Patent application number | Description | Published |
20080261919 | Camptothecin-analog with a novel, "flipped" lactone-stable, E-ring and methods for making and using same - The present invention discloses: (i) a novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need thereof. | 10-23-2008 |
20090111735 | Compounds and methods for reducing undesired toxicity of chemotherapeutic agents - Novel compositions and formulations are disclosed that have use to mitigate or prevent physiologically deleterious side-effects and/or modulate the intracellular balance of oxidized and reduced thioredoxin (Trx) in patients with cancer who are receiving treatment with one or more chemotherapeutic agents. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium (mesna). In addition, methods of administration and kits comprising these novel mesna heteroconjugates are disclosed. | 04-30-2009 |
20090232827 | Compositions and methods of use of compounds to increase cancer patient survival time - The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in time of survival in cancer patients, wherein the cancer either: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer. Further, the present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the treatment of patients with medical conditions and disease where there is the overexpression of thioredoxin and/or glutaredoxin, and wherein this overexpression is associated with deleterious physiological effects in the patients. | 09-17-2009 |
20090232906 | Treatment methods and compositions for lung cancer, adenocarcinoma, and other medical conditions - The present invention discloses and claims: (i) compositions, methods, and kits which lead to an increase in patient survival time in cancer patients receiving chemotherapy; (ii) compositions and methods which cause cytotoxic or apoptotic potentiation of the anti-cancer activity of chemotherapeutic agents; (iii) compositions and methods for maintaining or stimulating hematological function in patients in need thereof, including those patients suffering from cancer; (iv) compositions and methods for maintaining or stimulating erythropoietin function or synthesis in patients in need thereof, including those patients suffering from cancer; (v) compositions and methods for mitigating or preventing anemia in patients in need thereof, including those patients suffering from cancer; (vi) compositions and methods for maintaining or stimulating pluripotent, multipotent, and unipotent normal stem cell function or synthesis in patients in need thereof, including those patients suffering from cancer; (vii) compositions and methods which promote the arrest or retardation of tumor progression in those cancer patients receiving chemotherapy; (viii) compositions and methods for increasing patient survival and/or delaying tumor progression while maintaining or improving the quality of life in a cancer patient receiving chemotherapy; (ix) novel methods of the administration of taxane and/or platinum medicaments and a Formula (I) compound of the present invention to a cancer patient; and (x) kits to achieve one or more of the aforementioned physiological effects in a patient in need thereof, including those patients suffering from cancer. | 09-17-2009 |
20120070404 | Increasing cancer patient survival time by administration of dithio-containing compounds - The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in the time of survival in cancer patients, wherein the cancer: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer. Further, the present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the treatment of patients with medical conditions and disease where there is the overexpression of thioredoxin and/or glutaredoxin, and wherein this overexpression is associated with deleterious physiological effects in the patients. | 03-22-2012 |
Patent application number | Description | Published |
20120282261 | Deuterated analogs of (4S)-4-Ethyl-4-hydroxy-11-[2- (trimethylsilyl)ethyl]-1H-pyrano[3', 4':6,7] indolizino [1,2-b]quinoline-3,14(4H, 12H)-dione and methods of use thereof - The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof. | 11-08-2012 |
20140073793 | Germanium-containing camptothecin analogues - The present invention discloses: (i) the novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; (ii) methods of synthesis of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts; (iii) pharmaceutically-acceptable formulations comprising said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof; and (iv) methods of administration of said novel germanium-containing camptothecin compound, 7[2′-trimethylgermanyl]ethyl-20(S) camptothecin, and pharmaceutically-acceptable salts thereof to subjects in need thereof, including subjects with cancer. | 03-13-2014 |
