Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract: The present disclosure provides for compositions for the treatment of neurodegenerative diseases comprising one or more isolated phosphate complexes of platinum and methods of uses thereof for treating neurodegenerative diseases including amyotrophic lateral sclerosis, Alzheimer's disease, stroke, epilepsy, Parkinsons, Huntington's disease and diabetes associated peripheral neuropathy The present disclosure is also directed towards an anti-angiogenic composition useful for inhibiting angiogenesis related to age-related macular degeneration, diabetic retinopathy and tumor-associated angiogenesis. An embodiment of the present disclosure is also directed towards a method for modulating the expression of Pigment Epithelial Derived Factor (PEDF) gene in an individual in need thereof.

Abstract: The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: Bisphosphonamidate prodrugs of therapeutic bisphosphonate compounds and uses thereof to treat diseases are described.

Abstract: The present invention relates to various salts of inositol tripyrophosphate including the calcium, lithium, beryllium, magnesium, potassium, strontium, barium, rubidium and cesium salts of inositol tripyrophosphate, compositions comprising these salts, methods of making the various salts, and methods of use of the above salts. Methods of use include administering the above salts in an effective amount in individuals for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphospahte (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.

Abstract: The present invention provides phosphorylated and pyrophosphate derivatives of polyols, and structural derivatives of these compounds, and provides pharmaceutical compositions comprising the same. The compounds and compositions disclosed herein have various biological activities, including for example, as allosteric effectors of hemoglobin and/or as kinase inhibitors. The present invention further provides methods for therapy in human or mammalian patients, and methods for synthesis of biologically active compounds and their intermediates.

Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.

Abstract: Bisphosphonamidate prodrugs of therapeutic bisphosphonate compounds and uses thereof to treat diseases are described.

Abstract: Stable monomeric phosphaplatins, namely, (pyrophosphato)platinum(II) or platinum(IV) complexes containing a cis-cyclohexanediamine ligand or enantiomerically enriched or enantiopure trans-cyclohexanediamine ligands, and synthesis of these complexes, are provided. Efficacies and toxicities of the phosphaplatin compounds are determined toward a variety of cancers, including sensitive and resistant ovarian cancers, head and neck, and colon cancers. Compositions comprising the platinum complexes, and methods for treatment of proliferative diseases or disorders by means of the complexes or the compositions comprising them are disclosed.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering modified inositol hexaphosphate (IHP) comprising an internal pyrophosphate ring to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The present invention relates to a novel crystal form of calcium 3-acetylaminopropane-1-sulfonate, to a process for the preparation thereof, and to the use thereof in medicaments.

Abstract: The present invention provides a method of reducing phytotoxicity or plant injury at a crop plant locus caused by a herbicide application at the locus which method includes applying to the crop plant locus a chloronicotinyl insecticide before the herbicide application.

Abstract: The present invention relates to various salts of inositol tripyrophosphate including the calcium, lithium, beryllium, magnesium, potassium, strontium, barium, rubidium and cesium salts of inositol tripyrophosphate, compositions comprising these salts, methods of making the various salts, and methods of use of the above salts. Methods of use include administering the above salts in an effective amount in individuals for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis.

Abstract: Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate for the treatment of various types of cancers, Alzheimer's disease, stroke and osteoporosis.

Abstract: The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: Inositol-tripyrophosphate is an allosteric effector of hemoglobin due to its ability to cross the plasma membrane of red blood cells and deliver oxygen to solid tumors, by lowering the oxygen affinity of the hemoglobin of red blood cells. The present invention is directed to the use of inositol-tripyrophosphate to reduce hemoglobin's affinity for oxygen in circulating red blood cells. The present invention is further directed to the use of inositol-tripyrophosphate to inhibit angiogenesis and enhance radiation sensitivity of hypoxic tumors. The present invention is further directed to the use of inositol-tripyrophosphate to enhance PO2 in hypoxic tumors.

Abstract: The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.

