16279-88-2Relevant academic research and scientific papers
NOVEL COMPOUNDS
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Page/Page column 65-66, (2016/04/20)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
IMINOSUGARS USEFUL FOR THE TREATMENT OF VIRAL DISEASES
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Page/Page column 53, (2016/06/01)
Formula IA, ad their use for treating viral infections.
HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000186; 000187; 000501; 00050, (2016/05/02)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS
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Paragraph 2111; 2113, (2016/08/03)
The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5′ and R6 are described herein.
HIV PROTEASE INHIBITORS
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Page/Page column 33-34, (2013/05/21)
Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs
Jia, Zhaozhong J.,Wu, Yanhong,Huang, Wenrong,Zhang, Penglie,Clizbe, Lane A.,Goldman, Erick A.,Sinha, Uma,Arfsten, Ann E.,Edwards, Susan T.,Alphonso, Merlyn,Hutchaleelaha, Athiwat,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 1221 - 1227 (2007/10/03)
A variety of P4 motifs have been examined to increase the binding affinity and in vitro anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5- carboxylamide-based fXa inhibitors. Highly potent 2-naphthyl-P1 fXa inhibitors (Ki≤2 nM) with improved in vitro anticoagulant activity (2×TG≤1 μM) and respectable pharmacokinetic properties have been discovered.
Optically active antifungal azoles. XI. An alternative synthetic route for 1-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl )propyl]-3-[4-(1H-1-tetrazolyl)phenyl]-2-imidazolidinone (TAK-456) and its analog
Ichikawa, Takashi,Kitazaki, Tomoyuki,Matsushita, Yoshihiro,Hosono, Hiroshi,Yamada, Masami,Mizuno, Masahiro,Itoh, Katsumi
, p. 1947 - 1953 (2007/10/03)
New routes for the synthesis of the optically active antifungal triazoles 1-[(1R,2R)-2-(2,4-difluorophenyl)-2-Hydroxy-1-Methyl-3-(1H-1,2,4-triazol-1-Yl )propyl]-3-[4-(1H-1-tetrazolyl)phenyl]-2-imidazolidinone (1b) and the 3-[4-(1H-1,2,3-triazol-1-Yl)phenyl]-2-imidazolidinone analog (1a) that possess an imidazolidine nucleus were established. The key synthetic intermediates, (2R,3R)-3-(2,2-diethoxyethyl)amino-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol -1-Yl)-2-butanol (8) and (2R,3R)-2-(2,4-difluorophenyl)-3-(2-hydroxyethyl)amino-1-(1H-1,2,4-triazol-1- yl)-2-butanol (14), were prepared by the ring-Opening reaction of the oxirane (2) with the corresponding 2-Substituted ethylamines. The acetal (8) was converted to the imidazolidinones (1a, b) by condensation with the carbamates (10a, b) followed by treatment with hydrochloric acid and subsequent catalytic hydrogenation. The candidate selected for the clinical trials, 1b (TAK-456), was alternatively prepared from the hydroxyethylamino intermediate (14) via two reaction steps: condensation with the carbamate (10b) to the urea (15) and subsequent cyclization to the imidazolidinones. This newly developed synthetic route could be applied to a large scale preparation of 1b.
Optically active antifungal azoles. X. Synthesis and antifungal activity of N-[4-(azolyl)phenyl]- and N-[4-(azolylmethyl)phenyl]-N′-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy -1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-azolones
Kitazaki, Tomoyuki,Ichikawa, Takashi,Tasaka, Akihiro,Hosono, Hiroshi,Matsushita, Yoshihiro,Hayashi, Ryogo,Okonogi, Kenji,Itoh, Katsumi
, p. 1935 - 1946 (2007/10/03)
New optically active antifungal azoles, N-[4-(azolyl)phenyl]- and N-[4-(azolylmethyl)phenyl]-N′-[(1R,2R)-2-(2,4-difluorophenyl)-2-hydroxy -1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]azolones (1, 2, 3), were prepared in a stereocontrolled manner. Compounds 1
FT-IR and 13C-NMR Correlations for Some N-Substituted Azoles and Benzazoles
Elguero, Jose,Gil, Manuel,Iza, Nerea,Pardo, Carmen,Ramos, Mar
, p. 1111 - 1119 (2007/10/02)
The FT-IR (in carbon tetrachloride) and 13C-NMR (in deuterochloroform) spectra of six p-substituted aniline derivatives, as reference compounds, and nine 1-p-aminophenyl-azoles and benzazoles were recorded.The mesured spectral parameters from FT-IR were s
