Abstract: Disclosed are methods of treating viral disorders via the administration of an inducing agent and an anti-viral agent. In one embodiment, the inducing agent and the anti-viral agent are administered for about five days, and the anti-viral agent is subsequently administered without the inducing agent for an additional period of about sixteen days for a total cycle of about 21 days.

Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).

Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Abstract: The present invention relates to nucleic acids and polypeptides encoded thereby, whose expression is modulated in brain microvascular endothelial cells undergoing early dynamic inflammation-induced changes in blood-brain bather functionality. Such polypeptides are referred to as lipopolysaccharide-sensitive (LPSS) polypeptides. These nucleic acids and polypeptides may be useful in methods for controlling blood-brain bather properties in mammals in need of such biological effects. This includes the diagnosis and treatment of disturbances in the blood-brain/retina barrier, brain (including the eye) disorders, as well as peripheral vascular disorders. Additionally, the invention relates to the use of anti-LPSS polypeptide antibodies or ligands as diagnostic probes, as blood-brain barrier targeting agents or as therapeutic agents as well as the use of ligands or modulators of expression, activation or bioactivity of LPSS polypeptides as diagnostic probes, therapeutic agents or drug delivery enhancers.

Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.

Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract: We provide a set of novel mutations in HIST3H3, AMT, GLDC and PEX7 genes which we have discovered as causative of some autism spectrum disorders and/or intellectual disability after analysis of families with more than one affected child and with consanguineous parents. Based on some of these mutations, we also provide novel treatment options for autism spectrum disorders and/or intellectual disability wherein the novel mutations have been diagnosed. The invention is based on the discovery that certain specific mutations, particularly when present in a homozygous, compound heterozygous, or trans heterozygous combinations, result in a phenotype of an autism spectrum disorder and/or intellectual disability. Some mutations also cause the disorder or disease as heterozygous mutation.

Abstract: Treatment of lymphangioleiomyomatosis with the MEK1/2 inhibitor CI-1040 delayed the development of primary tumors and blocked the estrogen-induced lung metastases in treated animals. Such treatment also reduced the number of circulating ELT3 cells and decreased their lung colonization after intravenous injection.

Abstract: The invention provides for methods of treating a disease using HDAC6 inhibitors that modulate the extracellular level of a subset of cytokines. The invention also provides for compositions for treating a disease associated with a modulation in the extracellular level of a subset of cytokines.

Abstract: Disclosed are a composition and a method for treating skin disorders, including rosacea, pityriasis rosea, erythema, rhinophyma, and rosacea-associated disorders including pimples, papules, pustules, and telangiectasia.

Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.

Abstract: Hybrid molecules comprising a retinoic acid receptor agonist moiety and a histone deacetylase inhibitor (HDAC) moiety are disclosed. Hybrid molecule 3 (6-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)naphthalene-2-hydroxamic acid) was proven to posses HDAC activity while maintaining RAR agonist activity. Hybrid molecule 3 and pharmaceutical compositions thereof can be used in the treatment of breast cancer, leukemia, non-small cell lung cancer, colon cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and cancer of the CNS.

Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.

Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).

Abstract: The invention relates to compositions and methods for treating cancer comprising administering to a subject in need a pharmaceutically effective dose of a cancer stem cell inhibitor, methods of inhibiting the growth of cancer stem cells or tumor initiating cell comprising administering to a subject in need a pharmaceutically effective dose of a cancer stem cell inhibitor, and methods of enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells comprising administering to a subject in need a pharmaceutically effective dose of a chemotherapeutic drug and a pharmaceutically effective dose of a cancer stem cell inhibitor.

Abstract: The invention relates to the cancer antigen PRAME (PReferentially expressed Antigen in MElanoma) and its use in a method of treatment of a tumour which comprises administering to a subject in need of treatment an effective amount of an inhibitor of PRAME, in combination with a second agent selected from the group of an inhibitor of HDAC (an HDACi) and a retinoid.

Abstract: The present application refers to methods for cancer diagnosis and treatment, particularly in types of cancers associated with aberrant CpG methylation of the miR-34a promoter.

Abstract: An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula).

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

Abstract: The present application describes organic compounds of a general formula: and salts, and isomers thereof, wherein R, R2 and R3 are defined in the specification. The compounds are useful for treating a gram-negative bacterial infection.

Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.

