公开(公告)号：WO2011005310A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/001907

申请日：2010-07-07

Applicant: SHORR, Robert

Inventor： SHORR, Robert

IPC: A01N65/00 ,  A61K36/00

CPC classification number: A61K36/81 ,  A61K36/185 ,  A61K36/54 ,  A61K36/61 ,  A61K36/87 ,  A61K36/898 ,  A61K36/9066 ,  A61K2300/00

Abstract: Therapeutic and/or diagnostic formulations intended to improve glucose uptake and the oxidation of nutrients in warm-blooded animals, including humans, presenting with cancer, in a manner that diminishes toxic by-products generated by these metabolic events, may be administered either for single daily independent administration or a binary morning and nighttime administration which also promotes sleep. In a preferred embodiment of the present invention, effective amounts of derivatives of thiol-containing alkyl fatty acids, such as but not limited to those of lipoic acid and analogs thereof, are co-formulated with effective amounts of naturally-occurring or synthetic antioxidants, trace elements, botanical extracts, carbohydrates, and other substances. Pharmaceutically-acceptable carriers and excipients may be included in the formulation as necessary.

Abstract translation: 治疗和/或诊断制剂可以以减少由这些代谢事件产生的有毒副产物的方式改善呈现癌症的温血动物（包括人）中的葡萄糖摄取和营养物质的氧化， 每日独立行政管理或二进制早晨和夜间行政，也促进睡眠。 在本发明的优选实施方案中，有效量的含硫醇的烷基脂肪酸的衍生物，例如但不限于硫辛酸及其类似物的衍生物与有效量的天然存在或合成的抗氧化剂共配制， 微量元素，植物提取物，碳水化合物和其他物质。 根据需要可以在制剂中包括药学上可接受的载体和赋形剂。

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

Applicant: SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  ZACHAR, Zuzana ,  BOTEJU, Lakmal, W. ,  ZARETSKI, Patrick, P.

Inventor： SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  ZACHAR, Zuzana ,  BOTEJU, Lakmal, W. ,  ZARETSKI, Patrick, P.

IPC: A01N37/12 ,  A01N37/44 ,  A61K31/195

CPC classification number: A61K31/195

Abstract: 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.

Abstract translation: 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。

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

Applicant: SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  ZACHAR, Zuzana ,  BOTEJU, Lakmal, W. ,  ZARETSKI, Patrick, P.

Inventor： SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  ZACHAR, Zuzana ,  BOTEJU, Lakmal, W. ,  ZARETSKI, Patrick, P.

IPC: A01N37/00 ,  A61K31/20

CPC classification number: A61K47/542 ,  A61K47/60

Abstract: 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.

Abstract translation: 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。

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

Applicant: SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  BOTEJU, Lakmal, W. ,  ZACHAR, Zuzana

Inventor： SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  BOTEJU, Lakmal, W. ,  ZACHAR, Zuzana

IPC: A61K31/385 ,  A61K31/19

CPC classification number: A61K31/19 ,  A61K31/385

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2011102905A1

公开(公告)日：2011-08-25

申请号：PCT/US2011/000313

申请日：2011-02-22

Applicant: SHORR, Robert ,  RODRIGUEZ, Robert

Inventor： SHORR, Robert ,  RODRIGUEZ, Robert ,  GIBSON, Frank

IPC: A61B5/055

CPC classification number: A61K49/0002 ,  A61K49/0078

Abstract: A stable lipid-oil-water nanoemulsion associated with an imaging agent and a diagnostic agent is useful both for imaging cells characterized by aberrant lipid metabolism and/or cellular hyperproliferation, such as cancer cells, and for diagnosing the cancer in an exquisitely specific and selective manner compared to non-transformed cells.

Abstract translation: 与成像剂和诊断剂相关的稳定的脂质 - 油 - 水纳米乳剂对于以异常脂质代谢和/或细胞过度增殖为特征的成像细胞如癌细胞是有用的，并且用于以精细特异性和选择性诊断癌症 方式与未转化细胞相比。

公开(公告)号：WO2011050261A1

公开(公告)日：2011-04-28

申请号：PCT/US2010/053728

申请日：2010-10-22

Applicant: CORNERSTONE PHARMACEUTICALS, INC. ,  SHORR, Robert, G.L. ,  RODRIGUEZ, Robert, J. ,  BHASIN, Rajinder

Inventor： SHORR, Robert, G.L. ,  RODRIGUEZ, Robert, J. ,  BHASIN, Rajinder

IPC: A01N43/26

CPC classification number: A61K47/18 ,  A61K31/19 ,  A61K31/20 ,  A61K31/381 ,  A61K45/06 ,  A61K47/183 ,  A61K47/22 ,  A61K47/36 ,  A61K47/541 ,  Y02A50/409 ,  Y02A50/475 ,  Y02A50/479 ,  A61K2300/00

Abstract: Pharmaceutical formulations containing lipoic acid derivatives and ion pairs thereof are described. The pharmaceutical formulations are useful in the treatment of medical disorders, such as cancer.

