摘要:
The present disclosure relates to compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing diseases, disorders, or conditions (e.g., associated with mitochondria).
摘要:
L'invention concerne des composés chimiques C dérivés de la norbixine et présentant un tropisme pour l'œil, destinés à être utilisés dans le traitement de maladies oculaires chez le mammifère, notamment dans le contexte d'une altération de l'épithélium pigmentaire rétinien et plus particulièrement dans le cadre de la dégénérescence maculaire liée à l'âge (DMLA) et la maladie de Stargardt.
摘要:
This invention relates to compounds that are agonists or partial agonists of the histamine site of the NMDA receptor, the method of preparation thereof and applications thereof.
摘要:
The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).
摘要:
The present invention relates to 2-adamantyl-butyramide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
摘要:
The invention relates to a new method for producing enantiomer-enriched 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivatives of the general formulae (I) and (II) in which R is hydrogen or a possibly substituted C1-8 alkyl rest, aryl rest or cycloalkyl rest and R is a possibly substituted acyl. According to said method a racemic 1-amino-4-(hydroxymethyl)-cyclopent-2-ene derivative of general formula (III), in which R has the meaning given above, is converted using a hydrolase and in the presence of an acylation agent.
摘要:
The present invention relates to novel nitric acid esters of cyclohexanol derivatives of formula (I) in which A is a valency line or a C1-C6 alkylene chain and B is the group -NR1-CO-Z, -NR1-SO2-Z or -CO-NR2-Z, where R1 is hydrogen or a C¿1?-C6-alkyl group, R?2¿ is hydrogen, a hydroxy, hydroxy-C¿1?-C6-alkyl, C1-C6-alkoxy, C1-C6-alkyl, C2-C6-alkenyl or C2C6-alkinyl group and Z is hydrogen, a C1-C6-alkyl, C2-C6-alkenyl or C2C6-alkinyl group, which may be substituted once or several times by a hydroxy, C1-C6-alkylcarbonyloxy, C1-C6-alkoxy, halogen, cyano, carboxy, C1-C6-alkoxycarbonyl, -CO-NR?3R4¿, mercapto, C¿1?-C6-alkylcarbonyl mercapto group, or Z is a C3-C6-cycloalkyl group or a pyridine, N-oxypyridine, tetrazolyl or pyrrolidinone ring, or Z together with R?2¿ and the nitrogen atom to which Z and R2 are bonded, form a heterocyclic ring which may additionally contain an oxygen, sulphur or nitrogen atom, whereby the heterocyclic ring with an additional nitrogen atom may be acylated, possibly on the nitrogen atom, by a C¿1?-C6-alkylcarbonyl group, and if B is a -NR?1¿-CO-Z- group, Z may also be a C¿1?-C6-alkoxy group, or if Z is a C1-C6-alkyl or C2-C6-alkenyl group substituted by a mercapto, C1-C6-alkylmercapto or C1-C6-alkylcarbonyl mercapto, the C1-C6-alkyl or C2-C6-alkenyl group may be additionally substituted by the NR?4/R5¿ or a C¿1?-C4-alkylcarbonyl group and R?3 and R4¿ may be the same or different and mutually independently hydrogen, a C¿1?-C6-alkyl group or R?3 and R4¿ together with the nitrogen atom to which they are bonded form a heterocyclic ring, their optically active forms and physiological permissible salts, and medicaments containing these compounds. The invention also concerns processes for producing compounds of formula (I) and novel intermediate products.
摘要:
The present invention relates to a process for the preparation of amino alcohol derivatives or salts thereof. In particular the present invention relates to process for the preparation of amino alcohol derivatives or salts thereof which may be used as intermediates in the preparation of HIV reverse transcriptase inhibitors, more preferably Carbovir and 5 Abacavir. The present invention more specifically relates to a process for the preparation of (1S, 4R)-4-amino-2-cyclopentene-1-methanol of Formula IIIa. The present invention also specifically relates to process for the preparation of Abacavir sulfate of Formula II using compound of Formula IIIa prepared according to the process of the present invention.
摘要:
The invention relates to derivatives of cyclopropenylceramide used as desaturase inhibitors characterised by the general formula I, wherein R1 may be an alkyl, alkenyl, alkynyl, aryl or any heterocyclic group, n can have any value whatsoever, be branched or not and contain unsaturations, and R2 and R3 can have the same or different values, represent aryl, heteroaryl, alkyl or acyl groups with one or more unsaturations in the chain, which may be branched or not and substituted by OH groups. The members of this new class of compounds have demonstrated an extraordinary activity as inhibitors of dihydroceramide desaturase and of ceramide biosynthesis and are useful for the treatment of pathologies associated with increases in intracellular ceramide levels.