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Cross coupling of 3-bromopyridine and sulfonamides (R1NHSO2R2¡¤R1 = H, Me, alkyl; R2 = alkyl and aryl) catalyzed by CuI/1,3-di(pyridin-2-yl)propane-1,3-dione

N-(3-Pyridinyl)-substituted secondary and tertiary sulfonamides have been synthesized in good to excellent yields by the reaction of 3-bromopyridine with primary and secondary alkyl and aryl sulfonamides (MeSO2NH2, MeSO2NHMe, TolSO2NH2, TolSO2NHMe, 1,3-propanesultam, and 1,4-butanesultam), catalyzed by CuI (20 mol %) and 1,3-di(pyridin-2-yl)propane-1,3-dione (20 mol %) with K2CO3 (200 mol %) in DMF (0.17 M for ArBr) at 110-120 C over 36-40 h. 2-Bromopyridine, 4-bromopyridine, and a wide variety of substituted phenyl bromides can also be successfully coupled with sulfonamides under these reaction conditions.

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NOVEL RAPAMYCIN DERIVATIVES

The disclosure relates to compounds of formula (I) and pharmaceutically acceptable salts, and compositions thereof, wherein the substituents are as defined herein. Also provided are methods of making compounds of formula (I), and methods involving the compounds or compositions for treating disorders and diseases described herein.

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5,6-DIHYDRO-1H-PYRIDIN-2-ONE COMPOUNDS

The invention is directed to 5,6-dihydro-lH-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

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PYRAZOLE DERIVATIVES AS SGC STIMULATORS

There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.

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HEPATITIS B ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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Oxadiazole derivative containing heterocyclic side chain, synthesis method and application thereof (by machine translation)

The invention discloses an oxadiazole derivative containing a heterocyclic side chain, a synthesis method and application, wherein the structure of the oxadiazole derivative is as shown in the formula I, wherein each substituent is defined in the specification and claims. The compound, provided by the invention, has strong IDO inhibiting activity, has good drug absorption potentiality, and has a good development prospect. (by machine translation)

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POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC M2 RECEPTOR

The present application relates to positive allosteric modulators of the muscarinic M2 receptor, especially to novel 7-substituted 1-arylnaphthyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular disorders and/or renal disorders.

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Quinuclidine – Wikipedia,
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Sulfonamidyls. 5. Electron Spin Resonance Spectroscopic Evidence for Four- and Five-Membered-Ring Sulfonamidyls and Sulfonyl Nitroxides

Cyclic sulfonamidyl radicals, generated by photolysis of the N-bromo (or N-chloro) beta- and gamma-sultams 1-3 and of N-bromo-2,3-dihydro-1,2-benzisothiazole 1,1-dioxide (4) have been characterized by solution ESR studies.The nitrogen and beta hyperfine splitting constants of 1-4 are in agreement with a PiN electronic ground state involving a planar geometry around the nitrogen free radical center.The corresponding nitroxides (6-9) were generated from 1-4 by reaction with nitrogen dioxide.In the same way, four additional sulfonyl nitroxides (10-13), derived from 3-alkyl-1,2 -thiazoline 1,1-dioxide systems, were generated and studied by ESR.The possible geometry around the nitroxide nitrogen atom and further conformational implications are discussed.

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Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors

A series of transition state analogues of beta-secretases 1 and 2 (BACE1, 2) inhibitors containing fused-ring or biaryl moieties were designed computationally to probe the S2 pocket, synthesized, and tested for BACE1 and BACE2 inhibitory activity. It has been shown that unlike the biaryl analogs, the fused-ring moiety is successfully accommodated in the BACE1 binding site resulting in the ligands with excellent inhibitory activity. Ligand 5b reduced 65% of Abeta40 production in N2a cells stably transfected with Swedish human APP.

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PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS

Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R5, G1, and G2 are defined herein.

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