Patents Assigned to BioNumerik Pharmaceuticals, Inc.
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Patent number: 10413538Abstract: The present invention discloses and claims methods and compositions for the treatment of subjects having advanced ovarian cancer, including platinum and/or taxane chemotherapy resistant or refractory sub-populations, with the administration to the subject having advanced ovarian cancer of the silicon-containing highly lipophilic camptothecin derivative (HLCD), Karenitecin (also known as BNP1350; cositecan; 7-[(2?-trimethylsilyl)ethyl]-20(S) camptothecin) in an amount sufficient to provide a therapeutic benefit. The administration of Karenitecin by intravenous (i.v.) and/or oral methodologies are also disclosed and claimed. Methods for the administration of Karenitecin to increase Progression Free Survival (PFS) are also disclosed and claimed herein.Type: GrantFiled: May 1, 2014Date of Patent: September 17, 2019Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H Hausheer
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Publication number: 20180369173Abstract: 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.Type: ApplicationFiled: March 31, 2015Publication date: December 27, 2018Applicant: BIONUMERIK PHARMACEUTICALS, INC.Inventor: Frederick H. Hausheer
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Publication number: 20160287540Abstract: 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.Type: ApplicationFiled: March 31, 2015Publication date: October 6, 2016Applicant: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Publication number: 20160287539Abstract: 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.Type: ApplicationFiled: March 31, 2015Publication date: October 6, 2016Applicant: BIONUMERIK PHARMACEUTICALS, INC.Inventor: Frederick H. Hausheer
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Patent number: 9320760Abstract: 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.Type: GrantFiled: July 15, 2008Date of Patent: April 26, 2016Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Patent number: 9023805Abstract: 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.Type: GrantFiled: September 16, 2010Date of Patent: May 5, 2015Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Publication number: 20140336150Abstract: The present invention discloses and claims methods and compositions for the treatment of subjects having advanced ovarian cancer, including platinum and/or taxane chemotherapy resistant or refractory sub-populations, with the administration to the subject having advanced ovarian cancer of the silicon-containing highly lipophilic camptothecin derivative (HLCD), Karenitecin (also known as BNP1350; cositecan; 7-[(2?-trimethylsilyl)ethyl]-20(S) camptothecin) in an amount sufficient to provide a therapeutic benefit. The administration of Karenitecin by intravenous (i.v.) and/or oral methodologies are also disclosed and claimed. Methods for the administration of Karenitecin to increase Progression Free Survival (PFS) are also disclosed and claimed herein.Type: ApplicationFiled: May 1, 2014Publication date: November 13, 2014Applicant: BioNumerik Pharmaceuticals, Inc.Inventor: Hausheer H. Frederick
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Patent number: 8722886Abstract: 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.Type: GrantFiled: November 13, 2012Date of Patent: May 13, 2014Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Xinghai Chen, Frederick H. Hausheer, Andrey Malakhov, Harry Kochat
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Patent number: 8710095Abstract: Provided are pharmaceutical drugs for preventing or mitigating adverse actions associated with taxane antineoplastic drugs which are frequently and widely used in cancer chemotherapy, and pharmaceutical compositions which allow us to shorten the duration of treatment with taxane antineoplastic agents and/or to repeat the taxane treatment course more times, as well as drugs suitable for the therapeutic schedules.Type: GrantFiled: April 30, 2002Date of Patent: April 29, 2014Assignee: Bionumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Patent number: 8569265Abstract: 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.Type: GrantFiled: May 6, 2011Date of Patent: October 29, 2013Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Xinghai Chen, Qiuli Huang, Harry Kochat, Andrey Malakhov, Frederick H. Hausheer
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Patent number: 8143236Abstract: Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents. In addition compositions and methods for mitigating or preventing a novel form of chemotherapy-induced peripheral neuropathy are disclosed and claimed.Type: GrantFiled: March 14, 2008Date of Patent: March 27, 2012Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Patent number: 8026227Abstract: Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents.Type: GrantFiled: December 13, 2006Date of Patent: September 27, 2011Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Frederick H. Hausheer
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Patent number: 7829541Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.Type: GrantFiled: November 14, 2007Date of Patent: November 9, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Harry Kochat, Qiuli Huang
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Patent number: 7829540Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.Type: GrantFiled: November 14, 2007Date of Patent: November 9, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Harry Kochat, Qiuli Huang
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Patent number: 7829539Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.Type: GrantFiled: November 14, 2007Date of Patent: November 9, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Harry Kochat, Qiuli Huang
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Patent number: 7829117Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.Type: GrantFiled: November 14, 2007Date of Patent: November 9, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Harry Kochat, Qiuli Huang
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Patent number: 7829538Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.Type: GrantFiled: November 14, 2007Date of Patent: November 9, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Harry Kochat, Qiuli Huang
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Patent number: 7777060Abstract: Disclosed herein are novel platinum-based analogs possessing two nitrile substituent groups (bis-nitrile) covalently-bonded to the platinum. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as quantitative in vitro IC50 data.Type: GrantFiled: October 30, 2007Date of Patent: August 17, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Xinghai Chen, Pavankumar N. V. Petluru, Qiuli Huang, Kesavaram Narkunan, Frederick Hausheer
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Patent number: 7759488Abstract: Disclosed herein are novel platinum-based analogs with a single substituted azole ligand: RN?NR7, wherein the RN?NR7 functional group is covalently bonded to the platinum through nitrogen of NR7. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof.Type: GrantFiled: January 26, 2006Date of Patent: July 20, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Zejun Xiao, Harry Kochat, Frederick H. Hausheer
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Patent number: 7687497Abstract: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).Type: GrantFiled: October 16, 2007Date of Patent: March 30, 2010Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Kesavaram Narkunan, Xinghai Chen, Harry Kochat, Frederick Hausheer