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1. 发明申请

WO2010110771A3 SUBSTITUTED THIOL-CONTAINING ALKYL FATTY ACIDS AND PROCESS FOR SYNTHESIZING DERIVATIVES THEREOF 审中-公开
公开(公告)号：WO2010110771A3
公开(公告)日：2010-09-30
申请号：PCT/US2009/001857
申请日：2009-03-25
申请人： GIBSON, Frank , BOTEJU, Lakmal, W. , SHORR, Robert , RODRIGUEZ, Robert
发明人： GIBSON, Frank , BOTEJU, Lakmal, W. , SHORR, Robert , RODRIGUEZ, Robert
IPC分类号： C11D1/28
摘要： An improved process for the synthesis of derivatives of substituted thiol-containing alkyl fatty acids, such as but not limited to lipoic acid, generates intermediate compounds and occurs in a temperature-controlled optimal sequence of monitored events to generate increased yield and purity of final product.

2. 发明申请

WO2015195071A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2015195071A1
公开(公告)日：2015-12-23
申请号：PCT/US2014/000150
申请日：2014-06-19
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
IPC分类号： A61K31/20 , A61P35/00 , C07C381/00
CPC分类号： C07F9/5442 , C07C321/20 , C07C323/12 , C07C323/25 , C07C323/60 , C07C323/66 , C07D257/04
摘要： Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
摘要翻译：治疗有效量的烷基脂肪酸的新型类似物或衍生物（例如但不限于硫辛酸）以及包含此类类似物或衍生物和药学上可接受的载体的药物制剂可用于治疗，预防，成像和/或诊断医学疾病。

3. 发明申请

WO2011143593A1 CONJUGATES OF A LIPOIC ACID DERIVATIVE AND ANTI-PROLIFERATION AGENT AND MEDICAL USES THEREOF 审中-公开
标题翻译：萝卜酸衍生物和抗增殖剂及其医药用途的结合
公开(公告)号：WO2011143593A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036491
申请日：2011-05-13
申请人： CORNERSTONE PHARMACEUTICALS, INC. , SHORR, Robert, G.l. , RODRIGUEZ, Robert, J. , BOTEJU, Lakmal
发明人： SHORR, Robert, G.l. , RODRIGUEZ, Robert, J. , BOTEJU, Lakmal
IPC分类号： C07H19/02 , A61K31/513 , A61P35/00
CPC分类号： C07H19/06
摘要： The invention provides conjugate compounds, pharmaceutical compositions, therapeutic methods, and kits for use in treating cell proliferation disorders, such as cancer. The conjugates comprise a redox-modulating compound, such as a lipoic acid derivative, chemically bonded to an anti-proliferation agent, such as gemcitabine.
摘要翻译：本发明提供缀合物化合物，药物组合物，治疗方法和用于治疗细胞增殖病症例如癌症的试剂盒。缀合物包含化学键合到抗增殖剂如吉西他滨的氧化还原调节化合物，例如硫辛酸衍生物。

4. 发明申请

WO2010110771A2 SUBSTITUTED THIOL-CONTAINING ALKYL FATTY ACIDS AND PROCESS FOR SYNTHESIZING DERIVATIVES THEREOF 审中-公开
标题翻译：取代的含THIOL的烷基脂肪酸及其衍生物的合成方法
公开(公告)号：WO2010110771A2
公开(公告)日：2010-09-30
申请号：PCT/US2009001857
申请日：2009-03-25
申请人： GIBSON FRANK , BOTEJU LAKMAL W , SHORR ROBERT , RODRIGUEZ ROBERT
发明人： GIBSON FRANK , BOTEJU LAKMAL W , SHORR ROBERT , RODRIGUEZ ROBERT
IPC分类号： C07D339/04
CPC分类号： C07D339/04
摘要： An improved process for the synthesis of derivatives of substituted thiol-containing alkyl fatty acids, such as but not limited to lipoic acid, generates intermediate compounds and occurs in a temperature-controlled optimal sequence of monitored events to generate increased yield and purity of final product.
摘要翻译：用于合成取代的含硫醇烷基脂肪酸（例如但不限于硫辛酸）的衍生物的改进方法产生中间体化合物，并且以受温度控制的监测事件的最佳序列发生，以产生最终产物的增加的产率和纯度。

