In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.

In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability. ##STR00001##
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.

In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.

In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.

The present invention provides a compound having the structure: ##STR00001## wherein X is a therapeutic agent containing at least one amine nitrogen and the amine nitrogen on the therapeutic agent covalently bonds directly to carbon ; Z is CH.sub.3 or CF.sub.3; R.sub.1 is H, NR.sub.2R.sub.3, NHC(O)R.sub.4, NHC(O)OR.sub.4, CH.sub.2C(O)NR.sub.5R.sub.6, OR.sub.7, CO.sub.2R.sub.7, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, aryl, or heteroaryl, wherein R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each, independently, H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, an amino acid or an oligopeptide; wherein an amine of the amino acid or oligopeptide is substituted or unsubstituted; and n is an integer from 0 to 6;
or a diastereomer, enantiomer or pharmaceutically acceptable salt of the compound.

The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH-1/3T3 (non cancer cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability.

##STR00001##

Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.