- The pyrazole derivative or its salt in a pharmaceutical composition containing them
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PROBLEM TO BE SOLVED: To provide a novel compound and a pharmaceutical composition useful for treatment and/or prevention of HIV virus infections.SOLUTION: Provided is a pyrazole derivative represented by the general formula (I) or a salt thereof (in the
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Paragraph 0081
(2017/01/26)
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- Structure-activity relationship study of phenylpyrazole derivatives as a novel class of anti-HIV agents
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The structure-activity relationship of phenylpyrazole derivative 1 was investigated for the development of novel anti-HIV agents. Initial efforts revealed that the diazenyl group can be replaced by an aminomethylene group. In addition, we synthesized various derivatives by the reductive amination of benzaldehydes with 5-aminopyrazoles and carried out parallel structural optimization on the benzyl group and the pyrazole ring. This optimization led to a six-fold more potent derivative 32j than the lead compound 1, and this derivative has a 3′,4′-dichloro-(1,1′-biphenyl)-3-yl group.
- Mizuhara, Tsukasa,Kato, Takayuki,Hirai, Atsushi,Kurihara, Hideki,Shimada, Yasuhiro,Taniguchi, Masahiko,Maeta, Hideki,Togami, Hiroaki,Shimura, Kazuya,Matsuoka, Masao,Okazaki, Shiho,Takeuchi, Tomoki,Ohno, Hiroaki,Oishi, Shinya,Fujii, Nobutaka
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p. 4557 - 4561
(2013/08/23)
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- Copper-catalyzed chlorination of functionalized arylboronic acids
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"Chemical Equation Presented" A mild, efficient, Cu(I)-catalyzed method for the conversion of arylboronic acids to aryl chlorides Is reported. This method is particularly useful for the conversion of electron-deficient arylboronic acids to aryl chlorides, a transformation that is inefficient In the absence of Cu catalysis.
- Wu, Hong,Hynes Jr., John
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supporting information; experimental part
p. 1192 - 1195
(2010/04/27)
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- Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus
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Inhibition of the protein chaperone Hsp90 is a promising new approach to cancer therapy. We describe the preparation of potent non-benzoquinone ansamycins. One of these analogues, generated by feeding 3-amino-5-chlorobenzoic acid to a genetically engineer
- Menzella, Hugo G.,Tran, Thomas-Toan,Carney, John R.,Lau-Wee, Janice,Galazzo, Jorge,Reeves, Christopher D.,Carreras, Christopher,Mukadam, Sophie,Eng, Sara,Zhong, Ziyang,Timmermans, Pieter B. M. W. M.,Murli, Sumati,Ashley, Gary W.
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supporting information; experimental part
p. 1518 - 1521
(2010/02/28)
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- Macrolactams by engineered biosynthesis
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Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the biosynt
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Page/Page column 14
(2008/12/07)
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- QUINAZOLINE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to the use of quinazoline derivatives of formula (I) wherein A, B, R1, R2, R3 and R4 are defined herein, and pharmaceutically acceptable salts thereof, for the treatment or preventi
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Page/Page column 35
(2010/11/26)
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