Abstract:
The present invention describes pyridazinone compounds which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX/2), COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important 'housekeeping' enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
Abstract:
Composés ayant la formule (I), dans laquelle A est sélectionné entre NR1R2 et N(OR6)R2, et B et C sont du chlore lorsque A est N(OR6)R2 ou sont indépendamment sélectionnés entre NHR3 et NR4R5, où R1, R2, R3, R4 et R5 sont indépendamment sélectionnés dans le groupe composé d'alkyle, de cycloalkyle et d'alkylaryle, dont chacun peut être substitué ou non avec un ou plusieurs substituants sélectionnés dans le groupe composé d'hydroxyle, OR, NRR, OCOR, OCONRR, NRCOR et NRCONRR; R étant sélectionné dans le groupe composé d'hydrogène, alkyle, aryle, alkylaryle, alkoxyle et hydroxyle; ou R1 et R2 ou R4 et R5 peuvent former ensemble un groupe hétéroaryle et R6 est un élément sélectionné dans le groupe composé d'hydrogène, alkyle, alkylaryle et trialkylsilyle; sels pharmaceutiquement acceptables de ces composés, utiles comme inhibiteurs d'enzymes de la lipoxygenase.
Abstract:
Compounds of formula (I) Z-Ar 1 -Ar 2 wherein Z is a diazabicyclic amine, Ar 1 is a 5- or 6-membered aromatic ring, and Ar 2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
Abstract:
The present invention describes pyridazinone compounds of formula (I) which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important 'housekeeping' enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectively of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
Abstract:
Compounds having formula (I) are useful for treating diseases that are prevented by or ameliorated with Interleukin-2, Interleukin-4, or Interleukin-5 production inhibitors.
Abstract:
The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.