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RORgamma ANTAGONIST AND APPLICATION THEREOF IN MEDICINE

Provided herein are compounds as RORgamma antagonist having Formula (I). The compounds or pharmaceutical composition thereof can be used for regulating Retinoid-related orphan receptor gamma t (RORgammat). Also provided herein are methods of preparation of the compounds and composition thereof, and uses thereof in treating or preventing RORgammat mediated inflammation or autoimmune diseases in mammals, particularly humans.

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4-PYRAZOLYL-N-ARYLPYRIMIDIN-2-AMINES AND 4-PYRAZOLYL-N-HETEROARYLPYRIMIDIN-2-AMINES AS JANUS KINASE INHIBITORS

The present invention provides substituted bicyclic heteroaryl compounds, 5 including, for example, 4-pyrazoIyI-N-arylpyrirnidin-2-arnines and 4-pyrazolyl-N-heteroarylpytimidin-2-amines that modulate the activity of kinases and are useful in the treatment of diseases related to activity of kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.formule :(1)

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Stereo-complementary bioreduction of saturated N-heterocyclic ketones

The asymmetric bioreduction of several saturated N-heterocyclic ketones is demonstrated in a stereo-complementary fashion using the ketoreductases READH and ChKRED20 for the production of (S)- and (R)-alcohols, respectively. The reaction accepts substrates with a five-, six- or seven-membered ring, and exhibits excellent stereoselectivity when using 2-propanol as both the ultimate reducing agent and cosolvent, achieve >99% ee in the majority of cases for both enantiomers.

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Photochemical Preparation of Tricyclic Hydroxyketones by Transanular Cyclization of Bridged 4-Benzoylcyclohexanones

The bridged 4-benzoyl-cyclohexanones 3a-f were synthesized by alpha,alpha?-annelation of cyclic ketones. Irradiation of 3a-f revealed a strong dependence of the photochemical behaviour on the ring size and the introduction of a nitrogen atom. Ketones which are able to form 1,6-biradicals (3b,c,e) undergo unselective photolytic decomposition, whereas 3a,d,f afforded tricyclic hydroxyketones. The diastereoselectivity of ring closure is remarkably improved by introduction of a protected nitrogen atom (3d,f) in comparison to the carbocyclic diketone 3a. Moreover, the N protective group of 4-azatricyclo-[4.3.1.03,8]decan-7-one (7) could be removed affording the free hydroxy amino ketone 8 in good yields. An explanation of the diastereoselective cyclization of 3a and of the surprisingly low quantum yield of 3d was found by conformational analysis of the corresponding triplet biradicals.

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Intramolecular N-H insertion of alpha-diazocarbonyls catalyzed by Cu(acac)2: An efficient route to derivatives of 3-oxoazetidines, 3-oxopyrrolidines and 3-oxopiperidines

Cu(acac)2 was found to be an efficient catalyst for the intramolecular N-H insertion by carbenoids. The competitive intramolecular C-H insertion by carbenoids is not a problem in the diazo decomposition reaction with Cu(acac)2 as catalyst. The reaction provided derivatives of 3-oxoazetidine, 3-oxopyrrolidine and 3-oxopiperidine in moderate to good yields.

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ARGINASE INHIBITORS AND METHODS OF USE

Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.

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Heterocyclic spiro-derivative

The present invention provides an antibacterial compound useful as medicines, animal drugs, fisheries drugs or antibacterial preservatives and to an antibacterial agent or preparation which contains the same, more particularly a compound which possesses high safety and excellent activity against a broad range of bacterial species including quinolone-resistant strains. A quinolone derivative of the following formula (I) which has a group derived from the heterocyclic spiro-compound at the 7-positioned R2 and the halogenocyclopropyl group at the N1-position, prefereably a compound of pure isomer, and an antibacterial agent containing the derivative compound.

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PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

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MGLUR REGULATORS

Provided herein are compounds of the formula I: (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.

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Archives for Chemistry Experiments of (S)-Azetidine-2-carboxylic acid

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Biocatalysis in Drug Development – Highlights of the Recent Patent Literature

The recent patent literature on biocatalysis is reviewed, with a focus on significant advances in enzymatic catalysis involving ketoreductases, transaminases, hydroxylases, sulfur oxidation, and nitrilase resolutions and a progress report on the emerging area of imine reductases highlighting collaborations between academia and pharmaceutical companies.

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