- SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS NADPH OXIDASE INHIBITORS
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The present application relates to substituted fused heteroaryl and heterocyclic compounds, useful as nicotinamide adenine dinucleotide phosphate oxidase inhibitors (NADPH oxidase inhibitors), processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by NADPH oxidase. (Formula I)
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Page/Page column 151
(2018/12/03)
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- Synthesis of new multi-functionalised 1,1'-carbonylbispyrazole derivatives
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A new series of multi-functionalised 1,1'-carbonylbispyrazole derivatives were synthesised through cyclisation of pyrazole carbohydrazides with some substituted methylene malononitriles in very good yields. The structures of all synthesised compounds were established on the basis of NMR, IR, MS and elemental analysis.
- Mohadeszadeh, Manijeh,Eshghi, Hossein,Saberi, Sattar,Gholizadeh, Mostafa
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p. 220 - 222
(2015/06/02)
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- A one-pot, three-component, microwave-assisted synthesis of novel 7-amino-substituted 4-aminopyrazolo[1,5-a][1,3,5]triazine-8-carbonitriles
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The synthesis of novel 7-amino-substituted pyrazolo[1,5-a][1,3,5]triazine-8-carbonitriles was achieved via a three-component reaction of 3-amino-substituted 5-aminopyrazole-4-carbonitriles, cyanamide and triethyl orthoformate under microwave irradiation.
- Lim, Felicia Phei Lin,Luna, Giuseppe,Dolzhenko, Anton V.
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p. 7016 - 7019
(2015/11/27)
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- Synthesis, antibacterial activity and cytotoxicity of new fused pyrazolo[1,5-a]pyrimidine and pyrazolo[5,1-c][1,2,4]triazine derivatives from new 5-aminopyrazoles
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New 5-aminopyrazoles 2a-c were prepared in high yields from the reaction of known α,α-dicyanoketene-N,S-acetals 1a-c with hydrazine hydrate under reflux in ethanol. These compounds were utilized as intermediates to synthesize pyrazolo[1,5-a]-pyrimidines 3a-c, 4a-d, 5a-c, and 6a-c, as well as pyrazolo[5,1-c][1,2,4]triazines 7a-c and 8a-c, by the reaction of 2-[bis(methylthio)methylene]malononitrile, α,α-dicyanoketene-N,S- acetals 1a-b, acetylacetone, acetoacetanilide as well as acetylacetone, and malononitrile, respectively. Furthermore, cyclization of 2a-c with pentan-2,5-dione yielded the corresponding 5-pyrrolylpyrazoles 9a-c. Moreover, fusion of 2a-c with acetic anhydride resulted in the corresponding 1-acetyl-1H-pyrazoles 10a-c. The antibacterial activity and cytotoxicity against Vero cells of several selected compounds are also reported.
- Al-Adiwish, Wedad M.,Tahir,Siti-Noor-Adnalizawati,Hashim, Siti Farah,Ibrahim, Nazlina,Yaacob
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p. 464 - 476
(2013/07/27)
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- One-pot synthesis of new tetrasubstituted thiophenes and selenophenes
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In this work, we described the synthesis of new tetrasubstituted thiophenes and selenophenes achieved by an easy one-pot four-step procedure. Expected compounds were obtained in good yield from ketene dithioacetals.
- Thomae, David,Perspicace, Enrico,Henryon, Dorothée,Xu, Zhanjie,Schneider, Serge,Hesse, Stéphanie,Kirsch, Gilbert,Seck, Pierre
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experimental part
p. 10453 - 10458
(2010/02/28)
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- Pyrimidine derivatives and processes for the preparation thereof
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4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I wherein the substituents are as defined in claim 1, are described.These compounds inhibit the tyrosine kinase activity of the receptor for epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.
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- Synthesis and bactericidal activity of some symmetrical bisthioalkyl derivatives
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The paper deals with the synthesis of some bactericides.The dithioacetal required are obtained by the reaction of active methylene compounds and aryl sulphonamides with carbon disulphide in alkaline conditions and subsequent alkylation with dimethyl sulphate.These compounds are then reacted with various pharmacopohores.All the compounds show moderate to significant activity with few compounds showing very high broad spectrum activity.
- Seshadri, S.,Sanghavi, N. M.,Naik, R. V.,Tawate, S. R.,Trivedi, M. N.,Fruitwala, M. A.
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p. 688 - 692
(2007/10/02)
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- Polarized Ethylenes. IV. Synthesis of Polarized Ethylenes Using Thioamides and Methyl Dithiocarboxylates and their Application to Syntheses of Pyrazoles, Pyrimidines, Pyrazolopyrimidines, and 5-Azacyclazines
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Polarized ethylenes having both electron-donating (an amino or a methylthio group) and electron-accepting (cyano, carbamoyl, methyl ester) groups on the adjacent two olefinic carbon atoms were prepared by the condensation of S-alkylthioamidinium salts or
- Tominaga, Yoshinori,Matsuoka, Yoshiki,Oniyama, Yukio,Uchimura, Yoshimitsu,Komiya, Hirofumi,et al.
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p. 647 - 660
(2007/10/02)
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- A NOVEL PREPARATION OF POLARIZED ETHYLENES BY THE REACTION OF THIOAMIDES OR DITHIOCARBOXYLATES WITH TETRACYANOETHYLENE OXIDE. SYNTHESIS OF PYRAZOLES AND PYRIMIDINES
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Polarized ethylenes having both electron-donating (an amino or a methylthio group) and electron-accepting (two cyano groups) groups on the adjacent two olefinic carbon atoms were prepared by the reaction of thioamides or methyl dithiocarboxylates with tetracyanoethylene oxide in good yields.Reactions of these polarized ethylenes with hydrazine or guanidine carbonate gave the corresponding pyrazole and pyrimidine derivatives in good yields.
- Tominaga, Yoshinori,Matsuoka, Yoshiki,Kohra, Shinya,Hosomi, Akira
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p. 613 - 616
(2007/10/02)
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- SYNTHESIS OF THIENOPYRIDINES
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Several thienopyridines could be easily synthesized by methallation using LDA directly from 3-(disubstituted amino)-2-cyano-3-methylthioacrylonitriles.
- Yokoyama, Masataka,Tohnishi, Masanori,Kurihara, Akemi,Imamoto, Tsuneo
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p. 1933 - 1936
(2007/10/02)
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