20140135499 | METHODS FOR THE TOTAL CHEMICAL SYNTHESIS OF ENANTIOMERICALLY-PURE 7-(2'-TRIMETHYLSILYL) ETHYL CAMPTOTHECIN - The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material. | 05-15-2014 |
20160038519 | ADMINISTRATION OF KARENITECIN FOR THE TREATMENT OF ADVANCED OVARIAN CANCER, INCLUDING CHEMOTHERAPY-RESISTANT AND/OR THE MUCINOUS ADENOCARCINOMA SUB-TYPES - The present invention discloses and claims methods and compositions for the treatment of platinum and/or taxane cancer treating agent-resistant/-refractory sub-populations and/or the mucinous adenocarcinoma sub-type of ovarian cancer subjects with the silicon-containing highly lipophilic camptothecin derivative (HLCD), Karenitecin (also known as BNP1350; cositecan; 7-[(2′-trimethylsilyl)ethyl]-20(S) camptothecin). The administration of Karenitecin by intravenous (i.v.) and/or oral methodologies are also disclosed and claimed. Karenitecin analogues, including but not limited to, Germanium-substituted Karenitecin, Deuterated Karenitecin, and “flipped” E-ring Karenitecin, are disclosed and claimed. In addition, Karenitecin and one or more cancer treating agents administered either concomitantly or in series via oral and/or i.v. means, are also disclosed and claimed. Methods for the administration of Karenitecin to: (i) increase Progression Free Survival (PFS); (ii) increase the platinum-free time interval; (iii) decrease CA-125 marker levels; and (iv) mitigate or prevent chemotherapeutic drug-resistance from developing are disclosed and claimed herein. Methods for the use of Karenitecin to treat advanced solid tumors; refractory or recurrent solid tumors; recurrent malignant glioma; primary malignant glioma; persistent or recurrent epithelial ovarian or primary peritoneal carcinoma; and other identified cancer types are also disclosed and claimed. | 02-11-2016 |
Patent application number | Description | Published |
20090194513 | Method and apparatus for operating traveling spark igniter at high pressure - An ignition circuit and a method of operating an igniter (preferably a traveling spark igniter) in an internal combustion engine, including a high pressure engine. A high voltage is applied to electrodes of the igniter, sufficient to cause breakdown to occur between the electrodes, resulting in a high current electrical discharge in the igniter, over a surface of an isolator between the electrodes, and formation of a plasma kernel in a fuel-air mixture adjacent said surface. Following breakdown, a sequence of one or more lower voltage and lower current pulses is applied to said electrodes, with a low “simmer” current being sustained through the plasma between pulses, preventing total plasma recombination and allowing the plasma kernel to move toward a free end of the electrodes with each pulse. | 08-06-2009 |
20110309749 | METHOD AND APPARATUS FOR OPERATING TRAVELING SPARK IGNITER AT HIGH PRESSURE - An ignition circuit and a method of operating an igniter (preferably a traveling spark igniter) in an internal combustion engine, including a high pressure engine. A high voltage is applied to electrodes of the igniter, sufficient to cause breakdown to occur between the electrodes, resulting in a high current electrical discharge in the igniter, over a surface of an isolator between the electrodes, and formation of a plasma kernel in a fuel-air mixture adjacent said surface. Following breakdown, a sequence of one or more lower voltage and lower current pulses is applied to said electrodes, with a low “simmer” current being sustained through the plasma between pulses, preventing total plasma recombination and allowing the plasma kernel to move toward a free end of the electrodes with each pulse. | 12-22-2011 |
20140091712 | METHOD AND APPARATUS FOR OPERATING TRAVELING SPARK IGNITER AT HIGH PRESSURE - An ignition circuit and a method of operating an igniter (preferably a traveling spark igniter) in an internal combustion engine, including a high pressure engine. A high voltage is applied to electrodes of the igniter, sufficient to cause breakdown to occur between the electrodes, resulting in a high current electrical discharge in the igniter, over a surface of an isolator between the electrodes, and formation of a plasma kernel in a fuel-air mixture adjacent said surface. Following breakdown, a sequence of one or more lower voltage and lower current pulses is applied to said electrodes, with a low “simmer” current being sustained through the plasma between pulses, preventing total plasma recombination and allowing the plasma kernel to move toward a free end of the electrodes with each pulse. | 04-03-2014 |