Abstract: The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.

Abstract: The present invention relates to an azetidine derivative for use as a Janus kinase (JAK) inhibitor, a drug composition comprising same, a preparation method therefor, and a use thereof in the treatment of JAK-related diseases comprising, for example, inflammatory diseases, autoimmune diseases, and cancers.

Abstract: The present invention is directed to combinations of a ?-lactamase inhibitor with sulbactam and, optionally, imipenem/cilastatin. The combinations are useful for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant pathogens. More particularly, the invention relates to a combination of ?-lactamase inhibitor compound 1: or a pharmaceutically acceptable salt thereof, with sulbactam, or a pharmaceutically acceptable salt thereof, and, optionally, imipenem/cilastatin, or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein, inter alia, are compounds and methods useful for increasing stress resistance.

Abstract: Provided herein, inter alia, are methods and compounds for inhibiting K-Ras and for treating cancer.

Abstract: The present invention relates to certain novel substituted thiophene compounds and the finding that they display useful efficacy in the inhibition of the p38? MAPK enzyme. This provides for use of the compounds in various treatment methodologies related to MAPK inhibition, including the treatment of inflammation.

Abstract: The present application relates to novel combinations of at least two components, component A and component B: ?component A is an IRAK4-inhibiting compound of the formula (I) as defined herein, or a diastereomer, an enantiomer, a metabolite, a salt, a solvate or a solvate of a salt thereof; ?component B is a BTK-inhibiting compound, or a pharmaceutically acceptable salt thereof; and, optionally, ?one or more components C which are pharmaceutical products; in which one or two of the above-defined compounds A and B are optionally present in pharmaceutical formulations ready for simultaneous, separate or sequential administration, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis, lymphoma, macular degeneration, COPD, neoplastic disorders and psoriasis.

Abstract: Disclosed are crystalline free base ansolvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).

Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: A pharmaceutical composition comprises a solution having a pH of from 5 to 7.5, including loratadine and/or desloratadine. The composition is suitable for treatment of e.g. allergic rhinitis and allergic conjunctivitis.

Abstract: The present invention relates to CCRS antagonists for use in the treatment of cancer, either in monotherapy or in combination therapy. The invention also relates to methods for determining whether a subject suffering from cancer benefits from an ongoing therapeutic treatment with a CCRS antagonist or whether a subject suffering from cancer will benefit from a planned therapeutic treatment with a CCRS antagonist.

Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.

Abstract: The present disclosure provides methods and compositions for the treatment, identification, diagnosis, and prognosis of dystonia, or dystonia related disorders.

Abstract: Described herein are combinations comprising a SMAD7 oligonucleotide and a Toll-like receptor (TLR) modulator. Methods for using such combinations to treat disease conditions, including inflammatory disorders, such as inflammatory bowel disease (IBD), are also provided herein.

Abstract: Provided are methods for inducing apoptosis of cells using quinolinol compounds. Combinations of quinolinol compounds can be used in the methods. Combinations of one or more quinolinol compound and one or more inhibitors of cell growth arrest, e.g., Nutlin3a, can also be used in the methods. Also provided are compositions comprising of one or more quinolinol compound and one or more pharmaceutically acceptable carrier. The compositions can comprise one or more quinolinol compound, one or more pharmaceutically acceptable carrier, and one or more inhibitors of cell growth arrest, e.g., Nutlin3a.

Abstract: The present invention relates to a combination comprising (a) RAD001, or a pharmaceutically acceptable salt thereof, and (b) BEZ235, or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential use for enhancement of an immune response; a pharmaceutical composition comprising such combination; a method of enhancing immune response in a subject comprising administration of said combination to a subject in need thereof; use of such combination for preparation of a medicament for the enhancement of an immune response; and a commercial package thereto.

Abstract: Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a ?-elimination mechanism.

Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.

Abstract: The present disclosure relates to cured pharmaceutical compositions designed to reduce the potential for improper administration of drugs that are subject to abuse, the process of curing such composition in order to improve the dissolution stability, method of using the same for treatment of pain.

Abstract: The invention relates to a transdermal therapeutic system for administering the active substance buprenorphine. Said system comprises at least one carboxylic acid that determines the solubility of buprenorphine in the matrix layer and that can likewise be absorbed. The transdermal therapeutic system according to the invention is used in the treatment of pain and characterized by a considerably increased utilization of the active substance.

Abstract: The invention features sublingual formulations of apomorphine and apomorphine prodrugs, and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

Abstract: The present invention provides compounds that can modulate the amount of Nav 1.7 protein, a key protein in pain signaling, that is present in the cellular surface and methods for using such compounds. In particular, compounds of the invention modulate the amount of Nav 1.7 protein on the cellular surface by modulating SUMOylation of CRMP2. Thus, compounds of the invention can be used to treat various clinical conditions associated with the presence and/or activation of Nav 1.7 protein on the cellular surface and/or SUMOylation of CRMP2.

Abstract: Topical administration of VEGF inhibitors such as, without limitation, rifamycin compounds are useful for treating skin disorders such as treating and/or reducing scars such as hypertrophic scars, and useful for treating acne and underlying acne symptoms such as skin redness.

Abstract: The invention relates to methods of treating a central nervous system disorder in a subject, comprising reducing the level of LPA in the brain of said subject

Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.

Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.

Abstract: Disclosed is use of NK3R antagonists for the therapeutic treatment of pathological excess body fat and/or prevention of body fat gain in patients. Also disclosed is a cosmetic method for stimulating the loss of excess of body fat, including the administration of a NK-3 receptor antagonist.

Abstract: The present invention relates to 2,4-diaminopyrimidines and pharmaceutically acceptable salts thereof, purification methods for the same, pharmaceutical compositions containing them, methods of obtaining and using them for the treatment of disease states, disorders, and conditions mediated by the histamine H4 receptor activity.

Abstract: The present disclosure provides compositions comprising a lyn kinase activator and TRPM8 agonist, and to methods of: reducing blood glucose levels, weight gain, or fat depot levels; treating metabolic syndrome, Syndrome X, obesity, prediabetes, type II diabetes, type I diabetes; treating hypercholesterolemia, hypertension, coronary heart disease, diabetic neuropathy, lipodystrophy, diabetic retinopathy, erectile dysfunction, kidney disease, dyslipidemia, dyslipoproteinemia, a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, or pancreatitis; inducing the beiging of adipocytes; and preventing pancreatic beta cell degeneration.

Abstract: A composition comprising about 10 mg or less of dipyridamole formulated for oral administration and a physiologically acceptable carrier.

Abstract: The present invention relates to methods of decreasing inflammation by inhibiting polo-like kinase (Plk)

Abstract: The present invention is directed to pemetrexed formulations comprising a non-aqueous solvent that remains stable after dilution for at least about 48 hours when stored at 2° C. to 8° C. The present invention is also directed to pemetrexed formulations comprising a non-aqueous solvent that remains stable for at least about 24 months when stored at 2° C. to 8° C.

Abstract: The present invention provides methods for increasing plasma dUrd levels comprising the administration of 6R-MTHF. The methods of increasing plasma dUrd increase dUrd levels compared to equimolar concentrations of LV. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF.

Abstract: The present invention provides pharmaceutical compositions comprising a compound of formula (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the pharmaceutical compositions comprising a compound of formula (I) and their use as medicaments.

Abstract: The present invention provides compounds of formula (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof for use in the treatment, prevention and/or delay of progression of amyotrophic lateral sclerosis (ALS). Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

Abstract: The present invention relates to a method of preparing 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin dihydrochloride dihydrate.

Abstract: Described herein are cocrystals of epigallocatechin gallate (ECGC) and caffeine, compositions comprising such cocrystals, methods of making such cocrystals, and methods of improving animal or human health by treating with such cocrystals. In particular, Form I and Form II of a 1:2 (epigallocatechin gallate to caffeine) cocrystal are described.

Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.

Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

Abstract: The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABAA ?5) and act as GABAA ?5 negative allosteric modulators (GABAA ?5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABAA ?5 such as Alzheimer's disease.

Abstract: A technique is provided for reducing the discoloration of an aqueous composition containing a halogenated isoquinoline derivative during high-temperature preservation. An aqueous composition comprising a compound represented by Formula (1): wherein X represents a halogen atom, or a salt thereof, or a solvate of the compound or the salt thereof, and a prostaglandin.

Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Abstract: The subject matter provides ready to inject fulvestrant compositions with improved solubility and stability, and methods for preparing the same. Contemplated compositions include fulvestrant at a concentration of greater than 100 mg/ml, that exhibit degradation of the fulvestrant at a level of less than 5 wt % when stored over at least three months at 25° C.

Abstract: Fulvestrant formulations suitable for intramuscular injection at concentration in excess of 40 mg/ml in the absence of castor oil and castor oil derivatives are disclosed.

Abstract: Disclosed herein is, among other things, a soft gel vaginal pharmaceutical composition and dosage form containing solubilized estradiol for the treatment of vulvovaginal atrophy (VVA) and female sexual dysfunction (FSD).

Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

Abstract: In one aspect, the invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing to an animal in need thereof an effective amount of a compound. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: To provide a multidrug-resistant Gram positive bacteria antibacterial agent containing as an active ingredient a novel component to which multidrug-resistant bacteria are not resistant, and an external agent containing the same. The multidrug resistant Gram-positive bacteria antibacterial agent according to the present invention contains an amphipathic compound having an HLB value of greater than 9.5 and 20 or less and an acyl group as an active ingredient. The external agent according to the present invention contains the multidrug resistant Gram-positive bacteria antibacterial agent.

Abstract: The present invention relates to a pharmaceutical composition containing ginsenoside F1 or Rh1 for preventing or treating vascular leak syndrome, to a method for treating vascular leak syndrome using the pharmaceutical composition, and to a food composition containing ginsenoside F1 or Rh1 for preventing or ameliorating vascular leak syndrome. The ginsenoside F1 or Rh1 provided in the present invention can promote angiogenesis and suppress vascular leakage, and thus can be widely utilized in the effective prevention or treatment of vascular leak syndrome.

Abstract: A method of treating an inflammation or a hyperproliferative disease in a subject in need thereof is disclosed. The method comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of: a compound represented by Formula I: or a pharmaceutically acceptable salt thereof, a compound represented by Formula II: and a compound represented by Formula III: wherein the variables in Formulae I, II and III are as defined in the specification.