Abstract: The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).

Abstract: A problem to be solved by the present invention is to provide a method for ameliorating pollakiuria and nocturia, in particular, nocturia caused by nocturnal polyuria by finding a composition that enhances the antidiuretic action of vasopressin or a vasopressin V2 receptor agonist. As a result of the studies, it has been found that imidafenacin enhances the antidiuretic action of vasopressin or the vasopressin V2 receptor agonist, whereby the present invention has been completed. According to the present invention, a composition containing imidafenacin can enhance the antidiuretic action of vasopressin or the vasopressin V2 receptor agonist, making it possible to ameliorate pollakiuria and nocturia, in particular, nocturia caused by nocturnal polyuria.

Abstract: The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).

Abstract: Certain embodiments are directed to C70 fullerene derivatives N—N-dimethyl [70]fulleropyrrolidinium iodide. Certain further embodiments are directed to ?, ? and ? isomer of N—N-dimethyl[70]fulleropyrrolidinium iodide.

Abstract: The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor.

Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.

Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.

Abstract: Provided is an agricultural plant-protecting agent including a dipeptide derivative or an agro-pharmaceutically acceptable salt thereof as an active ingredient, which has a plant disease-preventing effect, a plant growth-promoting effect, and a plant immunity-activating effect.

Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.

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: Disclosed are peptides having biological and therapeutic activity. Particularly disclosed are lipidated di- or tri-peptides analogs of KPV or KdPT that exhibit antimicrobial activity. In particular, the peptides of this invention provide enhanced anti-microbial activity over the base tri-peptides, lysine-proline-valine and lysine-d-proline-tyrosine. The disclosed peptides have the general formula of C12-18 lipid-KXZ-NH2i wherein K is lysine; X is proline, d-proline, histidine or arginine; Z is optional and if present Z is valine, threonine, alanine or leucine; and the terminal COOH is NH2 amidated. The C12-18 lipid is preferably the lipid moiety of lauric acid (C12), myristic acid (C14), pentadecanoic acid (C15), palmitic acid (C16), or stearic acid (C18). The invention is further related to methods of using of these peptides to treat various insults, inflammations or bacterial infections affecting the skin and other related mucosal body surfaces such as the oral cavity.

Abstract: The invention relates to medicine and comprises an agent for the treatment of a viral hepatitis C, which is glutaryl histamine or a pharmaceutically acceptable salt thereof. This agent can also be administered in combination with a pegylated interferon and ribavirin. The invention further relates to a pharmaceutical composition for the treatment of a viral hepatitis C. This invention solves the problem of providing a novel agent, which is effective in the treatment of a viral hepatitis C and makes it possible to produce a sustained virologic response.

Abstract: The present invention relates to N-acyl derivatives of amino acids and pharmaceutically acceptable salts thereof wherein n is 2 or 3; and R1 represents or pharmaceutically acceptable salts thereof, to novel processes for preparing the same, to use thereof as anti-allergic, anti-anaphylactic, anti-inflammatory and hypolipidemic agents as well as to a pharmaceutical composition comprising the indicated compounds in an efficient amount and to a method for treating allergic and inflammatory diseases and lipid metabolism disorders: bronchial asthma, allergic rhinitis, pollinoses, seasonal and year-round rhinitis, allergic pneumonitis, atopic dermatitis, psoriasis, urticaria, allergic (including anaphylactic) reactions to insect stings and medicaments, cold allergy, allergic conjunctivitis, atherosclerosis, obesity, ischemic heart and cerebral disease, myocardial infarction and stroke.

Abstract: This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.

Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.

Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

Abstract: Described is a dipeptide comprising a non-proteogenic amino acid, methods of making such and methods of using said dipeptide in a process of making a polypeptide or protein comprising one or more non-proteogenic amino acids.

Abstract: The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.

Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.

Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.

Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.

Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Abstract: Cell culture media comprising antioxidants are provided herein as are methods of using the media for cell culturing and polypeptide production from cells. Compositions comprising polypeptides, such as therapeutic polypeptides, produced by the methods herein are also provided.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: A method for treating an autism spectrum condition includes administering an effective dose of a TNF-? inhibiting agent to a person having an autism spectrum condition or pervasive development disorder and at least one of elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum, as compared to normal conditions; and lowering at least one of the elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum. A TNF-? inhibiting agent includes at least one of Lenalinomide; Thalidomide; L-Carnosine; Infliximab; Etanercept; a stem cell preparation; derivatives thereof, isomers thereof, or pharmaceutically acceptable salts thereof.

Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Abstract: The present invention aims to provide a compound superior in broad utility and stability, which is useful as a protecting reagent (anchor) of amino acid and/or peptide in liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide (—CONHR)-type, an organic synthesis reaction method (particularly peptide liquid phase synthesis method) using the compound, and a kit for peptide liquid phase synthesis containing the compound, and has found that the object can be achieved by a particular compound having a diphenylmethane skeleton.

Abstract: New cationic lipids are provided that are useful for delivering macromolecules, such as nucleic acids, into eukaryotic cells. The lipids can be used alone, in combination with other lipids and/or in combination with other transfection enhancing reagents to prepare transfection complexes.

Abstract: A multifunctional polymerizable ionic liquid is described comprising an anion and a cationic group having at least two ethylenically unsaturated polymerizable groups, each bonded to the cationic group via a divalent non-alkyl linking group. The multifunctional linking groups independently comprise a heteroatom such as oxygen or nitrogen. The linking groups may independently comprise one or more linkages such as an amide, urea, and more typically a urethane or ester linkage. The ethylenically unsaturated polymerizable groups are typically (meth)acrylate groups. Coatings and coated articles are also described.

Abstract: The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: An amphoteric liposome comprising neutral lipids wherein said neutral lipids are selected from the group comprising cholesterol or mixtures of cholesterol and at least one neutral or zwitterionic lipid and wherein K (neutral) of said mixtures is 0.3 or less. Said amphoteric liposome may encapsulate an active agent, such as nucleic acid therapeutics. Also disclosed are pharmaceutical compositions comprising said amphoteric liposomes as a carrier for the delivery or targeted delivery of active agents or ingredients.

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.

Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.

Abstract: An ionic compound has the formula (I): in which, R1 is selected from the group consisting of hydrogen, a C1-C20 alkyl, and an aromatic group; R2 is selected from the group consisting of a carbonyl and a C1-C10 alkyl; and R3 is selected from the group consisting of an imidazole ring, a C1-C20 alkyl, an acrylic group, and an aromatic group; X? is selected from the group consisting of Cl?, Br?, I?, NO3?, AlCl4?, BF4?, CF3SO3?, (CF3SO3)?, CF3COO?, CH3COO?, and PF6?; and k is an integer 1 or 2. The ionic compound can be added in a pressure-sensitive adhesive of a polarizer of a liquid crystal display panel to avoid the phenomenon of the static electricity residual when the release film is removed from the pressure-sensitive adhesive.

Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.

Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.

Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

Abstract: This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.

Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).