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公开(公告)号：US06552078B2
公开(公告)日：2003-04-22
申请号：US09823000
申请日：2001-03-30
IPC分类号： A61K3124
CPC分类号： A61K31/085 , A61K31/16 , A61K31/165 , A61K31/21 , A61K31/216 , A61K31/235 , A61K31/265
摘要： The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is In another embodiment, the composition is In yet another embodiment, the composition is Additional alternative embodiments are R or R″ are therapeutic moieties.
摘要翻译： 本发明提供了可用于治疗人类炎症的组合物及其相关治疗方法。 在一个实施方案中，组合物在另一个实施方案中，组合物在另一个实施方案中，组合物是另外的替代实施方案是R或R“是治疗性部分。
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公开(公告)号：US08754197B2
公开(公告)日：2014-06-17
申请号：US13680434
申请日：2012-11-19
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. 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独立地为氢或C 1至C 4烷基，R 2为：其中R 5选自氢和C 1至C 4烷基，或其中R 6， R7和R8独立地是氢或C1-C4烷基; 或其酯或药理学上可接受的盐。 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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公开(公告)号：US08329958B2
公开(公告)日：2012-12-11
申请号：US11174938
申请日：2005-07-05
摘要： A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
摘要翻译： 建立了一种简单的扩链方法，用于单保护单分散PEG二醇材料的放大。 在碱性条件下，THP-（OCH2CH2）n-OMs（n = 4,8,12）与大量过量的市售H-（OCH2CH2）n-OH（n = 1-4）的反应导致THP-（OCH2CH2 ）n-OH（n = 5-15）。 类似地，Me-（OCH 2 CH 2）n-OM（n = 3,7,11）制备Me-（OCH 2 CH 2）n -OH（n = 4-11,13）。 对于链延伸步骤，通过萃取纯化获得40-80％的产率。 通过THP-（OCH2CH2）n-OH（n = 1-15）的烷基化或酰化，然后脱保护，产生PEG低聚物文库I和II以50-95％的总收率产生。 Me-（OCH2CH2）n-OH（n = 1-11,13）与X-（CH2）m-CO2R（X = Br或OMs）的烷基化，随后的水解导致PEG低聚物文库III的总体含量在30-60％ 产量。 组合纯化技术适应较大规模的文库合成。 共合成498种化合物，每种化合物的重量为2-5g，最低纯度为90％。
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公开(公告)号：US20110201792A1
公开(公告)日：2011-08-18
申请号：US13094135
申请日：2011-04-26
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 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独立地为氢或C 1至C 4烷基，R 2为：其中R 5选自氢和C 1至C 4烷基，或其中R 6， R7和R8独立地是氢或C1-C4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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5.发明授权Immunoregulatory compounds and derivatives and methods of treating diseases therewith 有权免疫调节化合物及其治疗疾病的衍生物和方法公开(公告)号：US06583128B2
公开(公告)日：2003-06-24
申请号：US09942464
申请日：2001-08-29
IPC分类号： A61K31655
CPC分类号： A61K31/195 , A61K31/196 , A61K31/215 , A61K31/24 , C07C229/42 , C07C245/08 , Y02A50/475 , Y02A50/481 , A61K2300/00
摘要： Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.
摘要翻译： 公开了具有式I结构的化合物：其中R 1，R 3和R 4独立地为氢或C 1至C 4烷基，R 2为：其中R 5选自氢和C 1至C 4烷基，或其中R 6，R 7 和R8独立地是氢或C1-C4烷基; 或其酯或药理学上可接受的盐。 这些化合物可用于预防或治疗各种疾病，特别是GI道的炎性病症。 还公开了使用具有下式的化合物治疗胃肠道炎症状况如炎症性肠病的方法：其中R9，R10和R11独立地选自氢和C1至C4烷基，R12选自 由氢和-C（O）R 13组成的基团，其中R 13是C 1至C 6烷基或芳基。
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公开(公告)号：US07932366B2
公开(公告)日：2011-04-26
申请号：US11631582
申请日：2005-07-07
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 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独立地为氢或C 1至C 4烷基，R 2为：其中R 5选自氢和C 1至C 4烷基，或其中R 6， R7和R8独立地是氢或C1-C4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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7.发明授权Immunoregulatory compounds and derivatives and methods of treating diseases therewith 有权免疫调节化合物及其治疗疾病的衍生物和方法公开(公告)号：US07119119B2
公开(公告)日：2006-10-10
申请号：US11144093
申请日：2005-06-03
IPC分类号： A61K31/196 , A61P1/00
CPC分类号： A61K31/195 , A61K31/196 , A61K31/215 , A61K31/24 , C07C229/42 , C07C245/08 , Y02A50/475 , Y02A50/481 , A61K2300/00
摘要： Compounds are disclosed having the structure of Formula I: where R1 , R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.
