Abstract: The invention relates to therapeutic agents for use in the prevention or treatment of Alzheimer's disease. In particular the invention relates to use of inhibitors of cell cycle reentry and progression to the G1/S transition or inhibitors of progression of the cell cycle through the G1/S transition point in the prevention or treatment of Alzheimer's disease.

Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.

Abstract: The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Another aspect of the subject invention concerns compositions formulated for administration as an enema. The subject invention also concerns compositions formulated for oral administration. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient. In another embodiment, compounds or compositions are orally administered.

Abstract: The invention provides a topical formulation adapted for treatment of a skin condition comprising (i) at least one retinoid; and (ii) salicylic acid or an ester, amide, salt, or solvate thereof. The invention also includes a kit for treatment of skin conditions comprising a retinoid and salicylic acid, as well as a method of treating skin conditions utilizing the inventive formulation and kit.

Abstract: The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.

Abstract: Compositions and methods for anti-thrombotic and antiplatelet therapy in a subject are provided. Administration of an MAO-B inhibitor results in reduced platelet aggregation or reversion of platelet aggregation. Methods of administering an MAO-B inhibitor with at least one antiplatelet agent are also disclosed. Such combination therapies result in an additional protective effect, and in some instances a synergistic effect. The compositions and methods of the present invention are useful for treating and preventing recurrence of several cardiovascular, cerebrovascular and peripheral vascular diseases and injuries, and may be applied to subjects displaying traditional drug resistances.

Abstract: Substantially optically pure (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, or a salt thereof, or a solvate thereof, which has actions of reducing amount of PCSK9 protein and increasing amount of LDL receptor.

Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.

Abstract: Provided herein are biomarkers for hepatocellular carcinoma and uses thereof.

Abstract: This invention relates to a composition containing quercetin, vitamin B3, vitamin C, and folic acid. Also disclosed is a method of using the composition for enhancing physical or mental performance or treating various diseases or disorders.

Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.

Abstract: Methods for treating a disease condition in a subject are provided. The subject methods are characterizing by enhancing at least one symptom of the disease condition in a manner effective to cause the subject to mount a compensatory response effective to treat the disease condition. Also provided are compositions, kits and systems for practicing the subject methods.

Abstract: The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are also disclosed.

Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.

Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.

Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.

Abstract: Aspects of the invention pertain to chemical compounds, therapeutic compositions, and methods for treating neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau.

Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.

Abstract: This invention relates to enhancing sensitivity of cytotoxic drugs by targeting their interfering mechanisms induced in the tumor microenvironment which lead to drug resistance, using combinatorial therapy with carboxyamidotriazole orotate. Specific doses of cytotoxic drugs are titrated with carboxyamidotriazole orotate to improve the sensitivity and anticancer activity of cytotoxic drugs.

Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.

Abstract: The present invention relates to beta-O/S/N fatty acids and derivatives thereof, in particular the compounds of formula (I) as described and defined herein, and their pharmaceutical use, including their use in the treatment or prevention of bacterial as well as protozoan infections, in particular the treatment or prevention of infections with Gram-positive and/or Gram-negative bacteria and infectious diseases caused by and/or related to Gram-positive and/or Gram-negative bacteria. The invention further relates to the use of these compounds for preventing or eliminating biofilms.

Abstract: In one embodiment, provided is a composition including a prostaglandin compound for modulating stem cell proliferation and/or differentiation in a mammalian subject. In another embodiment, the instant application is directed to a composition which includes a prostaglandin compound for modulating proliferation and/or differentiation of stem cells of a mammalian subject, in which the stem cells are contacted directly or indirectly with the composition of the invention.

Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.

Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: Methods to synthesize self-assembling peptides embedded with complex organic electronic subunits are provided.

Abstract: The disclosure herein relates to nuclear hormone receptors including steroid hormone receptors, for example in connection with estrogen, progesterone, and androgen. Embodiments of compositions and methods are disclosed including such relating to compounds, including substituted theophyllines, capable of functioning as inhibitors of estrogen receptor alpha-mediated gene expression and having the ability to modify cancer cells and treat cancer, including breast cancers and resistant breast cancers, particularly those that are resistant to tamoxifen. In embodiments, methods of inhibiting breast cancer cells and resistant breast cancer cells are provided. In embodiments, a useful inhibitor compound includes TPSF/NSC 97998 and other compounds.

Abstract: The invention provides 19-substituted geldanamycin derivatives, and pharmaceutically acceptable salts thereof that are potent Hsp90 binding agents useful for the treatment of, and/or the amelioration of symptoms of, cancer or neurodegenerative disorders.

Abstract: Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.

Abstract: The invention provides a topical formulation adapted for treatment of a skin condition comprising (i) at least one retinoid; and (ii) salicylic acid or an ester, amide, salt, or solvate thereof. The invention also includes a kit for treatment of skin conditions comprising a retinoid and salicylic acid, as well as a method of treating skin conditions utilizing the inventive formulation and kit.

