Patent classifications
C07D211/06
Lipids and Lipid Compositions for the Delivery of Active Agents
This invention provides for a compound of formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.3, n, p, L.sub.1 and L.sub.2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
METHODS FOR FORMING ARYL CARBON-NITROGEN BONDS USING LIGHT AND PHOTOREACTORS USEFUL FOR CONDUCTING SUCH REACTIONS
The disclosure relates to a method for forming aryl carbon-nitrogen bonds and to photoreactors useful in these and other light-driven reactions. The method comprises contacting an aryl halide with an amine in the presence of a Ni salt catalyst solution and an optional base, thereby forming a reaction mixture; exposing the reaction mixture to light under reaction condition sufficient to produce the aryl carbon-nitrogen bonds. In certain embodiments, the amine may be present in a molar excess to the aryl halide. In certain embodiments, the Ni salt catalyst solution includes a Ni(II) salt and a polar solvent, wherein the Ni(II) salt is dissolved in the polar solvent. In certain embodiments, the reactions conditions include holding the reaction mixture at between about room temperature and about 80 C. for between about 1 hour and about 20 hours such that at least about 50% yield is obtained.
METHODS FOR FORMING ARYL CARBON-NITROGEN BONDS USING LIGHT AND PHOTOREACTORS USEFUL FOR CONDUCTING SUCH REACTIONS
The disclosure relates to a method for forming aryl carbon-nitrogen bonds and to photoreactors useful in these and other light-driven reactions. The method comprises contacting an aryl halide with an amine in the presence of a Ni salt catalyst solution and an optional base, thereby forming a reaction mixture; exposing the reaction mixture to light under reaction condition sufficient to produce the aryl carbon-nitrogen bonds. In certain embodiments, the amine may be present in a molar excess to the aryl halide. In certain embodiments, the Ni salt catalyst solution includes a Ni(II) salt and a polar solvent, wherein the Ni(II) salt is dissolved in the polar solvent. In certain embodiments, the reactions conditions include holding the reaction mixture at between about room temperature and about 80 C. for between about 1 hour and about 20 hours such that at least about 50% yield is obtained.
Lipids and lipid compositions for the delivery of active agents
This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.3, n, p, L.sub.1 and L.sub.2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. ##STR00001##
Lipids and lipid compositions for the delivery of active agents
This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.3, n, p, L.sub.1 and L.sub.2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. ##STR00001##
Muscarinic M1 receptor agonists
This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R.sub.1-R.sub.6 are as defined herein. ##STR00001##
Muscarinic M1 receptor agonists
This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R.sub.1-R.sub.6 are as defined herein. ##STR00001##
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
Substituted 4-phenylpiperidines, their preparation and use
The present invention provides a compound having the structure: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently H, halogen, CF.sub.3 or C.sub.1-C.sub.4 alkyl, wherein two or more of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 are other than H; R.sub.6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is H, R.sub.2 is CF.sub.3, R.sub.3 is H, R.sub.4 is CF.sub.3, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is H, R.sub.3 is H, R.sub.4 is F, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, then B is other than ##STR00002##
or a pharmaceutically acceptable salt thereof.