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 invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, ##STR00001## In formula (I), R.sub.1 is COR.sub.6, COOR.sub.6 or CONR.sub.7aR.sub.7b; R.sub.2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R.sub.3 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6 or OCONR.sub.7aR.sub.7b; R.sub.4 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6, OCONR.sub.7aR.sub.7b or H; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R.sub.7a and R.sub.7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R.sub.1 is COR.sub.6 or COOR.sub.6; R.sub.2 is an aromatic group; R.sub.3 is OR.sub.6; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, ##STR00001## In formula (I), R.sub.1 is COR.sub.6, COOR.sub.6 or CONR.sub.7aR.sub.7b; R.sub.2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R.sub.3 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6 or OCONR.sub.7aR.sub.7b; R.sub.4 is OR.sub.6, OCOOR.sub.6, OCOSR.sub.6, OCONR.sub.7aR.sub.7b or H; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R.sub.7a and R.sub.7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), R.sub.1 is COR.sub.6 or COOR.sub.6; R.sub.2 is an aromatic group; R.sub.3 is OR.sub.6; wherein, R.sub.6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.

The present invention involves a compound represented by general formula (I), a derivative thereof and a use thereof: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c and X are defined as in the description.

The present invention involves a compound represented by general formula (I), a derivative thereof and a use thereof: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c and X are defined as in the description.

Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G or Formula M: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G or Formula M: ##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

This document relates to non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising non-covalently bound complexes comprising cabazitaxel and human serum albumin. This document also relates to compositions comprising cabazitaxel and human serum albumin. This document also relates to compositions consisting essentially of cabazitaxel and human serum albumin.

Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.