Abstract: Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, are described including corresponding contraceptive and therapeutic compositions and method for providing contraception and selective killing of testicular germ cells. Included among the vanadium complexes are bis(methyl cyclopentadienyl)vanadium dichloride, vanadocene di-pseudohalides, and others. Most active found was vanadocene diselenocyanate.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
December 31, 2002
Assignee:
Parker Hughes Institute
Inventors:
Osmond D'Cruz, Phalguni Ghosh, Fatih M. Uckun
Abstract: The invention provides a method for preventing the development or recurrence of cancer in a mammal by administering to the mammal a compound comprising an isoflavone, such as Genistein, conjugated to epidermal growth factor (EGF).
Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.
Type:
Grant
Filed:
March 19, 2001
Date of Patent:
December 17, 2002
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Elise A. Sudbeck, Marina Cetkovic, Ravi Malaviya, Xing-Ping Liu
Abstract: The method of the invention includes use of Syk, Syk-conjugte, Syk-binding ligand, or Syk inhibitor as a marker for the analysis of a cell's centrosome, centrioles, or mitiotic spindle, for example, in the diagnosis of cellular proliferation disorders, or for the study of cell cycle. In addition, the method of the invention included use of Syk-binding ligand or Syk inhibitors to inhibit the function of centrosome, centrioles, or mitiotic spindle, for example in the inhibition of cell proliferation, particularly cancer.
Abstract: The present invention is directed to a method of preventing the development or recurrence of colorectal cancer in a mammal comprising adminstering to the mammal an effective cancer preventive amount of 4(4′-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline or a pharmaceutically acceptable salt thereof.
Abstract: Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5-halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.
Type:
Grant
Filed:
December 1, 2000
Date of Patent:
November 19, 2002
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Osmond D'Cruz, Taracad Venkatachalam
Abstract: Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.
Abstract: The present invention is directed to a method of preventing the development or recurrence of colorectal cancer in a mammal comprising administering to the mammal, an effective cancer preventative amount of 4-(4′-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline or a pharmaceutically acceptable salt thereof.
Abstract: Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.
Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering to the subject a pharmaceutically effective amount of a compound or composition that inhibits BTK and collagen-induced platelet aggregation. The condition of platelet aggregation includes cardiovascular, hematopoietic and cerebrovascular diseases.
Abstract: Novel substituted quinozaline compounds and conjugates useful to inhibit the growth of brain tumor cells and to inhibit adhesion and migration of brain tumor cells. The compounds of the invention include 4-(3′-bromo-4′-hydroxy phenyl)-amino-6,7-dimethoxyquinazoline and this compound covalently bound to EGF.
Type:
Application
Filed:
July 11, 2001
Publication date:
October 31, 2002
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.
Type:
Grant
Filed:
May 16, 2001
Date of Patent:
October 22, 2002
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Elise A. Sudbeck, Marina Cetkovic, Ravi Malaviya, Xing-Ping Liu
Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
October 22, 2002
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Ventatachalam
Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
Abstract: A method for the preparation of 5′-hydroxy phosphorylated nucleoside derivatives in a single reaction vessel is provided. The method includes contacting phosphorous oxychloride with a halophenyl moiety followed by contacting the resulting halophenylphosphorodichloridate with a carboxy-protected amino acid and finally contacting the resulting halophenyl carboxy-protected amino acid phosphorochloridate with a nucleoside.
Abstract: Vanadium (IV) complexes containing a substituted or unsubstituted catecholate ligand, and the spermicidal activity of such compounds. Preferred compounds are vanadocene (IV) complexes containing alkyl substituted catecholate ligands.
Type:
Grant
Filed:
September 19, 2001
Date of Patent:
October 15, 2002
Assignee:
Parker Hughes Institute
Inventors:
Phalguni Ghosh, Fatih M. Uckun, Osmond D'Cruz
Abstract: Pharmaceutical compositions for parenteral administration of poorly soluble quinazoline compounds in the form of microemulsions or micellar solutions are described. The compositions are useful in treating patients suffering from cancer or having allergic reactions.
Type:
Application
Filed:
September 19, 2001
Publication date:
August 15, 2002
Applicant:
PARKER HUGHES INSTITUTE
Inventors:
Seang H. Yiv, Mingshu Li, Fatih M. Uckun