Abstract translation: 描述了含有硫辛酸衍生物及其离子对的药物制剂。 药物制剂可用于治疗诸如癌症的医学病症。

公开(公告)号：WO2011005311A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/001908

申请日：2010-07-07

Applicant: SHORR, Robert

Inventor： SHORR, Robert

IPC: A01N65/00 ,  A61K36/00

CPC classification number: A61K36/81 ,  A61K36/185 ,  A61K36/54 ,  A61K36/61 ,  A61K36/87 ,  A61K36/898 ,  A61K36/9066 ,  A61K2300/00

Abstract: Therapeutic and/or diagnostic formulations intended to improve glucose uptake and the oxidation of nutrients in warm-blooded animals, including humans, presenting with cancer, in a manner that diminishes toxic by-products generated by these metabolic events, may be administered either for single daily independent administration or a binary morning and nighttime administration which also promotes sleep. In a preferred embodiment of the present invention, effective amounts of thiol-containing alkyl fatty acids, such as but not limited to those of lipoic acid and analogs thereof, are co-formulated with effective amounts of naturally- occurring or synthetic antioxidants, trace elements, plant extracts, carbohydrates, and other substances. Pharmaceutically-acceptable carriers and excipients may be included in the formulation as necessary.

Abstract translation: 治疗和/或诊断制剂可以以减少由这些代谢事件产生的有毒副产物的方式改善呈现癌症的温血动物（包括人）中的葡萄糖摄取和营养物质的氧化， 每日独立行政管理或二进制早晨和夜间行政，也促进睡眠。 在本发明的一个优选实施方案中，有效量的含硫醇的烷基脂肪酸，例如但不限于硫辛酸及其类似物的那些，与有效量的天然存在或合成的抗氧化剂，微量元素 ，植物提取物，碳水化合物等物质。 根据需要可以在制剂中包括药学上可接受的载体和赋形剂。

公开(公告)号：WO1992010756A1

公开(公告)日：1992-06-25

申请号：PCT/US1991009302

申请日：1991-12-06

Applicant: BOMALASKI, John, S. ,  CLARK, Mike, A. ,  SHORR, Robert, G., L.

IPC: G01N33/535

CPC classification number: C12N15/113 ,  A61K38/00 ,  C07K14/4705 ,  C07K16/18 ,  C07K2319/00 ,  C07K2319/40 ,  C07K2319/61

Abstract: The invention provides methods for detecting elevated levels of phospholipase A2, activating protein in persons suspected of having rheumatoid arthritis to thereby indicate the presence of rheumathoid arthritis in the person comprising the steps of providing a sample of body fluid or tissue from said person; contacting the sample with an antibody specific for phospholipase A2, activating protein such that the antibody binds with phospholipase A2, activating protein in the sample; detecting the antibody thereby indicating the presence of phospholipase A2 activating protein, whereby elevated levels of phospholipase A2 activating protein in the sample as compared with levels found in persons not having rheumatoid arthritis indicates the presence of rheumatoid arthritis in the person. Kits and reagents for detecting rheumatoid arthritis are also provided.

公开(公告)号：WO1991014489A1

公开(公告)日：1991-10-03

申请号：PCT/US1991001856

申请日：1991-03-19

Applicant: AT BIOCHEM, INC. ,  SHORR, Robert

Inventor： AT BIOCHEM, INC.

IPC: B01D15/08

CPC classification number: G01N27/44747

Abstract: Electrophoretic media based on polymers with novel structures are disclosed. The polymers are formed by polymerization of acrylamide monomers, such as N-methylolacrylamide, with cross-linking agents or comonomer agents such as tetraethylene diacrylate and bisacrylamide methylether.

Abstract translation: 公开了基于具有新颖结构的聚合物的电泳介质。 聚合物通过丙烯酰胺单体如N-羟甲基丙烯酰胺与交联剂或共聚单体试剂如四亚乙基二丙烯酸酯和双丙烯酰胺甲基醚的聚合形成。

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

Applicant: SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  BOTEJU, Lakmal ,  KWOK, Thomas ,  MARECEK, James

Inventor： SHORR, Robert ,  RODRIGUEZ, Robert ,  BINGHAM, Paul ,  BOTEJU, Lakmal ,  KWOK, Thomas ,  MARECEK, James

IPC: A61K31/20 ,  A61P35/00 ,  C07C381/00

CPC classification number: C07F9/5442 ,  C07C321/20 ,  C07C323/12 ,  C07C323/25 ,  C07C323/60 ,  C07C323/66 ,  C07D257/04

Abstract: 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.

Abstract translation: 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。