5. 发明申请

WO2015195070A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2015195070A1
公开(公告)日：2015-12-23
申请号：PCT/US2014/000149
申请日：2014-06-19
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
IPC分类号： C07C323/62 , A61K31/20
CPC分类号： C07F17/02 , C07C271/22 , C07C309/15 , C07C323/22 , C07C323/52 , C07C323/54 , C07C323/60 , C07D295/125 , C07D295/13 , C07D295/185 , C07F1/005 , C07F3/003
摘要： Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
摘要翻译：治疗有效量的烷基脂肪酸的新型类似物或衍生物，例如但不限于硫辛酸，以及包含此类类似物或衍生物的药物制剂及其药学上可接受的载体，可用于治疗，预防，成像和/ 或医疗障碍的诊断。

6. 发明申请

WO2014098926A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2014098926A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/000276
申请日：2013-12-19
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal , KWOK, Thomas , MARECEK, James
IPC分类号： A61K31/555 , A61K33/24
CPC分类号： C07F5/003 , C07F1/005 , C07F15/0093
摘要： Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty, acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
摘要翻译：治疗有效量的烷基脂肪酸，酸，例如但不限于硫辛酸的新类似物或衍生物，以及包含此类类似物或衍生物的药物制剂及其药学上可接受的载体可用于治疗，预防，成像和 /或医学病症的诊断。

7. 发明申请

WO2009110859A1 MODULATION OF ENZYMATIC STRUCTURE, ACTIVITY, AND/OR EXPRESSION LEVEL 审中-公开
标题翻译：酶结构，活性和/或表达水平的调节
公开(公告)号：WO2009110859A1
公开(公告)日：2009-09-11
申请号：PCT/US2008/002853
申请日：2008-03-04
申请人： SHORR, Robert , RODRIGUEZ, Robert , BHASIN, Rajinder , BINGHAM, Paul , BOTEJU, Lakmal, W. , ZACHAR, Zuzana
发明人： SHORR, Robert , RODRIGUEZ, Robert , BHASIN, Rajinder , BINGHAM, Paul , BOTEJU, Lakmal, W. , ZACHAR, Zuzana
IPC分类号： C07C271/02
CPC分类号： C07C323/52 , A61K31/19 , A61K31/381 , A61K31/385 , C07C327/32 , C07D339/00
摘要： A pharmaceutically-acceptable modulator of the structure, activity, or expression level of an enzyme complex, such as the pyruvate dehydrogenase (PD) complex, in the mitochondria of warm-blooded animals, including humans, and methods of use thereof, comprises an effective amount of at least one lipoic acid derivative and at least one pharmaceutically-acceptable carrier thereof. By preventing the detoxification of toxic metabolites of anaerobic glycolysis through inhibition of the activity of the PD complex Elα subunit, the modulator increases PD kinase activity and concomitantly decreases PD phosphatase activity, obliging increased oxidative phosphorylation activity in the mitochondrion. As a cell characterized by hyperprolif eration, such as a tumor cell, cannot also generate acetyl-CoA and NADH because of the action of the modulator in inhibiting the action of the E2 subunit of the PD complex, the mitochondrial membrane polarization is lost, facilitating cell death.
摘要翻译：在温血动物（包括人）的线粒体中，酶复合物如丙酮酸脱氢酶（PD）复合物的结构，活性或表达水平的药学上可接受的调节剂及其使用方法包括有效的至少一种硫辛酸衍生物和至少一种药学上可接受的载体的量。通过抑制PD复合物Ela亚基的活性来防止厌氧糖酵解的有毒代谢物解毒，调节剂增加PD激酶活性，同时降低PD磷酸酶活性，有助于增加线粒体中的氧化磷酸化活性。由于调节剂在抑制PD复合物的E2亚单位的作用下，由于肿瘤细胞特征在于超扩增特征的细胞，如肿瘤细胞，也不能产生乙酰辅酶A和NADH，线粒体膜极化丧失，促进细胞死亡。

8. 发明申请

WO2007100617A2 IMIDAZOLE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE 审中-公开
标题翻译：基于咪唑的化合物，包含它们的组合物及其使用方法
公开(公告)号：WO2007100617A2
公开(公告)日：2007-09-07
申请号：PCT/US2007/004648
申请日：2007-02-21
申请人： LEXICON GENETICS INCORPORATED , AUGERI, David, J. , BAGDANOFF, Jeffrey , BOTEJU, Lakmal, W. , CARSON, Kenneth, G. , JESSOP, Theodore, C. , KIMBALL, David, S.
发明人： AUGERI, David, J. , BAGDANOFF, Jeffrey , BOTEJU, Lakmal, W. , CARSON, Kenneth, G. , JESSOP, Theodore, C. , KIMBALL, David, S.
CPC分类号： C07D233/64 , A61K31/4164 , C07D401/12
摘要： Imidazole-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed. Particular compounds are of formula (I).
摘要翻译：公开了基于咪唑的化合物，包含它们的组合物及其用于治疗，预防和治疗炎症和自身免疫性疾病和病症的方法。特定的化合物具有式（I）。

