Abstract: The present invention concerns compounds derived from the anaesthetic propofol that are useful as analgesics and methods of using the same. The compounds act as co-activators of strychnine-sensitive glycine receptors and may have greater activity at those glycine receptors than at GABAA.

Abstract: Vitamin K is effective in counteracting (1) increase of body weight and body mass index (BMI), (2) accumulation of body fat mass and (3) accelerates weight loss during calory restriction or other life style interventions aiming weight reduction. A pharmaceutical composition or nutritional formulation comprising vitamin K is provided which can be used to combat overweight or obesity, either as a single, dedicated product or in combination with other slimming products or life style changes.

Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said composition dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.

Abstract: A method for diagnosing a cardiac ischemic event and a kit for detecting biomarkers used in the method. Also provided is a method for treating a PPAR-related disorder by administering a pharmaceutical composition containing one or more long chain fatty acids.

Abstract: An enteric-coated bead dosage form of cysteamine, and related methods of manufacture and use, are disclosed.

Abstract: Methods for improving the gastrointestinal tolerability of biguanide compounds and for treating metabolic disorders and/or inducing weight loss in patients in need thereof, particularly in individuals having a contraindication for treatment with biguanide compounds, are provided comprising administering delayed release formulations of such biguanide compounds, including metformin, targeted to the small intestine.

Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of a TRPV1 compound (e.g., capsaicinoid compound) at or near a target site, one can relieve pain caused by diverse sources, including but not limited to, postoperative pain, spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

Abstract: An effective dose of intravenous ibuprofen administered co-adminstered with intravenous acetaminophen in surgery patients is a safe and effective way to reduce both pain and the need for opioid analgesics. In preferred embodiments, the administration of intravenous ibuprofen and intravenous acetaminophen starts no later than at approximately the completion of wound closure.

Abstract: In certain aspects the methods comprise administering an inhibitor of hydrogen sulfide biosynthesis, a cystathionine-?-synthase (CBS) inhibitor, or a hydrogen sulfide neutralizing agent to a patient having a cancer associated with elevated production of hydrogen sulfide.

Abstract: The composition comprises 0.5% to 10% by weight of a neuropathic analgesic; 0.5% to 10% by weight of a muscle relaxant; 0.5% to 20% by weight of an anti-inflammatory analgesic; and 0.5% to 10% by weight of an anesthetic.

Abstract: The present invention is directed to a method of preventing or treating a gastrointestinal condition in a subject, that includes administering one or more branched chain fatty acid to the subject under conditions effective to prevent or treat the gastrointestinal condition in the subject. The present invention is also directed to methods of promoting gastrointestinal health in a subject and propagation of probiotic organisms. Also disclosed is a formulation which includes one or more branched chain fatty acid and an aqueous phase emulsified with the one or more branched chain fatty acids, where the formulation includes over 25 wt % of the one or more branched chain fatty acid.

Abstract: The present invention provides a food or drink that emits no offensive odor typified by a fish odor in any form of the food or drink, such as liquid, gel, semi-solid, or solid form, and also suppresses emission of an offensive odor due to time-dependent changes. Further, a food or drink is provided that has, particularly, a superior action of inhibiting platelet aggregation to that of conventional fish-derived EPA and DHA-containing food. The food or drink comprise an algae extract oil, an animal or plant protein, and an emulsifier.

Abstract: The invention provides pharmaceutical compositions containing omega-3 oil and a non-hydrophilic co-solvent that have an increased absorption rate. The pharmaceutical compositions may further contain one or more pharmaceutical organic molecules. The invention further provides kits containing these pharmaceutical compositions, methods for formulating pharmaceutical compositions containing omega-3 oil, and methods for decreasing the likelihood of developing cardiovascular disease, decreasing triglyceride or LDL cholesterol levels, decreasing pain or inflammation, treating diabetes, chronic pulmonary diseases, or irritable bowel syndrome, decreasing symptoms of an autoimmune disease or allergic conditions.

