摘要:
Derivatives of known bio-affecting carboxylic acids, their non-toxic pharmaceutically acceptable acid addition salts and N-oxides as well as processes for preparing those novel derivatives are disclosed. Those derivatives having the wherein R-COO- is the acyloxy residue of a bio-affecting monocarboxylic acid; Y and Y' are each hydrogen or alkyl; n is zero or one; R1 and R2 are each inter alia alkyl, alkenyl, aryl, cycloalkyl, cycloalkenyl, aralkyl or alkaryl; and R3 is inter alia hydrogen; orthe structural formula wherein -OOC-R'-COO- is the di(acyloxy) residue of a bio-affecting dicarboxylic acid.
摘要:
L'invention concerne les produits 1: où R 1 est hydrogène, alkyle (1 à 4 C) éventuellement substitué par une fonction oxygénée ou azotée ou par un halogène, où R 1 est alkényle ou alkynyle (2 à 4 C), R 2 est alkyle (1 à 4 C), les noyaux A,B,C, et D portent éventuellement un ou plusieurs doubles liaisons et sont éventuellement substitués par une ou plusieurs OH, CO, Halogènes, alkyles ou alkoxy (1 à 4 C), alkényles ou alkynyles (2 à 4 C); leur préparation à partir des dérivés 17 (20)ène 20-formamido 21-oates d'alcoyles correspondants et leur application à la préparation des dérivés 17-hydroxy acétyl correspondants, dérivés utiles dans l'industrie pharmaceutique.
摘要:
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.
摘要:
This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.
摘要:
Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
摘要:
The present invention relates to chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, the invention enables improvement of muscular quality in sarcopenic mammals and treatment and/or prevention of sarcopenia and, in particular, sarcopenic obesity and the associated complications and/or pathologies thereof, such as loss of strength, muscle mass, performance and of physical and movement capacity. The invention also enables improvement of muscle quality in obese mammals and the treatment and/or prevention of obesity and associated complications and/or pathologies, advantageously type 2 diabetes and metabolic syndrome.