- PYRAZOLONE DERIVATIVE HAVING CYCLIC SIDE CHAIN
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PROBLEM TO BE SOLVED: To provide a compound that has excellent inhibitory action on ATPase activity of TIP48/TIP49 complex and is therefore useful for the treatment of tumor, or a pharmacologically acceptable salt thereof. SOLUTION: The present invention provides a compound having a structure represented by general formula (I), its pharmacologically acceptable salt, or a pharmaceutical composition comprising the compound (where R1, R2, R3, R4, R5, R6, R7, W, and Z are as defined in the specifications). SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0414; 0415
(2016/10/08)
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- Synthesis of 3-(2-aminoethyl)-5-hydroxy-1H-pyrazole derivatives
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Treatment of β-keto ester 8 with hydrazines 9a-g gave 1'-substituted tert-butyl 2-(5-hydroxy-1Hpyrazol- 3-yl)ethylcarbamates 10a-e and 2-(5-oxo-2,5-dihydro-1H-pyrazol-3-yl)ethylcarbamates 11f,g. Acidolytic deprotection of 10b,c afforded the corresponding 3-(2-aminoethyl)-5-hydroxy- 1H-pyrazoles 6b,c in good yields. Acylation of 6 gave either the N-acyl compounds 12b,c and 13c, or the N,O-diacyl derivative 14. Next, three N,N-dialkyl analogues 15a,b and 26c were prepared from dimethyl acetone-1,3-dicarboxylate 21 via condensation with hydrazines 9a and 9h followed by hydrolysis of the esters 22a,b, amidation of the carboxylic acids 23a,b, and reduction of the tertiary carboxamides 24a and 25b,c. ARKAT-USA, Inc.
- Groselj, Uros,Kralj, David,Wagger, Jernej,Dahmann, Georg,Stanovnik, Branko,Svete, Jurij
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scheme or table
p. 49 - 65
(2012/03/11)
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- Transformations of alkyl (5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl)acetates into 5-heteroaryl-3-oxo-2-phenyl-3,5-dihydro-2H-pyrazolo[4,3-c] pyridine-7-carboxylates
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Alkyl [(Z)-4-dimethylaminomethylidene-5-oxo-1-phenyl-4,5-dihydro-1H-pyrazol-3-yl] acetate (4) was transformed with N- and C-nucleophiles into alkyl [4-(substituted amino)methylidene-4,5-dihydro-1H-pyrazol-3- yl] acetates (7) and alkyl (4-heteroarylmethylidene-4,5-dihydro-1H -pyrazol-3-yl)acetates (8), respectively. Compounds (7) cyclize by heating with DMFDMA in DMF into 2H-pyrazolo[4,3-c]pyridine-7-carboxylates (9).
- Bevk, David,Jak?e, Renata,Svete, Jurij,Golobi?, Amalija,Goli?, Ljubo,Stanovnik, Branko
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p. 197 - 223
(2007/10/03)
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