Abstract: The invention is directed to delayed gelation agents comprising a degradable polymeric cage containing therein one or more gelation agents. The cage degrades in situ, e.g, in an oil reservoir, thus releasing the gelation agent(s), which can then crosslink second polymers in situ to form a gel.

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

Abstract: Methods of treating a head and neck cancer are disclosed.

Abstract: The present invention provides methods of maintaining stable remission or stable response achieved by a patient with depression following administration of a therapeutically effective amount of esketamine during an initial administration phase, comprising continuing administration of a therapeutically effective amount of esketamine for at least five months during a subsequent administration phase. The present invention also provides methods for the long term treatment of depression in a patient, comprising administering to the patient in need of the treatment a clinically proven safe and clinically proven effective therapeutically effective amount of esketamine for at least six months. In some embodiments, the depression is major depressive disorder or treatment resistant depression.

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

Abstract: An object of the present invention is to provide a method for stabilizing a substance DFP-11207 sensitive to humidity and unstable at high humidity, and a stabilized preparation thereof, and more specifically, provide a capsule preparation for treating cancer, containing DFP-11207 or a pharmaceutically acceptable salt thereof and a hygroscopic agent.

Abstract: Disclosed herein are novel drug carriers including a non-aqueous pH dependent release system and a non-aqueous pH dependent reassembly/assembly and reabsorption/absorption system. The carriers are capable of pH dependent release of biologically active agents and assembly or reassembly when the carrier transitions from a low pH environment, to a high pH environment and back to a low pH environment.

Abstract: A cocrystal containing the 1?R-diastereomer and the 1'S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1?R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.

Abstract: The invention relates to surfactants of general formula (I) in which R1 and R2 represent independently of one another represent H and SO3?X+ with the proviso that at least one of R1 and R2 is not H, n and m represent independently from each other numbers from 0-21 under the proviso that 4<n+m<26, and X+ represents a charge-balancing anion. The surfactants can be incorporated into detergents or cleaning agents, have excellent technological application properties and can be produced based on renewable raw materials.

Abstract: Disclosed is a pharmaceutical composition in dry powder form for intranasal administration, having an anti-anaphylactic adrenergic receptor agonist in the form of dry powder for intranasal administration, the composition having solid particles of the active agent in combination with at least one functional additive, and solid particles of an inert carrier.

Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.

Abstract: The present disclosure may disclose a new crystal form D of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one ((1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl) methanesulfonic acid salt, preparation method therefor and a medicinal use. Compared to the existing crystalline forms, this new crystalline form has clear advantages with respect to solubility, stability, and the preparation process.

Abstract: Methods and compositions related to molecules and formulations comprising antibiofilm materials are provide, including new formulations of Deep Eutectic Solvents (DES) that are chemically related to choline geranate. Specifically, geranic acid (a component of choline geranate DES) is a molecule from the isoprenoid/terpene family of compounds. Other members of this family as DES components include isoprenoid acids and chemical derivatives thereof.

Abstract: A composition comprising at least one TCA useful in a method for treating an anorectal disorder, a rectal device and method of treating the anorectal disorder by anorectally administering an effective amount of the TCA, e.g. amitriptyline.

Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Provided in the present invention are ingenol compounds and a use thereof in preparing an anti-HIV latency drug. In particular, provided in the present invention is a use of ingenol compounds and pharmaceutically acceptable salts thereof for preparing a drug for: (a) intervening with HIV viral latency; (b) activating an HIV virus that has been integrated into mammalian genomes; and/or (c) inducing the expression of the dormant HIV provirus in infected cells. The compounds of the present invention may also be used in combination with antiretroviral drugs to accelerate the removal of latent viral reservoirs.

Abstract: The present disclosure relates to the use of cannabidiol (CBD) for the treatment of Tuberous Sclerosis Complex (TSC). In particular the TSC is treatment resistant and is characterised by generalised seizures or focal seizures with impairment. The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).

Abstract: The present invention relates to use of antipsychotic phenothiazine derivative for treatment of cancer. The invention also provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating a cancer, and/or preventing or delaying cancer recurrence based on trifluoperazine. The invention further provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating cancer based on thioridazine and its enantiomers. Additionally, the invention provides a use for manufacture a medicament, a pharmaceutical composition and a method for treating KRAS mutant NSCLC comprising thioridazine.

Abstract: The present invention discloses an N-sulfonyl benzamide derivative with a heterocyclic substituent, and a preparation method therefor and a pharmaceutical application thereof. More specifically, the invention discloses a compound represented by formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug thereof, and a preparation method therefor and an application thereof. Refer to the specification for definitions of each group in the formula.

Abstract: The invention provides liquid or semi-solid pharmaceutical compositions for topical administration comprising a semifluorinated alkane. The compositions are useful for the delivery of active ingredients into the deep layers of the skin or skin appendages. Various active ingredients may be incorporated, such as immunosuppressants, antiinfectives, antifungal agents, antiinflammatory agents, and retinoids.

Abstract: The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol.

Abstract: The present invention relates to the use of cannabidiol (CBD) in the treatment of focal seizures. In one embodiment the patients suffering from focal seizures are children and young adults. CBD appears particularly effective in reducing focal seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; CDKL5; Neuronal ceroid lipofuscinoses (NCL); febrile infection related epilepsy syndrome (FIRES); Aicardi syndrome and brain abnormalities in comparison to other seizure types. Significantly CBD additionally is very effective in the reduction of a sub-type of focal seizures, focal seizures with impairment.

