- Derivatives of m-Guaiacol, Their Preparation and Their Uses
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The invention concerns derivatives of m-guaiacol, their preparation and their uses as biocides, in particular as antibacterials or disinfectants.
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Paragraph 0125; 0138
(2021/11/05)
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- Copper-Catalyzed Hydroxylation of (Hetero)aryl Halides under Mild Conditions
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The combination of Cu(acac)2 and N,N′-bis(4-hydroxyl-2,6-dimethylphenyl)oxalamide (BHMPO) provides a powerful catalytic system for hydroxylation of (hetero)aryl halides. A wide range of (hetero)aryl chlorides bearing either electron-donating or -withdrawing groups proceeded well at 130 °C, delivering the corresponding phenols and hydroxylated heteroarenes in good to excellent yields. When more reactive (hetero)aryl bromides and iodides were employed, the hydroxylation reactions completed at relatively low temperatures (80 and 60 °C, respectively) at low catalytic loadings (0.5 mol % Cu).
- Xia, Shanghua,Gan, Lu,Wang, Kailiang,Li, Zheng,Ma, Dawei
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supporting information
p. 13493 - 13496
(2016/10/31)
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- PROTEIN KINASE INHIBITORS
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The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
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Paragraph 0173
(2015/07/15)
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- 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
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Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like.)
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Page/Page column 57
(2012/09/11)
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- Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses
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Biaryl ethers were recently reported as potent NNRTIs. Herein we disclose a detailed SAR study that led to the biaryl ether 6. This compound possessed excellent potency against WT RT and key clinically observed RT mutants and had an excellent pharmacokinetic profile in rats, dogs, and rhesus macaques. The compound also exhibited a clean safety profile in preclinical safety studies.
- Su, Dai-Shi,Lim, John J.,Tinney, Elizabeth,Wan, Bang-Lin,Young, Mary Beth,Anderson, Kenneth D.,Rudd, Deanne,Munshi, Vandna,Bahnck, Carolyn,Felock, Peter J.,Lu, Meiquing,Lai, Ming-Tain,Touch, Sinoeun,Moyer, Gregory,DiStefano, Daniel J.,Flynn, Jessica A.,Liang, Yuexia,Sanchez, Rosa,Perlow-Poehnelt, Rebecca,Miller, Mike,Vacca, Joe P.,Williams, Theresa M.,Anthony, Neville J.
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experimental part
p. 7163 - 7169
(2010/06/16)
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- HIV reverse transcriptase inhibitors
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Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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Page/Page column 57-58
(2010/11/25)
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- CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
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Page/Page column 48
(2008/06/13)
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- PHENOXYETHER DERIVATIVES AS PPAR MODULATORS
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The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR), such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
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Page/Page column 94-95
(2008/06/13)
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