摘要:
On a découvert que par l'utilisation de diméthyle formamide comme élément de solvant, le procédé d'Albertson de préparation d'amino-acides est applicable à la préparation avec un bon rendement d'amino-acides aliphatiques à chaîne longue que l'on obtenait antérieurement avec un mauvais rendement. Les produits, dont certains sont nouveaux, ont des propriétés intrinsèquement utiles, du fait de leur structure analogue à celle d'un lipide; par des réactions d'accouplement utilisant un carbodiimide et un catalyseur de transfert de phase, ces produits peuvent en outre être hétéro-oligomérisés pour obtenir des lipopeptides utiles. On peut incorporer ces monomères ou lipopeptides dans des peptides bioactifs afin d'augmenter leur caractère hydrophobe, ou les conjuguer avec des agents pharmaceutiques afin de modifier leurs propriétés pharmaceutiques, comprenant la translocation à travers des membranes biologiques et la stabilité métabolique. On peut ainsi les polymériser, via leurs anhydrides Leuchs ou des esters actifs, pour obtenir des lipoprotéines.
摘要:
The invention relates to novel Rauwolfia alkaloid derivatives of formula (I) combinations of Rauwolfia alkaloid derivatives and a mitochondrial inhibitor, e.g. metformin, and the use of Rauwolfia alkaloid derivatives in combination with mitochondrial inhibitor for the treatment of cancer and for achieving clinical immunosuppression. The invention also relates to a fluorescence-based method for predicting the sensitivity of a cancer cell towards a compound of formula (I).
摘要:
The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
摘要:
The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).
摘要:
Disclosed are nitrosated and nitrosylated α-adrenergic receptor antagonists, compositions of an α-adrenergic receptor antagonist (α-antagonist), which can optionally be substituted with at least one NO or NO 2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO + ) or nitroxyl (NO - ), or as the neutral species, nitric oxide (NO.); and uses for each of them in treating human impotence or erectile dysfunction.
摘要:
Disclosed are nitrosated and nitrosylated α-adrenergic receptor antagonists, compositions of an α-adrenergic receptor antagonist (α-antagonist), which can optionally be substituted with at least one NO or NO 2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO + ) or nitroxyl (NO - ), or as the neutral species, nitric oxide (NO.); and uses for each of them in treating human impotence or erectile dysfunction.
摘要:
The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).