Abstract: Disclosed herein are pharmaceutical compositions with fencamfamine or fencamfamine related prodrug derivatives. The pharmaceutical compositions are for targeted therapeutic applications including, but not limited to, treating cancer-related fatigue, apathy in Alzheimer's Disease, major depression, and attention deficit-hyperactivity disorder. Also disclosed are methods of synthesizing the pharmaceutical compositions with fencamfamine or fencamfamine related prodrug derivatives.

Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).

Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.

Abstract: The present invention relates to a pharmaceutical composition for treating macular degeneration, and more particularly to a pharmaceutical composition for treating macular degeneration, which comprises an inhibitor of mTOR gene expression. The pharmaceutical composition according to the present invention can effectively treat age-related macular degeneration, a representative retinal disease that causes blindness in adults.

Abstract: Method for ameliorating secondary pulmonary hypertension in a patient including determining a pulmonary vascular resistance (PVR) of the patient suffering from secondary pulmonary hypertension; assessing a change in the PVR in response to a selection treatment; and treating the patient with a pulmonary artery manipulation device to provide pulmonary artery denervation if the patient is determined to suffer from fixed PH, thereby ameliorating the secondary pulmonary hypertension of the patient.

Abstract: A methylphenidate, particularly including dextro-threo-methylphenidate, is administered to a subject to treat a speech, gait or limb impairment secondary to a genetically acquired pre-frontal cortex processing disease or disorder, particularly including multiple sclerosis, cerebral palsy, Angelman syndrome, Rett syndrome and Fragile-X syndrome.

Abstract: The present invention relates to a carbazole compound having anti-virus activity, and more particularly, to a novel compound selected from the group of consisting of a carbazole compound which shows excellent anti-proliferative efficacy against hepatitis C virus (HCV), a pharmaceutically acceptable salt thereof, a hydrate thereof, and an isomer thereof; an anti-virus pharmaceutical composition including the novel compound as an active ingredient; a pharmaceutical composition for preventing or treating liver diseases caused by hepatitis C virus; and a method of preparing the novel compound.

Abstract: Compositions and methods for the treatment and prevention of at least one of a sign and a symptom associated with an eye disease are disclosed. Preferred compositions could comprise a liquid formulation including Cineraria maritima and at least one of a nonsteroidal anti-inflammatory drug, a carnosine, and a cannabinoid.

Abstract: An aqueous composition having an excellent antiseptic effect is provided. An aqueous composition containing: a compound represented by Formula (1), a salt thereof, or a solvate of the compound or the salt thereof, where X represents a halogen atom, and a quaternary ammonium surfactant. A method for producing an aqueous composition with an antiseptic effect, by incorporating a compound represented by Formula (1), a salt thereof, or a solvate of the compound or the salt thereof and a quaternary ammonium surfactant into the aqueous composition.

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein R1-R3 have any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various disorders.

Abstract: The invention relates to a production method of pyrazole derivative (6) by reacting compound (5) with an oxidant. wherein R1, R2, R3, X1, X2 and Z1 are as defined herein.

Abstract: The present invention relates to use of novel securinine and norsecurine analogs to bind and/or inhibit myeloperoxidase activity.

Abstract: A methylphenidate, particularly including dextro-threo-methylphenidate, is administered to a subject to treat a speech, gait or limb impairment secondary to a genetically acquired pre-frontal cortex processing disease or disorder, particularly including multiple sclerosis, cerebral palsy, Angelman syndrome, Rett syndrome and Fragile-X syndrome.

Abstract: Tricyclic chemical modulators of protein phosphatase 2A are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.

Abstract: A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

Abstract: Methods of treating developmental disorders by administering a pharmaceutical composition of pipradrol or a pharmaceutically acceptable salt thereof are provided. The methods may be used to treat conditions such as epilepsy, Landau-Kleffner Syndrome, Lennox-Gastaut syndrome (LGS) and Dravet syndrome.

Abstract: Described is the use of L-tryptophan for treating a subject with parasomnia and associated methods of treating a subject with parasomnia. Optionally, the subject may be a child or adolescent between about 3 years of age and 18 years of age. The methods and uses described herein are useful for treating parasomnia in a subject exhibiting sleep walking, sleeptalking, confusional arousals, nightmares, night terrors, rhythmic movement disorder, sleep related eating disorder and/or bruxism. Optionally, subjects are treated with a dose L-tryptophan of about between 700 mg and 5 g per day.

Abstract: The use of 5H-dibenz/b,f/azepine-5-carboxamide derivatives for treating fibromyalgia. Useful 5H-dibenz/b,f/azepine-5-carboxamide derivatives include compounds of the formula (I): where R1 is hydrogen, alkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, aryl, or pyridyl; the term alkyl means a straight or branched hydrocarbon chain containing from 1 to 18 carbon atoms; the term halogen means fluorine, chlorine, bromine or iodine; the term cycloalkyl means an alicyclic saturated group with 3 to 6 carbon atoms; and the term aryl means an unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group.

Abstract: The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

Abstract: New applications of eslicarbazepine and eslicarbazepine acetate in the treatment of intractable conditions.

Abstract: The invention relates to the compounds of formula I and formula IA or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I and formula IA; and methods for treating or preventing neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, bipolar disorder, trigeminal neuralgia, attention-deficit hyperactivity disorder (ADHD), schizophrenia, neuropathic pain, seizures, bipolar disorder, mania, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, Myotonia congenita and post-traumatic stress disorder.

Abstract: The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: This disclosure relates to N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8 -(dimethylamino)naphthalen-1(4H)-ylidene)-N-methylmethanaminium, derivatives, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I. In certain embodiments, the disclosure relates to methods of treating or preventing Nox related diseases and conditions comprising administering an effective amount of compounds disclosed herein to a subject in need thereof. In certain embodiments, the Nox related disease or condition is cancer.

Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.