Abstract: The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: The present invention provides phosphaplatins, stable isolated monomeric phosphato complexes of platinum (II) and (IV), and methods of use thereof for treating cancers, including cisplatin- and carboplatin-resistant cancers. Unlike cisplatin, these complexes do not readily undergo hydrolysis and are quite soluble and stable in aqueous solutions. Moreover, these complexes—unlike cisplatin, carboplatin, and related platinum-based anti-cancer agents—do not bind DNA. Rather, data suggests that phosphaplatins trigger overexpression of fas and fas-related transcription factors and some proapoptotic genes such as Bak and Bax. Nevertheless, the complexes exhibit tremendous cytotoxicity towards cancer cells. Thus, the present invention provides novel platinum anticancer agents that have a different molecular target than those in the art.

Abstract: A method for treating inflammatory diseases through an anti-inflammatory type activation of monocytes, the method includes the administration to a patient in need thereof of an effective quantity of at least one dendrimer with mono- or biphosphonic terminations.

Abstract: Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: or a pharmaceutically acceptable salt thereof, wherein R1 is structure (a), (b), (c) or (d): and Ra, Rb, Rc, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.

Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variabables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to mixed calcium/sodium salt of inositol tripyrophosphate, methods of preparing and methods of use. The mixed calcium/sodium salt may be a monocalcium tetrasodium salt of inositol tripyrophosphate. Methods of use include administering the above salts in an effective amount to treat diseases caused by hypoxia or other conditions associated with inadequate function of the lungs or circulatory system, such as various types of cancer and Alzheimer's disease.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

Abstract: Cyclic glycerophosphates and analogs thereof (CGs) are shown to exert neutral promoting activities in target cells. Such activities include promotion of neuronal outgrowth, promotion of nerve growth, provision of dopaminotrophic supporting envrionment in a diseased portion of the brain, prevention of nerve degeneration and nerve rescue. These activities of the CGs render them useful for treatment of various disorders including but not limited to mental disorders such as, for example, schizophrenia, dementia or disorders resulting in learning disablities. In addition, these CGs may be used for the treatment of neurodegenerative conditions such as Altzheimer's diesease, Parkinson's disease, conditions resulting from exposure to harmful environmental factors or resulting from a mechanical injury. The CGs may also be used to treat an individual suffering from a primary neurodengenerative condition in order to prevent or reduce the appearance of secondary degeneration in additional nerves (“nerve rescue”).

Abstract: Cyclic glycerophosphates as well as some analogs thereof (CGs) are shown to increase phosphorylation of intracellular proteins in various cells. Such activity is not found with linear ? or ? glycerophosphates. The phosphorylating activity of the CGs render them useful in the prevention and treatment of various disorders and diseases such as, for example, different kinds of malignancies as well as disorders involving hormone and hormone-like signaling. The CGs are also useful for promotion of target cell differentiation and for detection of abnormal conditions in target cells.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: This invention is directed to pharmaceutical compositions and methods for treating demyelinating disorders based upon inhibitors of the interaction of glutamate with the AMPA and of the interaction of glutamate with the kainate receptor complex.

Abstract: Compounds which are &agr;-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

Abstract: Novel compounds according to formula I 1

Abstract: Compounds which are &agr;-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin-like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

Abstract: The invention discloses compositions, combination therapies and methods of treating B-cell lymphomas and leukemias, as well as other CD40+ malignancies. The primary active agent of the composition is an anti-CD40L antibody or other CD40L antagonist that inhibits CD40-CD40L interaction. Compositions may additionally contain or utilize any one or more of the following in combination for the treatment of said disease: anti-CD20 antibodies, chemotherapeutic agents, chemotherapy cocktails, and radiotherapy.

Abstract: This invention provides a method of treating a tumor in a warm-blooded animal, including humans, by administering, in combination, an anti-tumor effective amount of tegafur, uracil, folinic acid or pharmaceutically acceptable salt thereof and cyclophosphamide.

