Abstract: The present invention relates to compounds showing pharmacological activity towards the subunit ?2?#of voltage-gated calcium channels (VGCC), especially the ?2?-1 subunit of voltage-gated calcium channels. More particularly, the invention relates to alkylaminoproline derivatives having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain and/or as neuroprotective agents.

Abstract: The invention relates to a mousse composition comprising: a) a base composition comprising: (i) from 0.0001 to 5 wt. % of a lactam; (ii) from 0.1 to 10 wt. % of an alcohol; and, b) a propellant; and to the use of a combination of a lactam with an alcohol, in a mousse composition to collapse the resulting mousse foam quicker; and to the use of a combination of a lactam with an alcohol, in a mousse composition to make the resulting mousse foam easier to rinse.

Abstract: This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g., Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PLpro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MPpro), which function as therapeutics for the treatment of viral infection characterized with PLPpro and/or Mpro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLPpro and/or Mpro protease activity and/or expression.

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

Abstract: Pharmaceutical compounds are disclosed which may be useful for treating asthma, ongoing lung disease, chronic obstructive pulmonary disease (COPD), chronic bronchitis, and/or emphysema. A pharmaceutical composition may include a therapeutically effective amount of the compound and a pharmaceutically acceptable vehicle therefor. The pharmaceutical composition may be administered for treating such disorders as asthma, ongoing lung disease, chronic obstructive pulmonary disease (COPD), chronic bronchitis, or emphysema.

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: Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises hydrogenating a compound represented by Formula II and cyclopropyl formaldehyde as raw materials in the presence of an acid and catalyst to generate an N-cyclopropylmethyl aniline compound represented by Formula I, wherein R is alkoxy, alkylamino or a substituted anilino group represented by Formula III.

Abstract: Methods and uses for diagnosing and treating Tourette syndrome are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.

Abstract: Methods and uses for diagnosing and treating anxiety disorders are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.

Abstract: This invention provides methods for preventing, mitigating, ameliorating and/or controlling psychiatric disorders, including depression, major depression, bipolar disorder, schizophrenia and substance abuse (including addiction and dependence) by administration of an agent that increases epoxy-fatty acids (e.g., an inhibitor of soluble epoxide hydrolase), as sole active agent or in combination with another agent (e.g., an antidepressant, an antipsychotic, an anxiolytic). When co-administered in combination with another agent, one or both agent may be administered at a subtherapeutic dose.

Abstract: The present invention is directed to compounds, compositions and methods for preventing, treating or curing Norovirus infection in human subjects or other animal hosts.

Abstract: Lactams for use in the treatment of respiratory tract infections, including chronic lung infections in patients having cystic fibrosis.

Abstract: This invention relates to methods and compositions for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), alone or in combination with valproate, in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment.

Abstract: A process for the preparation of Brivaracetam, an anti-convulsion drug, is provided comprising Hofmann rearrangement of (S)-3-(2-(chloroamino)-2-oxoethyl) hexanoic acid, followed by cyclization resulting in (R)-4-propyl-pyrrolidin-2-one which on condensation with bromo butyric acid or ester followed by reaction with ammonia results in Brivaracetam.

Abstract: Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

Abstract: A maleamic acid monomer, and a preparation method and a use of the maleamic acid monomer. The structural formula of the monomer is as follows: formula (1), wherein, R is selected from The maleamic acid monomer provided in the present invention may be used as a comonomer to prepare temperature-tolerant and calcium salt-tolerant polymers.

Abstract: The present invention describes the combination of topically inhaled medicinal formulations comprising an anticholinergic component and a glucocorticosteroid component and its use in the symptomatic and prophylactic treatment of diseases of the respiratory tract, especially with an obstructive component or underlying inflammation like asthma and chronic obstructive pulmonary disease (COPD). It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the NOVOLIZER®.

Abstract: This invention relates to a group of compounds for repelling blood-feeding ectoparasitic arthropods, and a method of deterring their landing and feeding on animals including humans, by applying in one or more formulations compounds that incorporate one or more sulfide and one or more hydroxyl groups to the skin, clothing or environment of animals, including humans. A method of repelling and deterring landing and feeding by blood-feeding arthropods on an animal by applying in effective amount one or more compounds that incorporate alkyl sulfide and alcohol moieties, or alkyl sulfide and amide moieties, or alkyl sulfide and amide moieties to the skin, clothing or environment of an animal.

Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.

Abstract: A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water within a period of less than about 15 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to levetiracetam.

Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.

Abstract: Compounds are of the class of 1-pyrrolidinyloxy,1-piperidinyloxy, and 1-azepanyloxy derivatives of formula (I): The compounds are useful in prevention, treatment or management of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction. The compounds include 2,2,5,5,-tetramethyl-3-(nitrooxymethyl)pyrrolidin-1-yl acetate.

Abstract: The present invention is directed to a pharmaceutical composition comprising a Compound (a) of a class of peptide Compounds and at least one further Compound (b) for the prevention, alleviation or/and treatment of epileptic seizures.

Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.

Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Abstract: A method of stimulating germination in plant seeds and/or releasing plant tissue or plant organs from dormancy, comprising applying to a seed, plant, plant organ or plant tissue a compound of formula (I): where: R1 is alkyl or H; R2, R3, R4 and R5 are independently selectable from H, halide, —NO2, —SO2R?, —OH, —Oalkyl where R? is alkyl or aminoalkyl; and/or R1 and R5 are joined as —O(CH2)m—, where m is 1, 2, 3 or 4; R6 is a substituted or non-substituted alkyl, and/or substituted or non-substituted aryl; and n is an integer of 1 to 4.

Abstract: A composition in the form of an oil in water emulsion, preferably without emulsifier, is described. The composition can include, in a physiologically acceptable environment, at least one new retinoid. Also described, is the method of preparing the composition and its use in cosmetics and dermatology.

Abstract: Compositions including at least 3?-tert-butyl-4?-(2-hydroxy-ethoxy)-4?-pyrrolidin-1-yl-[1,1?;3,1?]-terphenyl-4-carboxylic acid are described. The compositions can be oil-in-water emulsions made up of oily liquid globules each provided with a lamellar liquid crystal coating dispersed in an aqueous phase; a retinoid is either in the oily liquid globules or in the aqueous phase; each oily liquid globule is individually coated with a unilamellar or oligolamellar layer, obtained from at least one lipophilic surfactant, at least one hydrophilic surfactant and at least one separate anionic surfactant, and the coated oily liquid globules have a mean diameter lower than 800 nm.

Abstract: Inhalation solutions for administration of beta 2-agonists or combinations of muscarinic antagonists and beta 2-agonists for the treatment of breathing disorders, such as COPD, are provided. The inhalation solutions are administered by nebulization, particularly with a high efficiency nebulizer.

Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.

Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.

Abstract: The present invention provides methods of treating and pharmaceutical compositions useful for treating a mood disorder or depressive symptoms associated with pain, inducing analgesia and treating pain in a subject by administering a pharmaceutically effective amount of an agent capable of one or more of increasing GluA1 level, expression, concentration, or biological activity, increasing calcium permeable AMPA (? amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor (CPAR) level, expression, concentration, or biological activity or potentiating a CPAR current. The agent may be an AMPA potentiator or ampakine. The agent may increase AMPA receptor currents by slowing the deactivation of open channels and may be, for instance, 2-pyrrolidinone, 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluorophenoxyacetamide (PEPA) or LY451646. The agent may also be a protein, RNA or DNA product.

Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.

Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,

Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.

Abstract: The present invention provides methods of treating and preventing arrhythmia and other diseases or disorders, using ion channel modulating compounds, including vernakalant hydrochloride. The present invention further provides controlled release oral formulations and dosages of vernakalant hydrochloride, which are effective in preventing arrhythmia. Certain methods and formulations of the present invention are adapted for the treatment and prevention of arrhythmia and other disease or disorders in subjects identified as having altered drug metabolism due to polymorphism of the gene encoding cytochrome P450 2D6.

Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.

Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.

Abstract: This invention relates to treating age-related cognitive impairment. This invention in particular relates to the use of inhibitors of synaptic vesicle protein 2A (SV2A), such as levetiracetam, seletracetam, and brivaracetam, in improving cognitive function in subjects that exhibit age-related cognitive impairment or are at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-related Cognitive Decline (ARCD) or Age-Associated Memory Impairment (AAMI).

Abstract: The present invention provides STAT3 inhibitors which preferentially suppress proliferation of cancer over non-cancer cells and inhibit migration and invasion of malignant cells. The inhibitors of the present invention selectively inhibit STAT3 binding to DNA without affecting the activation and dimerization of STAT3. Furthermore, the inhibitors of the present invention inhibit expression of STAT3 downstream target genes and STAT3 binding to chromatin in situ.

Abstract: Carrier particles in which at least 60% of the surface is coated with magnesium stearate are useful for preparing dry powder formulations for inhalation.

Abstract: The present invention is based, in part, on our studies of molecular pathways that include the deubiquitinase CYLD. Accordingly, the present invention features, inter alia, nucleic acid constructs that express CYLD or a biologically active variant thereof (e.g., a variant including the catalytic domain), nucleic acids that inhibit the expression of a negative regulator of CYLD (e.g., PDE4B or LNK2), nucleic acids that modulate the expression of downstream CYLD targets (e.g., Akt, by inhibiting or promoting the expression of the downstream target), compositions including one or more of these types of constructs (e.g., pharmaceutical compositions), kits including one or more of the compositions described herein and instructions for use, screening methods to identify therapeutic agents {e.g., anti-inflammatory agents) that upregulate CYLD, downregulate a negative regulatory of CYLD, or modulate (e.g., inhibit) a downstream CYLD target (e.g.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

Abstract: A method is disclosed for making a pharmaceutical composition for pulmonary administration, the method comprising a step in which an inhalable pharmaceutically active material is acoustically blended in a resonant acoustic blender. The invention also relates to compositions for inhalation prepared by the method.

Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.

Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.

Abstract: The present invention is directed to the treatment of demyelination as an underlying cause of the disease of multiple sclerosis (MS) in a mammal, the method comprising promoting remyelination of myelination of axonal cells by administering to the mammal a 2-oxopyrrolidine compound having a general formula I: wherein R?R??H, and R??CH2CONH-(2,6CH3)C6H3 or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.