Abstract: The inventors have discovered that hematologic disorders, e.g., both neoplastic (hematologic cancers) and non-neoplastic conditions, can be treated by the induction of mixed chimerism using myeloreductive, but not myeloablative, conditioning. Methods of the invention reduce GVHD, especially GVHD associated with mismatched allogeneic or xenogeneic donor tissue, yet provide, for example, significant graft-versus-leukemia (GVL) effect and the like.

Abstract: A method of treating cystic fibrosis in a patient comprising: administering to said patient an effective amount of a type V cyclic nucleotide phosphodisterase inhibitor, wherein said inhibitor is a compound of formula (I):  wherein A is a five- or six-membered ring containing one or more N atoms, X is a substituent of formula (II):  wherein R1 represents C1-4 alkyl, and X is positioned at either or both of the 2-position and/or the 8-position in (I).

Abstract: The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.

Abstract: The invention provides a method of treatment for an animal having a disease state associated with a genitourinary disorder with a purinergic receptor modulator. Also provided, is a transgenic animal having a disrupted purinergic receptor gene. The invention further provides for a method of screening using the transgenic animal as a positive control.

Abstract: This invention provides a soluble nano-sized particles formed of a core (water-insoluble lipophilic compound or hydrophilic compound) and an amphiphilic polymer and which demonstrated improved solubility and/or stability. The lipophilic compound within the soluble nano-sized soluble (“solu-nanoparticles”) may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products.

Abstract: The present invention is directed to compounds useful in inhibiting cellular proliferation. Processes of preparing such compounds are also disclosed.

Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): 1

Abstract: A method for identifying compounds binding to HCV polymerase comprising the steps of:contacting said HCV polymerase or an analog thereof with a probe formula I: 1

Abstract: The present invention relates to the use of at least one compound of the general formula I,

Abstract: The invention provides a method of inhibiting tumor growth in a mammal, by administering to the mammal composition containing taurolidine, taurultam, or a biologically active derivative thereof. The composition is administered to directly contact a tumor cell at a dose sufficient to induce cell death by apoptosis.

Abstract: The invention relates to cis-nucleosides of formula (I): and pharmaceutically acceptable salts thereof, wherein X, R3, R4 and are as defined herein. The nucleosides can be in racemic form or in the form of their (+) or (−) enantiomers. The compounds are useful for treating HBV and/or HIV infections, alone or in combination with other therapeutic agents.

Abstract: Disclosed are novel compounds having the formula 1

Abstract: This invention provides a soluble inclusion complex formed of a water-insoluble lipophilic compound and an amphiphilic polymer and which demonstrated improved solubility and stability. The lipophilic compound within the inclusion complex may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products. The invention also provides novel methods for preparing the inclusion complex, as well as a novel chemical reactor for forming the inclusion complex.

Abstract: A method for treating arrhythmia in mammals is provided comprising administering a low dose of an adenosine receptor agonist of the Formula I: wherein R1 is an optionally substituted heterocyclic group, preferably monocyclic.

Abstract: This invention is directed to the use phosphodiesterase type 5 (PDE5) inhibitors in the treatment of selective serotonin reuptake inhibitor (SSRI) induced sexual dysfunction. Specifically, this invention is directed to a method for treating an animal to cure; prevent or ameliorate SSRI induced sexual dysfunction which comprises administering to the animal an effective amount of the inhibitor. The animal may be a male or a female human. The invention also includes the use of such inhibitors in the manufacture of a medicament to prevent; cure or ameliorate SSRI induced sexual dysfunction. Moreover, the invention includes a kit comprising a SSRI, such as sertraline, fluoxetine, paroxetine, and a PDE5 inhibitor, such as sildenafil citrate, for the treatment or prevention of serotonergic associated disorders such as depression, obsessive compulsive disorder or panic disorder, while reducing or preventing sexual dysfunction.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.

Abstract: The present invention relates to chimeric protein kinase molecules and methods for designing inhibitors of protein kinases using the chimeric protein kinases of the present invention. The chimeric protein kinase of the present invention comprise inhibitor binding site residues of a non-crystallizable protein and non-inhibitor binding site residues of a crystallizable protein. The chimeric protein is preferably crystallizable and is useful for designing inhibitors for the non-crystallizable protein. In addition, the present invention is directed to a protein kinase inhibitor binding site which is outside the ATP binding site of the protein kinase and methods of use therefore.

Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.

Abstract: Methods for treating patients with CLL with pharmaceutical agents are disclosed. The methods of the present invention can be used in patients that have not responded to standard treatment. In addition, the methods can be used to augment the impact of standard chemotherapy.

Abstract: The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

Abstract: This invention provides caspase inhibitors having the formula: 1

Abstract: Disclosed are compounds of the formula: 1

Abstract: Human mast cell activation is modulated by ATP binding to P2-purinoceptors on the mast cell surface. ATP binding to the purinoceptors provides a target for therapeutic intervention for the treatment of disorders characterized by undesireable mast cell mediator release, such as asthma and allergy. Inhibitors of ATP binding to mast cell P2-purinoceptors are useful therapeutic agents for treatments of those disorders. Methods of treatment using agents, and in vitro screening assays for selection of the therapeutic agents, are described.

Abstract: Disclosed are compounds of the formula: 1

Abstract: Human mast cell activation is modulated by ATP binding to P2-purinoceptors on the mast cell surface. ATP binding to the purinoceptors provides a target for therapeutic intervention for the treatment of disorders characterized by undesireable mast cell mediator release, such as asthma and allergy. Inhibitors of ATP binding to mast cell P2-purinoceptors are useful therapeutic agents for treatments of those disorders. Methods of treatment using agents, and in vitro screening assays for selection of the therapeutic agents, are described.