Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: Pharmaceutical compositions may include a complex of a radionuclide and a compound of Formula I or Formula II.

Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.

Abstract: Methods of treating diabetic ketoacidosis are disclosed. The methods utilize an endothelin antagonist to treat diabetic ketoacidosis in mammals, including humans.

Abstract: A pharmaceutical composition comprising 3 wt. % to 50 wt. % telmisartan dispersed in a dissolving matrix comprising: (a) a basic agent in a molar ratio of basic agent:telmisartan of 1:1 to 10:|1|; (b) about 1 wt. % to about 20 wt. % of a surfactant or emulsifier; (c) 25 wt. % to 70 wt. % of a water-soluble |diluent|; and (d) 0 wt. % to 20 wt. % of one or more additional excipients and/or |adjuvants|; wherein the sum of all components is 100%, methods of making such pharmaceutical compositions, and their use.

Abstract: A method for preventing and/or treating a functional gastrointestinal disorder, comprising administering, to a subject with the functional gastrointestinal disorder, rifaximin as an effective ingredient. The functional gastroinstestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.

Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions.

Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.

Abstract: The present invention provides for methods of using tert-butyl alcohol (TBA) co-solvent systems in the formulation and production of a pharmaceutical agent with low solubility. The present invention also provides for pharmaceutical compositions made using the novel co-solvent system. In one embodiment, the invention provides for a method of making dantrolene sodium (DS) formulation for intravenous use (DS-IV). This instantaneous reconstitution of the DS-IV product constitutes a significant improvement in the pharmacotherapy of patients undergoing malignant hyperthermia during surgery.

Abstract: Methods for treating a patient using therapeutic spinal neuromodulation and associated devices, systems, and methods are disclosed herein. One aspect of the present technology is directed to methods including modulating nerves of one or more targeted organs proximate one or more dorsal root ganglia, stellate ganglia, vertebral ganglia, or cervical ganglia of the nerves using an intravascularly-positioned therapeutic element. One or more measurable physiological parameters corresponding to at least one condition associated with sympathetic activity in the targeted organs and/or central sympathetic activity in the patient can thereby be reduced.

Abstract: The present invention discloses an aryloxy dihalopropenyl ether compound with the structure shown as general formula (I), of which the group definitions can be seen in the specification. The present invention also discloses the use of the compound with general formula (I) as an insecticide in the agricultural field and an insecticidal composition using the compound with general formula (I) as an active component.

Abstract: The invention generally relates to the compositions and methods related to the use of adrenergic receptor agonists solutions for the treatment of skin and mucosal superficial wounds. Some of the preferred adrenergic receptor agonists include epinephrine, phenylephrine, norepinephrine, methoxamine, and mixtures thereof. The invention also relates to devices suitable for applying these solutions to the skin or the mucosal area. Methods according to the invention are especially effective to control superficial skin and mucosal bleeding and accelerate healing time.

Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.

Abstract: According to some embodiments, a method of treating a subject having diabetes or symptoms associated with diabetes is provided. The method includes delivering a neuromodulation catheter within a vessel (e.g., hepatic artery) having surrounding nerves that innervate the liver (e.g., sympathetic nerves of the hepatic plexus). The method may also include modulating (e.g., disrupting, ablating, stimulating) the nerves by mechanical compression, energy delivery, or fluid delivery.

Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.

Abstract: The invention relates to the use of a chemical substance selected from the group consisting of N-?2-hydroxy-3-(1-piperidinyl)-propoxyl 1-pyridine-1-oxide-3-carboximidoyl chloride, the optically active enantiomers and the mixtures of enantiomers thereof and pharmaceutically acceptable salts of the racemic and optically active compounds in the preparation of a pharmaceutical composition for the treatment or prevention of neurodegenerative diseases.

Abstract: Disclosed is a novel family of macrocyclic compounds, coined calixurenes, which comprises linear and cyclic oligomers composed of alternating moieties of an aromatic unit and a ureatic unit, linked to one another via a bridging moiety. The disclosed calixurenes feature multiple heteroatom-containing groups, and can be designed so as to feature other functionalities, and can thus be used in a variety of applications. Further disclosed are processes of preparing the calixurenes, articles containing same and uses thereof.

Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.

Abstract: The present invention concerns the uses of an azaphilone compound of formula (I): formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification for modulation of the activity of a nuclear hormone receptor and for prevention and/or treatment of a disease or disorder related to nuclear hormone receptor activity.

