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The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.

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A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as STR1 which are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.

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Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.

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Provided are aryl analogs?pharmaceutical compositions containing them and their use as NRF2 regulators.

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The key to shortening tuberculosis (TB) drug regimen lies in eliminating the reservoir of non-replicating persistent (NRP) Mycobacterium tuberculosis (Mtb). Pyrazinamide (PZA) is the only known drug used as part of a combination therapy that is believed to kill NRP Mtb and achieve sterilization. PZA is active only under low pH screening conditions. Screening and identification of NRP-active anti-TB compounds are severely limited because compounds are usually inactive under regular assay conditions. In an effort to design novel NRP-active anti-TB compounds, we used pyrazinamide as a core and hybridized it with the fragments derived from marketed drugs. One of these designs, compound 8, was a hybrid with fluoroquinolone. This compound exhibited >10 fold improvement in NRP activity under low pH condition as compared to pyrazinamide and a modest activity (0.8 log10 kill) under nutritionally starved NRP condition. Furthermore, compound 8 was active against fluoroquinolone-resistant strains and did not show any activity in a DNA supercoiling assay (gyrase inhibition), suggesting that its mechanism of action is not that of the parent fluoroquinolone. These results provide a novel avenue in the exploration of new chemotypes that are active against non-replicating Mtb.

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Substituted quinoline compounds and intermediates thereto, processes for producing those compounds and intermediates, pharmaceutical compositions using those compounds, methods for treating bacterial infections using those compounds, and methods for disinfecting using those compounds.

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The A-values of the acetamido and the acetoxy group were determined by low-temperature 1H-n.m.r. spectroscopy.The limiting values for the relevant vicinal coupling constants of the newly prepared trans- (22) and cis-5-acetoxy-2-(1-hydroxy-1-methylethyl)tetrahydropyran (24) were obtained at room temperature.The attractive gauche effect of AcNH-3 and AcO-3 in piperidines, piperidinium trifluoroacetates, and tetrahydropyrans was investigated by 1H-n.m.r. spectroscopy both at low temperature (integrals) and at room temperature (band widths and coupling constants).The results obtained at low temperature are more reliable.The position of the conformational equilibrium of N-(3-piperidyl)acetamide (11), N-(1-methyl-3-piperidyl)acetamide (12), and N-(tetrahydropyran-3-yl)acetamide (17) depends strongly upon the nature of the solvent and, in apolar solvents, upon the concentration.

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We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1?14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure?activity relationship, which is helpful for further optimization.

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The present invention relates to compounds of formula (I) which are inhibitors of NF-kB-inducing kinase (NIK – also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders

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The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein A; X;n; R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.

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