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Antiviral Compounds

Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.

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PYRROLOTRIAZINE COMPOUNDS AND METHODS OF INHIBITING TAM KINASES

Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat cancer. (II), or a pharmaceutically acceptable salt thereof, wherein: R1 is pyridin-3-yl, pyridin-4-yl, pyrazol-4-yl, cyclohexyl, or 8-azabicyclo[3.2.1]oct-2- ene-3-yl, wherein R1 is optionally substituted with up to four independently selected substituents; R2 is cyclohexyl substituted with hydroxy and optionally substituted with one or two additional substituents independently selected from C1-C4 alkyl and fluoro, or is 4,5,6,7- tetrahydro-lH-indazolyl optionally substituted with one to three substituents independently selected from C1-C4 alkyl and fluoro; and R3 is -C3-C8 alkyl, -(C2-C6 alkylene)-0-(C1-C6 alkyl), C3-C6 cycloalkyl, or -(C2-C6 alkylene)-C3-C6 cycloalkyl, wherein R3 is optionally substituted with 1-5 substituents inde endentl selected from deuterium, halo, and -OH.

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N-SULFONYLATED PYRAZOLO[3,4-B]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE

The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjoegren’s syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors

A series of 4-anilino-7-pyridyl-3-quinolinecarbonitriles was prepared as Src kinase inhibitors. A systematic SAR study of substitutions on both the pyridine ring and the 3-quinolinecarbonitrile core established the requirements for optimal activity. The lead compound, 17, showed potent activity in both the Src enzyme assay and cell assays, and demonstrated in vivo anti-tumor activity in a xenograft model.

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PYRAZOLE COMPOUNDS

Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.

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INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP)

The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I)

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Preparation method of (by machine translation)

The method of the invention widens the substrate range 1 by directly conducting 4 – coupling suzuki and,formyl phenylboronic acid to carry out reductive amination reaction 4, with thiomorpholine 1,1 – dioxides or the hydrochloride thereof through reductive amination reaction, to obtain the phenetinib product 9; and reduces the process cost 1 and routes the route through improving the crystallization property, of the intermediate to obtain the phenanthrenitiamide product, and the route is easy 4 – to obtain a product with higher total yield, 1,1 – The method of the invention is favorable for improving the purity 9. of the final finished products . The method of the invention is favorable for improving the purity, of the final finished product; through a reductive amination reaction step, The method of the invention is favorable for, increasing the production . of finished products. (by machine translation)

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PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA

Provided are compounds of formula (I) or a pharmaceutically acceptable salts or stereoisomer thereof, which are PI3K-delta inhibitors, and are useful for the treatment of PI3K-delts-mediated diseases such as inflammation, asthma, COPD and cancer.

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MULTI-KINASE INHIBITOR COMPOUND, AND CRYSTAL FORM AND USE THEREOF

The present invention relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt and stereoisomer thereof, wherein R1, R2, X, Y, P, W, and Ar are as defined in the description. The compound of formula (I) of the present invention can be used in the preparation of a drug for treating cancers mediated by abnormality of multi-kinases. Also provided is a crystal form I of a compound 4-(5-(2-chlorophenyl)-3-methyl-2,10-dihydropyrazolo[4,3-b]pyrido[4,3-e][1,4]diazepin-8-yl)morpholine, wherein in an X-ray powder diffraction pattern of crystal form I, there are characteristic peaks at 7.4¡À0.20, 17.9¡À0.2, 18.9¡À0.2, 19.4¡À0.2, 21.5¡À0.2, and 23.7¡À0.2.

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ETHER DERIVATIVES OF BICYCLIC HETEROARYLS

The invention relates to compounds of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease

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