- BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
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Paragraph 0309
(2015/06/25)
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- Direct guanylation of amino groups by cyanamide in water: Catalytic generation and activation of unsubstituted carbodiimide by scandium(iii) triflate
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Guanylation proceeded efficiently upon treatment of the various amines with cyanamide in the presence of catalytic amounts of scandium(III) triflate under mild conditions. The method did not require the guanylation reagents to be preactivated, and the reaction proceeded efficiently in water. The method, therefore, has practical utility for substrates that dissolve only in aqueous solutions, for example, peptides or pharmacologically important compounds. Georg Thieme Verlag Stuttgart New York.
- Tsubokura, Kazuki,Iwata, Takayuki,Taichi, Misako,Kurbangalieva, Almira,Fukase, Koichi,Nakao, Yoichi,Tanaka, Katsunori
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p. 1302 - 1306
(2014/06/10)
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- Synthesis and antitumor activities of a new series of 4,5-dihydro-1H- thiochromeno[4,3-d]pyrimidine derivatives
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A new series of 4,5-dihydro-1H-thiochromeno[4,3-d ]pyrimidine derivatives have been designed and synthesized. The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-(benzo[d][1,3]dioxol-5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4, 5-dihydro-1H-thiochromeno[4,3-d]pyrimidine (CH05) (IC50 = 0.44 μM, 3.07 μM) was 2.0 and 8.4 times more active than gefitinib (IC50 = 0.89 μM, 16.81 μM) against A549 and H460 cell lines, respectively.
- Guo, Dexiang,Liu, Yajing,Li, Ting,Wang, Nan,Zhai, Xin,Hu, Chun,Gong, Ping
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experimental part
p. 347 - 351
(2012/08/08)
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- Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
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A series of 2,5-disubstituted pyrimido[5,4-c]quinoline derivatives were synthesized and their cytotoxic activity against H460, HT-29 and MDA-MB-231 cell lines was evaluated in vitro. It was found that most of the tested compounds especially compound 17, s
- Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
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scheme or table
p. 1277 - 1280
(2012/01/06)
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- Amidination of amines under microwave conditions using recyclable polymer-bound 1H-pyrazole-1-carboxamidine
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A convenient one-step transformation of primary and secondary amines into the corresponding unprotected guanidines using 4-benzyl-3,5-dimethyl-1H- pyrazole-1-carboxamidine and its polymer-bound variant is described. The scopes and limitations of the method, the microwave-assistance of amidination as well as a recycling protocol are examined. Georg Thieme Verlag Stuttgart.
- Solodenko, Wladimir,Broeker, Patrick,Messinger, Josef,Schoen, Uwe,Kirschning, Andreas
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p. 461 - 466
(2007/10/03)
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- Optimisation of the synthesis of guanidines from amines via nitroguanidines using 3,5-dimethyl-N-nitro-1H-pyrazole-1-carboxamidine
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The synthesis of the useful reagent for the preparation of guanidines, 3,5-dimethyl-N-nitro-1-pyrazole-1-carboxamidine (DMNPC), has been optimised. A detailed protocol for using this reagent for the preparation in pure form of a range of guanidines via nitroguanidines is described. A comparison has been made regarding efficiency between DMNPC and the guanidinylating reagents N,N′-bis-Boc-1-pyrazole-1-carboxamidine (2) and N,N′-bis-Boc- N′-triflylguanidine (3).
- Castillo-Melendez, Joel A.,Golding, Bernard T.
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p. 1655 - 1663
(2007/10/03)
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- A new reagent and its polymer-supported variant for the amidination of amines
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New reagents for the high yielding amidination of primary and secondary amines are described. By attaching a benzyl substituent to the 3,5-dimethyl-1H-pyrazole-1-carboxamidine ring, a reagent 1 is obtained which allows easy work-up after amidination because of solubility of byproducts in organic solvents. In addition, the polystyrene-bound analogue 2 was prepared which allows amidination of various amines with high purity.
- Dr?ger, Gerald,Solodenko, Wladimir,Messinger, Josef,Sch?n, Uwe,Kirschning, Andreas
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p. 1401 - 1403
(2007/10/03)
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- Method of modifying wrinkles using guanidine derivatives
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The invention relates to wrinkling modifiers and anti-aging cosmetic compositions which each comprise a guanidine derivative represented by the following general formula (1): wherein is a heterocyclic group selected from azetidine, pyrrolidine, piperidine, piperazine or morpholine, and R1and R2are the same or different from each other and independently a hydrogen atom, or an alkyl, hydroxyl, hydroxyalkyl, carboxyl, carboxyalkyl or amidino group, or a salt thereof. The cosmetic compositions are excellent in the effects of suppressing wrinkling and of removing wrinkles and give users a pleasant feeling upon use.
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- Fluorophenoxyphenoxypropionates and derivatives thereof
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Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.
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- Fluorophenoxyphenoxypropionates and derivatives thereof
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Novel intermediates useful in the preparation of fluorophenoxyphenoxypropionates and derivatives thereof which possess herbicidal activity selectively in the presence of broadleaf crops.
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- Fluorophenoxyphenoxypropionates and derivatives thereof
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Novel intermediates useful in the preparation of fluorophenoxyphenoxypropionates and derivatives thereof which possess herbicidal activity selectively in the presence of broadleaf crops.
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- N1- and N2-Substituted 2-Amino-5,6-dihydro-4(1H)-pyrimidinones (Heterocyclic Compounds, 79)
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The reactions of the monosubstituted guanidines 2b-h with methyl acrylate in dimethylformamide or ethanol as solvent preferentially afford 1-substituted 2-amino-5,6-dihydro-4(1H)-pyrimidinones 6b-h.The structures of 1-hexyl- and 1-benzyl-4-pyrimidinones 6c, e and of the picrate of 1-phenylpyrimidinone 6g were proved by comparison with authentic samples, which were prepared from N-substituted ethyl 3-amino-propionates 14c, e and g and cyanamide.Accordingly, 6g is not identical with authentic 2-phenylaminopyrimidinone 7g (prepared from 2-methylthio-4-pyrimidinone 10 and 2-thioxo-4-pyrimidinone 12 respectively, compare.N,N-Disubstituted guanidines 2i-m react with methyl acrylate in dimethylformamide as solvent to afford N2,N2-disubstituted 2-amino-5,6-dihydro-4-(1H)-pyrimidinones 7i-m.Action of morpholine-4-carboxamidine (2l) on methyl acrylate in ethanol yields 2-morpholinopyrimidinone 7l as byproduct and 3-ethoxy-N-propionamide (9l) as mainproduct.Keywords: Acrylic acid methylester, reactions; Guanidines, mono- and N,N-disubstituted; Propionamide, 3-ethoxy-N-; 4(1H)-Pyrimidinones, 2-amino; Pyrimidine-1-propionic acid ethylester, hexahydro-4-oxo-2-thioxo
- Wendelin, Winfried,Riedl, Renate
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p. 237 - 252
(2007/10/02)
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