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1. 发明申请

WO2013104897A1 THERAPEUTIC BORON-CONTAINING COMPOUNDS 审中-公开
标题翻译：含治疗含硼的化合物
公开(公告)号：WO2013104897A1
公开(公告)日：2013-07-18
申请号：PCT/GB2013/050020
申请日：2013-01-08
申请人： UNIVERSITY OF TROMSØ , GARDNER, Rebecca
发明人： LEJON, Tore , SVENDSEN, John Sigurd , GOROVOY, Alexey , GOZHINA, Olga
IPC分类号： C07F5/02 , A61K31/69 , A61P31/06 , A61P31/10
CPC分类号： C07F5/04 , C07F5/02 , C07F5/025
摘要： The present invention relates to compounds of Formula (I) wherein R 1 and R 3 are hydrogen; R 2 and R 4 , which may be the same or different, are hydrogen, a C 1-6 alkyl group optionally substituted by an aryl group which may itself be substituted, the substituent group including an alkyl group or an -OR group in which R is a C 1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom; or an aryl group which may be substituted, the substituent group including an alkyl group or an -OR group in which R is a C 1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom; with the proviso that R 2 and R 4 are not both hydrogen; the atom of R 4 which is attached to C β is either a saturated carbon atom or an atom which is part of a 1 substituted aromatic ring; (AA) 0-5 is an amino acid, amino acid derivative, peptide of up to 5 amino acids or a peptidomimetic thereof which optionally incorporates an N-terminal capping group, when the group is (AA) 0 an N-terminal capping group is present, covalently attached to the nitrogen atom shown in Formula (I) and the capping group comprises at least 5 non-hydrogen atoms; R 5 is hydrogen or a C 1-3 20 alkyl group, when AA=0, R 5 may form a cyclic group with the N-terminal capping group; R 6 and R 7 independently of one another denote hydrogen or a C 1-6 alkyl group; or together with the boron atom and the oxygen atoms, form a mono-, bi- or tricyclic, saturated or partly unsaturated, mono-, di-, tri- or tetra- C 1-6 alkylated or phenylated ring system having 5-18 ring members; and salt forms and stereoisomers thereof. The invention further relates to pharmaceutical formulations containing these compounds and the use of these compounds in therapy, particularly as antimicrobial agents, more particularly as an agent effective in treating a Mycobacterium tuberculosis infection or a Candida albicans infection. (I)
摘要翻译：本发明涉及其中R 1和R 3为氢的式（I）化合物; R 2和R 4可以相同或不同，为氢，任选被本身可被取代的芳基取代的C 1-6烷基，包括烷基或-OR基团的取代基，其中R为具有一个或多个氢原子任选被卤素原子取代的C 1-3烷基; 或可被取代的芳基，所述取代基包括烷基或-OR基团，其中R为C 1-3烷基，一个或多个氢原子任选被卤素原子取代; 条件是R2和R4不同时为氢; 与Cbeta连接的R4的原子是饱和碳原子或作为1取代芳环的一部分的原子; （AA）0-5是氨基酸，氨基酸衍生物，最多5个氨基酸的肽或其肽模拟物，其任选地包含N-末端封端基团，当基团为（AA）0时，N-末端封端基团共价连接到式（I）所示的氮原子上，封端基包含至少5个非氢原子; R5为氢或C1-320烷基，当AA = 0时，R5可与N-末端封端基形成环状基团; R 6和R 7彼此独立地表示氢或C 1-6烷基; 或与硼原子和氧原子一起形成具有5-18个环的单 - ，二 - 或三环饱和或部分不饱和的单 - ，二 - ，三 - 或四-C 1-6烷基化或苯基环系成员; 及其盐形式和立体异构体。本发明还涉及含有这些化合物的药物制剂以及这些化合物在治疗中的用途，特别是作为抗微生物剂，特别是作为有效治疗结核分枝杆菌感染或白色念珠菌感染的药剂。（一世）

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