- VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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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.
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Paragraph 0134; 0135
(2018/06/23)
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- A catalytic oxidation fragrant boron class compound preparing phenol method (by machine translation)
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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)
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Paragraph 0073; 0123; 0124
(2017/08/08)
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- Further studies on 2-arylacetamide pyridazin-3(2H)-ones: Design, synthesis and evaluation of 4,6-disubstituted analogs as formyl peptide receptors (FPRs) agonists
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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
- 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.
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p. 512 - 528
(2013/07/27)
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- Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model
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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
- 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.
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supporting information
p. 6286 - 6291
(2012/11/07)
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- Synthesis of substituted pyridines and pyridazines via ring closing metathesis
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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.
- Donohoe, Timothy J.,Fishlock, Lisa P.,Basutto, Jose A.,Bower, John F.,Procopiou, Panayiotis A.,Thompson, Amber L.
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supporting information; experimental part
p. 3008 - 3010
(2009/12/01)
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- Ring-closing metathesis for the synthesis of heteroaromatics: evaluating routes to pyridines and pyridazines
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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.
- Donohoe, Timothy J.,Bower, John F.,Basutto, José A.,Fishlock, Lisa P.,Procopiou, Panayiotis A.,Callens, Cedric K.A.
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experimental part
p. 8969 - 8980
(2009/12/26)
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- ANTIVIRAL AGENT
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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)
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- COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
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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
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- Endothelin receptor antagonists
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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.
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- Reaction of Diazines and their Benzo derivatives with Benzonitrile oxide
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The reaction of diazines 1 and benzodiazines 2 with benzonitrile oxide in refluxing benzene affords regio, site and stereospecific cycloadducts to the diazine ring and/i43or products derived from them.
- Grassi, Giovanni,Risitano, Francesco,Foti, Francesco
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p. 11855 - 11862
(2007/10/02)
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- PREPARATION AND REACTIONS OF SOME 2-THIENYL AND 3-THIENYL PYRIDAZINONES AND PYRIDAZINES
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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.
- Powell, Paul,Sosabowski, Michael H.
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p. 1840 - 1852
(2007/10/03)
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- Nitrile oxide [3+2] cycloaddition: Application to the synthesis of 6-substituted 3(2H)-pyridazinones and 6-substituted 4,5-dihydro-4-hydroxy-3(2H)-pyridazinones
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An efficient method for the preparation of 6-substituted 3(2H)-pyridazinones and 6-substituted 4,5-dihydro-4-hydroxy-3(2H)-pyridazinones starting from 3,5-disubstituted 4,5-dihydroisoxazoles is described. N-O bond cleavage of the isoxazoline ring promoted
- Baraldi,Bigoni,Cacciari,Caldari,Manfredini,Spalluto
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p. 1158 - 1162
(2007/10/02)
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- Angiotensin II receptor antagonists
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Compounds are disclosed having the formula: STR1 The compounds of the invention are angiotensin II receptor antagonists.
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- Fungicidal pyridazines
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Plants are protected from the damaging effects of Phycomycetous fungi by a series of pyridazines of formula STR1 wherein R3 is chloro, bromo, methyl, cyano or iodo; R is chloro, bromo, iodo, methyl, cyano or furan-2-ylmethoxy; R1 is
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- Pyridazine derivatives useful as components of liquid crystal mixtures
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Compounds of the formula STR1 wherein B is --C C-- or --CH2 CH2 --, R1 is straight-chain C1 -C12 -alkyl and R2 is straight-chain C1 -C12 -alkyl or straight-chain C1 -C12 -alkoxy, their manufacture and use in liquid crystalline mixtures are described.
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- The Reaction of Meldrum's Acid with α-Dicarbonyl Monohydrazones: A New Synthesis of Pyridazin-3-ones
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Treatment of the monohydrazones of α-dicarbonyl compounds with Meldrum's acid gives the condensation products (13)-(19) under standard conditions.Reaction of pyruvaldehyde 2-phenylhydrazone or 2-t-butylhydrazone with Meldrum's acid at 80 deg C gives the corresponding 2-substituted-2,3-dihydro-6-methyl-3-oxo-pyridazine-4-carboxylic acids (29) and (30).Cyclisation of the other N-monosubstituted condensation products (13), (14), (16), (18), and (19) to 3-oxopyridazine-4-carboxylic acids (31)-(35) can be effected under basic conditions.Gas-phase pyrolysis of the N-aryl derivatives (13)-(16) at 550 deg C and 10E-2 Torr gives N-arylpyridazin-3-ones (38)-(41) while the N-t-butyl derivatives (18) and (19) at 750 deg C and 10E-2 Torr give N-unsubstituted pyridazin-3-ones (44) and (45) by additional loss of 2-methylpropene. 2-t-Butylpyridazin-3-ones (42) and (43) can be isolated from the same precursors under milder conditions (500 deg C and 10E-2 Torr).Pyrolysis of the N,N-dimethyl derivative (17) gave only polymeric material.
- McNab, Hamish,Stobie, Ian
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p. 1845 - 1854
(2007/10/02)
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- Catalytic dehydrogenation preparation of 3-pyridazones
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Pyridazones are prepared by heating 4,5-dihydro-3-pyridazones in the liquid phase in the presence of a dehydrogenation catalyst. The reaction temperature is in the range of from 150° to 350° C. The dehydrogenation catalyst contains a noble metal of subgroup 8 of the periodic table, which is generally supported on a carrier. The reaction is preferably carried out in the presence of a solvent.
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