- INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
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Paragraph 0424; 0425
(2018/09/16)
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- Design and synthesis of new peptidomimetics as potential inhibitors of MurE
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With the continuing emergence and spread of multidrug-resistant bacteria, there is an urgent need for the development of new antimicrobial agents. One possible source of new antibacterial targets is the biosynthesis of the bacterial cellwall peptidoglycan
- Zivec, Matej,Turk, Samo,Blanot, Didier,Gobec, Stanislav
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experimental part
p. 95 - 109
(2012/05/04)
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- PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
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Page/Page column 254; 255
(2008/06/13)
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- Prenyl carbamates: Preparation and deprotection
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Prenyloxycarbonylimidazole (PreocIm) and prenyl p-nitrophenyl carbonate (PreocOC6H4p-NO2), two substitutes for the unstable prenyl chloroformate, allowed an efficient introduction of the prenyloxycarbonyl group to a variety of primary and secondary amines. Deprotection of prenyl carbamates was readily achieved by, first their conversion to 2-iodo-3-methoxy-3-methylbutyl carbamates with iodine in methanol followed by reductive β-elimination with zinc powder. These reaction conditions are compatible with the presence of a number of functional groups such as Boc and Cbz carbamates, sulfides, double bonds, indoles and aromatic ethers.
- Vatèle, Jean-Michel
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p. 4251 - 4260
(2007/10/03)
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- One-pot selective cleavage of prenyl carbamates using iodine in methanol followed by zinc
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The prenyloxycarbonyl (Preoc) moiety was efficiently removed from carbamates to provde the corresponding amines in good to excellent yields (63-88 percent) by using iodine in methanol followed by treatment of the resulting β-methoxyiodides by zinc powder. The reaction conditions are compatible with the presence of a number of functional groups such as Boc and Cbz carbamates, sulfides, double bonds, indoles and aromatic methyl ethers.
- Vatele, Jean-Michel
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p. 9127 - 9130
(2007/10/03)
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- Naphthrydine compounds and their azaisosteric analogues as antibacterials
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Piperidine derivatives of formula (I) or a pharmaceutically acceptable derivative thereof and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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- QUINOLINE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS
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Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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Page/Page column 11
(2010/11/30)
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- Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 1: Design of potent and specific 3,9-diazaspiro[5.5]undecanes
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The synthesis and biological activity of novel glycoprotein IIb-IIIa antagonists containing the 3,9-diazaspiro[5.5]undecane nucleus are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the spirocyclic structures as a central template for nonpeptide RGD mimics.
- Smyth,Rose,Mehrotra,Heath,Ruhter,Schotten,Seroogy,Volkots,Pandey,Scarborough
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p. 1289 - 1292
(2007/10/03)
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