The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments. ##STR00001##

Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).

Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).

The present invention provides compounds of Formula I:

##STR00001##

wherein {circle around (A)}, X, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.

The present invention provides compounds of Formula I ##STR00001##
wherein ##STR00002##
X, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.

This invention relates to compounds that are agonists of the muscarinic M.sub.1 receptor or M.sub.1 and M.sub.4 receptors and which are useful in the treatment of muscarinic M.sub.1 or M.sub.1/M.sub.4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula ##STR00001##
wherein Q.sup.4, Q.sup.5, R.sup.5, p, V, Q.sup.1, Q.sup.2, X.sup.1, X.sup.2 and W are defined herein.

This invention relates to compounds that are agonists of the muscarinic M.sub.1 receptor or M.sub.1 and M.sub.4 receptors and which are useful in the treatment of muscarinic M.sub.1 or M.sub.1/M.sub.4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula ##STR00001##
wherein Q.sup.4, Q.sup.5, R.sup.5, p, V, Q.sup.1, Q.sup.2, X.sup.1, X.sup.2 and W are defined herein.

This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).