摘要翻译： 公开了具有式I结构的化合物：其中R 1，R 3和R 4独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C C 1至C 4烷基，或其中R 6，R 7和R 8是 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。 这些化合物可用于预防或治疗各种疾病，特别是GI道的炎性病症。 还公开了使用具有下式的化合物治疗胃肠道炎症性疾病如炎症性肠病的方法：其中R 9，R 10和R 11 独立地选自氢和C 1至C 4烷基，R 12选自基团 由氢和-C（O）R 13组成，其中R 13是C 1至C 6 - 烷基或芳基。
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公开(公告)号：US06730701B2
公开(公告)日：2004-05-04
申请号：US10282870
申请日：2002-10-29
IPC分类号： A61K31235
CPC分类号： A61K31/085 , A61K31/16 , A61K31/165 , A61K31/21 , A61K31/216 , A61K31/235 , A61K31/265
摘要： The present invention provides compositions useful for the treatment of inflammation in humans, and related methods of treatment for the same. In one embodiment the composition is: In another embodiment, the composition is: In yet another embodiment, the composition is: Additional alternative embodiments are R or R″ are therapeutic moieties.
摘要翻译： 本发明提供了可用于治疗人类炎症的组合物及其相关治疗方法。 在一个实施方案中，组合物是：在另一个实施方案中，组合物是：在另一个实施方案中，组合物是：另外的替代实施方案是R或R“是治疗性部分。
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9.发明授权5-ASA derivatives having anti-inflammatory and antibiotic activity and methods of treating diseases therewith 有权具有抗炎和抗生素活性的5-ASA衍生物及其治疗疾病的方法公开(公告)号：US06458776B1
公开(公告)日：2002-10-01
申请号：US09942510
申请日：2001-08-29
IPC分类号： A61K31655
CPC分类号： C07C311/51
摘要： Compounds are disclosed represented by the following formula: where R1 is a substituted or unsubstituted phenyl group, and where Z is selected such that a compound, Z-R1-NH2, formed by cleavage of the azo bond is a non-absorbable antibiotic; or an ester or pharmacologically acceptable salt of the compound of Formula I. Compounds of the present invention may be utilized for the prophylaxis or treatment of various diseases including, but not limited to, intestinal diseases such as inflammatory bowel disease and/or traveler's diarrhea, liver diseases such as hepatic encephalopathy, and/or diseases treatable by a non-absorbable antibiotic.
摘要翻译： 公开了由下式表示的化合物：其中R1是取代或未取代的苯基，并且其中Z选择为使得通过裂解偶氮键形成的化合物Z-R 1 -NH 2是不可吸收的抗生素; 或式I化合物的酯或药理学上可接受的盐。本发明的化合物可用于预防或治疗各种疾病，包括但不限于肠道疾病如炎性肠病和/或旅行者腹泻， 肝病如肝性脑病，和/或可由不可吸收的抗生素治疗的疾病。
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公开(公告)号：US20130096286A1
公开(公告)日：2013-04-18
申请号：US13680434
申请日：2012-11-19
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. 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： 的方法公开了制备式I的化合物：其中R1，R3，和R4独立地是氢或C1-C4烷基，且R 2是：其中R 5选自氢和C1至C4烷基，或其中R 6的组中选择， R7和R8独立地是氢或C1-C4烷基; 或其酯或药理学上可接受的盐。 的化合物和或它们的代谢物可用于治疗或预防各种疾病，胃肠道的特别炎性病症。
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