Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.

Abstract: The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a Fc?RI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a Fc?RI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient.

Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.

Abstract: Disclosed is a salt prepared from the STAT3 inhibitor known as 2-hydroxy-4-[[2-[[(4-methylphenyl)sulfonyl]oxy]acetyl]amino] benzoic acid and 2-amino-2-(hydroxymethyl)-1,3-propanediol. The salt is soluble in water and stable for extended periods of time. Further provided are pharmaceutical compositions comprising the salt and methods of administering the salt to prevent and treat cancer, such as breast cancer.

Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: The present invention is that provided a synthesis method of a series of isothiazole oxime ether containing strobilurin derivatives IV. The present invention relates to 3,4-dichloroisothiazolyl oxime ether strobilurin derivatives, and their chemical structural formula is as shown by IV. The invention discloses the structural formula of the above compound, the synthesis method and the use as an insecticide, a fungicide, an anti-plant virus agent, and an agriculturally acceptable auxiliary or synergist and a commercial insecticide. The use of a fungicide, an anti-plant virus agent and an acaricide in combination for controlling agricultural, forestry, horticultural plant pests, diseases, virus diseases and preparation methods.

Abstract: The invention relates to compounds having formula (I) wherein A is selected from the group consisting of: a) optionally substituted (C1-C8) alkyl; b) optionally substituted (C3-C6) cycloalkyl; c) optionally substituted (C6-C14) aryl; d) optionally substituted (C6-C14) heteroaryl; e) C(O)—(C6-C14) aryl, in which group (C6-C14) aryl is optionally substituted; f) C(O)—(C6-C14) heteroaryl, in which group (C6-C14) heteroaryl is optionally substituted; g) CH(OH)—(C6-C14) aryl, in which group (C6-C14) aryl is optionally substituted; and h) CH(OH)—(C6-C14) heteroaryl, in which group (C6-C14) heteroaryl is optionally substituted. The invention also relates to methods for the production of said compounds, to pharmaceutical and veterinary compositions comprising said compounds and to the therapeutic uses thereof, such as for the prevention and/or treatment of dry eye syndrome, vaginal dryness and/or burning mouth syndrome.

Abstract: A method is described for the prophylaxis or treatment of hypertension in a cat in need of such treatment. The method includes administration of a therapeutically effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to the cat, where the therapeutically effective amount of the sartan is administered in a daily dosage amount that is varied over a treatment period, the daily dosage amount of the sartan for a first period of time during the treatment period is 1.0 to 5.0 mg/kg of body weight, and the daily dosage amount of the sartan is decreased for a second period of time subsequent the first period of time during the treatment period.

Abstract: The disclosure provides monoamine neurotransmitter releaser and/or monoamine uptake inhibitor compounds having biogenic amine transporter activity but lacking substantial activity at 5-HT2 receptor subtypes. The phenethylamine or vinylogous phenethylamine compounds of the disclosure are useful in treating diseases, conditions and/or disorders mediated by activity of one or more of the monoamine neurotransmitters.

Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.

Abstract: Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Abstract: Aspects of the present disclosure include methods of reducing the deleterious impact of a target gene in a cell, such as the deleterious activity of a mutant extended nucleotide repeat (NR) containing target gene in a cell, by contacting the cell with an effective amount of an enantiomeric tetrahydrocarbazolamine compound. The deleterious activity (e.g., toxicity and/or dis-functionality of products encoded thereby) of a mutant extended NR containing target gene may be reduced, e.g., by reducing (and in some instances differentially, including selectively, reducing) the production or activity of toxic expression products (e.g., RNA or protein) encoded by the target gene. Kits and compositions for practicing the subject methods are also provided.

Abstract: The present invention concerns pyridinium compounds, a synthesis method for their preparation, metal or metal alloy plating baths containing said pyridinium compounds and a method for use of said metal or metal alloy plating baths. The plating baths are particularly suitable for use in filling of recessed structures in the electronics and semiconductor industry including dual damascene applications.

Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: A compound and method of producing the compound of formula (I) that has high absorption in the short wavelength spectral region of visible light and is capable of being used for an organic electronic component.

Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed.

Abstract: The present invention provides methods and compositions for treating cancer, reducing side effects, and reducing postmenopausal symptoms comprising anordrin or analog thereof (such as anordrin) alone or in combination with at least one other agent selected from the group consisting of tamoxifen, raloxifene or functional equivalent thereof, and an aromatase inhibitor.

Abstract: Disclosed herein are antibacterial compounds, pharmaceutical compositions including the antibacterial compounds, and methods of treating bacterial infections using the compounds and compositions.

Abstract: This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.

Abstract: The invention provides novel antibacterial diamide compounds, pharmaceutical compositions comprising the compounds and methods for treating or preventing an infection in a subject using the compounds.