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Procedures for the treatment of malaria, tuberculosis and MAC diseases

机译:疟疾,结核病和MAC疾病的治疗程序

摘要

A compound for use in the treatment of a disease selected from malaria, a Mycobacterium avium complex, a Mycobacterium tuberculosis or a Nocardia infection in a patient, where the compound has the formula ** Formula ** or a pharmaceutically acceptable salt of the same, where: R10 is hydrogen; X is H; and Y is OR7; where R7 is a monosaccharide or disaccharide, alkyl, aryl, heteroaryl, acyl, or -C (O) -NR8R9, where R8 and R9 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, aralkyl, alkylaryl , heteroalkyl, aryl, heteroaryl, alkoxy, dimethylaminoalkyl, acyl, sulfonyl, ureido and carbamoyl; or X and Y are taken together with the carbon to which they are fixed to form carbonyl; V is -C (O) -, -C ( = NR11) -, -CH (NR12, R13) -, or -N (R14) CH2-, where N (R14) is fixed to C-10 carbon; where R11 is hydroxy or alkoxy, R12 and R13 are each independently selected from the group consisting of hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, alkoxy, heteroalkyl, aryl, heteroaryl, dimethylaminoalkyl, acyl, sulfonyl, ureido and carbamoyl; R14 is hydrogen, hydroxy, alkyl, aralkyl, alkylaryl, alkoxy, heteroalkyl, aryl, heteroaryl, dimethylaminoalkyl, acyl, sulfonyl, ureido or carbamoyl; W is H, F, Cl, Br, I or OH; A is -CH2-, -C (O) -, -C (O) O-, -C (O) NH-, -S (O) 2-, -S (O) 2NH-, -C (O) NHS (O) 2-; B is - (CH2) n- where n is an integer between 0 and 10, or B is an unsaturated carbon chain of 2 to 10 carbons; and C is hydrogen, hydroxy, acyl, acyloxy, sulfonyl, ureido or carbamoyl, or optionally substituted C1-C12 alkyl, optionally substituted ar (C1-C12 alkyl), optionally substituted C1-C12 alkoxy, heteroalkyl, optionally substituted aryl or optionally heteroaryl replaced.
机译:在患者中用于治疗选自疟疾,鸟分枝杆菌复合物,结核分枝杆菌或诺卡氏菌感染的疾病的化合物,其中该化合物具有式**式**或该化合物的可药用盐,其中:R10是氢; X是H; Y是OR7;其中R7为单糖或二糖,烷基,芳基,杂芳基,酰基或-C(O)-NR8R9,其中R8和R9各自独立地选自氢,羟基,烷基,芳烷基,烷基芳基,杂烷基,芳基,杂芳基,烷氧基,二甲基氨基烷基,酰基,磺酰基,脲基和氨基甲酰基; X和Y与它们所固定的碳一起形成羰基;或V是-C(O)-,-C(> = NR11)-,-CH(NR12,R13)-或-N(R14)CH2-,其中N(R14)固定在C-10碳上;其中R11是羟基或烷氧基,R12和R13各自独立地选自氢,羟基,烷基,芳烷基,烷基芳基,烷氧基,杂烷基,芳基,杂芳基,二甲基氨基烷基,酰基,磺酰基,脲基和氨基甲酰基; R14为氢,羟基,烷基,芳烷基,烷基芳基,烷氧基,杂烷基,芳基,杂芳基,二甲基氨基烷基,酰基,磺酰基,脲基或氨基甲酰基; W是H,F,Cl,Br,I或OH; A是-CH2-,-C(O)-,-C(O)O-,-C(O)NH-,-S(O)2-,-S(O)2NH-,-C(O) NHS(O)2-; B为-(CH 2)n-,其中n为0至10之间的整数,或B为2至10个碳的不饱和碳链; C为氢,羟基,酰基,酰氧基,磺酰基,脲基或氨基甲酰基,或任选取代的C 1 -C 12烷基,任选取代的ar(C 1 -C 12烷基),任选取代的C 1 -C 12烷氧基,杂烷基,任选取代的芳基或任选杂芳基更换。

著录项

  • 公开/公告号ES2608285T3

    专利类型

  • 公开/公告日2017-04-07

    原文格式PDF

  • 申请/专利权人 CEMPRA PHARMACEUTICALS INC.;

    申请/专利号ES20100816209T

  • 发明设计人 FERNANDES PRABHAVATHI;

    申请日2010-09-10

  • 分类号A61P33/06;A61K31/4192;A61P31;A61P31/06;

  • 国家 ES

  • 入库时间 2022-08-21 13:35:24

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