Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Abstract: A treatment pack comprising: (a) multiple doses of a composition containing dipyridamole as an active ingredient; (b) packaging material; and (c) instructions for topical administration of said composition to the anterior segment of the eye to treat an anterior segment eye disorder.

Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1?,2-dihydroxy-1,2?-binaphthalen-4?-yl)-4-methoxybenzenesulfonamide.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.

Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.

Abstract: The invention is directed to topical formulations and methods of treating a migraines and/or cluster headaches, muscle sprains, muscle spasms, spasticity, tension headaches, tension related migraines and related conditions associated with muscle tension and pain with a therapeutically effective amount of an ergot alkaloid, skeletal muscle relaxant, serotonin agonist, combinations thereof, pharmaceutically acceptable salt thereof, prodrugs thereof or derivative thereof.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder or a condition, or in the manufacturing of a medicament for the treatment of a disease, a disorder or a condition.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.

Abstract: An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided.

Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.

Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.

Abstract: [Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.

Abstract: Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures. One disclosed composition comprises ketoprofen and nifedipine in a liquid irrigation carrier, and includes a solubilizing agent, stabilizing agents and a buffering agent.

Abstract: A method for trapping and neutralizing or killing microorganisms on a surface includes: applying a low tack coating composition that comprises an antimicrobial agent onto an inanimate surface; in the coating, killing or neutralizing microorganisms encountered on the surface and encountered from the environment after the applying step is performed; forming a coating layer on the inanimate surface. The composition comprises a humectant and an antimicrobial, the antimicrobial including a monoquaternary ammonium compound or pharmaceutically acceptable salt thereof. The coating layer has antimicrobial cidal or static activity for at least about one hour. A low-tack antimicrobial composition is also included.

Abstract: The present invention relates to 3-[(1,3-thiazol-4-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Abstract: The present invention provides a solid dispersion of febuxostat, processes for its preparation, pharmaceutical compositions comprising it and its use for the chronic management of hyperuricemia in patients with gout.

Abstract: The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.

Abstract: Provided is a mirabegron-containing pharmaceutical composition in which the leakage of mirabegron can be inhibited when the pharmaceutical composition is dispersed in a liquid, and in which the change in pharmacokinetics caused by the presence or absence of food intake is decreased. The pharmaceutical composition comprises an acid addition salt of alkyl sulfuric acid and mirabegron, and a base for modified release.

Abstract: The present invention relates to solid forms of the N-methyl-D-glucamine (meglumine) salt of 6-carboxy-2-(3,5-dichlorophenyl)-benzoxazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions.

Abstract: Use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of acute exacerbations of chronic obstructive pulmonary disease. Treatment may involve a single dose of the active ingredient by oral administration.

Abstract: The present invention provides a stabilized controlled-release pharmaceutical composition comprising gliclazide and sodium citrate as stabilizing agent; and process for the preparation of said pharmaceutical composition.

Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: The present invention relates to uses and methods involving Panobinostat and HIV-1. In particular relates the present invention to Panobinostat for use in the treatment of HIV-1 and especially latent HIV-1. This is done using a low dosage of Panobinostat which is highly effective in depleting the HIV-1 reservoir.

Abstract: The use of a compound of general formula (I), where: R1, R2, R3, R4, R5 are identical or different and each represent a hydrogen atom, a halogen atom, a hydroxyl group or an —OR? radical in which R? is a straight or branched, saturated or unsaturated C1-C16 hydrocarbon radical, wherein at least one group from among R1, R2, R3, R4, and R5 does not represent a hydrogen atom or a halogen atom; X is a halogen atom, a hydroxyl group, a nitro group, a straight or branched, saturated or unsaturated optionally substituted C1-C14 hydrocarbon radical, or an —OR? radical in which R? is a straight or branched, saturated or unsaturated optionally substituted C1-C14 hydrocarbon radical; and Z is a covalent bond or a spacer arm, or of one of the salts thereof, in a cosmetic composition for stimulating the cellular anti-aging functions of the skin.

Abstract: The present disclosure relates to the use of pharmaceutical agents to manipulate serotonin in animal mammary glands. Use of the serotonin agents results in increased PTHrP levels, resulting in the release of calcium from the bone, which improves lactation.

Abstract: Embodiments herein provide a therapy for uterine leiomyomata (UL) in women using a fatty acid synthase (FAS) inhibitor. Additionally, an analysis method for evaluating the likelihood of women developing UL during their lifetime is provided.

