Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.

Certain chemical entities, compositions and methods

Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

Processes for preparing isoquinolinones and solid forms of isoquinolinones

Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).

Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using pi3 kinase inhibitors

This invention relates to substituted bis-amide pyrimidine compounds of Formula (I), which are useful for the treatment of metalloprotease mediated diseases, in particular MMP-13 related diseases.

Substituted bis-amide metalloprotease inhibitors

5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2, 4-dione and analogues useful as inhibitors of macrophage elastase are disclosed.

5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2, 4-dione and analogues as inhibitors of macrophage elastase

A compound of formula (I) selected from: wherein: X represents oxygen or sulphur, Y represents oxygen, —NH— or —N(C 1 -C 6 )alkyl-, R a represents hydrogen, halogen, (C 1 -C 3 )alkyl, hydroxyl or (C 1 -C 3 )alkoxy, R b represents hydrogen, halogen or (C 1 -C 3 )alkyl, A represents phenyl, pyridyl, (C 5 -C 6 )cycloalkyl or (C 5 -C 6 )cycloalkenyl, R 1 and R 2 each represent a group selected from hydrogen, halogen, cyano, nitro, haloalkyl, haloalkoxy, alkyl, alkenyl, alkynyl, —OR 4 , —NR 4 R 5 , —S(O) n R 4 , —C(O)R 4 , —CO 2 R 4 , —O—C(O)R 4 , —C(O)NR 4 R 5 , —NR 5 —C(O)R 4 , —NR 5 —SO 2 R 4 , -T-CN, -T-OR 4 , -T-OCF 3 , -T- NR 4 R 5 , -T-S(O) n R 4 , -T-C(O)R 4 , -T-CO 2 R 4 , -T-O—C(O)R 4 , -T-C(O)NR 4 R 5 , -T-NR 4 —C(O)R 5 , -T-NR 4 —SO 2 R 5 , —R 6 and -T-R 6 in which n, T, R 4 , R 5 and R 6 are as defined in the description, R 3 represents an —R 7 or —U—R 11 group in which R 7 represents hydrogen, alkyl, aryl, cycloalkyl or heterocycle, U represents a linear or branched alkylene chain and R 11 is defined in the description, their optical isomers or their addition salts with a pharmaceutically acceptable acid or base, and their use as inhibitor of metalloproteinase and more specifically of metalloproteinase-12.

Novel thiophene derivatives, their process of preparation and the pharmaceutical compositions which comprise them

Composes de formule (I) caracterises en ce que .bullet. X represente oxygene ou soufre, .bullet. Y represente oxygene,-NH ou -N(C1-C6)alkyle, .bullet. Ra represente hydrogene, halogene, (C1-C3)alkyle, hydroxy, ou (C1-C3)alkoxy, .bullet. Rb represente hydrogene, halogene, ou (C1-C3)alkyle, .bullet. A represente phenyle, pyridyle, (C5-C6)cycloalkyle ou (C5-C6)cycloalkenyle, .bullet. R1 et R2 representent chacun un groupement choisi parmi hydrogene, halogene, cyano, nitro, halogenoalkyle, halogenoalkoxy, alkyle, alkenyle, alkynyle, -OR4, -NR4R5, -S(O)nR4, -C(O)R4, -C02R4, -OC(O)R4, -C(O)NR4R5, -NR5-C(O)R4, -NR5-S02R4, -T-CN, -T-OR4, -T-OCF3, -T-NR4R5, -TS(O)nR4, -TC(O)R4, -T-C02R4, -TOC(O)R4, -TC(O)NR4R5, -T-NR4-C(O)R5, -T-NR4-S02R5, -R6, et -T-R6 dans lesquels n, T, R4, R5 et R6 sont tels que definis dans la description, .bullet. R3 represente un groupement -R7 ou -U-R11, dans lesquels R7 represente hydrogene, alkyle, aryle, cycloalkyle ou heterocycle, U represente une chaine alkylene lineaire ou ramifiee, et R11, est tel que defini dans la description, leurs isomeres optiques ou leurs sels d'addition a un acide ou a une base pharmaceutiquement acceptable, et leur utilisation en tant qu'inhibiteur de metalloproteinase et plus specifiquement de la metalloproteinase -12.

Pierre Ducrot

Papers

Novel thiophene derivatives, their process of preparation and the pharmaceutical compositions which comprise them

Novel thiophene derivatives, preparation method thereof and pharmaceutical compositions containing same