COMPOUNDS BASED ON PLATINUM AND LIPIDS AND NANOPARTICLES Russian patent published in 2020 - IPC C07F15/00 C07H23/00 C07J41/00 A61K31/282 A61K31/56 A61P35/00 

FIELD: nanotechnology; cancer therapy.

SUBSTANCE: present disclosure relates to a compound of formula (VIII): Q-linker-lipid (VIII), where Q is: (i) , where X is NH or N (CH₂COO-); and Z is a platinum-containing compound, wherein platinum forms part of a cycle; (ii) , where X is S⁺, C, S⁺=O, N⁺H or P=O; X₁ represents -CH-, -CH₂- or -CH₂O-; X₂ is C=O; and Z is a platinum-containing compound, wherein platinum forms part of a cycle; (iii) , where X₁ is (CH₂)_n ; X₂ is C = O; Z is platinum-containing compound, where platinum forms part of cycle; and n is equal to 0, 1 or 2; (iv) , where R₁, R₂ and R₃ independently represent halogen, amino, alkylamino, dialkylamino, hydroxyl, thiol, thioalkyl, O-acyl, -linker-lipid or a combination thereof; or (v) , where R₁, R₂, R₃, R₄ and R₅ independently represent halogen, amino, alkylamino, dialkylamino, hydroxyl, thiol, thioalkyl, O-acyl, -linker-lipid or a combination thereof; linker is: (i) -X-CH₂-X₂-X₁-, where: X is NH; X₁ is C(O)O, C(O)NH, O(CH₂)-O, NH, or O; X₂ represents a (CH₂)_n or C(O); and n is equal to 0, 1, 2, 3, 4 or 5; (ii) -(CH₂)_nO-, -(CH₂)_nNHC(O)O-, -(CH₂)_nOC(O)NH-, -(CH₂)_nC(O)NH(CH₂)_mO-, -(CH₂)_nO(CH₂)_mO-, -(CH₂)_nC(O)-, -(CH₂)_n NHC(O)(CH₂)_mO- or -(CH₂)_nC(O)O-; where n and m are independently 0, 1, 2, 3, 4 or 5; (iii) -X₃-X₄X₅-X₆-, where: X₃ is CH₂ or O; and X₄, X₅ and X₆ independently represent -CH₂O- or O; or (iv) or combination (i)–(iii); lipid is fat, wax, sterol, steroid, bile acid, fat-soluble vitamin, monoglyceride, diglyceride, phospholipid, glycolipid, sulpholipid, aminolipid, chromolipid, glycerophospholipid, sphingolipid, prenol lipid, sugar lipid, polyketide, fatty acid or a combination thereof. Also disclosed are the preparation of said compound, a nanoparticle and a method for production thereof, a pharmaceutical composition, a method of treating or controlling cancer.

EFFECT: disclosed compounds show higher absorption of platinum in cancer cells relative to cisplatin and oxaliplatin and can be used for treating or eliminating cancer.

25 cl, 28 dwg, 1 tbl, 10 ex