Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: To improve the signal quality of the optical signal emitted by a reconfigurable transmitter after a reconfiguration event, an optical transmitter includes a modulator, a digital signal processor, and a controller. The modulator is for modulating light by a driving signal with a reconfigurable format. The digital signal processor is for processing digital data to be transmitted by using parameters in order to generate the driving signal. The controller is for controlling the digital signal processor changing the parameters so as to keep the driving signal stable before and after changing the reconfigurable format.

Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

Abstract: The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment and prophylaxis of visual hallucinations associated with Lewy Body dementia.

Abstract: A method of treating a condition of in a human patient comprising pharmacologically activating a translocator protein of 18 kDa (TSPO), wherein the condition is one of a chronic methamphetamine addiction, a medical consequence of methamphetamine use; a behavioral consequence of methamphetamine use, an HIV associated cognitive motor disorder, an HIV-associated neurodegenerative disorder, and a neuroinflammatory response.

Abstract: The present invention provides a resin composition capable of forming a film exhibiting a small humidity-dependent variation in optical values; a triazole compound to be incorporated into the resin composition; an optical film and an optical lens, each of which is prepared from the resin composition and exhibits a small humidity-dependent variation in optical values; and a polarizing plate, a circularly polarizing plate, and an image display device, each of which includes the optical film and exhibits excellent moisture resistance. The resin composition of the present invention contains a resin and a compound having a 5-membered or 6-membered aromatic hydrocarbon or heterocyclic ring, wherein the resin is a hygroscopic resin, the compound has at least three specific aromatic rings having a specific NICS value, and the specific aromatic rings are bonded to one another via a single bond or one or two atoms.

Abstract: The present invention provides a process for producing the compound having the structure: comprising (a) reacting a compound having the structure: with a compound having the structure: in the presence of a first organic solvent under conditions sufficient to produce the compound, wherein the first organic solvent is a substituted benzene.

Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

Abstract: The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase.

Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Abstract: The present invention relates to an oral solid dosage form, in particular a tablet, comprising macitentan free base polymorphic form I.

Abstract: Provided herein are compounds of Formula (I) or (II): (I) (II) pharmaceutically acceptable salts, tautomers, prodrugs, and stereoisomers thereof, and pharmaceutical compositions thereof, wherein X, RN, R1, R3, R4, p, and m are as defined herein. Such compounds and compositions have been found useful in the treatment or prevention of viral infections, e.g., polyomaviral infections, and are further envisioned useful in treatment or prevention of other pathogenic conditions associated with endosomal trafficking. Methods of treating or preventing an infection by a pathogen secreting an AB5 toxin is also contemplated.

Abstract: The subject invention describes a method of use of Ropinirole™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Ropinirole as a dopamine agonist with affinity for the dopamine D2, D3, or D4 receptors. Ropinirole may also be used to treat menopausal symptoms in conjunction with Tizanidine™ to further reduce the effects menopausal symptoms by providing a sedative and muscle relaxant effect which aids in sleep. The combination of Ropinirole and Tizanidine provides a useful new compound for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.

Abstract: In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

Abstract: A method of treating a proliferative disease, such as cancer, is disclosed. The method comprises administering to a mammal in need thereof synergistically therapeutically effective amounts of: (i) (2R,3S)—N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-di-hydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide; (ii) 2-deoxy-2,2-difluorocytidine monohydrochloride (beta-isomer); and (iii) optionally, one or more additional anticancer agents.

Abstract: The subject invention describes a method of use of Ropinirole™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Ropinirole as a dopamine agonist with affinity for the dopamine D2, D3, or D4 receptors. Ropinirole may also be used to treat menopausal symptoms in conjunction with Tizanidine™ to further reduce the effects menopausal symptoms by providing a sedative and muscle relaxant effect which aids in sleep. The combination of Ropinirole and Tizanidine provides a useful new compound for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.

Abstract: Enantiomerically-pure (S)-tofisopam is administered to lower serum uric acid levels in a mammal.

