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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO2009123597A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2009123597A1
公开(公告)日：2009-10-08
申请号：PCT/US2008/004410
申请日：2008-04-04
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal, W. , ZACHAR, Zuzana
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , BOTEJU, Lakmal, W. , ZACHAR, Zuzana
IPC分类号： A61K31/385 , A61K31/19
CPC分类号： A61K31/19 , A61K31/385
摘要： A pharmaceutically-acceptable modulator of the regulation or perturbation of the structure, expression, and/or activity of at least one enzyme and/or enzyme complex, or subunit thereof, such as via the altered mitochondrial energy metabolism of the pyruvate dehydrogenase (PDH) complex 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 to affect the complex's phosphorylation state. By increasing PDH kinase activity and/or decreasing PDH phosphatase activity, the modulator prevents the detoxification anaerobic glycolytic toxic metabolites through inhibition of the activity of the PDH complex's El α subunit, obliging increased mitochondrial oxidative phosphorylation activity. As cells characterized by hyperproliferation, such as tumor cells, cannot also generate acetyl-CoA and NADH because of the modulator's additional action in inhibiting the action of the PDH complex's E2 subunit, the mitochondrial membrane polarization is lost, facilitating cell death.
摘要翻译：调节或扰动至少一种酶和/或酶复合物或其亚单位的结构，表达和/或活性的药学上可接受的调节剂，例如通过改变的丙酮酸脱氢酶（PDH）的线粒体能量代谢，包括人类的温血动物的复合物及其使用方法包括有效量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，以影响复合物的磷酸化状态。通过增加PDH激酶活性和/或降低PDH磷酸酶活性，调节剂通过抑制PDH复合物的E1a亚基的活性来阻止厌氧的糖酵解毒性代谢物的解毒，从而增加线粒体氧化磷酸化活性。由于调节剂在抑制PDH复合物的E2亚基的作用方面的附加作用，由于过度增殖的特征，如肿瘤细胞，细胞不能产生乙酰辅酶A和NADH，线粒体膜极化丧失，促进细胞死亡。

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

WO2010019225A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2010019225A1
公开(公告)日：2010-02-18
申请号：PCT/US2009/004604
申请日：2009-08-12
申请人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , ZARETSKI, Patrick, P.
发明人： SHORR, Robert , RODRIGUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana , ZARETSKI, Patrick, P.
IPC分类号： A01N37/00 , A61K31/185
CPC分类号： A61K31/185
摘要： Pharmaceutically-acceptable agents modulate the structure, function, activity, cellular location or compartmentalization, and/or expression levels of fatty acid-containing, -binding, and/or -interacting enzymes, proteins, metals, ions, lipids, and/or nucleic acids in diseased cells, thereby facilitating the destruction of these cells. More specifically, these agents target and perturb the activity, or regulation thereof, of the altered mitochondrial energy metabolism observed in the modified pyruvate dehydrogenase (PDH), α-ketoglutarate dehydrogenase (α- KDH), and/or branched-chain α-ketoacid dehydrogenase (BCAKDH) complexes associated with most cancers by modification of the oxidation-reduction state therein, such as but not limited to affecting concentrations of metabolic by-products of PDH, α-KDH, and/or BCAKDH complex activity, including reactive oxygen and nitrogen species.
摘要翻译：药学上可接受的试剂调节脂肪酸，结合和/或相互作用的酶，蛋白质，金属，离子，脂质和/或核酸的结构，功能，活性，细胞位置或分隔和/或表达水平患病细胞中的酸，从而促进这些细胞的破坏。更具体地，这些试剂靶向和扰乱在改良的丙酮酸脱氢酶（PDH），α-酮戊二酸脱氢酶（a-KDH）和/或支链α-酮酸中观察到的改变的线粒体能量代谢的活性或调节脱氢酶（BCAKDH）复合物，其通过修饰其中的氧化还原状态而与大多数癌症相关，例如但不限于影响PDH，a-KDH和/或BCAKDH复合物活性的代谢副产物的浓度，包括活性氧和氮物种。

9. 发明申请

WO2011046583A1 PHARMACEUTICAL EXPLOITATION OF OXIDATIVE STRESS IN TRANSFORMED CELLS 审中-公开
标题翻译：转化细胞中氧化应激的药物开发
公开(公告)号：WO2011046583A1
公开(公告)日：2011-04-21
申请号：PCT/US2010/002455
申请日：2010-09-09
申请人： SHORR, Robert , RODRIQUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana
发明人： SHORR, Robert , RODRIQUEZ, Robert , BINGHAM, Paul , ZACHAR, Zuzana
IPC分类号： A61K38/44
CPC分类号： A61K31/192
摘要： Pharmaceutically-acceptable agents, and pharmaceutical compositions thereof, inhibit the reduction of oxidized peroxiredoxin and isoforms thereof, and mutant forms thereof, in the mitochondria and cytoplasm of diseased cells in a warm-blooded animal through interaction with a variety of target enzymes and substrates. These agents upregulate intramitochondrial and intracellular levels of reactive oxygen and nitrogen species and/or the structure, function, activity level, and/or expression level of apoptosis signal-regulating kinase 1. Such upregulation culminates in increased cytochrome c release from the mitochondria, resulting in cell death. These agents and compositions thereof are useful in the treatment, prevention, diagnosis, and/or imaging of diseased cells characterized by cellular hyperproliferation, such as but not limited to cancer.
摘要翻译：药学上可接受的试剂及其药物组合物通过与各种靶酶和底物的相互作用，抑制温血动物的病变细胞的线粒体和细胞质中的氧化过氧化还原毒素及其同种型及其突变形式的减少。这些药物上调细胞内线粒体和细胞内水平的活性氧和氮物质和/或细胞凋亡信号调节激酶1的结构，功能，活性水平和/或表达水平。这种上调最终导致细胞色素c从线粒体释放增加，从而导致在细胞死亡。这些药剂及其组合物可用于以细胞过度增殖为特征的疾病细胞的治疗，预防，诊断和/或成像，例如但不限于癌症。

10. 发明申请

WO2008131117A1 LIPOIC ACID DERIVATIVES 审中-公开
标题翻译： LIPOIC酸衍生物
公开(公告)号：WO2008131117A1
公开(公告)日：2008-10-30
申请号：PCT/US2008/060655
申请日：2008-04-17
申请人： CORNERSTONE PHARMACEUTICALS, INC. , BINGHAM, Paul , KWOK, Tom , ZACHAR, Zuzana
发明人： BINGHAM, Paul , KWOK, Tom , ZACHAR, Zuzana
IPC分类号： A01N43/26 , A61K31/385
CPC分类号： C07C323/52 , C07C323/56 , C07C323/60 , C07C327/32 , C07D207/34 , C07D213/64 , C07D213/70 , C07D213/81 , C07D277/74 , C07D339/08 , C07D409/04 , C07D495/04 , C07D519/00 , C07F17/02
摘要： Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.
摘要翻译：硫辛酸衍生物和含有硫辛酸衍生物的药物制剂可用于治疗和预防以对硫辛酸衍生物敏感的疾病细胞为特征的疾病。

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