13327-27-0Relevant articles and documents
VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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, (2018/06/23)
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
A catalytic oxidation fragrant boron class compound preparing phenol method (by machine translation)
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Paragraph 0073; 0123; 0124, (2017/08/08)
The invention discloses a method for catalytic oxidation of phenolic compounds fragrant boron class compound synthesis method, the flux in the solvent in the aqueous solution, under the action of alkali, adding hydrazine hydrate or acid hydrazides catalyst, catalytic oxidation fragrant boron class compound directly for the preparation of phenolic compound. The invention of the method of preparation of the phenol compound, the catalyst is a cheap hydrazine hydrate or hydrazine compound, the oxidizing agent is atmospheric pressure of air or oxygen, the reaction does not need good and activeness metal catalyst, is extensive and stable substrate, substrate-sensitive functional group compatibility good and wide range of application. In the optimized under the reaction conditions, the yield of the target product separation up to 99%. (by machine translation)
Further studies on 2-arylacetamide pyridazin-3(2H)-ones: Design, synthesis and evaluation of 4,6-disubstituted analogs as formyl peptide receptors (FPRs) agonists
Giovannoni, Maria Paola,Schepetkin, Igor A.,Cilibrizzi, Agostino,Crocetti, Letizia,Khlebnikov, Andrei I.,Dahlgren, Claes,Graziano, Alessia,Dal Piaz, Vittorio,Kirpotina, Liliya N.,Zerbinati, Serena,Vergelli, Claudia,Quinn, Mark T.
, p. 512 - 528 (2013/07/27)
Formyl peptide receptors (FPRs) play an essential role in the regulation of endogenous inflammation and immunity. In the present studies, a large series of pyridazin-3(2H)-one derivatives bearing an arylacetamide chain at position 2 was synthesized and te
Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model
Banerjee, Abhisek,Patil, Sandip,Pawar, Mahesh Y.,Gullapalli, Srinivas,Gupta, Praveen K.,Gandhi, Maulik N.,Bhateja, Deepak K.,Bajpai, Malini,Sangana, Ramachandra Rao,Gudi, Girish S.,Khairatkar-Joshi, Neelima,Gharat, Laxmikant A.
supporting information, p. 6286 - 6291 (2012/11/07)
The synthesis and structure-activity relationship studies of a series of compounds from imidazopyridazinone scaffold as PDE7 inhibitors are disclosed. Potent analogs such as compounds 7 (31 nM), 8 (27 nM), and 9 (12 nM) were identified. The PDE selectivit
Synthesis of substituted pyridines and pyridazines via ring closing metathesis
Donohoe, Timothy J.,Fishlock, Lisa P.,Basutto, Jose A.,Bower, John F.,Procopiou, Panayiotis A.,Thompson, Amber L.
supporting information; experimental part, p. 3008 - 3010 (2009/12/01)
RCM can be used to make aromatic heterocycles, namely pyridines and, for the first time, pyridazines; the key step after RCM involves elimination of sulfinate to provide the aromatic system. The Royal Society of Chemistry 2009.
Ring-closing metathesis for the synthesis of heteroaromatics: evaluating routes to pyridines and pyridazines
Donohoe, Timothy J.,Bower, John F.,Basutto, José A.,Fishlock, Lisa P.,Procopiou, Panayiotis A.,Callens, Cedric K.A.
experimental part, p. 8969 - 8980 (2009/12/26)
Ring-closing olefin metathesis (RCM) has been applied to the efficient synthesis of densely and diversely substituted pyridine and pyridazine frameworks. Routes to suitable metathesis precursors have been investigated and the scope of the metathesis step has been probed. The metathesis products function as precursors to the target heteroaromatic structures via elimination of a suitable leaving group, which also facilitates earlier steps by serving as a protecting group at nitrogen. Further functionalisation of the metathesis products is possible both prior to and after aromatisation. The net result is a powerful strategy for the de novo synthesis of highly substituted heteroaromatic scaffolds.
COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
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Page 34; 36, (2008/06/13)
The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors
ANTIVIRAL AGENT
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Page 174, (2010/02/06)
The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)
Endothelin receptor antagonists
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, (2008/06/13)
This invention relates to pyridizinone derivatives of formula I STR1 wherein the various substituents are defined in the specification, and salts thereof, which have useful pharmacological properties, in particular endothelin receptor-antagonistic properties. The compounds are thus useful for the treatment of illnesses associated with endothelin activities, such as hypertension, cardiac insufficiency, coronary heart disease, renal, cerebral and myocardial ischaemia, renal insufficiency, cerebral infarct, subarachnoid haemorrhage, arteriosclerosis pulmonary high blood pressure, inflammations, asthma, prostate hyperplasia, endotoxic shock and in complications after the administration of immunosuppressants which produce renal vasoconstriction.
PREPARATION AND REACTIONS OF SOME 2-THIENYL AND 3-THIENYL PYRIDAZINONES AND PYRIDAZINES
Powell, Paul,Sosabowski, Michael H.
, p. 1840 - 1852 (2007/10/03)
The preparation and reactions of some pyridazinone derivatives with 2- and 3-thienyl substituents are described.Precursor 4-oxobutanoic acids Ar2COCH2CH(Ar1)CO2H (Ar1=Pb, Ar2=2-thienyl and Ar1=2-thienyl, Ar2=Pb) were obtained by addition of HCN to the chalcones Ar1CH=CHCOAr2 followed by acid hydrolysis of the resulting nitrile.Nitriles, ArCOCH(CH3)CH2CN were prepared by the Michael-Stetter reaction and converted via the acids to the 4,5-dihydropyridazin-3(2H)-ones.Two methods wereused to obtain pyridazin-3(2H)-ones viz oxidation of the 4,5-dihydro derivatives with selenium dioxide and base-catalyzed condensation of methanal or aryl aldehydes at the 4-position of the 4,5-dihydro compound.
