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公开(公告)号:US07700646B2
公开(公告)日:2010-04-20
申请号:US11455889
申请日:2006-06-20
IPC分类号: A61K31/353 , C07D311/60 , C07D311/62
CPC分类号: C07D311/62 , C07D311/60
摘要: There is provided a novel compound of the general formula I in which each of R8 to R10 is hydrogen, aryl, C1-6 alkyl, trialkylsilyl or acyl; R1 to R5 are individually selected from hydrogen, hydroxy, C1-6 alkoxy and acyloxy; R6 and R7 are H, C1-4 alkyl, trialkylsilyl or acyl; X is O or NR, and R is H or Me; in which any of the alkyl groups including alkyl groups in alkoxy, acyl and acyloxy groups may be substituted by aryl, C1-4 alkyl, C1-4 alkoxy, hydroxyl, trialkylsiloxy or acyloxy groups; with the proviso that R2 and R3 are not both OH when R4 is H or OH, R1 and R5 are both H, and X is O. The amide compounds (X is NR) are analogues of epigallocatechin gallate or epicatechin galate, with an amide bond in place of the natural ester bond, with resistance to hydrolysis by esterase enzymes. The ester compounds (X is O) have a different hydroxylation pattern on the B ring as compared to the natural products. The compounds may be used to modulate the resistance to β-lactam antibiotics of various infections, especially methicillin resistant Staphylococcus aureus (MRSA). Pharmaceutical compositions containing the novel compounds and combinations of the novel compounds and β-lactam antibiotics are described.
摘要翻译: 提供了通式I的新化合物,其中R 8至R 10各自为氢,芳基,C 1-6烷基,三烷基甲硅烷基或酰基; R 1至R 5分别选自氢,羟基,C 1-6烷氧基和酰氧基; R6和R7是H,C1-4烷基,三烷基甲硅烷基或酰基; X是O或NR,R是H或Me; 其中包括烷氧基,酰基和酰氧基中的烷基的任何烷基可以被芳基,C 1-4烷基,C 1-4烷氧基,羟基,三烷基甲硅烷氧基或酰氧基取代; 条件是当R 4为H或OH时,R 2和R 3不同时为OH,R 1和R 5都为H,且X为O.酰胺化合物(X为NR)为表没食子儿茶素没食子酸没食子酸酯或表儿茶素加成酸盐的类似物,具有酰胺 键代替天然酯键,具有抗酯酶的水解作用。 与天然产物相比,酯化合物(X为O)在B环上具有不同的羟基化模式。 这些化合物可用于调节对各种感染,特别是耐甲氧西林金黄色葡萄球菌(MRSA)的β-内酰胺抗生素的抗性。 描述了含有新化合物和新化合物和β-内酰胺抗生素的组合的药物组合物。
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公开(公告)号:US20090082429A1
公开(公告)日:2009-03-26
申请号:US12250202
申请日:2008-10-13
申请人: Paul Stapleton , Shinich Uesato , Peter W. Taylor , Yukihiko Hara
发明人: Paul Stapleton , Shinich Uesato , Peter W. Taylor , Yukihiko Hara
IPC分类号: A61K31/353 , A61P31/04
CPC分类号: A61K31/353 , G06Q50/22
摘要: A catechin is modified in at least one position (most preferably in the 3-position of the C-ring) to increase its lipophilicity. Contemplated catechins are demonstrated to have significantly improved antibacterial properties, likely due to catastrophic membrane damage.
摘要翻译: 儿茶素在至少一个位置(最优选在C环的3-位)被修饰以增加其亲油性。 被证明的儿茶素具有显着改善的抗菌性能,可能是由于灾难性的膜损伤。
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公开(公告)号:US5342030A
公开(公告)日:1994-08-30
申请号:US82964
申请日:1993-06-29
申请人: Peter W. Taylor
发明人: Peter W. Taylor
CPC分类号: B27F7/155 , B23Q16/001 , B23Q5/00 , Y10S269/91 , Y10T29/5397
摘要: An assembly table for roof trusses has open parallel channels located on the table which contain jig stops. The jig stops are moveable along their respective channels by means of a connector head which can be raised and lowered from a gantry carriage located on a gantry which spans the table and runs along tracks located on each side of the table. The respective movements and operation of the gantry, gantry carriage and connector head are controlled by a computer.
