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    • 43. 发明申请
      US20060035850A1 Plant thymidine kinases and their use 失效
    • Plant thymidine kinases and their use
    • 植物胸苷激酶及其用途
    • US20060035850A1
    • 2006-02-16
    • US10515417
    • 2003-05-21
    • Wolfgang Knecht , Birgitte Munch-Petersen , Jure Piskur
    • Wolfgang Knecht , Birgitte Munch-Petersen , Jure Piskur
    • A61K48/00 , A01N43/04
    • C12N15/8261 , A61K31/7072 , A61K38/45 , A61K45/06 , C12N9/1205 , C12N9/1211 , C12Y207/01076 , Y02A40/146
    • This invention relates to novel plant thymidine kinases and their use in gene therapy. More specifically the invention provides novel thymidine kinases derived from tomato, pine, rice or thale cress. In further aspects the invention provides novel polynucleotides encoding the plant thymidine kinases, vector constructs comprising the polynucleotide, host cells carrying the polynucleotide or vector, methods of sensitising cells to prodrugs, methods of inhibiting pathogenic agents in warm-blooded animals, methods for biocontrol of plants, methods of synthesizing monophosphates and pharmaceutical compositions comprising the plant thymidine kinases of the invention. In a preferred embodiment the invention provides a unique combination of a plant thymidine kinase and the nucleoside analog AZT to treat abnormal cell growth.
    • 本发明涉及新型植物胸苷激酶及其在基因治疗中的应用。 更具体地，本发明提供了衍生自番茄，松树，水稻或鲟鱼水芹的新型胸苷激酶。 在另外的方面，本发明提供了编码植物胸苷激酶的新型多核苷酸，包含多核苷酸的载体构建体，携带多核苷酸或载体的宿主细胞，使前体药物致敏细胞的方法，温血动物中抑制病原体的方法，生物防治方法 植物，合成单磷酸盐的方法和包含本发明的植物胸苷激酶的药物组合物。 在优选的实施方案中，本发明提供植物胸苷激酶和核苷类似物AZT的独特组合以治疗异常细胞生长。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 45. 发明申请
      US20040072823A1 Heteroaryl diazacycloalkanes, their preparation and use; 失效
    • Heteroaryl diazacycloalkanes, their preparation and use;
    • US20040072823A1
    • 2004-04-15
    • US10677240
    • 2003-10-03
    • Neurosearch A/S
    • Dan Peters , Gunnar M. Olsen , Simon Feldback Nielsen , Elsebet Ostergard Nielsen
    • A61K031/551 , A61K031/496 , A61K031/495 , C07D43/02
    • C07D213/22 , C07D213/74 , C07D215/38 , C07D243/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14
    • The present invention discloses compounds of the formula 1 any of its enantiomers or any mixture thereof, isotopes thereof or a pharmaceutically acceptable salt thereof; wherein n is 1, 2 or 3; m is 0, 1 or 2; R represents hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, or aralkyl; and R1 represents aminophenyl; nitrophenyl; hydroxyphenyl, alkoxyphenyl; a monocyclic 5 to 6 membered heterocyclic group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino, nitro, nullCOOR3, nullCONR2R3, nullNHnullCO2R2, NHCOnullR2, nullOCOnullNR2R3; wherein R2 and R3 independently represents hydrogen or alkyl; aryl optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; nullX-alkyl-Y-alkyl wherein X and Y independently represents O, S, NH, N-alkyl or Se; and alkyl is optionally substituted with alkoxy or thioalkoxy; nullX-(alkyl)o-aryl wherein o is 0 or 1 and X represents O, S, NH, N-alkyl or Se; optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; nullX-(alkyl)o-Z wherein o is 0 or 1 and X represents O, S, NH, N-alkyl or Se and Z represents a 5- or 6-membered monocyclic heterocyclic group; optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; a monocyclic 5 to 6 membered heterocyclic group optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; or or R1 represents a bicyclic heterocyclic group, composed of a 5 to 6 membered monocyclic heterocyclic group fused to a benzene ring, and which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, alkoxy-alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino, nitro, aryl optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; and a monocyclic 5 to 6 membered heterocyclic group optionally substituted one or more times with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halogen, CF3, OCF3, CN, amino and nitro; The compounds of the invention are useful as nicotinic ACh receptor ligands.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 47. 发明授权
      US6124285A Indole-2,3-dione-3-oxime derivatives 失效
    • Indole-2,3-dione-3-oxime derivatives
    • 吲哚-2,3-二酮-3-肟衍生物
    • US6124285A
    • 2000-09-26
    • US77554
    • 1998-06-01
    • Frank Watjen , Jorgen Drejer
    • Frank Watjen , Jorgen Drejer
    • A61K20060101 , A61K31/00 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61K31/55 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/40 , C07D471/04 , C07D487/04 , A61K31/4375 , A61K31/5375 , C07D417/12
    • C07D471/04 , C07D487/04
    • The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R.sup.3 represents "Het", or a group of formula (II), wherein "Het" represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R.sup.31, R.sup.32, and R.sup.33 independendy represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R.sup.31, R.sup.32, and R.sup.33 independently represents (CH.sub.2).sub.n R.sup.34 ; wherein R.sup.34 represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkyl-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR.sup.35 R.sup.36, or "Het"; wherein n is 0, 1, 2, or 3; and R.sup.5 represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. "A" represents a ring of five to seven atoms fused with the benzo ring at the positions marked "a" and "b", and formed by the following bivalent radicals: a-NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --H.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a--CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; or a-CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; wherein R.sup.6 represents hydrogen, alkyl or CH.sub.2 CH.sub.2 OH; or a pharmaceutically acceptable salt thereof.
    • PCT No.PCT / DK97 / 00418 Sec。 371日期1998年6月1日 102（e）日期1998年6月1日PCT 1997年10月1日PCT PCT。 公开号WO98 / 14447 日期：1998年4月9日本发明涉及能够拮抗兴奋性氨基酸如谷氨酸的作用的新的吲哚-2,3-二酮-3-肟衍生物。 更具体地，本发明的新的吲哚-2,3-二酮-3-肟衍生物可以由通式（I）描述，其中R 3表示“Het”，或式（II）的基团，其中“Het”表示 饱和或不饱和的4至7元单环杂环，R 31，R 32和R 33独立的至少一个表示氢，烷基或羟基烷基，并且R 31，R 32和R 33中的至少一个独立地表示（CH 2） nR34; 其中R34表示羟基，羧基，烷氧基羰基，烯氧基羰基，炔氧基羰基，环烷氧基羰基，环烷基 - 烷氧基羰基，芳氧基羰基，芳烷氧羰基，CONR35R36或“Het”。 其中n为0,1,2或3; 并且R 5表示苯基，萘基，噻吩基或吡啶基，它们都可以被取代。 “A”表示在标记为“a”和“b”的位置与苯并环稠合的5至7个原子的环，由以下二价基团形成：a-NR6-CH2-CH2-b; a-CH2-NR6-CH2-b; a-CH2-CH2-NR6-b; a-NR6-CH2-CH2-H2-b; a-CH2-NR6-CH2-CH2-b; a-CH2-CH2-NR6-CH2-b; a-CH2-CH2-CH2-NR6-b; a-NR6-CH2-CH2-CH2-CH2-b; a-CH 2 -NR 6 -CH 2 -CH 2 -CH 2 -B; a-CH2-CH2-NR6-CH2-CH2-b; a-CH2-CH2-CH2-NR6-CH2-b; 或a-CH2-CH2-CH2-CH2-NR6-b; 其中R6表示氢，烷基或CH2CH2OH; 或其药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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