127799-54-6Relevant articles and documents
FACTOR XIA-INHIBITING PYRIDOBENZAZEPINE AND PYRIDOBENZAZOCINE DERIVATIVES
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, (2017/10/10)
The invention relates to substituted pyridobenzazepine and pyridobenzazocine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Substituted Oxopyridine Derivatives and Use Thereof in the Treatment of Cardiovascular Disorders
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, (2016/05/02)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS
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, (2016/10/07)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Aza-amino acid scan for rapid identification of secondary structure based on the application of N-Boc-aza1-dipeptides in peptide synthesis
Melendez, Rosa E.,Lubell, William D.
, p. 6759 - 6764 (2007/10/03)
Azapeptides, peptide analogues in which the α-carbon of one or more of the amino acid residues is replaced with a nitrogen atom, exhibit propensity for adopting β-turn conformations. A general protocol for the synthesis of azapeptides without racemization on solid phase has now been developed by introducing the aza-amino acid residue as an N-Boc-aza1-dipeptide. This approach has been validated by the synthesis of six N-Boc-aza 1-dipeptides and their subsequent introduction into analogues of the C-terminal peptide fragment of the human calcitonin gene-related peptide (hCGRP). By performing an aza-amino acid scan of such antagonist peptides, a set of aza-hCGRP analogues was synthesized to examine the relationship between turn secondary structure and biological activity.
PYRROLIDINE COMPOUNDS
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, (2008/06/13)
The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in
Synthesis of fused 1,2,5-triazepine-1,5-diones and some N2- and N3-substituted derivatives: Potential conformational mimetics for cis-peptidyl prolinamides
Lenman, Morag M.,Lewis, Arwel,Gani, David
, p. 2297 - 2311 (2007/10/03)
The synthesis of a new fused 1,2,5-triazepine-1,5-dione heterocycle, which is expected to mimic structural features of cis-peptldyl prolinamides, is described. The required parent heterocycle, corresponding to cis-glycy-(2S)-prolinamide, has been prepared in good yield by the cyclisation of N-(2-bromoacetylprolyl)-hydrazine which is itself generated in situ from the bromoacetyl proline methyl ester. Analogues corresponding to cis-(2R)-alanyl- and cis-(2S)-alanyl-(2S)-prolinamide have been similarly prepared from the appropriate N-(2-bromopropionyl)proline methyl esters and hydrazine hydrate where the cyclisation step, involving the displacement of bromide, has been shown to occur with inversion of configuration at C-2 of the propionyl moiety. Acylation at the N-3 position of the triazepine is equivalent to N-terminal acylation of the residue preceding the proline residue in cis-aminoacyl prolinamides. This has been achieved without incident using standard peptide coupling procedures. Extension at the 'C-terminal' has been achieved by preparing elaborated hydrazine precursors which are reacted with suitably activated esters of N-α-halogenoacylprolines, prior to cyclisation, to give the required fused triazepine dione. Thus it is possible to prepare constrained cis-peptidyl prolyl peptide mimetics of defined stereochemistry based upon this new triazepine dione in which all of the non-proline residues can be varied.
Synthesis and structure of AzAsx-pro-containing Aza-peptides
Andre, Frederic,Marraud, Michel,Boussard, Guy,Didierjean, Claude,Aubry, Andre
, p. 183 - 186 (2007/10/02)
One possible α-modification in peptides is the substitution of a nitrogen for the CαH group. We propose triphosgene as a carbonylating agent for coupling the properly substituted hydrazide to the proline nitrogen to obtain the AzAsx-Pro or AzAl
Conformational perturbations induced by N-amination and N-hydroxylation of peptides
Dupont, Virginie,Lecoq, Alain,Mangeot, Jean-Paul,Aubry, André,Boussard, Guy,Marraud, Michel
, p. 8898 - 8906 (2007/10/02)
Amination and bydroxylation of the amide nitrogen in a peptide chain have little influence on the local geometry, but both affect the hydrogen-bonding network, and therefore the conformational properties of the modified peptide. An experimental study in solution (IR spectroscopy and 1H-NMR) and in the solid state (X-ray diffraction) has been carried out on the N-amino and N-hydroxy analogues of the two RCO-Pro-NHMe and RCO-Pro-Gly-NHiPr peptides known to adopt preferentially the γ- and β-turn structures, respectively. The N-amino group is a weak proton donor which does not interact significantly with the peptide chain. On the contrary, the N-hydroxyl group is a strong proton donor giving close contacts with the peptide carbonyls. The resulting folded conformers of an expanded γ- or β-like type, presenting an 8- or 11-membered cycle instead of a 7- or 10-membered cycle in the cognate peptides have been also analyzed by a SYBYL molecular dynamics simulation.
Monobactam hydrazide derivatives
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, (2008/06/13)
Compounds having the formula I and pharmaceutically acceptable salts thereof which possess antibacterial activity. Rs is a substituted hydroxy pyridone of the formulae: II and III wherein Y1 is CH2X; COOR6; CONR7R8; OH; OCH2R9; CHF2; CHO; CH=N-OR10; CH=CH-R11; CN; CH=N-NHR12, and Y2 is hydrogen; COOH; CONH2; CN; CSNH2; COO lower alkyl; CONR7/R8
MONOBACTAM HYDRAZIDES CONTAINING CATECHOL SULFONIC ACID GROUPS
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, (2008/06/13)
Antibacterial activity is exhibited by novel compounds having the formula or a pharmaceutically acceptable salt thereof. R3 and R4 are the same or different and each is hydrogen or alkyl or R3 and R4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring. Y1 and Y2 are either hydrogen or OR11 but are not the same. R11 is hydrogen, alkanoyl of from one to ten carbon atoms, substituted alkanoyl of from two to ten carbon atoms, phenylcarbonyl, (substituted phenyl) carbonyl, heteroarylcarbonyl, phenylalkanoyl, (substituted phenyl) alkanoyl, or heteroarylalkanoyl