Patent classifications
A61K31/425
Cosmetic or dermatological preparation containing an aqueous and a lipophilic fish egg extract
A cosmetic or dermatological preparation that contains an aqueous and a lipophilic fish egg extract for replumping skin; for increasing the incorporation of triglycerides in adipocytes; for increasing the expression of laminin, preferably of laminin-5 and most preferably of laminin-5 β sub-unit; and/or for maintaining the skin elasticity and/or resilience of human skin.
Cosmetic or dermatological preparation containing an aqueous and a lipophilic fish egg extract
A cosmetic or dermatological preparation that contains an aqueous and a lipophilic fish egg extract for replumping skin; for increasing the incorporation of triglycerides in adipocytes; for increasing the expression of laminin, preferably of laminin-5 and most preferably of laminin-5 β sub-unit; and/or for maintaining the skin elasticity and/or resilience of human skin.
A METHOD FOR ENHANCING THE PHARMACOKINETICS OR INCREASING THE PLASMA CONCENTRATION OF METHYL 3-((METHYLSULFONYL)AMINO)-2-(((4-PHENYLCYCLOHEXYL)OXY)METHYL)PIPERIDINE-1-CARBOXYLATE OR A SALT THEREOF WITH AN INHIBITOR OF CYTOCHROME P450
Described herein are compositions comprising (a) methyl 3 -((methyl sulfonyl)amino)-2-(((4-phenylcyclohexyl)oxy)methyl)piperidine- 1 -carboxylate or a salt thereof; and (b) an agent for reducing metabolism of (a) and uses thereof.
A METHOD FOR ENHANCING THE PHARMACOKINETICS OR INCREASING THE PLASMA CONCENTRATION OF METHYL 3-((METHYLSULFONYL)AMINO)-2-(((4-PHENYLCYCLOHEXYL)OXY)METHYL)PIPERIDINE-1-CARBOXYLATE OR A SALT THEREOF WITH AN INHIBITOR OF CYTOCHROME P450
Described herein are compositions comprising (a) methyl 3 -((methyl sulfonyl)amino)-2-(((4-phenylcyclohexyl)oxy)methyl)piperidine- 1 -carboxylate or a salt thereof; and (b) an agent for reducing metabolism of (a) and uses thereof.
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
##STR00001##
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
##STR00001##
Combinations of RAD51 and PARP inhibitors
This application is directed to inhibitors of RAD51 represented by the following structural formula: ##STR00001##
in combination with a PARP inhibitor, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.
Combinations of RAD51 and PARP inhibitors
This application is directed to inhibitors of RAD51 represented by the following structural formula: ##STR00001##
in combination with a PARP inhibitor, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.
Bicyclic heteroaryl derivatives and preparation and uses thereof
The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans. ##STR00001##
Compositions and methods of using (R)-pramipexole
Pharmaceutical compositions of (R)-pramipexole and one or more secondary therapeutic agents such as, for example, dopamine agonists, dopaminergic agonists, COMT inhibitors, MOA inhibitors, excitatory amino acid antagonists, growth factors, neurotrophic factors, antioxidants, anti-inflammatory agents, immunomodulators, anti-glutamatergics, ion channel blockers, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, heat shock protein inducers/protein disaggregators and downregulators, monoamine oxidase type B (MOAB) inhibitors, multi-target agents, kinase inhibitors, Bcl inducers, histone deacetylase (HDAC) mediators, glial modulators, mitochondrial energy promoting agents, myostatin inhibitors, caspase inhibitors and combinations thereof or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.