Abstract: The present invention relates to methods and compositions for modulating receptors in postsynaptic neurons of damaged or diseased retinas. The invention also related to methods for using the compositions set forth herein for treatment of diseases of hyperexcitability such as epilepsy.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: The use of ORL-1 receptor antagonists of the formula: for the treatment of alcohol use disorders is described.

Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.

Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: The present invention relates to unique delivery systems and the use of an imidazobenzodiazepine derivative, such as flumazenil either alone or in combination with other receptor antagonists in the treatment of disease or medical disorders.

Abstract: The present invention relates to the field of thermostable enzymes, methods for their inactivation, and related uses, kits and reagents. In particular, the invention relates to a method for reversible inactivation of thermophilic enzymes by chemical modification under aqueous or non-aqueous conditions.

Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, AbI, DCAMKL1, ABL1, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS 1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: A pH sensitive carrier which includes at least one pH sensitive compound selected from the group consisting of deoxycholic acid, cholic acid, ursodeoxycholic acid, chenodeoxycholic acid, hyodeoxycholic acid, C27 bile acid, glycodeoxycholic acid, glycyrrhizic acid, glycyrrhetinic acid and salts thereof, and at least one amphipathic substance selected from the group consisting of a phosphatidylcholine having 10 to 12 carbon atoms, a polyoxyethylene sorbitan monofatty acid ester having 12 to 18 carbon atoms, a sorbitan fatty acid ester having 16 to 18 carbon atoms, glycerol monooleate, glycerol dilaurate, glycerol distearate, glycerol dioleate, polyoxyethylene castor oil and ?-tocopherol, and which is capable of developing a membrane disruptive function promoting effect.

Abstract: Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning.

Abstract: The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.

Abstract: The present invention discloses compounds of Formulae I and II, wherein the variables in Formulae I and II are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formulae I and II in the treatment of HCV infection.

Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep

Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2- a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R1-R8 are as defined herein.

Abstract: A protocol or procedure is provided for lowering sympathetic nervous system arousal in a person in order to prepare that person for a medical or dental procedure. First, a therapeutic dosage of one or more neurotransmitter supplements, such as a gamma aminobutyric acid formulation, a tryptophan-derived neurotransmitter precursor, and dehydroepiandrosterone are administered to the patient. Concomitantly, gelled electrodes are placed adjacent or below the mastoid. The gelled electrodes are connected to a cranial electrotherapy stimulation device that administers a sub-sensation level current to the patient. Also, a noise dampening headset is placed on the patient and a neuroacoustic entrainment recording or program is played. Next, light is blocked with black out glasses. Then, the medical or dental procedure is performed.

Abstract: Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: where X, R1, R2, subscript m, subscript n and subscript v are as defined herein.

Abstract: The provided embodiments are based in some aspects on the demonstration herein of a role for gastrin in regulating the aging gut-ovary axis and effects of targeting gastrin activity in reversing gastrin-mediated bone loss. Provided are methods, compositions and agents, including gastrin antagonists, for treatment, amelioration, and prevention of bone diseases and conditions. Methods for treating a bone disease or condition associated with hypergastrinemia in a subject in need thereof may comprise administering to the subject at least one dose of a therapeutically effective amount of a gastrin receptor-targeting agent, thereby treating the bone disease or condition associated with hypergastrinemia.

Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

Abstract: Provided is a method for detecting injury to the brain comprising: a) determining the level of a tight junction (TJ) protein in exosomes isolated from a test sample from a subject, wherein the TJ protein is occludin, claudin-3, claudin-5, claudin-12, ZO-1, ZO-2, ZO-3, JAM-A, JAM-B or JAM-C, or any combination thereof; b) comparing the level of the TJ protein in the test sample to the level of the TJ protein in a control sample, wherein an elevated level of the TJ protein in the test sample relative to the level of the TJ protein in the control sample indicates that the subject has an injury to the brain.

Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.

Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.

Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.

Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.

Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.

Abstract: Particles of an organic acid salt of an amino acid amide or ester local anesthetic are employed as agents for the improved alleviation of pain. Particularly, the particles find use with surgically created wounds, where the particles may be administered directly into the bed of the wound or topically for transdermal transport.