Abstract: A new class of anti-microbial agents and methods for preventing or reducing the risk of sexually transmitted infections and/or diseases is provided. Preferably, these anti-microbial agents are also contraceptive and, thus, also prevent or reduce the risk of unplanned pregnancies. The anti-microbial agents comprise a delivery vector having anti-microbial activity (and preferably contraceptive activity) coupled with a nitric oxide donor moiety.

Abstract: Disclosed are methods and compositions for treating or preventing diseases or disorders associated with mitochondrial calcium uniporter (MCU) activity. The methods may include administering a modulator of MCU activity to a patient in need thereof.

Abstract: Polymeric conjugates comprising a polymeric backbone having attached thereto a bone targeting moiety and a therapeutically active agent, wherein the bone targeting moiety is attached to one end of the polymeric backbone via a branching unit such that a molar ratio of the bone targeting moiety to the polymer is at least 2:1, are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of bone related disorders are also disclosed.

Abstract: Dopamine reuptake inhibitors, and their analogs, are disclosed for treating and delaying the progression of autoimmune diseases.

Abstract: Combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.

Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.

Abstract: A pharmaceutical combination comprising an alpha-isoform specific phosphatidylinositol 3-kinase inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof and a fibroblast growth factor receptor (FGFR) kinase inhibitor, particularly for simultaneous, separate or sequential use for the treatment of a cancer; use of such pharmaceutical combination for the preparation of a medicament for the treatment of a cancer; use of such pharmaceutical combination for the treatment a cancer; a method for treating a cancer comprising administering to a subject having said cancer a jointly therapeutically effective amount of such combination; and related pharmaceutical compositions or kits thereof.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lo

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating cancer, comprising (S)-(?)-benproperine or a pharmaceutically acceptable salt thereof as an active ingredient, and a method for preventing or treating cancer using the same.

Abstract: The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable sale thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.

Abstract: The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. In other aspects the invention relates to pharmaceutical compositions comprising a deuterated analog of Pridopidine of the invention, and to therapeutic applications of these analogs.

Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.

Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.

Abstract: Methods and compositions for treatment of human immunodeficiency virus (HIV) infections have been developed which dampen immune activation with a bias more on the CD4 T cells relative to the CD8 T cell response, inhibit HIV replication, reactivate latent HIV, and inhibit infection of cells by HIV. Pushing latent HIV into active infections with hindrance of cell infection by the reactivated HIV can substantially reduce the number of cells infected with HIV and the viral load of HIV, which is not achieved using just the combination of ART and compounds which activate latent HIV. The methods involve administering to an HIV-infected subject three or more compounds which collectively dampen immune activation with a bias more on the CD4 T cells relative to the CD8 T cell response, inhibit HIV replication, reactivate latent HIV, and inhibiting infection of CD4 T cells by HIV.

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 liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

Abstract: The present invention relates to storage stable prolonged release pharmaceutical dosage forms comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof, the manufacture thereof as well as their use for administration to human beings.

Abstract: Provided are opioid receptor antagonists represented by the formula (I): where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.

Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.

Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.

Abstract: Improved methods and compositions for safe and effective treatment of erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.

Abstract: The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

Abstract: This disclosure relates to the uses of compounds that target an interaction between CHFR and PARP1. In certain embodiments, the disclosure relate to treating cancer by administering a mitotic inhibitor such as a taxane and a vinca alkaloid in combination with a compound that inhibits CHFR and PARP1 interactions, such as 5-((1-benzyl-1H-indol-3-yl)methylene)-1-(3,4-dimethylphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, derivatives or salts thereof, optionally in further combination with a third anti-cancer agent.

Abstract: The present invention relates to a pharmaceutical composition which comprises progestogens, preferably drospirenone, estrogens, preferably ethinylestradiol and 5-methyl-(6S)-tetrahydrofolate, can be employed as oral contraceptive and moreover prevents disorders caused by folate deficiency in the consumers, in particular cardiovascular disorders and, after conception of the embryo, congenital malformations caused by folate deficiency such as, for example, neural tube defects, ventricular valve defects, urogenital defects, and cleft lip, jaw and palate, without masking the symptoms of vitamin B12 deficiency, and at the same time even in the case of homozygous or heterozygous polymorphism of methylenetetrahydrofolate reductase facilitates unimpaired utilizability of the folate component 5-methyl-(6S)-tetrahydrofolate by the body and thus its biological activity for preventing the abovementioned congenital malformations caused by folate deficiency.