Abstract: Compositions incorporating small interfering ribonucleic acid (siRNA) and certain lipid-conjugated polyamide compound-based delivery vehicles that are particularly useful in the delivery siRNA and other polynucleotides to cells. Also, methods of making and using the compositions.

Abstract: The invention provides a method of determining the prognosis of cancer in a subject. The method comprises (a) obtaining a sample from the subject, (b) analyzing the sample for the expression level of a carboxypeptidase E (CPE) splice variant, and (c) correlating the expression level in the sample with the prognosis of cancer in the subject. The invention further provides a method of diagnosing cancer, methods of treatment, kits for detecting mRNA expression of a CPE-?N, and inhibitors of CPE-?N and compositions thereof.

Abstract: The present disclosure is directed to nanoconjugates that cross the blood-brain barrier and methods of their therapeutic use.

Abstract: Disclosed herein are methods and kits useful for providing neuroprotection to neurons in the inner ear and to methods of treating inner ear diseases and disorders, including tinnitus and Mnire's disease.

Abstract: Disclosed herein are antisense compounds and methods for decreasing Factor VII and treating, preventing, or slowing progression of thromboembolic complications, hyperproliferative disorders, or inflammatory conditions in an individual in need thereof.

Abstract: There is provided a method of identifying candidate agents capable of modulating interaction between a first polypeptide and a second polypeptide, wherein the first polypeptide is ZO-2/TJP2 or a functional variant thereof and the second polypeptide is a Snail zinc finger transcription factor family member or a functional variant thereof.

Abstract: A method of determining the Crohn's disease status of a subject comprising the steps of determining the level of miR-29 in a sample from said subject; and comparing the level of miR-29 determined in step (a) with one or more reference values.

Abstract: The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Brain derived neurotrophic factor (BDNF), in particular, by targeting natural antisense polynucleotides of Brain derived neurotrophic factor (BDNF). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of BDNF.

Abstract: The disclosure provides compositions and methods for treating an ovarian cancer in a subject. More specifically, the disclosure provides microRNA (miRNA) inhibitor molecules that target to different miRNAs for treating different types of ovarian cancers in a subject. Furthermore, different modifications of miRNA inhibitor molecules as well as different derivatives of miRNA inhibitor molecules are also described.

Abstract: The present invention is related to a lipid composition comprising at least a first lipid component, at least a first helper lipid, and a shielding compound which is removable from the lipid composition under in vivo conditions.

Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.

Abstract: The present invention relates to a nucleic acid aptamer molecule that includes a domain that binds to an estrogen receptor, molecular complexes that include the nucleic acid aptamer molecule and an estrogen receptor, and constructed DMA molecules and expression systems, as well as host cells, that the contain an RNA aptamer molecule of the invention. Use of these aptamers and encoding constructs to inhibiting estrogen receptor activity in a cell and to treat estrogen receptor-positive cancers is also described.

Abstract: The present invention is related to a nucleic acid molecule capable of binding to CGRP, wherein the nucleic acid molecule comprises a central stretch of nucleotides, wherein the central stretch of nucleotides comprises a nucleotide sequence of 5? HWn1n2YGGAn3An4UMn5n6Yn7n8n9n10n11Kn12Rn13ADn14n15 ARn16Un17Cn18n19Un20n21 3? [SEQ ID NO: 99], wherein H, W, Y, G, A, U, M, B, K, R, D, C are ribonucleotides, and n1 is R or dG, n2 is U or dT, n3 is K or dG, n4 is C or dC, n5 is M or dC, n6 is B or dU, n7 is N or dG, n8 is Y or dT, n9 is N or dC, n10 is R or dG, n11 is V or dA, n12 is K or dT or dU, n13 is G or dG, n14 is A or dA, n15 is U or dT, n16 is R or dG, n17 is Y or dC, n18 is C or dC, n19 is B or dC, n20 is C or dC, n21 is C or dC, and dG, dT, dC, dA and dU are 2?-deoxyribonucleotides.

Abstract: The invention relates to compositions containing polynucleotide vectors capable of expressing a nucleic acid encoding a fusion polypeptide on the surface of a viral particle and/or a eukaryotic cell.

Abstract: This document provides methods and materials related to treating glaucoma, ocular hypertension, cardiovascular diseases, and renal diseases. For example, this document provides isolated nucleic acid molecules and viral vectors (e.g., lentiviral vectors) containing isolated nucleic acid molecules. Methods for reducing intraocular pressure as well as symptoms and progression of cardiovascular and renal diseases also are provided.

Abstract: The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof.