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公开(公告)号:US5246931A
公开(公告)日:1993-09-21
申请号:US694538
申请日:1991-05-01
申请人: Daniel W. Norbeck , Jacob J. Plattner , Terry J. Rosen , David L. Garmaise , Richard J. Pariza , Steven M. Hannick , Thomas J. Sowin
发明人: Daniel W. Norbeck , Jacob J. Plattner , Terry J. Rosen , David L. Garmaise , Richard J. Pariza , Steven M. Hannick , Thomas J. Sowin
IPC分类号: C07C215/42 , C07C271/18 , C07C271/20 , C07C271/24 , C07C275/50 , C07D213/69 , C07D239/46 , C07D239/54 , C07D251/16 , C07D253/065 , C07D471/04 , C07D473/00 , C07D487/04 , C07F7/18 , C07F9/6561
CPC分类号: C07D213/69 , C07C215/42 , C07C271/18 , C07C271/20 , C07C271/24 , C07C275/50 , C07D239/47 , C07D239/54 , C07D251/16 , C07D253/065 , C07D471/04 , C07D473/00 , C07D487/04 , C07F7/1856 , C07F9/65616 , C07C2101/04
摘要: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is as defined above, --CH.sub.2 CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 and R.sub.23 are as defined above, --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2, --CH.sub.2 OPO.sub.3 H.sub.2, --OCH.sub.2 PO.sub.3 H.sub.2 and --CH.sub.2 CO.sub.2 R.sub.3 wherein R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 to C.sub.10 alkyl and R.sub.3 is hydrogen, C.sub.1 to C.sub.10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译: 下式的化合物:其中A是嘌呤-9-基,嘌呤-9-基的杂环等价基,嘧啶-1-基或嘧啶-1-基的杂环等价基 组; E是氢,-CH 2 OH或-OH; 并且G和D独立地选自氢,C1-C10烷基,-OH,-CH2OH,-CH2OR20,其中R20是C1-C6烷基,-CH2OC(O)R21,其中R21是C1-C10烷基,-CH2OC(O) CH(R22)(NHR23)其中R22是任何天然存在的氨基酸的侧链,R 23是氢或-C(O)CH(R 24)(NH 2),其中R 24是任何天然存在的氨基酸的侧链 发生的氨基酸,-CH 2 SH,-CH 2 Cl,-CH 2 F,-CH 2 Br,-CH 2 I,-C(O)H,-CH 2 CN,-CH 2 N 3,-CH 2 NR 1 R 2,-CO 2 R 1,-CH 2 CH 2 OH,-CH 2 CH 2 OR 20,其中R 20如上定义, -CH 2 CH 2 OC(O)R 21,其中R 21如上定义,-CH 2 CH 2 OC(O)CH(R 22)(NHR 23)其中R 22和R 23如上定义,-CH 2 CH 2 PO 3 H 2,-CH 2 OPO 3 H 2,-OCH 2 PO 3 H 2和-CH 2 CO 2 R 3,其中R 1和R 2是 独立地选自氢和C1至C10烷基,R3是氢,C1至C10烷基,羧基烷基或氨基烷基; 或其药学上可接受的盐。
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公开(公告)号:US4137317A
公开(公告)日:1979-01-30
申请号:US851003
申请日:1977-11-14
IPC分类号: C07C69/52 , A61K31/215 , C07D471/04 , C07D499/32 , C07D501/16 , A61K31/455
CPC分类号: C07D471/04
摘要: Triglycerides carrying an anti-bacterial drug moiety in the 2-position and a hydrocarbon acyl moiety in the 1- and 3-positions exhibit excellent anti-bacterial properties without causing the side effects often associated with oral antibiotics when used by themselves.
摘要翻译: 在2-位上携带抗细菌药物部分的甘油三酸酯和1-和3-位上的烃酰基部分表现出优异的抗细菌性质,而不会引起常常与口服抗生素相关的副作用。
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