公开(公告)号：US07435555B2

公开(公告)日：2008-10-14

申请号：US10490085

申请日：2002-09-18

申请人： Murray L Whitelaw ,  David Lando ,  Daniel J Peet ,  Jeffrey J Gorman ,  Sarah Linke

发明人： Murray L Whitelaw ,  David Lando ,  Daniel J Peet ,  Jeffrey J Gorman ,  Sarah Linke

IPC分类号： C12Q1/00 ,  C12Q1/16 ,  C12Q1/68

CPC分类号： G01N33/6875 ,  C07K14/4702 ,  C12Q1/26 ,  G01N2500/00

摘要： A target asparagine residue of HIF 1 alpha and 2 alpha is hydroxylated at high oxygen tension to render HIF as a weak transcription factor. An asparagine hydroxylase hydroxylation motif and binding motif is proposed. A method of screening for agonists or antagonists of an asparagine hydroxylase is also proposed and involves mixing peptides or proteins having the hydroxylation and or the binding motif with asparagine hydroxylase and a candidate agonist or antagonist. The extent of inhibition or enhancement of binding; level of asparagine hydroxylation or transactivation may be measured depending on the nature of the protein or peptide. Additionally altered proteins resistant to hydroxylation are described as are nucleic acids encoding such proteins.

摘要翻译： HIF1α和2α的目标天冬酰胺残基在高氧压下被羟基化，使HIF作为弱转录因子。 提出了天冬酰胺羟化酶羟化基序和结合基序。 还提出了筛选天冬酰胺羟化酶的激动剂或拮抗剂的方法，并且涉及将具有羟基化和/或结合基序的肽或蛋白质与天冬酰胺羟化酶和候选激动剂或拮抗剂混合。 抑制或增强结合的程度; 天冬酰胺羟化或反式激活的水平可以根据蛋白质或肽的性质来测量。 另外，抗羟化反应的改变的蛋白质被描述为编码这种蛋白质的核酸。

公开(公告)号：US4664693A

公开(公告)日：1987-05-12

申请号：US600072

申请日：1984-04-13

申请人： Graham J. Bird ,  Graeme J. Farquharson ,  Keith G. Watson ,  Murray L. Whitelaw

发明人： Graham J. Bird ,  Graeme J. Farquharson ,  Keith G. Watson ,  Murray L. Whitelaw

IPC分类号： A01N35/10 ,  A01N43/12 ,  A01N43/38 ,  A01N43/52 ,  A01N43/74 ,  A01N43/78 ,  C07C45/51 ,  C07C47/453 ,  C07C67/00 ,  C07C239/00 ,  C07C251/44 ,  C07D209/14 ,  C07D263/54 ,  C07D277/62 ,  C07D277/66 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D333/54 ,  C07D333/58 ,  A01N43/00 ,  A01N43/02

CPC分类号： C07D307/79 ,  A01N35/10 ,  A01N43/12 ,  A01N43/38 ,  A01N43/52 ,  A01N43/74 ,  C07C45/513 ,  C07C47/453 ,  C07D209/14 ,  C07D277/66 ,  C07D307/80 ,  C07D307/81 ,  C07D333/54

摘要： The invention concerns novel compounds of the formula I ##STR1## wherein: A is selected from CH and N;B is selected from oxygen, sulfur, CH.sub.2 and the group N-Z wherein Z is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, benzyl and substituted benzyl;X, which may be the same or different, and X.sup.1, which be the same or different, are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl;n is 0 or an integer chosen from 1 to 4; andn.sup.1 is 0 or an integer chosen from 1 to 4.The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.

摘要翻译： 本发明涉及式I的新型化合物其中：A选自CH和N; B选自氧，硫，CH 2和基团N-Z，其中Z选自氢，烷基，烯基，炔基，环烷基，苄基和取代的苄基; X可以相同或不同，X 1相同或不同，选自卤素，硝基，氰基，烷基，取代的烷基，羟基，烷氧基，取代的烷氧基，烯基，烯氧基，炔基，炔氧基，酰氧基 烷氧基羰基，烷硫基，烷基亚磺酰基，烷基磺酰基，氨磺酰基，取代氨磺酰基，烷酰氧基，苄氧基，取代的苄氧基，氨基，取代的氨基，以及甲酰基和烷酰基及其肟，亚胺和席夫碱衍生物。 R 1选自氢，烷基，烯基，炔基，取代的烷基，烷基磺酰基，芳基磺酰基，酰基和无机或有机阳离子; R2选自烷基，取代的烷基，烯基，卤代烯基，炔基和卤代炔基; R3选自烷基，氟烷基，烯基，炔基和苯基; R4选自氢，卤素，烷基，氰基和烷氧基羰基; n为0或选自1至4的整数; 本发明的化合物显示出除草性质和植物生长调节性质，并且在进一步的实施方案中，本发明提供制备式I化合物的方法，可用于制备式I化合物的中间体 式I化合物，含有作为活性成分的式I化合物的组合物，以及利用式I化合物的除草和植物生长调节方法。