Abstract: The embodiments of present invention provide processes for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms, such as tablets, made by these processes. Additionally, embodiments of the present invention provide tablets including 25 mg, 50 mg, 100 mg, or 200 mg free base equivalent of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide hemisuccinate.

Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R6, R7, R8 and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.

Abstract: A pharmaceutical composition comprises a Quisqualis indica extract as an active ingredient, for preventing or treating prostatic hyperplasia, and may also be used in a food composition. The Quisqualis indica extract may be used to treat and prevent prostatic hyperplasia by exhibiting effects of a reduction in prostate weight, a reduction in DHT as a prostatic hyperplasia inducing factor, and a reduction in prostate epithelial cell hyperplasia.

Abstract: A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I).

Abstract: Compounds and compositions are disclosed in which a NAMPT Drug Unit is linked to a targeting Ligand Unit through a Unit from which a NAMPT inhibitor compound or derivative thereof is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease, using the compounds and compositions of the invention are also disclosed.

Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R6, R7, R8 and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: The present invention provides a drug for preventing or treating chronic pain and a method for preventing or treating chronic pain. A pharmaceutical composition comprising a serotonin-3 receptor agonist such as a compound represented by the following formula (I): [wherein: m is an integer of 1 to 4; and R1 is each independently selected from the group consisting of a hydrogen atom, a halogen atom, a methyl group optionally substituted with 1 to 3 halogen atom(s), a methoxy group optionally substituted with 1 to 3 halogen atom(s), and a methylthio group optionally substituted with 1 to 3 halogen atom(s)] or a pharmaceutically acceptable salt thereof is useful for preventing or treating chronic pain. The above pharmaceutical composition is also useful for preventing or treating acute pain. Further, the present invention provides a method for screening a compound for preventing or treating chronic pain, the method comprising measuring a serotonin-3 receptor agonist activity.

Abstract: The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme.

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure and related disorders thereto.

Abstract: The present invention relates to an active pharmaceutical ingredient selected from N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride, its stereoisomers and the acid addition salts thereof (arimoclomol), for use in a method of treating glucocerebrosidase associated disorders.

Abstract: Disclosed is a new crystal form of a 5-aminopyrazole carboxamide compound as shown in Formula (I). Also disclosed are a preparation method for said crystal form of said compound, a pharmaceutical composition of said crystal form of said compound, and uses thereof.

Abstract: The subject disclosure is directed to functionalized bile acids, preparation thereof, and usage thereof for therapeutic and material applications. In one embodiment, a method of generating functionalized bile acid materials can comprise directly activating a carboxylic acid of a bile acid compound using a coupling agent comprising an amide or ester compound, thereby generating an intermediate bile acid derivative material. The method can further comprise attaching a functional group material to the intermediate bile acid derivative material by reacting the functional group material and the intermediate bile acid derivative material, thereby generating a functionalized bile acid material.

Abstract: Disclosed herein are substituted imidazopyridine compounds of formula (I) which are inhibitors of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan-2,3-dioxygenase (TDO) enzymes: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.

Abstract: The present invention provides a drug for treating cocaine addiction or preventing the relapse of the same. Specifically, the present invention provides a drug for treating cocaine addiction or preventing the relapse of the same containing (R)-2-{3-[1-(5-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are novel dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.

Abstract: Provided herein are small molecule compounds of the following formula (I): or a stereoisomer, tautomer, solvate, ester or pharmaceutically acceptable salt thereof, wherein A, B, C, L1, L2, R2, R3, R4, R3, w, x, y and z are as defined herein. Methods for treating diseases/disorders by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also disclosed. Such diseases/disorders are e.g. neurological diseases/disorders such as e.g. Alzheimer's Disease, Lewy Body Dementia and the cognitive deficits associated with schizophrenia, Parkinson's Disease, drug induced Parkinsonism, dyskinesias, dystonia, chorea, levodopa induced dyskinesia, cerebral palsy, progressive supranuclear palsy, and Huntington's disease. Preferred compounds are e.g. N-[2-(1-benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1-carboxamide derivatives and related compounds wherein the pyrazine has been replaced by e.g. pyridazine, pyrimidine, pyridine or phenyl.

Abstract: Compounds of the formula I in which X, Q, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.

Abstract: Disclosed are compounds that are shown to inhibit the biological activity of nitric oxide synthases (NOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of nitric oxide synthases (NOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with NOS activity.

Abstract: Novel compositions including bepotastine besilate and a corticosteroid are provided, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

Abstract: The present invention relates to the crystalline forms of a 5-HT1F receptor agonist 2,4,6-trifluoro-N-[6-[(1-methyl-piperidine-4-yl)carbonyl]pyridin-2-yl]-benzene formamide (lasmiditan) and its hydrochloride. The crystalline forms of the present invention have advantages in crystallinity, hygroscopicity, morphology, crystal form stability, and chemical stability as compared with the known forms of lasmiditan and lasmiditan hydrochloride. The present invention also relates to processes for the preparation of the crystalline forms of lasmiditan and lasmiditan hydrochloride, pharmaceutical compositions thereof and their use in treating and/or preventing a patient's migraine and other diseases or conditions associated with 5-HT1F receptor dysfunction.

Abstract: The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention.

Abstract: The invention concerns compounds that possess a high affinity at 5-HT1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.

Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.

Abstract: The disclosure relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl)amino)benzoate, including the polymorphic form A, mixtures of the polymorphs, process for the preparation thereof and the use thereof in a pharmaceutical composition containing thereof.

Abstract: The present invention provides N-benzyl-3-sulfonamidopyrrolidines and related compounds, as well as pharmaceutical compositions and sanitizing compositions containing the same. The compounds and compositions are useful as antibiotic agents. Methods for making and using the compounds and compositions are also described.

Abstract: Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): wherein all symbols represent the same meanings as those described in the description, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.

Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

Abstract: Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: X1-L-X2 wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.

Abstract: A medicament or pharmaceutical composition for the treatment of exacerbations of asthma and chronic obstructive pulmonary disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating exacerbations of asthma and chronic obstructive pulmonary disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.

Abstract: A medicament or pharmaceutical composition for the treatment of respiratory syncytial virus, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating respiratory syncytial virus includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.

Abstract: A method for preparing a compound of formula I: or a pharmaceutically acceptable salt thereof, by heating of dicarboxylic acid monoamide of formula II with a dehydrating agent in an organic solvent.

Abstract: Biologically active glutarimide derivatives of the following formula: or a pharmaceutically acceptable salt thereof.

Abstract: A medicament or pharmaceutical composition for the treatment of a respiratory tract disease, which is a compound having the following formula: or a pharmaceutically acceptable salt thereof. A method of treating a respiratory tract disease includes administering to a patient an effective amount of the compound or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention relates to a compound of formula (I), a stereomeride, pharmaceutically acceptable salt, a solvate or an N-oxide thereof, a medicine composition comprising the compound, a method for preparing the compound, and a usage of the compound in treating diseases related to Hsp70. The diseases are preferably selected from tumors, neurodegenerative diseases, and allogeneic transplantation rejection and infection.

Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.

Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

Abstract: Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: X1-L-X2 wherein L is a linking moiety comprising an enone; and X1 and X2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.

Abstract: This invention relates to novel pyrazole-substituted amino-heteroaryl compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of anaplastic lymphoma kinase (ALK).

Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: The invention relates to protein-adhesive dyes, to the preparation thereof and to preparations comprising same, and to a method for coloring keratin-containing fibers, in particular for coloring human hair.