C07D203/10

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

##STR00001##

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

##STR00001##

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30alkyl, optionally substituted C.sub.10-C.sub.30alkenyl, optionally substituted C.sub.10-C.sub.30alkynyl, optionally substituted C.sub.10-C.sub.30acyl, or -linker-ligand; R3 is H, optionally substituted C.sub.1-C.sub.10alkyl, optionally substituted C.sub.2-C.sub.10alkenyl, optionally substituted C.sub.2-C.sub.10alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O).sub.2N(Q), S(O).sub.2, N(Q)S(O).sub.2, SS, ON, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, -aminoalkyl, -(substituted)aminoalky, -phosphoalkyl or -thiophosphoalkyl.

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30alkyl, optionally substituted C.sub.10-C.sub.30alkenyl, optionally substituted C.sub.10-C.sub.30alkynyl, optionally substituted C.sub.10-C.sub.30acyl, or -linker-ligand; R3 is H, optionally substituted C.sub.1-C.sub.10alkyl, optionally substituted C.sub.2-C.sub.10alkenyl, optionally substituted C.sub.2-C.sub.10alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O).sub.2N(Q), S(O).sub.2, N(Q)S(O).sub.2, SS, ON, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, -aminoalkyl, -(substituted)aminoalky, -phosphoalkyl or -thiophosphoalkyl.

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

##STR00001##

wherein: R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

Cannabinoid derivatives

The current application relates to cannabinoid derivatives of formula (I) and pharmaceutical compositions comprising the same. The cannabinoid derivative can be used for the treatment of diseases associated with cannabinoid receptor such as pain, ADHD/ADD, alcohol use disorder, anxiety disorder, and dementias.

Cannabinoid derivatives

The current application relates to cannabinoid derivatives of formula (I) and pharmaceutical compositions comprising the same. The cannabinoid derivative can be used for the treatment of diseases associated with cannabinoid receptor such as pain, ADHD/ADD, alcohol use disorder, anxiety disorder, and dementias.

Lipids and compositions for the delivery of therapeutics

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: ##STR00001##

Lipids and compositions for the delivery of therapeutics

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure ##STR00001##
wherein:
R.sub.1 and R.sub.2 are each independently for each occurrence optionally substituted C.sub.10-C.sub.30 alkyl, optionally substituted C.sub.10-C.sub.30 alkenyl, optionally substituted C.sub.10-C.sub.30 alkynyl, optionally substituted C.sub.10-C.sub.30 acyl, or -linker-ligand; R.sub.3 is H, optionally substituted C.sub.1-C.sub.10 alkyl, optionally substituted C.sub.2-C.sub.10 alkenyl, optionally substituted C.sub.2-C.sub.10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, -aminoalkyls, -(substituted)aminoalkyls, -phosphoalkyls, -thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40 K), optionally substituted mPEG (mw 120-40 K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).