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Pharmaceutical composition containing phospholipid, sterol and negative charge carrier, useful in human or veterinary medicine for treating e.g. arthropod, protozoal and bacterial infections or tumors

机译:包含磷脂,固醇和负电荷载体的药物组合物,可用于人类或兽医学,例如治疗节肢动物,原生动物和细菌感染或肿瘤

摘要

Pharmaceutical composition (A) comprises (a) a phospholipid (A1); (b) cholesterol, 7-beta -hydroxycholesterol and/or a beta -sitosterol (A2); and (c) a negative charge carrier (A3). Pharmaceutical composition (A) comprises: (a) a phospholipid (A1) of formulae R 1O-PO 2 --O(CH 2) nN +R 2R 3R 4 (I), cyclic phosphate of formula (II), R 1OCH 2CH 2OP (III), R 1OCH 2CH(OP)(CH 2) xMe (IV), R 21OCH 2CH(OR 22)CH 2OP (V), R 31OCH 2C[((CH 2) zH)(CH 2) yH]CH 2OP (VI) or R 41OCH 2C(OH)(Me)CH 2OP (VII); (b) cholesterol, 7beta -hydroxycholesterol and/or a beta -sitosterol (A2); and (c) a negative charge carrier (A3), i.e. a 16-36C carboxylic acid, preferably saturated or (poly)unsaturated, especially with cis-double bonds; a bile acid; an amide of an amino acid with a fatty acid (saturated or (poly)unsaturated) or compound of formula R 51CONHCH 2CH 2OPO 2 --OCH 2CH(OH)CH 2OH Na + (VIII). R 1optionally saturated 15-26C hydrocarbyl; R 2-R 4H, 1-6C alkyl, 3-6C cycloalkyl or 2-5C alkylene, or two of them together form 2-5C alkylene; n : 2-6; R 11, R 21, R 31, R 4115-26C hydrocarbyl, saturated or (poly)unsaturated; R 12, R 13H, 1-6C alkyl or 2-6C hydroxyalkyl; m : 1 or 2; P : -PO 2 --O(CH 2) nN +R 2R 3R 4 or the residue of (II) after removing R 11O; x : 0-4; R 221-6C alkyl; y, z : 0-3, but not both 0; R 5115-25C hydrocarbyl; proviso: in (V) residues R 21, R 22 and P can be distributed as wished over the positions in the glycerol molecule Independent claims are also included for: (1) use of erufosin (not identified) to prepare a composition for treating tumors; (2) (VII) as new compounds; and (3) method for preparing alkylphosphocholine compounds using plant oil, particularly olive oil, as starting material. [Image] ACTIVITY : Acaricide; Cytostatic; Protozoacide; Antibacterial; Ophthalmological; Fungicide. No details of tests for any of these activities are given. MECHANISM OF ACTION : Stimulation of leucopoiesis.
机译:药物组合物(A)包含(a)磷脂(A1); (b)胆固醇,7-β-羟基胆固醇和/或β-谷甾醇(A2); (c)负电荷载体(A3)。药物组合物(A)包括:(a)式R 1> O-PO 2->-O(CH 2)nN +> R 2> R 3> R 4>(I)的磷脂(A),环状磷酸盐式(II)的基团,R 1> OCH 2CH 2OP(III),R 1> OCH 2CH(OP)(CH 2)xMe(IV),R 21> OCH 2CH(OR 22>)CH 2OP(V),R 31> OCH 2C [(((CH 2)zH)(CH 2)yH] CH 2OP(VI)或R 41> OCH 2C(OH)(Me)CH 2OP(VII); (b)胆固醇,7β-羟基胆固醇和/或β-谷甾醇(A2); (c)带负电荷的载体(A3),即16-36℃的羧酸,最好是饱和的或(多)不饱和的,尤其是带有顺式双键的;胆汁酸;氨基酸与脂肪酸(饱和或(多)不饱和)的酰胺或式R 51> CONHCH 2CH 2OPO 2->-OCH 2CH(OH)CH 2OH Na +(VIII)的化合物。 R 1>任选地饱和的15-26C烃基; R 2> -R 4> H,1-6C烷基,3-6C环烷基或2-5C亚烷基,或它们中的两个一起形成2-5C亚烷基; n:2-6; R 11>,R 21>,R 31>,R 41> 15-26C饱和或(多)不饱和烃基; R 12>,R 13> H,1-6C烷基或2-6C羟烷基; m:1或2; P:-PO 2->-O(CH 2)nN +> R 2> R 3> R 4>或除去R 11> O后的(II)残基; x:0-4; R 22> 1-6 C烷基; y,z:0-3,但不全为0; R 51> 15-25C烃基;条件:在(V)中,残基R 21>,R 22>和P可以根据需要分布在甘油分子的各个位置上,也包括以下独立权利要求:(1)芥酸(未鉴定)用于制备用于治疗肿瘤; (2)(VII)作为新化合物; (3)以植物油,特别是橄榄油为原料制备烷基磷酸胆碱化合物的方法。 [活动]:杀螨剂;细胞抑制原虫;抗菌;眼科杀菌剂。没有提供任何针对这些活动的测试的详细信息。作用机理:刺激白细胞生成。

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