Abstract: A therapeutic process is provided for the inhibition of NF-?B in mammals in whose cells NF-?B has been activated by an agency external to said cell.

Abstract: The present invention relates to a composition comprising an organic preservative acid and a UV-active indicator substance for preserving wood and for detection of the sufficient preservation of wood.

Abstract: Selected compounds of formula (I) are antibacterial agents: formula (I) wherein R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl (C1-C6 alkyl)- or aryl (C1-C6 alkyl)-group, and A represents a group of formula (IA), or (IB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 are each independently hydrogen or C1-C6 alkyl, heterocyclic or aryl (C1-C6 alkyl)-, R5 and R6 when taken together with the nitrogen atom to which they are attached from an optionally substituted saturated heterocyclic ring of 3 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: The invention provides methods and compositions relating to Kuz involvement in angiogenesis.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: A method of increasing the uptake of an adenoviral agent by a cell, which method comprises contacting the cell with a histone deacetylase inhibitor in an amount sufficient to increase the expression of coxsackie-adenovirus receptors and/or &agr;v integrins on the surface of the cell and subsequently containing the cell with the adenoviral agent, whereupon the uptake of the adenoviral agent by the cell is increased relative to an otherwise identical cell that has not been contacted with a histone deacetylase inhibitor; and a method or preferentially increasing the uptake or an adenoviral agent by a cancerous cell over a normal cell, which method comprises contacting a collection of cells comprising normal cells and a cancerous cell with a histone deacetylase inhibitor i an amount sufficient to increase preferentially the expression of CAR and/or &agr;, integrin on the surface of the cancerous cell over the normal cells and subsequently contacting the collection of cells with the adenoviral agent, whereupon the

Abstract: The invention concerns the use of ketol-acid reductoisomerase inhibitors for treating fungal diseases affecting crops. The invention concerns methods for treating crops against fungal diseases comprising applying a ketol-acid reductoisomerase inhibitor. The invention also concerns methods for identifying novel fungicidal compounds comprising a step which consists in identifying ketol-acid reductoisomerase inhibitors.

Abstract: The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: The present invention relates to compounds that are capable of modulating CD154 mobilization and that are useful for stabilizing the thrombotic process and reducing the activation of cells involved in an inflammatory response. The present invention also relates to methods useful for identifying such compounds. The present invention also relates to the treatment of platelets for transfusion with metalloproteinase inhibitors to treat or prevent inflammation. The present invention also includes compositions and methods to treat injury and disease related to such biological processes.

Abstract: The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAM-mediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant 1 and ADAM15 variant 2, now identified and isolated.

Abstract: A therapeutic and/or prophylactic drug for cardiac failure and cardiac hypertrophy, comprising a derivative of hydroxamic acid, which is represented by the formula (I) 1

Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.

Abstract: Method of inhibiting or treating Human Immunodeficiency Virus (HIV) infection, comprising administering to a patient in need thereof an effective amount of a pharmaceutically acceptable composition comprising a PEG-ASNase compound or asparaginase, and optionally at least one compound selected from the group consisting of protease inhibitor compounds, ribonucleotide reductase inhibitor compounds and HIV reverse transcriptase inhibitor compounds.

Abstract: Compounds of the formula: 1

Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.

Abstract: Hydroxamic acid derivatives of the formula (I) 1

Abstract: Compounds of formula I 1

Abstract: The present invention provides HDAC inhibitors for use in inhibiting proliferation and/or migration of smooth muscle cells. The present invention further provides medical devices coated with the HDAC inhibitors. The present invention also provides use of the medical devices in methods for inhibiting proliferation and/or migration of smooth muscle cells. Additionally, the present invention provides methods for inhibiting proliferation and/or migration of non-neoplastic smooth muscle cells. Finally, the present invention provides methods for preventing or treating restenosis after angioplasty or stent implantation in a subject.

Abstract: Compounds of a histone deacetylase inhibitor. The compounds are capable of simultaneously stimulating epithelium regrowth, inhibiting cutaneous fibroblast proliferation, decreasing collagen deposit, suppressing fibrogenic growth factor and subsiding inflammatory cytokine, and are useful inhibiting the main features of radiation cutaneous syndrome. Results include a decrease in skin swelling, promotion of epithelium healing, and prevention of cutaneous fibrosis, ulceration and necrosis. The present invention provides methods of treating, preventing or ameliorating radiation-induced skin damage by administering a therapeutically effective amount of a histone deacetylase inhibitor.

Abstract: Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administering to a patient suffering from the disease a therapeutically effective amount of a DNA methylation inhibitor such as a cysteine analog such as decitabine, in combination with an effective amount of histone deacetylase inhibitor such as hydroxamic acid, cyclic peptide, benzamide, butyrate, and depudecin.

Abstract: The present invention provides a method for treating elevated serum triglycerides or hypertension via administering to a human subject with elevated serum triglycerides or hypertension an effective amount of pharmaceutical composition comprising a 5-lipoxygenase inhibitor, in an effective amount which is sufficient to reduce elevated serum triglycerides or hypertension, wherein the 5-lipoxygenase inhibitor is not NDGA or curcumin.