Abstract: The present invention provides ophthalmic ointments for treating infective eye diseases containing valganciclovir hydrochloride as an active ingredient in the amount of from about 0.01% to about 10.0% w/w. These ophthalmic ointments are particularly effective for treating eye diseases caused by herpesviruses in the eye. Compared with oral administration, topical administration of valganciclovir hydrochloride is not accompanied by systemic side effects such as bone marrow suppression. Compared with topical administration of ganciclovir, topical administration of valganciclovir hydrochloride is much more effective in treating infective diseases in the eye and is not accompanied by toxicity to the surface of the eye.

Abstract: Drug eluting implants for targeted delivery of a nerve-blocking agent to inhibit neural traffic along renal nerves of a human patient.

Abstract: The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof in combination with Quizartinib or a salt thereof or the hydrate thereof for treating patients suffering from acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).

Abstract: A composition for reducing cell senescence including a Rho-kinase inhibitor and method of treating a cell senescence-related symptom in mammals.

Abstract: The invention discloses application of an enrofloxacin salt in preparation of an oral preparation for pigs. The enrofloxacin salt is at least one of salts formed by enrofloxacin and metal ions, and the metal ions are zinc, copper, calcium, magnesium, iron, cobalt, manganese, chromium, silver or nickel. The enrofloxacin salt formed by the enrofloxacin and the metal ions can significantly improve the palatability of the enrofloxacin to pigs; furthermore pharmacokinetics and artificial infection prove that the enrofloxacin salt formed by the enrofloxacin and the metal ions does not affect bioavailability, so enrofloxacin salt can be developed into the oral preparation administrated via the digestive tract, for pig-raising without affecting normal feed intake of the pigs.

Abstract: The present invention provides novel chemical compounds characterized as Rho kinase (ROCK) inhibitors, methods for their discovery, and their therapeutic, research, and diagnostic use. In particular, the present invention provides 1,4-benzodiazepine-2,5-dione compounds and related compounds having ROCK inhibitory activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with ROCK activity.

Abstract: Method for treating cardiac diseases using BET inhibitors including JQ1 are provided. Methods for treating cardiac hypertrophy, method for treating heart failure not arising from inflammation, methods for treating myocardial infarction, methods for cardioprotection and methods for inhibiting restenosis are described herein. The methods involve the use of effective amounts of BET inhibitors such as JQ1.

Abstract: The present disclosure provides compositions and formulations comprising botanicals and natural compounds for the promotion of healthy brain aging in adults, especially adult women, and for prevention of age associated neurodegenerative changes resulting in cognitive, memory and executive dysfunction including modulation of the age related predisposition to mild cognitive impairment, Alzheimer's disease, hormonal and other dementia related conditions. The present disclosure also provides methods of using the compositions and formulations in treating and preventing neurodegenerative changes resulting in cognitive, memory and executive dysfunction.

Abstract: An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. An exemplary embodiment provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ?F508-CFTR, or another mutation of class II.

Abstract: A method of forming a compound in a subject can include: providing a composition having a prodrug compound represented by a structure of Formula 1 or stereoisomer thereof or pharmaceutically acceptable salt thereof; and administering the composition to a subject such that the prodrug compound has a phosphoryloxyalkyl prodrug moiety removed therefrom to form the compound in the subject and to form the separate phosphoryloxyalkyl compound. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, various cancers (e.g., bladder, breast, etc.), dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.

Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.

Abstract: Therapeutic compositions comprising substituted imidazole or imidazolium compounds may be used for a number of medical purposes, such as treatment of undesirable conditions or diseases, including disease or conditions related to bone, cancer, and/or pain.