- FACTOR XIA-INHIBITING PYRIDOBENZAZEPINE AND PYRIDOBENZAZOCINE DERIVATIVES
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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.
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Paragraph 0511-0512
(2017/10/10)
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- Substituted Oxopyridine Derivatives and Use Thereof in the Treatment of Cardiovascular Disorders
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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.
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Paragraph 0596-0598
(2016/05/02)
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- SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS
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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.
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Paragraph 0791-0794
(2016/10/07)
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- Preparation of Multiply Protected Alkylhydrazine Derivatives by Mitsunobu and PTC Approaches
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Alkylation reactions of hydrazine derivatives by Mitsunobu or PTC approaches are described. It has been shown that aminophthalimide derivatives are better acidic partners than their aminoimidodicarbonate (NBoc2) analogues, the presence of the phthaloyl group increasing the acidity of the sole proton and concomitantly reducing steric hindrance. Moreover, N-aminophthalimide derivatives can be efficiently converted into the corresponding N-amino-imidodicarbonates by a three-stage, one-flask procedure under very mild conditions. These procedures can also be efficiently used for the preparation of orthogonally Nα,Nβ -diprotected α-hydrazino esters. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003).
- Brosse, Nicolas,Pinto, Maria-Fatima,Jamart-Gregoire, Brigitte
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p. 4757 - 4764
(2007/10/03)
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- Very efficient one-pot conversion of N-aminophthalimide derivatives into the corresponding N-amino-di-tert-butyl imidodicarbonates
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The phthaloyl group can be efficiently converted in very mild conditions into bis-tert-butyloxycarbonyl group using MeNH2, then Boc2O/DMAP, in a one-flask protocol.
- Brosse, Nicolas,Jamart-Grégoire, Brigitte
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p. 249 - 251
(2007/10/03)
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- A practical reagent for the synthesis of substituted hydrazines
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A practical, inexpensive triprotected hydrazine reagent, 2-benzyloxycarbonyl-1 -tert-butoxycarbonyl-1- (4-methylphenylsulfonyl)-hydrazine, 1-Boc-1-Tos-2-Z-hydrazine (2), has been prepared on a 100 pnmol scale and examined with respect to application in st
- Grehn, Leif,Nyasse, Barthelemy,Ragnarsson, Ulf
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p. 1429 - 1432
(2007/10/03)
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- Synthesis of fused 1,2,5-triazepine-1,5-diones and some N2- and N3-substituted derivatives: Potential conformational mimetics for cis-peptidyl prolinamides
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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.
- Lenman, Morag M.,Lewis, Arwel,Gani, David
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p. 2297 - 2311
(2007/10/03)
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- Synthesis and structure of AzAsx-pro-containing Aza-peptides
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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
- Andre, Frederic,Marraud, Michel,Boussard, Guy,Didierjean, Claude,Aubry, Andre
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p. 183 - 186
(2007/10/02)
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- Conformational perturbations induced by N-amination and N-hydroxylation of peptides
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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.
- Dupont, Virginie,Lecoq, Alain,Mangeot, Jean-Paul,Aubry, André,Boussard, Guy,Marraud, Michel
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p. 8898 - 8906
(2007/10/02)
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- MONOBACTAM HYDRAZIDES CONTAINING CATECHOL SULFONIC ACID GROUPS
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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
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- Heteroaroylhydrazide derivatives of monocyclic beta-lactam antibiotics
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Compounds having the formula STR1 and pharmaceutically acceptable salts thereof and possessing antibacterial activity, and intermediates to compounds of formula I having the formula
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