Abstract: Glucocorticoid blockers, including glucocorticoid receptor antagonists, are effective to prevent glucocorticoid-induced decrease in permeability of the blood-brain barrier and to increase the permeability of the blood-brain barrier. Administration of glucocorticoid blockers, including glucocorticoid receptor antagonists, concomitant with administration of drugs for treating diseases of the central nervous system increases delivery of such drugs into the central nervous system.

Abstract: Administration of antisense oligodeoxynucleotides (ODN) targeted against the testosterone-repressed prostate message-2 (TRPM-2) gene can reduce the amount of TRPM-2 in renal cell cancer (RCC) cells and other cancer cells, and as a result enhance chemosensitivity of these cells to chemotherapy agents and radiation. Thus, for example, the sensitivity of renal cell cancer cells to a chemotherapeutic agent can be increased by exposing renal cell cancer cells to a chemotherapeutic agent and an agent which reduces the amount of TRPM-2 in the renal cell cancer cells. This provides an improved method for treatment of renal cell cancer, which is generally resistant to treatment with known chemotherapy agents.

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: Disclosed herein are therapeutic treatment protocols designed for the treatment of B cell lymphoma. These protocols are based upon therapeutic strategies which include the use of administration of immunologically active mouse/human chimeric anti-CD20 antibodies, radiolabeled anti-CD20 antibodies, and cooperative strategies comprising the use of chimeric anti-CD20 antibodies and radiolabeled anti-CD20 antibodies.

Abstract: The present invention relates to methods of treatment useful in chronic diseases, by means of the rupture of tolerance to self-antigens and increasing autoimmune response against these antigens. More particularly, the present invention relates to methods useful in the treatment of tumors that are growth dependent on the Epidermal Growth Factor, including non-small cell lung carcinoma.

Abstract: Compounds of the structure I: 1

Abstract: The present invention provides, in one embodiment, methods to treat, prevent the progression of, or facilitate elimination of a malignancy by increasing the supply of red blood cells using erythropoietin in conjunction with administration of an anti-tumor agent.

Abstract: The invention relates generally to the field of immunology, in particular, to bispecific antibodies. Methods for designing a bispecific antibody for use in treating diseases relating to the immune system are disclosed. Specific examples relate to bispecific antibodies which recognize an activating receptor and an inhibiting receptor.

Abstract: The present application discloses a method of treating alopecia which is based on the use of a tellurium compound such as ammonium trichloro(dioxoethylene-O,O-tellurate).

Abstract: The present invention relates to therapeutic associations for the treatment of cancer, comprising an effective amount of a camptothecin, or a camptothecin derivative, with an effective amount of an alkylating agent, such as melphalan, dacarbazine, or cyclophosphamide, and methods of using such therapeutic associations.

Abstract: The present invention is directed to compositions containing hapten-modified tumor cells and extracts and methods of treating cancer by administering a therapeutically effective amount of a composition containing a tumor cell or tumor cell extract to a subject in need of such treatment. The tumor cells and extracts of the invention and compositions thereof are capable of eliciting T lymphocytes that have a property of infiltrating a mammalian tumor, eliciting an inflammatory immune response to a mammalian tumor, eliciting a delayed-type hypersensitivity response to a mammalian tumor and/or stimulating T lymphocytes in vitro. The invention also relates to an effective vaccination schedule useful for inducing an antitumor response in a mammalian patient suffering from cancer by inducing at least one of the following: tumor necrosis, tumor regression, tumor inflammation, tumor infiltration by activated T lymphocytes, delayed-type hypersensitivity response, and prolongation of patient survival.

Abstract: The present invention is directed to compounds of the formula 1

Abstract: A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro,

Abstract: A pharmaceutical product comprising a nucleoside analogue active against herpes simplex virus, such as acyclovir/valaciclovir or penciclorivir/famciclovir, and an immunosuppressant, as a combined preparation for simultaneous, separate or sequential use in the treatment and/or prevention of herpes simplex virus infections.