摘要翻译: 屋顶桁架的装配台具有位于桌子上的开放的平行通道,其中包含夹具。 夹具止动件可以通过连接头来沿着它们各自的通道移动,该连接器头可以从位于台架上的台架上升起并降下,该台架跨越工作台并沿着位于工作台两侧的轨道运行。 龙门架,龙门架和连接头的相应运动和操作由计算机控制。
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公开(公告)号:US5616602A
公开(公告)日:1997-04-01
申请号:US269416
申请日:1994-06-30
IPC分类号: A61K9/06 , A61K9/127 , A61K31/555 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/32 , A61K47/34 , A61K47/38 , A61P17/00 , A61K31/40
CPC分类号: A61K47/20 , A61K31/555 , A61K47/18 , A61K47/22 , A61K9/0014 , A61K9/127 , Y10S514/863
摘要: A topically administrable pharmaceutical composition comprising (A) zinc phthalocyanine complex, (B) as carrier for the complex, (i) a N-alkylpyrrolidone together with a pharmaceutically acceptable co-solvent for the complex, (ii) dimethyl sulphoxide or a mixture thereof with a pharmaceutically acceptable co-solvent for the complex, (iii) a liposome, or (iv) a N,N-dialkylbenzamide or a mixture thereof with a pharmaceutically acceptable co-solvent for the complex, and (C) a gelling agent.
摘要翻译: 一种局部给药的药物组合物,其包含(A)酞菁酞菁络合物,(B)作为络合物的载体,(i)N-烷基吡咯烷酮以及用于络合物的药学上可接受的共溶剂,(ii)二甲基亚砜或其混合物 (iii)脂质体,或(iv)N,N-二烷基苯甲酰胺或其与药学上可接受的助溶剂的混合物,和(C)胶凝剂。
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公开(公告)号:US5100894A
公开(公告)日:1992-03-31
申请号:US684708
申请日:1991-04-12
IPC分类号: A61K31/395 , A61P3/06 , A61P9/10 , C07D498/08 , C07D498/18
CPC分类号: C07D498/08 , C07D498/18
摘要: Compounds of the general formula: ##STR1## in which R is a lower alkyl group, and R.sub.1 is a tri-lower alkylmethylcarbonyl group, the structure elements --A.sub.1 --A.sub.2 --, A.sub.3 --A.sub.4 -- or A.sub.5 --A.sub.6 -- each represent ethylene or vinylene, or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each represent ethylene and --A.sub.5 --A.sub.6 -- represents vinylene, their optical isomers and their salts exhibit valuable pharmaceutical properties.
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公开(公告)号:US4695541A
公开(公告)日:1987-09-22
申请号:US696827
申请日:1985-01-31
申请人: Peter W. Taylor
发明人: Peter W. Taylor
CPC分类号: C12Q1/34 , C12N7/00 , C12N9/14 , C12Q1/04 , A61K38/00 , C12N2795/00021 , G01N2333/22 , G01N2333/245 , G01N2333/924 , G01N2400/10 , Y10S435/81
摘要: A substantially pure enzyme which hydrolyzes a polymer containing an .alpha. 2,8-linked N-acetyl neuraminic acid is obtained from K1-specific bateriophages and used for assays of bacterial polysaccharides in samples such as cerebrospinal fluid for testing for various disorders such as bacterial meningitis, septicemia, bacteremia, and the like. The enzyme may also be used therapeutically in treating such disorders by attacking cells which have an increased level of a polymer containing an .alpha. 2,8-linked N-acetyl neuraminic acid.
摘要翻译: 水解含有α2,8连接的N-乙酰神经氨酸的聚合物的基本上纯的酶从K1特异性噬菌体获得,并用于样品如脑脊液中的细菌多糖的测定,用于测试各种疾病如细菌性脑膜炎 ,败血症,菌血症等。 该酶也可以治疗性地用于通过攻击具有含有α2,8连接的N-乙酰神经氨酸的聚合物含量增加的细胞来治疗这些疾病。
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