9. 发明申请

WO2010110887A1 FATTY ACIDS 审中-公开
标题翻译：脂肪酸
公开(公告)号：WO2010110887A1
公开(公告)日：2010-09-30
申请号：PCT/US2010/000879
申请日：2010-03-24
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , BOTEJU, Lakmal, W. , ZARETSKI, Patrick, P.
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , BOTEJU, Lakmal, W. , ZARETSKI, Patrick, P.
IPC分类号： A01N37/12 , A01N37/44 , A61K31/195
CPC分类号： A61K31/195
摘要： Organic metabolites are produced in vivo from derivatives of thiol-containing alkyl fatty acids, such as but not limited to lipoic acid. These metabolites are intended to perturb at least one enzyme or enzyme complex, receptor, ion channel, transport protein, or at least one subunit of each thereof, such as lipoate-containing or -utilizing dehydrogenase complexes and/or other enzymes. These metabolites are also intended to influence reactions which generate and/or regulate reactive oxygen and nitrogen species and/or other associated signal transduction pathways and cascades. The target enzymes, receptors, channels, proteins, reactions, pathways, and cascades are found in the organelles of diseased cells of warm-blooded animals, including but not limited to cancer cells. Also produced are structures which are resistant to or prevented from being metabolized into these metabolites, as well as a pharmaceutically-acceptable carrier formed from such metabolites, and methods of use thereof.
摘要翻译：有机代谢物在体内由含硫醇的烷基脂肪酸的衍生物制备，例如但不限于硫辛酸。这些代谢物旨在扰乱至少一种酶或酶复合物，受体，离子通道，转运蛋白或其各自的至少一个亚基，例如含有脂肪酸的或 - 使用脱氢酶复合物和/或其它酶。这些代谢物还意在影响产生和/或调节活性氧和氮物质和/或其他相关信号转导途径和级联的反应。目标酶，受体，通道，蛋白质，反应，途径和级联存在于温血动物的病变细胞的细胞器中，包括但不限于癌细胞。还产生了耐受或防止被代谢成这些代谢物的结构，以及由这些代谢物形成的药学上可接受的载体及其使用方法。

10. 发明申请

WO2010062381A1 ORGANELLE-SPECIFIC DRUG DELIVERY 审中-公开
标题翻译： ORGANELLE特异性药物递送
公开(公告)号：WO2010062381A1
公开(公告)日：2010-06-03
申请号：PCT/US2009/006218
申请日：2009-11-20
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , BOTEJU, Lakmal, W. , ZARETSKI, Patrick, P.
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , BOTEJU, Lakmal, W. , ZARETSKI, Patrick, P.
IPC分类号： A01N37/00 , A61K31/20
CPC分类号： A61K47/542 , A61K47/60
摘要： A pharmaceutical composition constructed from a compound comprising a fatty acid, or analogue thereof, conjugated to at least one polymer, non-polymer, or lipid-based particle and/or at least one therapeutic, imaging, or diagnostic agent, modulates the binding affinity of the compound to a carrier molecule in the blood of warm-blooded animals in such a way as to modulate the circulation time of the pharmaceutical composition, and consequently the penetration and distribution of the compound into a tumor mass, as well as to demonstrate selective uptake and transport into a specific organelle in a diseased cell. More specifically, increased depth of tumor cell layer penetration and more even distribution throughout a tumor mass, with a resulting active cellular uptake and transport into diseased-cell mitochondria, leading to enhanced diagnostic, imaging, or therapeutic benefit, is contemplated.
摘要翻译：由包含与至少一种聚合物，非聚合物或脂质基颗粒和/或至少一种治疗性成像或诊断剂缀合的脂肪酸或其类似物的化合物构成的药物组合物调节结合亲和力的化合物以温血动物的血液中的载体分子的方式调节药物组合物的循环时间，并因此调节化合物进入肿瘤块的渗透和分布，以及证明选择性摄入并转运到患病细胞中的特定细胞器中。更具体地，预期增加肿瘤细胞层穿透的深度并且更均匀地分布在整个肿瘤块中，导致活性细胞摄取并转运到患病细胞线粒体中，导致增强的诊断，成像或治疗益处。

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