Some scientific research about Tetrahydrofuran-3-carboxylic acid

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Visible Light-Induced Regioselective Decarboxylative Alkylation of the C(sp2)?H Bonds of Non-Aromatic Heterocycles

With sunlight or blue LEDs irradiation, regioselective decarboxylative alkylation of various non-aromatic heterocycles has been realized via C(sp3)-centered radical C(sp2)?C(sp3) bond formation under oxidant-free conditions at room temperature. This reaction readily incorporates various functional alkyl groups into heterocyclic compounds without observation of any alkyl radical rearrangement and represents a mild and general tool for the preparation of valuable alkyl group-functionalized heterocyclic compounds. (Figure presented.).

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NEW ENZYME INHIBITOR COMPOUNDS

Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R1, A, X and R2 are as defined in the claims

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Novel N-substituted tetrahydroisoquinoline/isoindoline hydroxamic acid compounds

Compounds of a certain formula I, wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors

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THIAZOLOPYRIMIDINONE DERIVATIVES AS PI3 KINASE INHIBITORS

This invention relates to the use of thiazolopyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3Kalpha, PI3Kdelta, PI3Kbeta, and/or PI3Kgamma. Suitably, the present invention relates to the use of thiazolopyrimidinones in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kbeta selective thiazolopyrimidinones compounds for treating cancer

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Iridium-catalyzed enantioselective hydrogenation of unsaturated heterocyclic acids

Spiral binding: A highly enantioselective hydrogenation of unsaturated heterocyclic acids has been developed by using chiral iridium/spirophosphino oxazoline catalysts (see scheme; BArF-=tetrakis[3,5- bis(trifluoromethyl)phenyl]borate, Boc=tert-butoxycarbonyl). This reaction provided an efficient method for the preparation of optically active heterocyclic acids with excellent enantioselectivities. Copyright

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The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability

Novel analogs of the allosteric, biased PAR1 ligand ML161 (parmodulin 2, PM2) were prepared in order to identify potential anti-thrombotic and anti-inflammatory compounds of the parmodulin class with improved properties. Investigations of structure-activity relationships of the western portion of the 1,3-diaminobenzene scaffold were performed using an intracellular calcium mobilization assay with endothelial cells, and several heterocycles were identified that inhibited PAR1 at sub-micromolar concentrations. The oxazole NRD-21 was profiled in additional detail, and it was confirmed to act as a selective, reversible, negative allosteric modulator of PAR1. In addition to inhibiting human platelet aggregation, it showed superior anti-inflammatory activity to ML161 in a qPCR assay measuring the expression of tissue factor in response to the cytokine TNF-alpha in endothelial cells. Additionally, NRD-21 is much more plasma stable than ML161, and is a promising lead compound for the parmodulin class for anti-thrombotic and anti-inflammatory indications.

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3-SUBSTITUTED PYRAZOLES AND USE AS DLK INHIBITORS

The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. (I) In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.

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AMELIORATION OF CATARACTS, MACULAR DEGENERATION AND OTHER OPHTHALMIC DISEASES

Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula where R1 and R2 are, independently, H or C1 to C3 alkyl ; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl ; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl ; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.

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Preparation of tetrahydro-3-furoic acid

Disclosed is a process for the preparation of tetrahydro-3-furoic acid by the thermal, non-catalytic oxidation of 3-formyltetrahydrofuran using molecular oxygen.

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SUBSTITUTED PHTHALAZINES

Provided are compounds of formula (I), Wherein R 1, R 2, R 3, R 4, R 5 and R 6 are as defined in the specification, and pharmaceutically acceptable salts thereof, which are useful as agents in the treatment of diseases and conditions mediated and modulated by SUV402H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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