Abstract: The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.

Abstract: In some aspects of the present invention is a formulation comprising a solid dispersion or intimate mixture of a poorly water soluble drug and an ionic polymer surprisingly exhibiting fast disintegration of tablet.

Abstract: Abuse deterrent solid dosage formulations containing 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 processes for the preparation and administration of these formulations.

Abstract: The present invention provides new compounds of formula I(a)-I(d) and II, The compounds can inhibit cancerous inhibitor of protein phosphate 2A (CIP2A), can be used as protein phosphate 2A (PP2A) accelerator and oncoprotein SET antagonist, and can treat cancers effectively.

Abstract: The present invention relates to 2,4-diaminopyrimidines and pharmaceutically acceptable salts thereof, purification methods for the same, pharmaceutical compositions containing them, methods of obtaining and using them for the treatment of disease states, disorders, and conditions mediated by the histamine H4 receptor activity.

Abstract: The present invention provides antibodies that bind FGFR2IIIb, wherein the antibodies are afucosylated. The present invention provides compositions comprising antibodies that bind FGFR2IIIb, wherein at least 95% of the antibodies in the composition are afucosylated. In some embodiments, methods of treating cancer comprising administering afucosylated anti-FGFR2IIIb antibodies are provided.

Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.

Abstract: The present invention relates to a composition for preventing or treating renal diseases. The composition of the present invention improves lipid metabolism, prevents histological damage including renal fibrosis, alleviates microalbuminuria, and maintains nephrons of renal glomeruli. Therefore, the composition is useful for treating renal diseases.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: Described herein, inter alia, are compositions and methods of using the same for modulating the activity of Ire1 using for example, substituted imidazopyrazine compounds.

Abstract: The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

Abstract: A method for selecting an access network in a terminal of a mobile communication system according to one embodiment of the present specification comprises the steps of: if traffic is generated in the terminal, selecting an access network according to the characteristics of the generated traffic and network selection policy information; and transmitting and receiving the generated traffic via the selected access network. According to the embodiment, the present invention adjusts priorities of accesses given to users and applications in a wireless communication system including heterogenerous networks, thereby reducing processes for reselecting an access network of a user terminal, and reducing the cases of unnecessarily accessing a network having a low priority or requiring high costs for a long time. Therefore, the present invention can enhance user convenience and improve communication efficiency.

Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

Abstract: This disclosure relates to: (a) compounds and salts of formula (I), formula (II), formula (III), and formula (IV), that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”) useful for the treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved (e.g. mood disorder, schizophrenia, etc.). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is one of the groups represented below wherein A is a bond, CH?CH or C?C; U is N or CH; V is N or CH; W represents N or CH; and R1A, R2A, R3A, R1B and R1C are as defined in the claims; and salts thereof.

Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: The present invention describes a novel process for preparing piperidine-4-carbothioamide hydrochloride.

Abstract: Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.

Abstract: The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N?-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer.

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

Abstract: Compositions comprising L-carnitine or a salt thereof, acetyl L-carnitine or a salt thereof, vitamin B9 (folic Acid), vitamin A, vitamin B12, vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine), arginine, vitamin C, vitamin E (?-Tocopherol), selenium, zinc, copper, iron, vitamin D and N-acetyl cysteine, and optionally one or more pharmaceutically acceptable excipients are provided. Dietary supplements comprising these compositions are also provided.

Abstract: The present invention relates to a novel 4-(aryl)-N-(2-alkoxythieno[3,2-b]pyrazin-3-yl)-piperazin-1-carboxamide derivative compound useful in the prevention or treatment of cancer; a preparation method thereof; and a pharmaceutical composition comprising the same. The novel 4-(aryl)-N-(2-alkoxythieno[3,2-b]pyrazin-3-yl)-piperazin-1-carboxamide derivative compound of the present invention can effectively inhibit the growth of proliferating cells, and thus can be useful in the prevention or treatment of cancer.

Abstract: The present invention provides a pharmaceutical composition, as an effective ingredient, a urea compound having a protein kinase inhibitory activity and containing a 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one skeleton, and a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to a compound of Formula (I).

Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as described in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.

