摘要:
The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection.
摘要:
The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要:
The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11Beta-HSD type 1 activity. X-17377
摘要:
Die vorliegende Erfindung betrifft flächenförmige, bei Kontakt mit Feuchtigkeit schnell zerfallende, Arzneimittelzubereitung auf Basis hydrophiler Polymere zur Behandlung von Demenzerkrankungen, wobei die Darreichungsform eine Wirkstoffkombination aus mindestens zwei Wirkstoffen enthält, die zur Behandlung von Demenzen (Antidementiva) geeignet sind. Bevorzugt sind die Antidementiva dabei aus der Gruppe ausgewählt, die Acetylcholinesterase-Hemmstoffe (AchE- Hemmer) und NMDA-Antagonisten (n-Methyl-D-Asparaginsäure- Antagonisten) umfaßt. Die Erfindung betrifft ferner die Verwendung einer solchen Wirkstoffkombination zur Herstellung eines oral verabreichbaren Arzneimittels zur Behandlung von Demenzerkrankungen wie Alzheimer, sowie ein Verfahren zur symptomatischen Behandlung von Alzheimer durch orale Verabreichung einer der genannten Arzneimittelzubereitungen.
摘要:
The present invention discloses novel compounds of Formula I: possessing 11 ß-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ß -HSD type 1 activity.
摘要:
Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
摘要:
La présente invention se rapporte aux nécessités de la vie et plus particulièrement au domaine de la cosmétologie et de la dermatologie. Elle a plus particulièrement pour objet de nouvelles compositions cosmétologiques et/ou dermatologiques, qui provoquent une augmentation très significative du dépôt de collagène de type (III) dans la matrice extra-cellulaire, caractérisées en ce qu'elles renferment à titre de principe actif une association d'un amidoester d'acide gras de 4-hydroxyproline, de formule (I) : dans laquelle R 1 et R' 1 sont des chaînes aliphatiques, identiques ou différentes, comportant de 10 à 24 atomes de carbone en ligne droite ou ramifiée et d'un extrait de l'épicarpe du fruit d’Opuntia Ficus-indica (Figue de Barbarie) dans un excipient ou un véhicule inerte non toxique approprié à l'usage topique. Utilisation sous forme de gel ou de crème grasse pour la production accrue de collagène, sans amplifier celle du pro-collagène (III) ni des enzymes de la famille des métallo- protéinases.
摘要:
Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.
摘要:
The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
摘要:
The present invention provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.