134965-39-2Relevant academic research and scientific papers
Synthesis of functionalized pyridazin-3(2 H)-ones via nucleophilic substitution of hydrogen (SNH)
Verhelst, Tom,Verbeeck, Stefan,Ryabtsova, Oxana,Depraetere, Stefaan,Maes, Bert U. W.
supporting information; experimental part, p. 272 - 275 (2011/04/22)
Reaction of 2-benzyl-5-halopyridazin-3(2H)-ones (3) with Grignard reagents followed by quenching with electrophiles unexpectedly yielded 4,5-disubstituted pyridazin-3(2H)-ones instead of 5-substituted pyridazin-3(2H)-ones. These reactions represent the fi
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase
Jerome, Kevin D.,Hepperle, Michael E.,Walker, John K.,Xing, Li,Devraj, Rajesh V.,Benson, Alan G.,Baldus, John E.,Selness, Shaun R.
scheme or table, p. 3146 - 3149 (2010/09/15)
The synthesis, structure-activity relationship and modeling of a series of 5-substituted-N-aryl pyridazinone based p38α inhibitors are described. In comparing the series to the similar N-aryl pyridinone series, it was found that the pyridazinones maintain
Synthesis of functionalized pyridazin-3(2H)-ones via bromine-magnesium exchange on bromopyridazin-3(2H)-ones
Ryabtsova, Oxana,Verhelst, Tom,Baeten, Mattijs,Vande Velde, Christophe M. L.,Maes, Bert U. W.
supporting information; experimental part, p. 9440 - 9445 (2010/03/24)
(Chemical Equation Presented) The potential of halogen-magnesium exchange reactions, followed by quenching with electrophiles, for the functionalization of the pyridazin-3(2H)-one core was investigated. 2-Benzyl-4-bromo-5-methoxy- (1), 2-benzyl-5-bromo-4-
Azabicyclic heterocycles as cannabinoid receptor modulators
-
Page/Page column 14, (2008/06/13)
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R6, R7, m and n are described herein.
Substituted pyridazinones
-
Page 32, (2008/06/13)
Disclosed are substituted pyridazinones that are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical composition containing the pyridazinone compounds, methods of preparing th
PYRIDAZINONES AS INHIBITORS OF CYCLOOXYGENASE-2
-
Page 40, (2010/02/07)
The invention encompasses the pyridazin-3-one compounds of formula (I) as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a
Synthesis of 4-aryl-5-hydroxy- and 5-aryl-4-hydroxypyridazin-3(2H)-ones and their use in the preparation of 4,5-diarylpyridazin-3(2H)-ones and hitherto unknown isochromeno[3,4-d]pyridazinediones
Maes, Bert U.W,Monsieurs, Katrien,Loones, Kristof T.J,Lemière, Guy L.F,Dommisse, Roger,Mátyus, Péter,Riedl, Zsuzsanna,Hajós, Gy?rgy
, p. 9713 - 9721 (2007/10/03)
Easily accessible 2-substituted 4-aryl-5-methoxy- and 2-substituted 5-aryl-4-methoxypyridazin-3(2H)-ones were transformed into the corresponding aryl-hydroxypyridazin-3(2H)-ones by alkaline hydrolysis. The use of these compounds in the synthesis of 2-substituted 4,5-diarylpyridazin-3(2H)-ones with two differently substituted aryl groups was investigated. Two aryl-hydroxypyridazin-3(2H)-ones, 2-(2-benzyl-5-hydroxy-3-oxo-2,3-dihydropyridazin-4-yl)benzaldehyde and 2-(1-benzyl-5-hydroxy-6-oxo-1,6-dihydropyridazin-4-yl)benzaldehyde, were transformed into 2-benzyl-1H-isochromeno[3,4-d]pyridazine-1,6(2H)-dione and 3-benzyl-3H-isochromeno[3,4-d]pyridazine-4,6-dione, respectively, via oxidation of the formyl group with KMnO4 followed by lactonization.
Prostaglandin endoperoxide H synthase biosynthesis inhibitors
-
, (2008/06/13)
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 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).
Pyridazinones as inhibitors of cyclooxygenase-2
-
, (2008/06/13)
The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
Novel Heterocyclization of Hydrazinopyridazinones with Dimethyl Acetylenedicarboxylate with Dehydrogenation and Rearrangement
Yamasaki, Tetsuo,Kawaminami, Eiji,Yamada, Tomomi,Okawara, Tadashi,Furukawa, Mitsuru
, p. 991 - 996 (2007/10/02)
5-Hydrazinopyridazin-3(2H)-ones 1 reacted with dimethyl acetylenedicarboxylate 2 to give 4,6-dihydropyridazinopyridazin-5-(1H)-ones 3 by cyclization with dehydrogenation.On the other hand, the reaction of 4-bromo-5-hydrazino- and 5-bromo-4-hydrazin