Abstract: The invention provides a hair shaping composition suitable for topical application to hair, the composition comprising from 1 to 25 wt % monoglucosamine adipate, dissolved or dispersed in an aqueous carrier. The invention also provides a method for improving hair volume-down which comprises the following steps: (i) treating the hair by topical application of the hair shaping composition as defined above; (ii) shaping the treated hair; (iii) allowing the composition to remain in contact with the shaped hair before drying. Advantageously the method of the invention does not require the breakage of the hair disulfide bonds, does not require the use of high temperature heated implements such as straightening irons, and can be accomplished by a consumer without intervention of a professional hairdresser.

Abstract: The present invention relates to a stable ophthalmic suspension formulation comprising (R)-(?)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3?-pyrrolidine-1,2?,3,5?-tetrone, which is useful for treating a disease in posterior eye segment and the like, avoiding side-effects due to systemic exposure.

Abstract: The present invention provides methods of preventing and/or reducing risk of neurodegeneration of association cortex, and/or inhibiting or reversing formation of phosphorylated tau or COXIV in the prefrontal cortex of a mammal in need thereof. In certain embodiments, the method comprises administering to the mammal a therapeutically effective amount of an ?2A-adrenergic receptor agonist.

Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

Abstract: The present invention relates to compounds of formula I wherein R1 is hydrogen, F or Cl; L is a bond or lower alkylene; R2 is —(CH2)nO-lower alkyl, lower alkyl substituted by halogen, —(CH2)nC(O)O-lower alkyl, phenyl substituted by lower alkyl or halogen, or is a 5 or 6-membered heteroaryl group, selected from pyridinyl, pyrimidinyl, pyridazinyl, thiazolyl, imidazolyl, pyrazolyl or triazolyl, which are optionally substituted by lower alkyl, halogen, lower alkoxy, ?O, benzyloxy, cycloalkyloxy, hydroxy, cyano, lower alkyl substituted by halogen, or by —(CH2)nO-lower alkyl; n is 1, 2 or 3; R3 is hydrogen, lower alkyl or —(CH2)nO-lower alkyl; R4 is phenyl, pyridinyl or pyrimidinyl, optionally substituted by F; Y is CF or CCl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomers thereof.

Abstract: The present disclosure provides substituted pyridyl-, pyrimidinyl-, pyrazinyl-, pyridazinyl-, and triazinyl-based carboxamides of Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein Z, HET, R10, and E are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I-A to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

Abstract: The present invention relates to pyridine, pyrimidine, and pyrazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I) The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

Abstract: Provided herein are substituted [1,2,4]triazlolo[1,5-?]pyrazine compounds, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorders.

Abstract: Provided herein are methods for treating or preventing chronic lymphocytic leukemia, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound to a patient having chronic lymphocytic leukemia.

Abstract: The invention relates to a 1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-amine compound of formula (I) below, addition salts thereof, optical isomers, geometrical isomers and tautomers thereof and/or solvates thereof: in which: .R2, R3, R4, R5, and R7 independently represent: a hydrogen or halogen atom; a C1-C4 alkyl radical; a C1-C4 hydroxyalkyl radical; a carboxyl radical; a (C1-C4)alkoxycarbonyl radical; .R1 and R6, which may be identical or different, represent: hydrogen atom; C1-C10 and preferably Ci-C6 alkyl radical,—optionally interrupted with one or more heteroatoms chosen from O and S or with one or more groups—NR and/or—optionally terminating with at least one group—NX1X2 or at least one group —OX3, .

Abstract: The present invention provides compounds of formula (I) wherein A, X1, X2, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

Abstract: A cancer cell proliferation inhibitor including at least one selected from compounds represented by Structural Formulae (1) to (8), wherein the cancer cell is at least one of a cancer cell overexpressing a wild-type epidermal growth factor receptor and a cancer cell expressing an epidermal growth factor receptor mutant vIII.

Abstract: The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).

Abstract: The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.

Abstract: The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, R6, Y1 and Y2 have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as acaricides and/or insecticides for controlling animal pests. The compounds of the formula (I) are also suitable as nematicides for plant-damaging pests and/or anthelminthics for endoparasites in humans and animals.

Abstract: The invention relates to new pyridinyl derivatives of the formula wherein R1 and A are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.