公开(公告)号：US06835754B2

公开(公告)日：2004-12-28

申请号：US10043659

申请日：2002-01-08

申请人： L. David Waterbury ,  Paul L. Wood ,  M. Amin Khan ,  Ravindra B. Upasani

发明人： L. David Waterbury ,  Paul L. Wood ,  M. Amin Khan ,  Ravindra B. Upasani

IPC分类号： A61K3114

CPC分类号： A61K31/075 ,  A61K31/13 ,  A61K31/14 ,  A61K31/15 ,  A61K31/165 ,  A61K31/24 ,  A61K31/325

摘要： 3,4,5-trisubstituted aryl nitrone compounds having the formula: where R1-R4 are as defined in the specification are useful as therapeutics for neuropathic pain conditions in mammals.

摘要翻译： 具有下式的3,4,5-三取代芳基硝酮化合物：其中R 1 -R 4如说明书中所定义，可用作哺乳动物神经性疼痛病症的治疗剂。

公开(公告)号：US07115666B2

公开(公告)日：2006-10-03

申请号：US10684810

申请日：2003-10-14

申请人： M. Amin Khan ,  Ravindra B. Upasani ,  Paul L. Wood

发明人： M. Amin Khan ,  Ravindra B. Upasani ,  Paul L. Wood

IPC分类号： A01N33/02

CPC分类号： C07C309/46 ,  C07C291/02 ,  C07C309/73 ,  C07C311/21 ,  C07C311/51 ,  C07C2601/14 ,  C07D309/12

摘要： Disclosed are nitrone compounds and pharmaceutical compositions containing such compounds. The nitrone compounds have one to six additional carbons bridging between the nitrone functionality and the nitrone aryl ring. The disclosed compositions are useful as therapeutics for inflammation-related conditions and analgesia in mammals, such as arthritis, and for neuropathic pain and traumatic injuries such as traumatic brain injury and acute spinal cord injury.

公开(公告)号：US20120035250A1

公开(公告)日：2012-02-09

申请号：US13141035

申请日：2009-12-18

申请人： M. Amin Khan ,  Paul L. Wood ,  Dayan Goodenowe ,  Rishikesh Mankidy ,  Pearson Ahiahonu

发明人： M. Amin Khan ,  Paul L. Wood ,  Dayan Goodenowe ,  Rishikesh Mankidy ,  Pearson Ahiahonu

IPC分类号： A61K31/232 ,  C07C69/587 ,  C07C227/18 ,  C07D339/04 ,  C07C231/12 ,  C07C233/47 ,  A61P25/28 ,  A61P25/16 ,  A61P27/02 ,  C07C229/30 ,  A61K31/385

CPC分类号： C07C323/59 ,  C07C229/22 ,  C07C279/14 ,  C07D339/04 ,  C07F9/106

摘要： Described herein are routes of synthesis and therapeutic uses of 1-alkyl, 2-acyl glycerol derivatives of formula I: which when administered to mammalian biological systems result in increased cellular concentrations of specific sn-2 substituted ethanolamine plasmalogens independent of the ether lipid synthesis capacity of the system. Elevating levels of the specific sn-2 substituted species in this way can cause lowering of membrane cholesterol levels and the lowering of amyloid secretion. These compounds can be used for the treatment or prevention of diseases of aging associated with increased membrane cholesterol, increased amyloid, and decreased plasmalogen levels, such as neurodegeneration (including Alzheimer's disease, Parkinson's disease and age-related macular degeneration), cognitive impairment, dementia, cancer (e.g. prostate, lung, breast, ovarian, and kidney cancers), osteoporosis, bipolar disorder and vascular diseases (such as atherosclerosis, hypercholesterolemia).

摘要翻译： 本文描述了式I的1-烷基，2-酰基甘油衍生物的合成途径和治疗用途：当向哺乳动物生物系统施用时，其导致独特于醚脂质合成能力的特异性sn-2取代的乙醇胺plasmalogen的细胞浓度增加 的系统。 以这种方式提高特定sn-2取代物种的水平可能导致膜胆固醇水平的降低和淀粉样蛋白分泌的降低。 这些化合物可用于治疗或预防与增加的膜胆固醇，增加的淀粉样蛋白相关的老化疾病和降低的血浆素水平，例如神经变性（包括阿尔茨海默病，帕金森病和年龄相关性黄斑变性），认知障碍，痴呆 ，癌症（例如前列腺癌，肺癌，乳腺癌，卵巢癌和肾癌），骨质疏松症，双相性精神障碍和血管疾病（如动脉粥样硬化，高胆固醇血症）。

公开(公告)号：US09334235B2

公开(公告)日：2016-05-10

申请号：US13141035

申请日：2009-12-18

申请人： M. Amin Khan ,  Paul L. Wood ,  Dayan Goodenowe ,  Rishikesh Mankidy ,  Pearson Ahiahonu

