- Unforeseen Possibilities to Investigate the Regulation of Polyamine Metabolism Revealed by Novel C-Methylated Spermine Derivatives
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The biogenic polyamines, spermine (Spm) and spermidine, are organic polycations present in millimolar concentrations in all eukaryotic cells participating in the regulation of vital cellular functions including proliferation and differentiation. The desig
- Khomutov, Maxim,Hyv?nen, Mervi T.,Simonian, Alina,Formanovsky, Andrey A.,Mikhura, Irina V.,Chizhov, Alexander O.,Kochetkov, Sergey N.,Alhonen, Leena,Veps?l?inen, Jouko,Kein?nen, Tuomo A.,Khomutov, Alex R.
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supporting information
p. 11335 - 11347
(2019/12/24)
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- CARBONITRILE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS
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The present invention relates to a compound of Formula 1, 2 or 3: I II III wherein A is N or -CR0--, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is -CRe --, or, -N--, where Re is hydrogen, C1 -C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1 -C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1 -C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1- C6 linear or branched chain alkyl, etc.; Q is --CO--, --(CH2)q--, --(CHRs)q--, or -(CRsRt)q- -, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to compbinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.
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Page/Page column 142
(2015/12/17)
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- Novel acetylcholine and carbamoylcholine analogues: Development of a functionally selective α4β2 nicotinic acetylcholine receptor agonist
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A series of carbamoylcholine and acetylcholine analogues were synthesized and characterized pharmacologically at neuronal nicotinic acetylcholine receptors (nAChRs). Several of the compounds displayed low nanomolar binding affinities to the α4β2 nAChR and pronounced selectivity for this subtype over α3β4, α4β4, and α7 nAChRs. The high nAChR activity of carbamoylcholine analogue 5d was found to reside in its R-enantiomer, a characteristic most likely true for all other compounds in the series. Interestingly, the pronounced α4β2 selectivities exhibited by some of the compounds in the binding assays translated into functional selectivity. Compound 5a was a fairly potent partial α4β2 nAChR agonist with negligible activities at the α3β4 and α7 subtypes, thus being one of the few truly functionally selective α4β 2 nAChR agonists published to date. Ligand-protein docking experiments using homology models of the amino-terminal domains of α4β2 and α3β4 nAChRs identified residues Val111(β2)/Ile113(β4) , Phe119(β2)/Gln121(β4), and Thr155(α4)/Ser150(α3) as possible key determinants of the α4β2/α 3β4-selectivity displayed by the analogues.
- Hansen, Camilla P.,Jensen, Anders A.,Christensen, Jeppe K.,Balle, Thomas,Liljefors, Tommy,Fr?lund, Bente
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experimental part
p. 7380 - 7395
(2009/12/07)
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- Stereoselective synthesis of 3-hydroxyproline benzyl esters from N-protected β-aminoaldehydes and benzyl diazoacetate
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The synthesis of a series of 3-hydroxyproline benzyl esters from α-alkyl and α-alkoxy N-protected aminoaldehydes with benzyl diazoacetate is described. Aldehydes with α-alkyl substituents afforded prolines as a single diastereomer with a trans-cis relativ
- Angle, Steven R.,Belanger, Dominique S.
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p. 4361 - 4368
(2007/10/03)
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- PROTECTION OF PRIMARY AND SECONDARY AMINES IN THE HYDROBORATION REACTION
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Trimethylsilyl groups are efficient to protect the N-H bonds of olefinic amines in the hydroboration reaction with BMS; deprotection is easily run with methanol and affords aminoorganoboranes which can be used without any oxydation.
- Dicko, A.,Montury, M.,Baboulene, M.
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p. 6041 - 6044
(2007/10/02)
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- Chemical process
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A process for the preparation of a compound of the formulae (Ia) and/or (Ib): STR1 wherein R1 and R2 are independently substituted or unsubstituted hydrocarbon groups or are joined together so as to form a carbocyclic or heterocyclic ring, and R3 is a substituted or unsubstituted hydrocarbon group; which process comprises the ring-closing cyclization of a compound of the formula (II): STR2 wherein R1, R2 and R3 are as defined in relation to formulae (Ia) and (Ib).
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- Substituted pyridines
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This invention relates to substituted pyridines prepared by reacting aldehydes, amines, lower carboxylic acids such as acetic acid in the presence of oxygen. The N-substituted pyridinium salts formed can be converted to pyridines by thermal dealkylation. The reactions can be summarized by the following equations: STR1
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