Abstract: A therapeutic and/or prophylactic drug for osteoarthritis, comprising a derivative of hydroxamic acid, which is represented by the formula (I) 1

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula(l) wherein: A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is an amide linkage selected from: —NR1C(═O)— and —C(═O)NR1—; R1 is an amido substituent; X is an ether heteroatom, and is —O— or —S—; and, R2 and R3 are each independently an ether group; and pharmaceutically acceptable salts, solvates, amides, esters, ether chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: Compositions and devices including collagen and a metalloprotease inhibitor, and methods of making and using same.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class II HDACs, which are known to participate in regulation of chromatin structure and gene expression, have been shown to have beneficial effects on cardiac hypertrophy. Surprisingly, the present invention demonstrates that HDAC inhibitors inhibit cardiac hypertrophy by inhibiting fetal cardiac gene expression and interfering with sarcomeric organization.

Abstract: Compounds of formula I are disclosed wherein R4 is an ester or thioester group, and R, R1, R2, and R3 are as defined in the specification are inhibitors of rapidly dividing tumor cells.

Abstract: An insecticide of formula 1 1

Abstract: Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.

Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity.

Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.

Abstract: The use of derivatives of hydroxamic acid having histone deacetylase enzyme-inhibiting activity for the preparation of anti-inflammatory medicaments is disclosed.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.

Abstract: Hydroxamic acid derivatives of the formula (I) (wherein all the symbols have the same meaning as defined in the specification.), non-toxic salt thereof or prodrugs thereof. The compounds of the formula (I) inhibit producing IL-6, so it may be used for the prevention and/or treatment of various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell carcinoma, Kaposi's sarcoma, rheumatoid arthritis, hypergammaglobulinemia, Castleman's disease, atrial myxoma, diabetes mellitus, autoimmune diseases, hepatitis, colitis, graft versus host disease, infectious diseases and endometriosis.

Abstract: The invention relates to a novel method for treating a variety of diseases and disorders, including polyglutamine expansion diseases such as Huntington's disease, neurological degeneration, psychiatric disorders, and protein aggregation disorders and diseases, comprising administering to patients in need thereof of a therapeutically effective amount of one or more deacetylase inhibitors. The invention is also directed to a transgenic fly useful as a model of polyglutamine expansion diseases, which may be used to test potential therapeutic agents.

Abstract: Sexual wellness or sexual fitness is enhanced over time by administrating on a daily basis a source of proanthocyanidins and a source of arginine. Both sources may be blended into a composition or taken separately from a kit. The source of arginine may be a salt or peptide of L-arginine and aspartic acid such as arginine aspartate. The proanthocyanidins stimulate an endothelial NO-synthase enzyme, which serves as a catalyst for synthesis of the nitric oxide from a substration that is the source of the arginine. A sufficient amount of the nitric oxide is released over time to enhance sexual wellness or sexual fitness. In case of low levels of androgenic hormones in both sexes, the combination may contain as a further ingredient a sex hormone or a sex hormone precursor or a sex hormone stimulant or a sex hormone bioavailability enhancer.

Abstract: Described is the use of histone deacetylase inhibitors for the treatment of a disease, preferably cervical cancer, associated with an HPV infection. Particularly useful inhibitors are sodium butyrate, phenylbutyrate and trichostatin A.

Abstract: The present invention relates to methods of treating cancers, e.g., leukemia. More specifically, the present invention relates to methods of treating acute and chronic leukemias including Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Chronic Lymphocytic leukemia (CLL), Chronic myeloid leukemia (CML) and Hairy Cell Leukemia, by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

Abstract: Disclosed herein are novel approaches to thyroid cancer therapy. These approaches include methods to enhance thyroid specific gene expression, for example methods to enhance expression of thyroglobulin and/or the Na+/I− symporter in thyroid cancer cells. Enhanced expression of thyroid-specific genes promotes cellular differentiation and reduces biologically aggressive behavior such as invasion and metastasis. In addition, enhanced expression of thyroglobulin and/or the Na+/I31 symporter increases the ability of thyroid cancer cells to concentrate iodine or iodide, thereby making the cells more susceptible to radioactive iodine therapy. Also disclosed herein are methods for detecting thyroid neoplasms in a subject, by administering a therapeutically effective amount of a histone deacetylase inhibitor, administering a detectable agent whose uptake or concentration in thyroid cells is increased by administration of the histone deacetylase inhibitor, and detecting the detectable agent.

Abstract: The use of an MMP inhibitor, especially a collagenase inhibitor, in the manufacture of a medicament for the treatment of a natural or artificial tissue comprising extracellular matrix components to inhibit contraction of the tissue and methods for the treatment of tissue comprising extracellular matrix components to inhibit contraction.

Abstract: The present invention provides methods of treating cancer using inhibitors of inosine monophosphate dehydrogenase (IMPDH). The IMPDH inhibitors are combined with compounds that inhibit cellular processes regulated by GTP or ATP. Also provided are prodrugs of the IMPDH inhibitor mizoribine and its aglycone. The prodrugs are useful in practicing the methods of the invention, including immunosuppressive therapy and treatment of cancer by prolonged administration without additional therapeutic compounds.

Abstract: The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.