term infants, toddlers, and children for improving airway defense mechanisms.

Abstract: A carrier enhancing absorption of medication includes a target medication, an emulsifier, a small-molecular hyaluronic acid (HA) component, an absorption enhancer and a cream base, wherein the carrier promotes infiltration of target medication from skin over affected area and enhance the absorption efficacy of human body by synergistic interaction.

Abstract: The present invention relates to a taste-masked dispersible tablet comprising a drug, a cation exchange resin, and other pharmaceutically acceptable excipients, such that the said drug and the said cation exchange resin are present in an un-complexed form in the tablet. It further relates to a process for the preparation of the same.

Abstract: Compounds of formula (I): wherein X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T and R5 are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

Abstract: A combination therapy for treating osteoarthritis is disclosed. The combination therapy includes the co-administration of a steroid and Zoledronic Acid. The coadministration of a steroid decreases the production of cytokines, and, therefore, decreases the pro-inflammatory effects of Zoledronic Acid. The co-administration of Zoledronic Acid with steroids treats osteoarthritis, and helps to prevent the onset of osteoarthritis in patients at risk for osteoarthritis.

Abstract: An ascorbic acid derivative composition of a first aspect according to the present invention consists of a salt of a compound (1) represented by a general formula (1) shown below; and a salt of a compound (2) represented by a general formula (2) shown below, wherein a ratio of the salt of the compound (2) with respect to a total amount of the salt of the compound (1) and the salt of the compound (2) is from 0.1 to 10% by mass, wherein R1 represents a linear or branched alkyl group of 6 to 20 carbon atoms, R2 represents a linear or branched alkyl group of 6 to 20 carbon atoms, and R1 and R2 are the same or are different from each other.

Abstract: The invention relates to prodrugs of vitamin K2, in particular prodrugs of MK-7 in which the diketone is converted to a monosubstituted or disubstituted ester type derivative. These compounds are shown to give MK-7 in plasma.

Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.

Abstract: The present invention relates to the treatment and/or prevention of Alzheimer's Disease or the symptoms associated therewith by daily administration of a drink formula comprising fresh marine omega-3 oil in an emulsion and resveratrol or derivatives thereof.

Abstract: Pharmaceutical formulations for co-administering estradiol and progesterone are provided herein. In some embodiments, the formulation comprises solubilized estradiol, suspended progesterone, and a medium chain (C6-C12) oil.

Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.

Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.

Abstract: The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R1 is selected from the group consisting of —OH, ?O(carbonyl), H, and C1-C3 alkyl; R2 is selected from the group consisting of —OH, H, and C1-C3 alkyl; R3 is selected from the group consisting of —OH, ?O, H, and C1-C3 alkyl; R4 is selected from the group consisting of —OH, H, and C1-C3 alkyl; and none, one, two, three or four of R1, R2, R3, and R4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

Abstract: This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.