Abstract: Amine substituted reverse pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.

Abstract: Disclosed herein are compositions and methods for treating or preventing certain cancers in a subject. In certain embodiments such compositions and methods generally relate to the use of G-coupled protein receptor 40 (GPR40) agonists to inhibit the growth or induce apoptosis of certain cancer cells. The compositions and related methods disclosed herein may be used to treat subjects affected by cancers, such as melanoma, medullary thyroid carcinoma, malignant peripheral nerve sheath tumors and neuroblastoma, and to reduce the incidence of metastases in such affected subjects.

Abstract: This invention is in the area of improved therapeutic combinations for and methods of treating selected retinoblastoma (Rb)-negative cancers and Rb-negative abnormal cellular proliferative disorders using particular topoisomerase inhibitors and specific cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. In one aspect, the improved treatment of select Rb-negative cancers is disclosed using specific compounds disclosed herein in combination with a topoisomerase I inhibitor.

Abstract: The present invention is effective for the treatment and relief of cough produced by posterior nasal secretion, through the use of the combination of Oximetazoline and Ipratropium. The active agents enunciated in the combination of the present invention have been used and marketed separately with different uses to those of the present invention. The oxymetazoline to eliminate nasal secretion and congestion (obstruction), and ipratropium bromide is marketed for the purpose of dilating the bronchial tubes in asthmatic patients with chronic obstructive pulmonary disease, although experimentally it has also been used to decrease nasal secretion. Both active agents, together or separately have not been used so far as antitussives intranasally. The cough produced by the posterior nasal secretion, is the most frequent cause of cough in the human being of any age, the present invention is effective for the treatment and relief of said symptom.

Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo.

Abstract: A composition for prevention or treatment of pulmonary fibrosis comprising chromenone derivatives represented by Formula I of the present invention or pharmaceutically acceptable salts thereof as an active ingredient, produces altered heat shock protein 27 (HSP27) dimers, thereby preventing normal HSP27 non-phosphorylated polymers from performing a chaperone function and reducing a cell protection function that chaperone originally performs. Thus the inventive composition has a remarkable inhibitory effect on pulmonary fibrosis, in particular, an irradiation-induced pulmonary fibrosis phenomenon.

Abstract: Compositions and methods for improving the experience of bath time that promotes good skin-to-skin contact between caregiver and child are disclosed.

Abstract: Substituted 4-azaindoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.

Abstract: Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.

Abstract: The present invention is directed to the combination of the RSV inhibiting Compound A, i.e. 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl) 1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, and one or more RSV inhibiting Compound B selected from from ribavirin, GS-5806, MDT-637, BTA-9881, BMS-433771, YM-543403, A-60444, TMC-353121, RFI-641, CL-387626, MBX-300, AZ-27, MEDI8897, CR9501, palivizumab, 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-benzimidazol-2-yl}methyl)-1 cyclopropyl-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, 3-[[7-chloro-3-(2 ethyl-sulfonylethyl)imidazo[1,2-a]pyridin-2-yl]methyl]-1-cyclopropyl-imidazo[4,5-c]pyridin-2 one, N-(2-fluoro-6-methylphenyl)-6-(4-(5-methyl-2-(7-oxa-2-azaspiro[3.

Abstract: Compounds that are PSMA ligands, pharmaceutical compositions comprising these compounds, methods for treating and detecting cancers in a subject, methods for identifying cancer cells in a sample are described herein.

Abstract: Disclosed herein are methods, pharmaceutical combinations, or kits for the prevention or treatment of extrapyramidal syndromes, for example, dyskinesia, dystonia, akathisia, or drug-induced Parkinsonism, with the administration of a therapeutic effective amount of Trapidil, a derivative, a metabolite, a prodrug, an analog, or a pharmaceutically acceptable salt thereof.

Abstract: The object of the present invention is the combination of palmitoylethanolamide (PEA) and lycopene, and/or pharmaceutically acceptable salts and/or derivatives thereof, the pharmaceutical formulations comprising the combination of PEA and lycopene, and/or pharmaceutically acceptable salts or derivatives thereof, optionally together with at least one pharmacologically acceptable excipient, and the use of the combination of PEA and lycopene, and/or pharmaceutically acceptable salts or derivatives thereof, and of the formulations comprising such a combination, in the treatment of inflammatory diseases.

Abstract: The invention relates to a crystalline form of (S)-2-(8-((5-chloropyrimidin-2-yl)(methyl)amino)-2-fluoro-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as CRTH2 receptor modulators.

Abstract: The present invention relates to novel acid-free quaternized nitrogen compounds, to the preparation thereof and to the use thereof as a fuel and lubricant additive, more particularly as a detergent additive, as a wax antisettling additive (WASA) or as an additive for reducing internal diesel injector deposits (IDID); to additive packages which comprise these compounds; and to fuels and lubricants thus additized. The present invention further relates to the use of these acid-free quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct-injection diesel engines, especially in common-rail injection systems, for reducing the fuel consumption of direct-injection diesel engines, especially of diesel engines with common-rail injection systems, and for minimizing power loss in direct-injection diesel engines, especially in diesel engines with common-rail injection systems.

Abstract: The present invention relates to novel acid-free quaternized nitrogen compounds, to the preparation thereof and to the use thereof as a fuel and lubricant additive, more particularly as a detergent additive, as a wax antisettling additive (WASA) or as an additive for reducing internal diesel injector deposits (IDID); to additive packages which comprise these compounds; and to fuels and lubricants thus additized. The present invention further relates to the use of these acid-free quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct-injection diesel engines, especially in common-rail injection systems, for reducing the fuel consumption of direct-injection diesel engines, especially of diesel engines with common-rail injection systems, and for minimizing power loss in direct-injection diesel engines, especially in diesel engines with common-rail injection systems.

Abstract: Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone ?v?3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.

Abstract: The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator. The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.

Abstract: This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Abstract: A veterinary composition is disclosed and is based on anthelmintic compounds, particularly from the benzimidazole group, with delayed release properties, preferably in the form of granules or pellets, to be added to feed or feed supplements offered to ruminants in order to control eggs and larvae of helminths, preferably from the genus Haemonchus spp.