发明名称 PHARMACEUTICAL FORMULATIONS
摘要 The invention provides a pharmaceutical composition comprising (a) a compound of the formula (1), wherein R1, R2, R3 and R4 are substituents, at least one of which contains a carborane cluster; and M is selected from two hydrogen ions and one or two metal ions, wherein any metal ions present are charge-balanced by one or more counter ions; and (b) a vehicle comprising: (i) dimethylacetamide as solvent; and (ii) a co-solvent comprising one or more of tetraglycol; propylene glycol; polyethylene glycol; and a non-ionic surfactant. The pharmaceutical compositions are useful as radiation sensitizers in radiation treatment of cancers.;
申请公布号 US2015297717(A1) 申请公布日期 2015.10.22
申请号 US201314646527 申请日期 2013.11.22
申请人 MOREX DEVELOPMENT PARTNERS LLP 发明人 Beattie Chris
分类号 A61K41/00 主分类号 A61K41/00
代理机构 代理人
主权项 1. A pharmaceutical composition comprising: (a) a compound of the formula (1): wherein: R1, R2, R3, and R4 are selected from an electron withdrawing group, —NO2, —NH2, halogen, and a substituent represented by the following formula wherein Y can be on the ortho, meta or para position on the phenyl rings, and is selected from hydrogen, hydrocarbyl, non-aromatic carbocyclic, non-aromatic heterocyclic, aryl, alkylaryl, arylalkyl; or a hydrocarbyl, non-aromatic carbocyclic, non-aromatic heterocyclic, aryl, alkylaryl, or a arylalkyl group substituted with 1 to 4 hydrophilic groups selected from hydroxy, alkoxy, —C(O)OR5, —SORE, —SO2R6, nitro, amido, ureido, carbamato, —SR', —NR8R9, or poly-alkyleneoxide; or a substituent represented by formula (3) —X—(CR10R11)r—Z   (3); provided that at least one of R1, R2, R3, and R4 is the substituent represented by formula (2) wherein Y represents formula (3); wherein:X is selected from oxygen and sulfur;R5, R6, R7, R8, R9, R10, and R11 are selected from hydrogen and C1 to C4 hydrocarbyl;Z is a carborane cluster comprising at least two carbon atoms and at least three boron atoms, or at least one carbon atom and at least five boron atoms, within a cage structure;r is 0 or an integer from 1 to 20;a represents an integer from 1 to 4; and provided also that at least one of R1, R2, R3, and R4 is an electron withdrawing group, —NO2, —NH2, or halogen; and M is selected from two hydrogen ions, a single monovalent metal ion, two monovalent metal ions, a divalent metal ion, a trivalent metal ion, a tetravalent metal ion, a pentavalent metal ion, and a hexavalent metal ion, wherein the porphyrin-metal complex derived from a single monovalent metal ion is charge-balanced by a counter cation, and the porphyrin-metal complex derived from a trivalent, tetravalent, pentavalent, or hexavalent metal ion is charge-balanced by an appropriate number of counter anions, dianions, or trianions; (b) a vehicle comprising: (i) dimethylacetamide as solvent; and(ii) a co-solvent comprising one or more pharmaceutically acceptable glycol or non-ionic surfactant components.
地址 London GB