Abstract: The present invention relates to a process for preparation of intermediates (Z,2E)-5-hydroxy-2-methoxyimino-N-methyl-pent-3-enamides from 4-substituted 5-meth-oxyimino-2H-pyran-6-ones and their processing for example to (Z)-5-cyclyloxy-2-[(E)-methoxyimino]-3-methyl-pent-3-enic acid methyl amides. The invention also relates to a process for preparation of 4-substituted 5-imino-2H-pyran-6-ones and to novel intermediates for the preparation of fungicidal (Z)-5-cyclyloxy-2-[(E)-methoxyimino]-3-methyl-pent-3-enic acid methyl amides.

Abstract: Novel 2,2?-diamino biaryls of formula (I), (II) and (III), wherein R1-R10, R1?-R10?, X1-X3 and X1-X3? are defined in claim 1. The invention also relates to an electrochemical method for the production thereof.

Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

Abstract: Provided is a photochemical reaction device wherein two partitions formed from an optically transparent material are arranged apart from each other between a light source and a reaction liquid, and an optically transparent fluid introduction/discharge means for introducing an optically transparent fluid between the partitions and discharging the fluid and a state change detection means for detecting a change in the state of the optically transparent fluid at the discharge side of the optically transparent fluid introduction/discharge means are provided. Also provided are a photochemical reaction method that uses the photochemical reaction device and a lactam production method that uses the photochemical reaction method. The present invention prevents decreases in the performance of the light source even when the optically transparent material in the photochemical reaction device is damaged, and makes it possible to reliably prevent ignition even if the reaction liquid is a flammable liquid.

Abstract: The present invention discloses a pyrrolic amide compound shown as a formula I, or crystal forms thereof, and pharmaceutically acceptable salts, hydrates or solvates, wherein R1 is selected from hydrogen, hydroxyl, cyano, halogen, carboxyl, C1-C6 alkyl and the like; R2 is selected from hydrogen, hydroxyl, cyano, halogen and the like; R3 is selected from hydroxyl and the like; X is selected from group, m is equal to 0, 1, 2 or 3, and n is equal to 0, 1 or 2. The novel compound shown as the formular I provided by the present invention has high deacetylase inhibitory viability; and meanwhile, a method for preparing the novel compound in the present invention has the advantages of fewer steps, simple and convenient operation, safety, environment friendliness, high yield and the like and is very suitable for industrial application.

Abstract: The present invention concerns mono- or di-substituted indole derivatives (I) which are useful to prevent or treat dengue viral infections and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Abstract: A stable Crystalline Form II of non-solvate of Apremilast (Formula I), methods of making Form II, pharmaceutical compositions comprising Form II, and their uses are disclosed. Also discloses are mixed crystals comprising Form Hand Form B and methods of making the same. The crystalline forms are characterized using X-ray powder diffractometry (XRPD), infrared spectroscopy (IR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TG). As compared with Forms A, B, C, D, E, F, and G reported in prior art references, Apremilast Form II of the present invention is more stable to temperature, light, and humidity, and is more suitable for long term storage; the crystallization solvents are safe and can be easily removed; the Form II has a white or off white appearance, and can be directly used in preparation processing; the preparation methods are simple and easy to reproduce, and are suitable for industrialized production.

Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

Abstract: The invention generally relates to methods and compounds for treating proliferative disorders, viral infections, or both. In some embodiments, the invention provides an anticancer or antiviral compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating a proliferative disorder or a viral infection including administering an anticancer or antiviral compound that binds to a thromboxane receptor, has preferential binding for either TPalpha (TP?) or TPbeta (TP?) receptor subtype.

Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.

Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.

Abstract: A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates to a RAFT agent of formula (I) where R1, R2 and R3 are each independently selected from H and optionally substituted alkyl.

Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) 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 a method of manufacturing a fluorocytosine-based compound of Formula I. The invention also relates to a compound obtained by such a method, a pharmaceutical drug substance and a method for its manufacture, a pharmaceutical composition, and also various uses in therapy of the compounds, pharmaceutical drug substances, and pharmaceutical compositions of the invention.

Abstract: Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.

Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II. X1 to X4 of Formulas I and II may be characterized as electron withdrawing groups, while Y1 to Y4 of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may capable of one or both absorbing and emanating spectral energy of at least about 400 nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.

Abstract: Novel UV absorbers of benzotriazine type having a plurality of (meth)acryloxy groups have a UV absorbing capacity and a high solubility in multifunctional (meth)acrylate. By combining the (meth)acrylic functional UV absorber with various binder precursors such as photo-curable multifunctional (meth)acrylate, there are obtained coating compositions having improved crosslinking density, UV absorbing capacity, anti-bleeding property, and shelf stability.

Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Abstract: A catalytic system containing a titanium zeolite of structure type MWW optionally containing zinc and containing at least one of an inorganic potassium salt and an organic potassium salt is provided. The catalyst system is useful in the preparation of propylene oxide.

