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COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY

Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 14733-77-8, name is 5-Amino-2,3-dihydro-1,3-benzoxazol-2-one, introducing its new discovery. Application In Synthesis of 5-Amino-2,3-dihydro-1,3-benzoxazol-2-one

Polymer composition pigmented with copper or nickel complexes of ligands containing a semicarbazone moiety

High molecular weight organic material is effectively colored by the incorporation therein of a copper or nickel complex of the ligand compound of formula I STR1 wherein A is an isocyclic or heterocyclic aromatic moiety, R is H, halogen, lower alkyl or alkoxy, R1 is H, lower alkyl, phenyl or substituted phenyl, and B is H, lower alkyl, ureido or substituted ureido, guanidino, anilino, benzamido or a heterocyclic aromatic moiety.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Towards the development of an in vivo chemical probe for cyclin G associated kinase (GAK)

SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and in mice, which limited its utility in in vivo studies. Chemical modifications of 1 that improved metabolic stability, generally resulted in decreased GAK potency. The best analog in terms of GAK activity in cells was 6-bromo-N-(1H-indazol-6-yl)quinolin-4-amine (35) (IC50 = 1.4 muM), showing improved stability in liver microsomes while still maintaining a narrow spectrum activity across the kinome. As an alternative to scaold modifications we also explored the use of the broad-spectrum cytochrome P450 inhibitor 1-aminobenzotriazole (ABT) to decrease intrinsic clearance of aminoquinoline GAK inhibitors. Taken together, these approaches point towards the development of an in vivo chemical probe for the dark kinase GAK.

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COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY

Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds

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Monoazo compounds containing long-chain alkyl radicals

Compounds of the formulae I and II STR1 in which A is a radical of the formulae III, IV or V STR2 R1 and R4 are –H or –Cl, R2 and R5 are –H, halogen, –NO2, –CN, C1 -C4 -alkyl, C1 -C4 alkoxy, –CF3 or phenyloxy which is unsubstituted or substituted by one or two chlorine atoms and/or one or two methyl or methoxy groups, and R3 is alkyl having at least 10 C atoms, X is a radical of the formulae –NH–, –O–, STR3 n is the number 1 or 2, Y is the radical of the formulae –COO–, –OOC–, –CONH– or –NHCO– or a radical of the formulae STR4 in which R1 and R2 are as defined above, D is an aromatic heterocyclic 5- or 6-membered ring, in which the ring contains 1 or 2 N atoms and may additionally contain an O atom or S atom, Z is –H, –Br, –OCH3, –CN or –NO2 and X1 and X2, independently of one another, are –H, halogen, –CH3, –OCH3, –OC2 H5 or –NO2 and X3 is –H, –NHCO–C1 -C4 alkyl, benzoylamino or phenylcarboxamide which are each unsubstituted or substituted on the phenyl ring by one or two chlorine atoms and/or one or two methyl or methoxy groups or an –NHCO–C1 -C4 alkyl group, or X2 and X3 together with the carbon atom to which they are bound are an aromatic carbocyclic 6-membered ring or an aromatic heterocyclic 5- or 6-membered ring, in which the heterocyclic ring contains 1 or 2 N atoms and can additionally have an O atom or S atom, and Y1 is –H, –OCH3, –OC2 H5 or –NHCOCH3, with the proviso that X3 must not be H, if X is –O– or –NH–, are highly suitable for the mass coloration of plastics, in particular of polyolefins.

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