Polymer-sunitinib conjugates
Inventors
Culbertson, Sean M. • Kozlowski, Antoni • Vinson, Tony Drew
Assignees
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Publication Number
US-11419943-B2
Publication Date
2022-08-23
Expiration Date
Abstract
The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form.
Core Innovation
The invention relates to a method of treating a subject diagnosed with renal cancer, colorectal cancer, or gastrointestinal cancer by administering a pharmacologically effective amount of a compound having a defined structure. The compound includes a residue R that is a polyol, polythiol or polyamine bearing from 3 to about 50 hydroxyl, thiol or amino groups, and a linker Q connecting R to POLY, where Q comprises 1 to 10 atoms and at least one heteroatom selected from O, S or N.
The compound also includes a releasable linkage-containing spacer moiety Xr. Each Xr includes a releasable thioether, carbamate, ester, carbonate, urea, or enzyme-cleavable peptidic linkage, and the compound contains a poly(alkylene oxide) component POLY having a number of monomers from about 100 to about 2270.
The structured compound is defined to include q as a positive integer from 3 to about 50, and the method contemplates administering the compound or pharmaceutically acceptable salts thereof to a subject in need thereof. The disclosed subject matter additionally supports multi-arm, water-soluble, non-peptidic polymer conjugates, including multi-arm structures and sunitinib-conjugate intermediates and PEG-linked prodrugs as examples.
Claims Coverage
The consolidated claims coverage includes one independent treatment method for renal cancer, colorectal cancer, or gastrointestinal cancer. Across the claims, six core inventive features are present: the structured compound architecture, the functional-group-bearing residue R, the heteroatom-containing linker Q, the releasable spacer Xr, the poly(alkylene oxide) POLY range, and the arm count q.
Cancer treatment by administering a structured compound
A method of treating a subject diagnosed with renal cancer, colorectal cancer, or gastrointestinal cancer by administering a pharmacologically effective amount of a compound having the structure of claim 1, or pharmaceutically acceptable salts thereof.
Functional-group-bearing polyol, polythiol, or polyamine residue R
R is a residue of a polyol, polythiol or polyamine bearing from 3 to about 50 hydroxyl, thiol or amino groups.
Heteroatom-containing linker Q connecting R to POLY
Each Q is a linker connecting R to POLY, wherein Q comprises 1 to 10 atoms, at least one of which is a heteroatom selected from O, S or N.
Releasable linkage-containing spacer Xr with specified releasable linkages
Each Xr is a releasable linkage-containing spacer moiety that includes a releasable thioether, carbamate, ester, carbonate, urea, or enzyme-cleavable peptidic linkage.
Poly(alkylene oxide) POLY with defined monomer range
Each POLY is a poly(alkylene oxide) having a number of monomers from about 100 to about 2270.
Defined parameter q for the structured compound
q is a positive integer from 3 to about 50.
The claimed inventive concept is the cancer treatment method implemented by administering a pharmacologically effective amount of a structurally defined compound combining residue R, linker Q, spacer Xr, and POLY with the stated ranges and linkage types, optionally as pharmaceutically acceptable salts.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Method of treating a subject diagnosed with renal cancer, colorectal cancer, or gastrointestinal cancer by administering the defined compound or pharmaceutically acceptable salts thereof.
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