Abstract: The present invention relates to 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid.

Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

Abstract: This invention provides a pridopidine base in a solid form, a method of preparing the solid pridopidine base, and a composition comprising the pridopidine base including a pharmaceutical composition.

Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.

Abstract: The invention discloses compounds of Formula I wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

Abstract: The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.

Abstract: This invention relates to 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 a CFTR potentiator.

Abstract: The invention relates to a method for the production of 4,4?-methylenebis(phenylisocyanate) dimer (MDI dimer) which is distinguished by an MDI dimer being obtained which is present in high purity. The MDI dimer which is produced according to the method according to the invention is distinguished by being essentially free of MDI and also urea derivatives. Furthermore, the invention relates to a corresponding MDI dimer and also the use thereof as crosslinker for polyurethanes.

Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract: Newly synthesized thiourea-modified 3-chloro-4-fluoroanilino-quinazoline derivatives have been studied as terminal carrier ligands in linear gold(I) complexes. The molecules mimic the tyrosine kinase inhibitor gefitinib (by computational docking experiments). Thiourea groups were either directly attached to quinazoline-C6 or linked to this position via a flexible ethylamino chain. One compound tested acts as a thiourea-S/quinazoline-N1 mixed-donor ligand, giving an unusual dinuclear complex as determined by X-ray crystallography and/or electrospray mass spectrometry. One compound formed the desired stable linear complex. The biological activity of the carrier ligands and corresponding gold(I) complexes was studied in NCI-H460 and NCI-H1975 lung cancer cells. One compound that was tested partially overcomes resistance to gefitinib in NCI-H1975 (with IC50 values of 1.7 and 30 ?M, respectively), and the corresponding gold complex (13) maintains activity in the low-micromolar concentration range.

Abstract: A compound of Formula II, is provided. R1, R2 and R3 are independently either hydrogen, alkyl, aryl, halogen, alkoxy, nitro, amino or hydroxyl. X is either F, Cl, Br, I or CN. Y is either N or CH. Compositions that include Formula II can be used to inhibit vacuolar H+ ATPase.

Abstract: Described herein are kinase inhibitors represented by Formula I: pharmaceutical compositions thereof, and uses thereof including but not limited to uses in treatment of cancer.

Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

Abstract: Water-soluble triazabutadiene molecules and methods for producing and using such compounds. The triazabutadiene molecules may be more labile at pH levels below physiological pH, such as pH 7, pH 6, pH 5, etc. The triazabutadiene molecules and compounds may be used for depositing diazonium salt and/or cargo in a pH-sensitive manner. The triazabutadiene molecules may alternatively be cleaved in reducing conditions or as a light-catalyzed reaction. The compounds herein may be used for delivery of drugs, as part of detection systems, or for other applications such as underwater adhesive applications.

Abstract: Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided.

Abstract: A method for improving the oxygen-releasing ability of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes to organs or peripheral tissues in human bodies is disclosed by administering a compound of phthalides to a subject in need thereof. The compound of phthalides is characterized by a phthalide functional group which is represented as Formula I, and forms at least one hydrogen bond with ?Arg141 of hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes, stabilizing the ?1/?2 interface of hemoglobin, further stabilizing the oxygenated hemoglobin, hemoglobin variants, recombinant hemoglobin or hemoglobin-based blood substitutes in the low oxygen affinity “T” state and facilitating the oxygen release to the organs or the peripheral tissues.

Abstract: The invention relates to compounds of the following general formula (I) in the form of one of the enantiomers thereof or a mixture of the enantiomers thereof, and the pharmaceutically acceptable salts and/or solvates thereof, especially for the use thereof as a medicament, more specifically in cancer treatment. The invention also relates to pharmaceutical compositions containing same and to the methods for the production thereof.

Abstract: The present invention relates to a method of preparing chromanes from 2,5-dimethylfuran and substituted alkynes comprising an long chain unsaturated alkyl group as substituent in the alpha position of a substituted phenol followed by oxidation, reduction and acid ring closure. It is particularly advantageous to use 2,5-dimethylfuran as this offers an ecological beneficial synthesis of ?-tocopherol.

Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris

Abstract: The present invention provides a composition for preventing or treating kidney disease, the composition comprising a pyrazole derivative compound or a pharmaceutically acceptable salt thereof; and the composition of the present invention is effective in reducing proteinuria, reducing cell formation between glomerular blood vessels and suppressing kidney fibrosis.

Abstract: The problem addressed by the present invention is to provide a novel method for separating and purifying pure enantiomer of lenalidomide. Pure enantiomer of lenalidomide can be separated and purified by using, as the mobile phase, an organic solvent selected from the group consisting of aprotic solvents, secondary alcohols, and mixtures thereof.

Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.

Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.

Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: Z is selected from O, S and N; Y is N X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof.

Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.

Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.

Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the sam

Abstract: The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.

Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the A1-A4, T, W, Q, R1 and Z1-Z3 radicals are as defined in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Abstract: Provided herein are deuterated O-sulfated beta-lactam hydroxamic acids and deuterated N-sulfated beta-lactams, pharmaceutical compositions thereof and methods of treating infectious disease with deuterated compounds or pharmaceutical compositions thereof.

Abstract: Aminothiazole compounds of Formula (I) shown herein and pharmaceutical compositions containing one of such compounds.

Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.

Abstract: The invention relates to compounds of Formula (I) wherein R1 and R2 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.

Abstract: A compound according to Formula Ia: wherein L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

Abstract: This application relates to imidazolone compounds, pharmaceutically acceptable salts, solvents, polymorphs or prodrugs thereof, and further relates to pharmaceutical combinations comprising the foregoing substances and uses for preventing and treating protein kinase related diseases such as cancer, metabolic diseases, and cardiovascular diseases.

Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

Abstract: The present invention is directed to imidazo[1,5-a]pyridine and imidazo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.

Abstract: The present invention relates to novel antiproliferative 1H-1, 8-naphthyridin-2-ones of the general formula (I) or pharmaceutically acceptable salts thereof: In which the variable groups are as defined herein, and their preparation and use in therapeutic treatment of disorders related to inhibition of tyrosine kinases in warm blooded animals. The compounds can overcome imatinib induced drug resistance.

Abstract: In one embodiment, the present application discloses 2-aza-, 2-oxa- and 2-thia-2,3-dihydro-6-azaphenalene compounds and compositions, and methods for treating a neurological disease in a patient in need thereof using the compounds and compositions as disclosed herein.

Abstract: Provided herein are formulations, solid forms and methods of use relating to (1s,4s)-4-(2-(((3S,4R)-3-fluorotetrahydro-2H-pyran-4-yl)amino)-8-((2,4,6-trichlorophenyl)amino)-9H-purin-9-yl)-1-methylcyclohexane-1-carboxamide.

Abstract: A lubricating agent including an ionic liquid formed from a Bronsted acid (HX) and a Bronsted base (B), wherein the Bronsted base has a linear hydrocarbon group having 10 or more carbon atoms and the difference between the pKa value of the Bronsted acid in water and the pKa value of the Bronsted base in water is 12 or more.

Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.

Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.

Abstract: An improved process for the preparation of Triazole and salts thereof, a key intermediate for the synthesis of Sitagliptine is disclosed.

Abstract: The present patent application discloses at least the compounds according to Formula I? shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, ring E, ring F, JB, n, JD, J, o, RC1, RC2, W, JE, r, JF, s, Z1, Z2 and Z3 are as defined herein.

Abstract: The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.