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1. 发明申请

WO2006014549A3 SYNTHESIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
公开(公告)号：WO2006014549A3
公开(公告)日：2006-02-09
申请号：PCT/US2005/024109
申请日：2005-07-07
申请人： NOBEX CORPORATION , SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
发明人： SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
IPC分类号： C07D207/09 , C07D207/10 , A61K31/4025
摘要： Methods are disclosed for preparing compounds of Formula I: where R 1 , R 3 , and R 4 are independently hydrogen or C 1 to C 4 alkyl, and R 2 is: where R 5 is selected from the group consisting of hydrogen and C 1 to C 4 alkyl, or where R 6 , R 7 and R 8 are independently hydrogen or C 1 to C 4 alkyl; or the esters or pharmacologically acceptable salts thereof.. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

2. 发明申请

WO2006014549A2 SYNTHEIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
标题翻译： AZO结合免疫化合物的合成
公开(公告)号：WO2006014549A2
公开(公告)日：2006-02-09
申请号：PCT/US2005024109
申请日：2005-07-07
申请人： NOBEX CORP , SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
发明人： SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
IPC分类号： C07C245/06
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R
摘要翻译：公开了制备式I化合物的方法：其中R

3. 发明申请

WO2006014549A8 SYNTHESIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
标题翻译： AZO结合免疫化合物的合成
公开(公告)号：WO2006014549A8
公开(公告)日：2007-02-22
申请号：PCT/US2005024109
申请日：2005-07-07
申请人： NOBEX CORP , SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
发明人： SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
IPC分类号： C07D207/09 , A61K31/4025 , C07D207/10
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R 1 , R 3 , and R 4 are independently hydrogen or C 1 to C 4 alkyl, and R 2 is: where R 5 is selected from the group consisting of hydrogen and C 1 to C 4 alkyl, or where R 6 , R 7 and R 8 are independently hydrogen or C 1 to C 4 alkyl; or the esters or pharmacologically acceptable salts thereof.. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.
摘要翻译：公开了制备式I化合物的方法：其中R 1，...，R 3，...和R 4是独立地是氢或C 1至C 4烷基，R 2是：其中R 5选自由C 1〜C 4烷基构成的氢和C 1〜4的基团，或者R 6，R 6， >和R 8独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。

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