The present disclosure relates to a dendrimer-based conjugate of the formula V.sub.m-D-C-D-(T-F).sub.n, which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.

The present disclosure relates to a dendrimer-based conjugate of the formula V.sub.m-D-C-D-(T-F).sub.n, which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.

The invention includes taxoid compounds represented by the formula:

##STR00001##

wherein: R.sup.1 represents a methyl group or a fluorine; R.sup.2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R.sup.3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R.sup.4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.

The invention includes taxoid compounds represented by the formula:

##STR00001##

wherein: R.sup.1 represents a methyl group or a fluorine; R.sup.2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R.sup.3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R.sup.4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.

Aromatic entities that modulate HIF-2 activity, pharmaceutical compositions containing the aromatic entities, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2 activity are described herein.

Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect the function of ion channels in a cell, and are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including inflammatory eye diseases such as uveitis, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers.

Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect the function of ion channels in a cell, and are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including inflammatory eye diseases such as uveitis, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers.

Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.