Abstract: Contraceptive activity as well as anti-microbial, particularly anti-viral protection is provided by contraceptive compositions containing a thiourea compound of the invention exhibiting spermicidal or sperm-immobilizing activity. Preferred compounds of the invention are cyclohexenyl-substituted thiourea compounds.
Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors, including allergy treatments.
Abstract: The invention provides methods for treating cancer and compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds.
Type:
Grant
Filed:
May 8, 2002
Date of Patent:
June 1, 2004
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Yanhong Dong, Phalguni Gosh
Abstract: The present invention describes platinum (II) compounds and compositions useful for treating a subject with a tumor and/or inducing apoptosis in a population of cells. The present invention also describes pharmaceutical compositions containing the aforementioned inventive compound(s) in combination with a pharmaceutically acceptable carrier. Additionally, the invention further provides a method of inducing apoptosis in a population of cells and a method of treating a subject with a tumor, wherein the method comprises administering to the subject a therapeutically effective amount of the aforementioned compound(s) or composition(s).
Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).
Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.
Type:
Grant
Filed:
April 15, 2003
Date of Patent:
April 27, 2004
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.
Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.
Type:
Grant
Filed:
December 6, 2001
Date of Patent:
February 10, 2004
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
Abstract: Embodiments of the present invention provide methods for inhibiting tumor cell growth, or treating cancer cells, in a subject through the administration of a cathepsin inhibitor or inhibitors. Methods for inhibiting inflammatory disease cells as well as other cathepsin expressing cells in a subject with a cathepsin inhibitor or inhibitors are also within the present invention. Furthermore, the present invention relates to inducing cytotoxicity or apoptosis in cells by administering a cytotoxic or an apoptotic dose of a cathepsin inhibitor or inhibitors to the cell. Finally, the present invention relates to the administering of cathepsin expressing vectors to tumor cells so as to inhibit the tumor cells growth.
Abstract: Specific Ikaros mutations, as well as the correlation of the presence of the specific Ikaros mutations and other wild-type non-DNA binding Ikaros isoforms with lymphoid cell abnormality is provided in the in the invention. Methods for detecting and treating lymphoid cell abnormality, including hematologic malignancy, are also provided.
Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.
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:
July 23, 2002
Date of Patent:
December 23, 2003
Assignee:
Parker Hughes Institute
Inventors:
Phalguni Ghosh, Faith M. Uckun, Osmond D′Cruz
Abstract: Novel aromatic and heterocyclic thiazolyl thiourea compounds, pharameutical compositions including such, and methods for their use are disclosed. The compounds are effective agents for the treatment of HIV infection, including non-nucleoside inhibitor-resistant, and multi-drug resistant strains of HIV.
Type:
Application
Filed:
April 15, 2003
Publication date:
November 6, 2003
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
Abstract: Vanadium compounds as anti-proliferative agents. These compounds act to disrupt mitotic and meiotic spindle formation and thus are useful to prevent cell mitosis (proliferation) and meiosis.
Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.
Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.
Type:
Application
Filed:
April 15, 2003
Publication date:
October 2, 2003
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
Abstract: Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, including their corresponding therapeutic compositions are described.
Type:
Grant
Filed:
August 15, 2002
Date of Patent:
September 30, 2003
Assignee:
Parker Hughes Institute
Inventors:
Osmond D'Cruz, Phalguni Ghosh, Fatih M. Uckun
Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
Type:
Application
Filed:
January 21, 2003
Publication date:
September 25, 2003
Applicant:
Parker Hughes Institute located at Roseville, Minnesota
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam