Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Abstract: A noxious arthropod controlling composition comprising a heterocyclic compound represented by the formula (1) [wherein, A1 and A2 represent ?C(R6)—, nitrogen and so on, R1 represents a halogen and so on, R3 and R4 represent optionally substituted C1 to C4 chain hydrocarbon group and so on, R5 represents a hydrogen and so on, n represents 0 or 1] as an active ingredient has an excellent effect for controlling noxious arthropods.

Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.

Abstract: The purpose is to provide a compound which 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. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.

Abstract: This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.

Abstract: The present invention relates to novel compounds for the inhibition of cyclindependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R1, R2, R3, R4, R5, R6, R7, and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclindependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases.

Abstract: A topical pharmaceutical composition comprising tazarotene and one or more of an anti-inflammatory or anti-bacterial agent. Also provided is a method for treating skin conditions, such as acne utilizing the above topical pharmaceutical composition.

Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.

Abstract: The present invention relates to hydroximoyl-heterocycle derivatives, 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: 2-aryl and 2-heteroaryl 4h-1-benzopyran-4-one-6-amidino derivatives formula (I) useful as pharmacological agents for the treatment of arthritis, cancer and related pain.

Abstract: The present invention provides a compound of formula I; 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: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.

Abstract: Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: wherein ring A is benzene having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is alkylsulfonylamino, etc., R2 and R3 are (a) the same of different and are hydrogen, alkyl, or optionally substituted aryl, or (b) combined with each other to form an oxo group or (c) combined with each other at its terminal together with the adjacent carbon atom to form cycloalkyl, X is ?N—, ?C(R4)— or —CH(R4)—, R4 is (a) hydrogen, (b) cyano, (c) halogen, (d) alkyl, (e) alkenyl, (f) cycloalkyl, (g) alkanoyl, (h) carbamoyl, or (i) cycloalkenyl, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, useful e.g. as an antihypertensive agent.

Abstract: The disclosure provides compounds of formula I, including their 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 invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.

Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.

Abstract: The present invention provides oil compositions and associated methods and reagents, particularly useful for the treatment of dermatologic conditions. In some embodiments, provided compositions are formulated for and achieve transdermal delivery, for example by topical administration.

Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: Disclosed herein are topical dermal compositions comprising particles, wherein the particles comprise a) a biodegradable polymer, and b) a retinoid selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein the particles have an average diameter between 0.1 ?m and 10 ?m, and wherein the variables are as defined in the specification. The compositions are useful for treating a condition associated with excess sebum production.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.

Abstract: The disclosure provides compounds of formula I, including their 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: Pulmonary arterial hypertension in a mammal can be prevented or treated using combined 5-HT2A and 5-HT2B receptor antagonist. The antagonists can be present in a single compound or in two separate compounds.

Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus 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: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.

Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.

Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.

Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.

Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.

Abstract: Compositions and methods of treatment or prophylaxis of fragile-X associated disorders are provided, as well as methods of screening compounds and kits to screen a library of compounds.

Abstract: The invention relates to a composition for topical application comprising as an active ingredient a peroxide and a retinoid wherein one of said peroxide and retinoid is in the form of first microparticles comprising a solid particulate matter of the active ingredient coated by a metal oxide layer and the other of said peroxide and retinoid is present in an uncoated free form or in a coated form of the active ingredient. The invention further relates to method for treating a surface condition in a subject using said composition, a method for preparing a composition exhibiting improved stability, and a kit comprising: (a) a first composition comprising a peroxide as a first active ingredient; and (b) a second composition comprising a retinoid as a second active ingredient; at least one of said first and said second active ingredient being coated by a metal oxide layer.

Abstract: A drug delivery system (DDS) comprised of segmented biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The segmented implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer, and permit the DDS to have segments that possess individual and different drug release characteristics.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Abstract: The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.

Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from retinoid compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of retinoid compounds in a composition by at least 3-fold.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.

Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from resveratrol compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of resveratrol compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the resveratrol compound is concentration dependent, with the amount of resveratrol photostabilization increasing with the concentration of the alkoxycrylene compound.

Abstract: A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.

Abstract: A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.

Abstract: A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.

Abstract: Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.

Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: The present invention relates to a liquid pest control system that includes a synthetic pyrethroid as a pest control active ingredient and an agent selected from the group consisting of purified diethylene glycol monoethyl ether, tocopherol nicotinate and tocopherol succinate, and combinations thereof, to reduce or eliminate paresthesia of the synthetic pyrethroid. The system releases the synthetic pyrethroid efficiently and uniformly. The pest control system is less irritating to the animal's skin as compared to prior art systems, particularly to small breeds of dogs. The system is useful for making liquid spot-on treatments, sprays and the like.