Abstract: Methods of treating disorders mediated by ?-catenin comprising administration of Nefopam compounds are provided In particular, the treatment of disorders arising from excessive or undesired expression of ?-catenin is contemplated Said compounds include Nefopam, analogues thereof, prodaigs thereof, and salts and solvates of Nefopam The ?-catenin mediated disorders are preferably selected from the group consisting of fibroproliferative disorders (such as scars, aggressive fibramtoses, and fibroses) and cancer (such as colon cancer, melanoma, liver cancer, ovarian cancer, endometrial cancer, medullobalstoma pilomatricomas, and prostate cancer)

Abstract: In one aspect, the present invention provides a method for treating colon and/or ovarian cancer in a subject comprising administering to a subject in need thereof a compound of general formula (I): wherein R1-R6, R, -R, Q, Y1, Y2 and n are as defined herein, wherein the compound is present in an amount effective to inhibit colon and/or ovarian tumor metastasis.

Abstract: Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.

Abstract: One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.

Abstract: The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH?CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.

Abstract: The present invention discloses compounds of formula I and II or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.

Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to 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: The present invention provides methods for inhibiting or blocking TGF-? activity in cells and/or tissues expressing TGF-? comprising, contacting cells and/or tissues expressing TGF-? with an amount of cholesterol or cholesterol derivative effective to inhibit the activity of TGF-?. The present invention further provides a method for treating a condition associated with overactivity of TGF-? or negative regulation in normal physiology by TGF-? in a subject in need of treatment, comprising contacting cells and/or tissue overexpressing TGF-? in the subject with an amount of cholesterol or cholesterol derivative effective to inhibit activity of TGF-? thereby treating the condition. In a preferred embodiment, the cholesterol derivative is oxidized 7-DHC.

Abstract: The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.

Abstract: The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.

Abstract: Provided herein are methods of preventing skin cancer, where the methods comprise the step of administering an effective amount of at least one Hsp90 inhibitor to a subject at the risk of developing skin cancer, whereby the skin cancer is prevented in the subject.

Abstract: Presently disclosed are methods and compositions for treating or preventing WHIM syndrome and certain other disorders or conditions with a certain CXCR4 antagonist.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: This invention relates to the use of 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof in combination with another antimicrobial agent selected from the group consisting of a beta-lactam antimicrobial agent, mupirocin and chlorhexidine or a pharmaceutically acceptable derivative thereof, for the prevention and/or treatment of microbial infections.

Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.

Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

Abstract: Pharmaceutical compositions including an effective amount of a capsaicin and inhibitors of Hsp90 to decrease or inhibit Hsp70 and Hsp90 chaperone pathways in cells are disclosed. Methods of inhibiting the Hsp70 and Hsp90 chaperone pathways including contacting cells expressing the Hsp70/Hsp90 complex with an effective amount of a capsaicin in combination with inhibitors of Hsp90 to decrease or inhibit the Hsp70 and Hsp90 chaperone pathways are provided. The methods can reduce the viability of target cells, for example, by increasing apoptosis or pro-apoptotic pathways. In preferred embodiments, the methods reduce or do not increase Hsp70, Hsp90, Hsp40, or HOP expression; reduce or do not increase heat shock response; reduce or do not increase pro-survival pathways in cells. Methods of treating cancer and other diseases using the disclosed compositions and methods are provided.

Abstract: The invention provides a drug delivery system for a combination of therapeutic agents. The system includes a water soluble biodegradable ABA-type triblock copolymer that possesses thermosensitive gelation properties. The system can form a stable thermogel that includes a combination of therapeutic agents including, for example, rapamycin, paclitaxel, and 17-AAG. After administration to a subject, the drugs are released at a controlled rate from the thermogel, which biodegrades into non-toxic components. The polymer system can also function to increase the solubility and stability of drugs in the composition.

Abstract: The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.

Abstract: This invention relates to a method of controlling or preventing infestations of ectoparasites, preferably hematophageous ectoparasites, on an animal by administering to the animal a composition comprising an parasiticidally effective amount of a compound of Formula 1, or an N-oxide, or a pharmaceutically or veterinarily acceptable salt thereof, wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H; C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe, S(O)Me, S(O)2Me, and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl.

Abstract: The present invention concerns the compounds of formula wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH?CH—CH, N—CH?N—CH or CH—CH?N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6 alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or substituted C1-4alkyloxy; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents morpholinyl-C1-4alkyl; Het2 represents morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.

Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.

Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.

Abstract: Macrocycle containing carbamate compounds that inhibit HIV proteolytic enzymes and processes for preparing them are described. Compositions and methods for treating a patient infected with HIV are described.

Abstract: Edible phytosterol-containing compositions include molecular complexes of non-esterified phytosterols (P) and glycerine (G) in the form of liquid crystalline microparticles. Addition of an emulsifier (M) such as a monoglyceride or a modified lecithin, and optionally an ionic surfactant, to the complex facilitates its dispersal in an aqueous medium. A composition containing either the binary PG or ternary PGM molecular complexes can be formulated as a beverage, food product, or nutritional supplement. When administered to a human subject, the complexes sequester cholesterol in the gastrointestinal tract and reduce LDL cholesterol and total plasma cholesterol levels.

Abstract: Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.