发明人： M. Amin Khan ,  Paul L. Wood ,  Dayan Goodenowe ,  Rishikesh Mankidy ,  Pearson Ahiahonu

IPC分类号： C07C229/22 ,  C07C323/59 ,  C07C279/14 ,  C07D339/04 ,  C07F9/10

CPC分类号： C07C323/59 ,  C07C229/22 ,  C07C279/14 ,  C07D339/04 ,  C07F9/106

摘要： Described herein are routes of synthesis and therapeutic uses of 1-alkyl, 2-acyl glycerol derivatives of formula I: which when administered to mammalian biological systems result in increased cellular concentrations of specific sn-2 substituted ethanolamine plasmalogens independent of the ether lipid synthesis capacity of the system. Elevating levels of the specific sn-2 substituted species in this way can cause lowering of membrane cholesterol levels and the lowering of amyloid secretion. These compounds can be used for the treatment or prevention of diseases of aging associated with increased membrane cholesterol, increased amyloid, and decreased plasmalogen levels, such as neurodegeneration (including Alzheimer's disease, Parkinson's disease and age-related macular degeneration), cognitive impairment, dementia, cancer (e.g. prostate, lung, breast, ovarian, and kidney cancers), osteoporosis, bipolar disorder and vascular diseases (such as atherosclerosis, hypercholesterolemia).

摘要翻译： 本文描述了式I的1-烷基，2-酰基甘油衍生物的合成途径和治疗用途：当向哺乳动物生物系统施用时，其导致独特于醚脂质合成能力的特异性sn-2取代的乙醇胺plasmalogen的细胞浓度增加 的系统。 以这种方式提高特定sn-2取代物种的水平可能导致膜胆固醇水平的降低和淀粉样蛋白分泌的降低。 这些化合物可用于治疗或预防与增加的膜胆固醇，增加的淀粉样蛋白相关的老化疾病和降低的血浆素水平，例如神经变性（包括阿尔茨海默病，帕金森病和年龄相关性黄斑变性），认知障碍，痴呆 ，癌症（例如前列腺癌，肺癌，乳腺癌，卵巢癌和肾癌），骨质疏松症，双相性精神障碍和血管疾病（如动脉粥样硬化，高胆固醇血症）。

公开(公告)号：US20140012024A1

公开(公告)日：2014-01-09

申请号：US14006717

申请日：2012-03-16

申请人： Mohamed Amin Khan ,  Paul L. Wood

发明人： Mohamed Amin Khan ,  Paul L. Wood

IPC分类号： C07C51/09 ,  C07C303/28 ,  C07C67/317 ,  C07C69/606

CPC分类号： C07C51/09 ,  C07C29/103 ,  C07C67/30 ,  C07C67/303 ,  C07C67/317 ,  C07C69/606 ,  C07C303/28 ,  C07C309/73 ,  C07C69/608 ,  C07C69/587 ,  C07C57/03 ,  C07C33/04

摘要： A method for preparing docosahexaenoic acid (DHA). The method comprises coupling a compound represented by Formula I with a compound represented by Formula II followed by partial hydrogenation to obtain a compound represented by Formula III. The compound represented by Formula III acts as a DHA precursor and thus can be hydrolysed to obtain DHA. Novel starting materials represented by Formula I and Formula II, and synthetic routes for preparing the same are also provided.

摘要翻译： 二十二碳六烯酸（DHA）的制备方法。 该方法包括将由式I表示的化合物与由式II表示的化合物偶联，然后进行部分氢化，得到式III表示的化合物。 由式III表示的化合物用作DHA前体，因此可以水解以获得DHA。 还提供了由式I和式II表示的新型起始物质及其制备方法。

公开(公告)号：US06541486B1

公开(公告)日：2003-04-01

申请号：US09587043

申请日：2000-06-02

申请人： Catherine M. Bitler ,  Paul L. Wood ,  Duran T. Anstine ,  Anke Meyer-Franke ,  Qi Zhao ,  Mohamed A. Khan

发明人： Catherine M. Bitler ,  Paul L. Wood ,  Duran T. Anstine ,  Anke Meyer-Franke ,  Qi Zhao ,  Mohamed A. Khan

IPC分类号： A61K314184

CPC分类号： C07D233/64 ,  A61K31/437 ,  C07D235/08 ,  C07D235/10 ,  C07D235/16 ,  C07D235/20 ,  C07D401/06 ,  C07D403/06 ,  G01N2510/00

摘要： Compounds, pharmaceutical compositions, and methods of use are described which are effective in inhibiting cell death, particularly apoptotic cell death. The compositions may be used for prevention and treatment of injuries associated with cell death, including ischemia, such as results from stroke or myocardial infarction, trauma, neurodegeneration, and inflammation.

摘要翻译： 描述了有效抑制细胞死亡，特别是凋亡性细胞死亡的化合物，药物组合物和使用方法。 组合物可用于预防和治疗与细胞死亡相关的损伤，包括缺血，例如中风或心肌梗死，创伤，神经变性和炎症的结果。