Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,

Abstract: This disclosure provides novel imidazopyridazine compounds of formula (I) and pharmaceutical acceptable salt thereof, pharmaceutical compositions containing them, a process for preparing them, and their practical effect in inhibiting PI3K and potential use in treating a disease responsive to inhibition of PI3K, for example, an inflammatory disease, autoimmune disease or cancer.

Abstract: The present invention provides an agent for treating malignant tumor, comprising a compound of formula (1): wherein R1 to R4 are hydrogen atom, halogen, or etc., Y is optionally-substituted alkylene group or etc.

Abstract: The present invention relates to a compound represented by Formula I, a racemate or optical isomer thereof, or a pharmaceutically acceptable salt, a solvate or a hydrate thereof, a pharmaceutical composition comprising the compound, and a use thereof in the manufacture of a medicament for preventing and/or treating a disease or disorder associated with a viral infection.

Abstract: The present invention provides a 2,4,6-trisubstituted s-triazine compound represented by general formula (I) or pharmaceutically acceptable salts, prodrugs or solvates thereof, a preparation method therefor, and use of these compounds in preparing drugs for preventing or treating diseases associated with protein kinase and vimentin dysregulation, and cell vacuolization, and in particular, drugs for treating or preventing cancer growth and metastasis, tissue fibrosis and atherosclerosis.

Abstract: Provided herein are cinchonium betaine catalysts and methods of promoting asymmetric imine isomerization reactions using the same.

Abstract: The present invention is related to an improved process for the preparation of Ceritinib with high yield and high purity. The present process is cost effective and feasible in large scale production also. The present invention also related to a stable amorphous form of Ceritinib and its preparation. The present invention also relates to a process for the preparation of Crystalline form A of Ceritinib.

Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.

Abstract: The present application relates to treatment of myeloproliferative neoplasms using the JAK1/JAK2 inhibitor, ruxolitinib, in combination with a low dose of a Pim inhibitor, N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, wherein the combination is unexpectedly synergistic at a very low dose of the Pim inhibitor.

Abstract: Disclosed are compounds of formula (I) below or pharmaceutically acceptable salts thereof: in which each of variables R1-R6, L, m, and n is defined herein. Also disclosed are a method for treating an opioid receptor-associated condition with a compound of formula (I) and a pharmaceutical composition containing same.

Abstract: The present invention provides compounds of Formula I, Pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: The present invention relates to new compounds of general formula (I) that show great affinity and activity towards the subunit ?2? of voltage-gated calcium channels (VGCC), especially ?2?-1 subunit of voltage-gated calcium channels or dual activity towards subunit ?2? of voltage-gated calcium channels (VGCC), especially ?2?-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Abstract: Disclosed embodiments concern kinase inhibitors having a structure according to formula 1, such as interleukin receptor associated kinases (IRAK) inhibitors, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent a kinase-associated disease or condition, particularly an IRAK-associated disease or condition.

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: Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. More particularly, compounds of formula II have utility in a variety of therapeutic uses such as treatment of pain, inflammation, neuropathy, or appetite disorder.

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, R2, R3, R4 and R5 are defined herein, which are suitable for the treatment of diseases related to Bruton's tyrosine kinase (BTK), and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

Abstract: Provided is an EGFR inhibitor and a pharmaceutically acceptable salt and a polymorph thereof, and a use thereof. In particular, provided is a polymorph, a pharmaceutically acceptable salt or a prodrug of N-(2-(4-(dimethylamino)piperid-1-yl)-5-(5-fluoro-4-(1-methyl-1H-pyrazol-4-yl) pyrimidin-2-ylamino)-4-methoxy phenyl) acrylamide. In addition, also provided is a pharmaceutical composition containing the inhibitor and a use thereof.

Abstract: The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1, R2, R3, L1, L2, L3, L4, L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.

Abstract: The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.

Abstract: Orbit azine-fumarate compounds are provided having the following formula: Different crystal forms of orbit azine-fumarate, an orbit azine-fumarate hydrate and a crystal form thereof, and an amorphous form of orbit azine-fumarate are prepared by adjusting the ratio of orbit azine and fumaric acid and using different crystallization methods. The invention makes it possible to provide an orbit azine-fumarate which has a higher pharmaceutical effect, is easier to prepare, and has improved storage stability.