Abstract: The invention relates to compounds and methods for the prevention and/or treatment of infection after stroke.

Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.

Abstract: The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.

Abstract: This invention is a prosthetic device generally placed on the outside surface of the vessel or graft which then elutes antiproliferative drugs or agents from a drug-eluting matrix material. Methods of perivascular antiproliferative drug administration also are disclosed.

Abstract: In one aspect provided herein are methods of determining a triple negative breast cancer (TNBC) subtype in an individual in need thereof comprising determining expression of one or more genes in one or more TNBC cells of the individual; and comparing the expression of the one or more genes in the TNBC cells with the expression of the one or more genes in a control. In another aspect, the methods are directed to methods of determining a treatment protocol for the TNBC patient based on the TNBC subtype. In another aspect, the methods are directed to predicting whether an individual will benefit from a treatment for a particular TNBC subtype. In yet another aspect, the invention is directed to a method of determining whether an agent can be used to treat a TNBC subtype.

Abstract: Disclosed is a composition for reducing the exudation of the serum proteins. More specifically the composition of the present invention relates to a composition capable of improving conditions such as atopic dermatitis, atopic eczema, skin pruritus, atopic nasitis, atopic erythema or erythroderma, contact dermatitis, asthma, chronic obstructive pulmonary disease, etc. by reducing the exudation of the serum proteins in skin and mucosa.

Abstract: A pKa buffered vitamin C composition which includes a base alkalizer composition mixed with vitamin C (calcium ascorbate or ascorbic acid). The base alkalizer composition can be approximately 24% to 40% and the ascorbic acid or calcium ascorbate can be approximately 76% to 60% by weight of the vitamin C composition. When this vitamin C composition is orally administered to an individual (in capsule or tablet form), a rapid neutralization of his stomach acid occurs followed by a sustained pH of 6.0 to 7.5 for a thirty minute to two hour period. This allows the ingredients to be absorbed in his stomach, while preventing unpleasant reactions in his stomach. The base alkalizer composition can include the combination of a calcium carbonate carrier which acts as a mild alkalizer, an hydroxide (magnesium or potassium) which acts as a fast alkalizer, and a phosphate (dicalcium or tricalcium) which acts as a moderate alkalizer and which also maintains the pH fairly stable over a twenty to forty minute time period.

Abstract: Use of an orally or nasally available formulation of Tretazicar for poisoning vermin. An orally available or nasally available formulation of Tretazicar, wherein in the orally available formulation the Tretazicar is protected from acid hydrolysis, and provided that the formulation is not solid Tretazicar in a gelatin capsule. A formulation of Tretazicar in which the Tretazicar is protected from acid hydrolysis, wherein the formulation is present in a liquid form. A combination of Tretazicar and bait. A method of poisoning vermin comprising making available to the vermin an orally or nasally available formulation of Tretazicar and allowing the vermin to ingest or inhale the formulation of Tretazicar.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: A steroid derivative compound of formula (I) in which: one of R1 and R2 is hydroxy and the other is hydrogen; or R1 and R2 together represent oxo; R3 is hydrogen or hydroxy; and the dotted lines represent single or double carbon-carbon bonds; and pharmaceutically acceptable salts and esters thereof are useful for the prevention or treatment of pain, for improving nerve regeneration after nerve injury or damage or disease, for the prevention or treatment of brain injury, damage or disease and for neuroprotection. Particularly useful compounds are 11-hydroxy-?4-androstene-3,17-dione and 11-oxo-?4-androstene-3,17-dione or their derivatives.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.

Abstract: Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA-PACA2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed.

Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: Provided herein include compositions, all related stereoisomers as well as pharmaceutically acceptable salts provided as simplified analogs of pateamine A, in which the analogs generally are devoid of the C3-amino and C5-methyl groups, also referred to as desmethyl, desamino-pateamine A. Suitable analogs provide anticancer and antiproliferative effects in vivo and in vitro by a novel drugs mechanism of action described herein for pateamine A, including inhibition of eIF4A-dependent translation initiation. As with pateamine A, as described herein, suitable analogs cause cell cycle arrest or induce apoptosis in transformed cells. However, toxicity of such compounds to slow growing normal cells is low. In addition, such analogs, like pateamine A, target translation initiation factors and are useful as anticancer and antiproliferative agents in subjects in need thereof.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.

Abstract: A method for inhibiting tumor cell migration or metastasis of a cancer in a mammalian subject comprises one or more of the steps of administering to a subject a therapeutically effective amount of a composition comprising a molecule that: suppresses focal adhesion kinase (FAK) activity or phosphorylation; suppresses ULK1 kinase activity; suppresses activation or signaling of the mTORC1 (Ser757) pathway; activates AMPK; activates FIP200; or activates LKB1, in a cancer cell. Still another method of inhibiting tumor cell migration involves inhibiting phosphorylation of ULK1 on Ser757 in subjects with lung cancer. Suppressing activation or signaling of the mTORC1 (Ser757) pathway in subjects is in one aspect useful in treating lung cancer.