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
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: 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: The invention provides a method for inhibiting c-jun activation in mammalian or avian cells comprising contacting the cells with a substance that inhibits the activity of Janus family kinase 3 (JAK-3). The invention also provides a therapeutic method for preventing or treating a pathological condition in a mammal wherein c-jun activation is implicated and inhibition of its activation is desired comprising administering to a mammal in need of such therapy, an effective amount of a substance that inhibits the activity of JAK-3. Novel compounds that are JAK-3 inhibitors, as well as pharmaceutical compositions comprising the compounds are also provided.
Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors, including allergy treatments.
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 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:
Application
Filed:
October 22, 2002
Publication date:
July 3, 2003
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Ventatachalam
Abstract: Synthetic Phorboxazole A and derivatives thereof for the treatment of cancer, including inhibition of cancer cell growth, induction of apoptosis, and inhibition of metastises.
Type:
Application
Filed:
May 14, 2002
Publication date:
July 3, 2003
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Rama K. Narla, Craig Forsyth, Chi Sing Lee, Feryan Ahmed, Russel Drew Cink
Abstract: Novel phenylethyl-thiourea (PHET) 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:
September 7, 2001
Date of Patent:
July 1, 2003
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Ventatachalam
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:
Grant
Filed:
July 11, 2001
Date of Patent:
April 22, 2003
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
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:
Application
Filed:
May 8, 2002
Publication date:
April 17, 2003
Applicant:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Yanhong Dong, Phalguni Gosh
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:
Grant
Filed:
July 18, 2000
Date of Patent:
April 8, 2003
Assignee:
Parker Hughes Institute
Inventors:
Fatih M. Uckun, Taracad K. Venkatachalam
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: 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 hematoloic 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: 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: 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 vanadocene dichloride, vanadocene dibromide, bis (methyl cyclopentadienyl) vanadium dichloride, vanadocene diiodide, vanadocene di-pseudohalides, and others. Most active found was vanadocene diselenocyanate.
Type:
Application
Filed:
August 15, 2002
Publication date:
January 23, 2003
Applicant:
Parker Hughes Institute
Inventors:
Osmond D'Cruz, Phalguni Ghosh, Fatih M. Uckun
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.