C07D265/32

Amino acid-, peptide- and polypeptide-lipids, isomers, compositions, and uses thereof

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: ##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.

Amino acid-, peptide- and polypeptide-lipids, isomers, compositions, and uses thereof

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: ##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.

Quaternary heteroatom containing compounds

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.

Quaternary heteroatom containing compounds

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.

Enantioselective synthesis of α-quaternary Mannich adducts by palladium-catalyzed allylic alkylation

This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): ##STR00001##
comprising treating a compound of formula (II): ##STR00002##
with a transition metal catalyst under alkylation conditions.

Enantioselective synthesis of α-quaternary Mannich adducts by palladium-catalyzed allylic alkylation

This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): ##STR00001##
comprising treating a compound of formula (II): ##STR00002##
with a transition metal catalyst under alkylation conditions.

CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer

The present invention provides MDM2 inhibitor compounds of Formula I, or the pharmaceutically acceptable salts thereof, ##STR00001##
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer

The present invention provides MDM2 inhibitor compounds of Formula I, or the pharmaceutically acceptable salts thereof, ##STR00001##
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

DECARBOXYLASE INHIBITORS FOR TREATING PARKINSON'S DISEASE

Provided are inhibitors of pathogenic, bacterial metabolite production and conjugates of the inhibitors. Also provided are pharmaceutical compositions containing the inhibitors or conjugates and methods of using the same.

COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN

Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.