Abstract: A process for recovering an ethylene oxide (EO) enriched product stream from fat absorbent (FA) comprising water, EO, and acetaldehyde. The process comprises passing a feed of FA from a loopgas EO absorber to a multi-stage countercurrent distillation zone, the feed of FA having a concentration of EO in the range of from about 1 to about 15 wt % upon entering the distillation zone; and obtaining from the distillation zone an acetaldehyde enriched stream, a lean absorbent (LA) stream, a vapour stream enriched in light ends, a glycol enriched bottoms stream and an EO enriched product stream. Suitable apparatus is also disclosed.

Abstract: Industrial scale conversions of 5-hydroxymethylfurfural to commodity chemicals such as 1,2,6-hexanetriol and 1,6-hexanediol by chemocatalytic conversions using hydrogen and a heterogeneous reduction catalyst are provided. The reactions are suitable for use in continuous flow reactors. Methods of carrying out the conversions are provided, as are product and catalyst compositions.

Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

Abstract: The present invention discloses a fast and selective process for the preparation of ?-valerolactone (Gvl) by catalytic hydrogenation of biomass-derived levulinic acid (LA) using recyclable ruthenium (Ru)-based heterogeneous catalysts in aqueous medium in stoichiometric yields (100%) under mild reaction conditions using nearly required amount of hydrogen.

Abstract: There is provided a one-pot process for the conversion of sugars to furancarboxylic acids, such as 2,5-furancarboxylic acid (FDCA), in a triphasic system (e.g. water or tetraethylammonium bromide (TEAB)—methyl isobutyl ketone (MIBK)—water). In this reaction setup, sugars are first converted to 5-hydroxymethylfurfural (HMF) in a first phase. Then HMF is then extracted into a second phase and transferred to a third phase of water. In the third phase HMF is converted to the furancarboxylic acid. The overall acid yields obtainable are between about 78% and 50% for conversion from fructose and glucose, respectively. The invention further relates to an apparatus for the triphasic reaction. The apparatus comprises two chambers which allow for the chemically separated reaction of the sugars and the intermediate of the sugars to form the final product in one process. The process according to the invention may be useful for industrial fabrication.

Abstract: The present disclosure relates to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease.

Abstract: This specification generally relates to 1-alkyl-6-oxo-1,6-dihydropyridin-3-yl compounds (including salts thereof). This specification also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including treatment methods and medicament preparations), and processes for making such a compound.

Abstract: Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions.

Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu

Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.

Abstract: Deuterated domperidone compositions, methods of synthesis, methods of use, and dosing formulations providing beneficial safety and other effects.

Abstract: The present invention relates to specific novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy as bromodomain inhibitors.

Abstract: This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.

Abstract: The present disclosure relates to a bicyclic compound, a pharmaceutical composition thereof, and its novel use. More particularly, the present disclosure relates to the bicyclic compound according to Formula I or Formula II, the pharmaceutical composition for treating a stroke, and the use of the bicyclic compound treating the stroke.

Abstract: Described herein are ester prodrugs of gamma-lactam compounds of Formula (I): or pharmaceutically acceptable salt thereof, and methods of use of such compounds for the treatment of ocular diseases including, among other things, glaucoma and macular degeneration.

Abstract: An AdipoR activator for activating both AdipoR1 and AdipoR2 is provided. A compound represented by the following formula (1), wherein A is a substituted or unsubstituted aryl group or the like, Y1 is (CHR2)a— or the like, X is CH or N, R1 is a C1-7 alkyl group, m is an integer of 0-4, Y2 is *—O—CH2—CONH—, *—CONH—(CH2)b—CO— or the like, Z is a cyclic group, B may be a substituent of the cyclic group represented by Z, and n is an integer of 0-3.

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyrazinylamino)-propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.

Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

Abstract: The present patent application discloses at least the compounds according to Formula Ia and Formula Ib shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, JB, n, J, RC1, RC2, Z1, Z2, W, X, Y1, Y2, JF and R9 are as defined herein.

Abstract: Described herein are small-molecule compounds that specifically inhibit a wide range of HIV-1 isolates without interfering with CD4 or CCR5 binding. Methods of using die compounds for treating or preventing HIV infection are also described.

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: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect, e.g. a compound of Formula (I): wherein R2 is a hydrogen atom or the like; ring A is five- to seven-cycloalkane or the like; C is a carbon atom; Q1 and Q2 are carbon atoms or the like; R9a and R9b are carbon atoms or the like; R6 is cycloalkyl or the like; R7 is a group represented by the formula: wherein ring D is benzene or the like; carbon atom a and b are carbon atoms; ring B is an aromatic carbocyclic ring or the like; s and s? are 0 or the like; R9 and R9? are halogen or the like, or the like, or its pharmaceutically acceptable salt.

Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

Abstract: This invention relates to novel compounds. The compounds of the invention are kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Raf kinases, e.g., B-Raf and C-Raf. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Raf kinases, for example, cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia.