- PYRAZOLOPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR USE IN PREVENTING OR TREATING CANCER, AUTOIMMUNE DISEASE AND BRAIN DISEASE CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to a pyrazolopyrimidine derivative, a preparation method thereof and a pharmaceutical composition comprising the same as an active ingredient for the prevention or treatment of cancer, autoimmune disease and brain disease. The pyrazolopyrimidine derivative of the present invention exhibits excellent Bruton's tyrosine kinase inhibition activity, so that it can be effectively used as a pharmaceutical composition for the prevention or treatment of cancer, autoimmune disease and Parkinson's disease.
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- A systematic study on the use of different organocatalytic activation modes for asymmetric conjugated addition reactions of isoindolinones
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In this article we describe a series of new asymmetric Michael reactions of carboxylate-3-substituted isoindolinones used as nucleophiles in the synthesis of valuable chiral tetrasubstituted derivatives. It has been shown that the reactivity and enantiose
- Scorzelli, Francesco,Di Mola, Antonia,De Piano, Francesco,Tedesco, Consiglia,Palombi, Laura,Filosa, Rosanna,Waser, Mario,Massa, Antonio
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p. 819 - 828
(2017/01/28)
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- Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors
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A new series of indenoisoquinoline derivatives was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in HepG2, A549 and HCT-116 cell lines. Compounds 9a, 9b, 10a, 10c, 10e, 18a and 18b manifested potent inhibitory activity against the three tested cancer cell lines. Nineteen compounds were also tested for Top I inhibition at 50 μM. Almost all the tested compounds showed potent Top I inhibition activity at this concentration. The most potent compounds 9a and 10a demonstrated more cytotoxicity than HCPT and TPT and was comparable to CPT in inhibitory activities on Top I in our biological assay.
- Zhao, Qian,Xu, Xi,Xie, Zhouling,Liu, Xiao,You, Qidong,Guo, Qinglong,Zhong, Yi,Li, Zhiyu
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p. 1068 - 1072
(2016/05/24)
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- Synthesis and Biological Evaluation of Nitrated 7-, 8-, 9-, and 10-Hydroxyindenoisoquinolines as Potential Dual Topoisomerase i (Top1)-Tyrosyl-DNA Phosphodiesterase i (TDP1) Inhibitors
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The structure-activity relationships and hit-to-lead optimization of dual Top1-TDP1 inhibitors in the indenoisoquinoline drug class were investigated. A series of nitrated 7-, 8-, 9-, and 10-hydroxyindenoisoquinolines were synthesized and evaluated. Several compounds displayed potent dual Top1-TDP1 inhibition. The 9-hydroxy series exhibited potencies and cytotoxicities vs Top1 that surpassed those of camptothecin (CPT), the natural alkaloid that is being used as a standard in the Top1-mediated DNA cleavage assay. One member of this series was a more potent Top1 inhibitor at a concentration of 5 nM and produced a more stable ternary drug-DNA-Top1 cleavage complex than CPT. (Chemical Equation Presented).
- Nguyen, Trung Xuan,Abdelmalak, Monica,Marchand, Christophe,Agama, Keli,Pommier, Yves,Cushman, Mark
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p. 3188 - 3208
(2015/04/27)
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- HCV PROTEASE INHIBITORS
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The present invention discloses a compound of general formula (I); A is O, S, CH, NH or NR', when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C-Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or -Y1-Rm; A1 is NH or CH2; R1' is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalky etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
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Paragraph 0127; 0129
(2014/06/24)
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- HCV Protease Inhibitors
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A compound of general formula (I); A is O, S, CH, NH or NR′, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1′ is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
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Paragraph 0252; 0254-0257
(2014/06/24)
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- 2-HYDROXYISOQUINOLINE-1,3(2H,4H)-DIONES AND RELATED COMPOUNDS USEFUL AS HIV REPLICATION INHIBITORS
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The present invention relates to compounds and compositions acting as inhibitors of HIV integrase. The compound of the invention is of Formula (I), or a tautomer (I') thereof, or a pharmaceutically acceptable salt, or solvate of said compound or tautomer
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Page/Page column 111-112
(2012/07/13)
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- NOVEL INHIBITORS OF FLAVIVIRUS REPLICATION
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The present invention relates to a series of novel compounds, methods to prevent or treat viral infections by using the novel compounds, processes for preparation of the compounds, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Hepatitis C virus (HCV). The present invention also relates to the novel compounds for use as a medicine, more preferably for use as a medicine for the prevention or treatment of viral infections, preferably infections with viruses belonging to the family of the Flaviviridae.
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Page/Page column 135
(2010/06/15)
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- Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain
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We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3(2H,4H)-dione derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion catalytic active sites. The compounds were tested against HIV-1 reverse
- Billamboz, Muriel,Bailly, Fabrice,Barreca, Maria Letizia,De Luca, Laura,Mouscadet, Jean-Fran?ois,Calmels, Christina,Andréola, Marie-Line,Witvrouw, Myriam,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
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experimental part
p. 7717 - 7730
(2009/12/07)
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- Synthesis of alkoxynitrostilbenes as chromophores for nonlinear optical materials
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The synthesis of different unsymmetrical new alkoxy-nitrostilbenes bearing one or two monomers groups, as optimized nonlinear optical (NLO) chromophores, are described herein. The considered functions were acrylate and triethoxysilyl groups. The goal is t
- Diemer, Vincent,Chaumeil, Helene,Defoin, Albert,Carre, Christiane
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p. 3333 - 3338
(2008/09/21)
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- ISOQUINOLINE -1,3,4-TRIONE, THE SYNTHETIC METHOD AND THE USE THEREOF
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The invention relates to various substituted isoquinoline-1,3,4-trione, the synthetic method thereof and the use for treating neurodegenerative diseases, especially as the medicine for Alzhermer's disease, apoplexy and brain ischemic injuries. The compound is represented by the following structure formula: Wherein substituents R1 can be one, two or three groups optionally selected from the group consisting of H; alkyl; hydroxyl; alkyl substituted by the groups including halogen, alkoxyl or hydroxyl; alkoxyl or alkylamino substituted by the groups including halogen, alkoxyl or hydroxyl; C2-C6 alkenyl substituted by oxygen or amine; C3-C6 cycloalkyl; substituted aryl; benzyl; alkanoyl; alkanoyl substituted by the groups including halogen, alkoxyl or hydroxyl; C2-C6 enoyl; C3-C6 cycloalkanoyl; tert-butoxycarbonyl; benzoyl; benzoyl substituted by one, two or three groups including alkylamino; benzylacyl; benzylacyl substituted by one, two or three groups including alkylamino; thienoyl; adamantylcarbonyl; mandeloyl; alkoxyl; alkylamino; cycloalkoxyl; cycloalkylamino; amino; acylamino; alkyloxycarbonyl; cycloalkoxycarbonyl; alkanoylxy; alkanoylamino; cycloalkyanoylxy; cycloalkanoylamino; ureido; urenylene; alkanoyl; nitro; carboxyl; R2 is H; alkyl; alkyl or C1-C4 cycloalkyl substituted by the groups including halogen, alkoxyl or hydroxyl; C2-C6 alkenyl; aryl; substituted aryl; X is H, CH2, NH, O, or S; Y is CH, or N.
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Page/Page column 14
(2008/06/13)
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- Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new β-amyloid peptide production inhibitors and their activities on various classes of protease
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A series of new 7-substituted-4-chloro-3-alkoxy isocoumarin derivatives were synthesized and evaluated as inhibitors of representative classes of proteases: serine protease (α-chymotrypsin, trypsin), cysteine protease (Caspase-3), and aspartyl protease (H
- Bihel, Frederic,Quelever, Gilles,Lelouard, Hugues,Petit, Agnes,Da Costa, Cristine Alves,Pourquie, Olivier,Checler, Frederic,Thellend, Annie,Pierre, Philippe,Kraus, Jean-Louis
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p. 3141 - 3152
(2007/10/03)
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