18922-72-0Relevant articles and documents
HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Paragraph 000186; 000501, (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; 2112, (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.
NOVEL COMPOUNDS
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Page/Page column 65, (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.
Palladium-Catalyzed 2H-1,2,3-Triazole-Directed Oxidative Alkoxylation of Arenes with Alcohols
Shi, Wenjuan,Shi, Zhangjie
supporting information, p. 974 - 980 (2016/02/18)
A palladium catalyzed ortho-alkoxylation of aryl C-H bond was accomplished with primary and secondary alcohols as alkoxylation reagents and with triazole as new directing group. This transformation has a good functional group tolerance and is not sensitive to moisture and air. A palladium catalyzed ortho-alkoxylation of aryl C-H bond with alcohols was described. Trizaole was used as new directing group. A series of functional groups could be tolerated and the reaction is not sensitive to moisture and air.
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
Amide thiadiazole inhibitors of plasminogen activator inhibitor-1
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Page/Page column 24, (2010/02/12)
Methods of treating disorders associated with elevated levels of PAI-1 are disclosed comprising administering to a patient in need thereof a therapeutically effective amount of at least one compound of formula at least one compound of formula (I), or a ph
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.
Azole antifungal agents, processes for the preparation thereof, and intermediates
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Page 74-75, (2010/01/31)
A compound represented by the general formula: wherein R1 and R2 denote a halogen atom or hydrogen atoms; R3 means a hydrogen atoms or lower alkyl group; r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic rings, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for -S-, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.
Azole compounds, their production and use
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, (2008/06/13)
PCT No. PCT/JP96/00325 Sec. 371 Date Oct. 17, 1996 Sec. 102(e) Date Oct. 17, 1996 PCT Filed Feb. 15, 1996 PCT Pub. No. WO96/25410 PCT Pub. Date Aug. 20, 1996The present invention provides an azole compound represented by the formula (I): wherein Ar is an
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