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Relevant academic research and scientific papers

PYRIDAZINE DERIVATIVES AS RORC MODULATORS

Compounds of formula (I): (I) or pharmaceutical salts thereof, wherein m, n,, p, q A, B, Ri, R2, R3, R4, R5, R6and R7are as defined herein. Also disclosed are methods of making the compounds and using the compounds as RORs modulators for treatment of inflammatory diseases such as arthritis.

PYRIDAZINE DERIVATIVES AS RORc MODULATORS

Compounds of formula I: or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R1, R2, R3, R4 and R5are as defined herein. Also disclosed are methods of making the compounds and using the compounds f

PYRIDAZINE DERIVATIVES AS RORc MODULATORS

Compounds of formula I, or pharmaceutical salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory

PYRIDAZINE DERIVATIVES AS RORc MODULATORS

Compounds of formula (I): or pharmaceutical salts thereof, wherein m, n, A, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment o

PYRIDAZINE DERIVATIVES AS RORc MODULATORS

Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compou

Novel HldE-K inhibitors leading to attenuated gram negative bacterial virulence

We report here the optimization of an HldE kinase inhibitor to low nanomolar potency, which resulted in the identification of the first reported compounds active on selected E. coli strains. One of the most interesting candidates, compound 86, was shown to inhibit specifically bacterial LPS heptosylation on efflux pump deleted E. coli strains. This compound did not interfere with E. coli bacterial growth (MIC > 32 μg/mL) but sensitized this pathogen to hydrophobic antibiotics like macrolides normally inactive on Gram-negative bacteria. In addition, 86 could sensitize E. coli to serum complement killing. These results demonstrate that HldE kinase is a suitable target for drug discovery. They also pave the way toward novel possibilities of treating or preventing bloodstream infections caused by pathogenic Gram negative bacteria by inhibiting specific virulence factors.

Pesticidal triazine-derivatives

A compound of formula wherein R1 is unsubstituted or substituted aryl or heteroaryl, the substituents of the aryl and heteroaryl rings being selected, for example, from the group consisting of OH, halogen, CN, NO2, C1-C6alkyl, C3-C8cycloalkyl, C1-C6alkyl-C3-C8cycloalkyl, C3-C8cycloalkyl-C1-C6alkyl, C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6alkoxy and phenyl; phenoxy; phenylthio; phenylamino; and phenyl-(C1-C6alkyl)-amino; the substituents of the phenoxy, phenylthio, phenylamino and phenyl-(C1-C6alkyl)-amino groups being selected from the group consisting of halogen, CN, NO2, C1-C6alkyl, C3-C8cycloalkyl, C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6alkoxy, C3-C8cycloalkoxy, C1-C6alkylthio, C3-C8cycloalkylthio, C1-C6haloalkylthio and C3-C8halocycloalkylthio; R2 is, for example, H, OH, halogen, CN, NO2, C1-C6alkyl or C1-C6alkoxy; A is, for example, a single bond, C1-C12alkylene, O or O(C1-C12alkylene); R4 is H, C1-C6alkyl, C3-C8cycloalkyl, C1-C6haloalkyl, C1-C6alkoxy, N(R5)2 or C1-C6alkoxy-C2-C6alkyl; R5 is H, C1-C6alkyl, C3-C8cycloalkyl, C1-C6haloalkyl or aryl-C1-C6alkyl; X1 is R10; X2 and X3 are each independently of the other H or R10; R10 is, for example, halogen, CN, NO2, C1-C6alkyl or C3-C8cycloalkyl; and n is 0, 1 or 2, and to their physiologically tolerable and agrochemically acceptable addition compounds, and where appropriate to E/Z isomers, to mixtures of E/Z isomers and/or to tautomers, in each case in free form or in salt form. The compounds, in free form or in agrochemically acceptable salt form, exhibit advantageous pesticidal properties. They are suitable especially in the control of pests in agriculture and stored goods and also in the keeping of domestic animals.