Abstract: A first aspect of the invention relates to a combination comprising 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof. A second aspect relates to a pharmaceutical product comprising (i) 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and (ii) a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy.

Abstract: Described herein is the use of ribonucleotide reductase inhibitors in the prevention or treatment of restenosis and other vascular proliferative disorders.

Abstract: The invention relates to compositions and methods of treatment using an iron chelator, an antioxidant, estrogen, and/or combinations thereof, optionally, linked to a nanoparticle, to treat a subject in need thereof. The compositions and methods may be used to restore or protect the normal functions of osteoblast and osteoclast by depleting iron and inhibiting oxidative damage. The compositions and methods may also be used to increase the bone formation rate in a subject.

Abstract: A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed.

Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.

Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.

Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.

Abstract: Zn2+-chelating motif-tethered fatty acids as histone deacetylase (HDAC) inhibitors. Compounds performed well in in vitro and in vivo tests.

Abstract: Methods and systems for treating an infarct by delivery of zinc chelator to modulate tissue.

Abstract: The present invention is directed to a method of treating cancer, particularly canine hemangiosarcoma. The method includes the continuous and regular administration of a formulation including a histone deacetylase inhibitor as part of the standard canine diet. The preferred histone deacetylase inhibitor is SAHA. The formulation is administered following splenectomy to prevent tumor recurrence.

Abstract: This invention provides methods for treating a subject afflicted with cancer, comprising concurrently administering (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide. This invention also provides methods for inducing the death of a transformed cell such as a cancer cell, comprising concurrently contacting the cell with (i) an HDAC 6-selective inhibitor and (ii) a suitable cytotoxic agent such as SAHA, doxorubicin or etoposide.

Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.

Abstract: The invention provides methods for treatment of acute coronary syndrome and prediction of adverse cardiac events on the basis of elevations of catalytic iron in biological fluid of a human subject. An embodiment of the invention provides a method for early detection of acute coronary syndrome (ACS) in a human subject at the time of presentation of the chest pain. The method includes analyzing a test sample of the biological fluid for amount of catalytic iron and detecting acute coronary syndrome in the human subject.

Abstract: Herein is described the use of a collection of 50 breast cancer cell lines to match responses to 77 conventional and experimental therapeutic agents with transcriptional, proteomic and genomic subtypes found in primary tumors. Almost all compounds produced strong differential responses across the cell lines produced responses that were associated with transcriptional and proteomic subtypes and produced responses that were associated with recurrent genome copy number abnormalities. These associations can now be incorporated into clinical trials that test subtype markers and clinical responses simultaneously.

Abstract: The present invention relates to a protein, ADAM10, ADAM10 nucleic acid sequences and ADAM10 proteins encoded by these sequences that are involved in infection by one or more pathogen such as a virus, a parasite, a bacteria or a fungus or are otherwise associated with the life cycle of a pathogen.

Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.

Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.

Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

Abstract: Method of treating a tumor in a patient in need thereof by administering to the patient an effective amount of 4-[6-(diethylaminomethyl)naphth-2-ylmethyloxycarbamoyl]benzohydrozamic acid.

Abstract: Method for treating Philadelphia-negative myeloproliferative syndromes in a patient in need of such treatment, by administering to the patient diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride or other pharmaceutically acceptable salts and/or solvates thereof, in combination with N-hydroxyurea.

Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.

Abstract: A method for treating or ameliorating mucocutaneous, ocular toxicities, or side effects induced by blocking cellular growth and survival signal transduction pathways. The method comprises administering to a subject in need thereof an effective amount of a histone deacetylase inhibitor and a pharmaceutically acceptable carrier, salt or solvate thereof, wherein the cell growth and survival signal transduction pathways are blocked by an antibody targeted therapy agent, antibody fragment, targeted small-molecule chemical compound, low-molecular-weight tyrosine kinase inhibitor, peptide mimetic, anti-sense oligonucleotide (DNA and/or RNA), or ribozyme.

Abstract: The invention features compositions and methods for characterizing the methylation status of the Vitamin D Receptor (VDR) in neoplasia (e.g., breast carcinoma), selecting an appropriate therapy, and treating the neoplasia (e.g., breast carcinoma).

Abstract: Pharmaceutical compositions comprised of low-solubility and/or acid-sensitive drugs and neutralized acidic polymers are disclosed.