Abstract: Described are positive allosteric modulators of muscarinic acetylcholine receptor M1 (mAChR M1), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.

Abstract: Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders.

Abstract: The invention relates to the treatment of cognitive impairment associated with schizophrenia (CIAS) with a specific GlyT1 inhibitor ([5-(methylsulfonyl)-2-{[(2R)-1,1,1-trifluoropropan-2-yl]oxy}phenyl]{(1R,5R)-1-[5-(trifluoromethyl)-1,2-oxazol-3-yl]-3-azabicyclo[3.1.0]hex-3-yl}methanone). A 12-week treatment in a phase 2 study showed improvement in cognitive function as measured by the MATRICS Consensus Cognitive Battery (MCCB) overall composite score.

Abstract: The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as ?9-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.

Abstract: This invention pertains to pharmaceutical compositions comprising a glucocorticoid for use in the treatment of diseases by immunoablation. The compositions of the invention may be for use in the treatment of diseases that are mediated by immune cells such as lymphocytes.

Abstract: The present disclosure provides a compound of Chemical Formula (1) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same: wherein X, Z, R1 and R2 are as defined in the specification. The compound of Chemical Formula (1) or pharmaceutically acceptable salt thereof acts as a positive allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), thereby being useful in the prevention or treatment of disorder mediated by glutamate dysfunction and mGluR5.

Abstract: Pro-benefit-agent compounds having heterocyclic moieties that include a benefit agent fragment derived from benefit agents, such as perfume raw materials, that include an aldehyde moiety or a ketone moiety. The pro-benefit-agent compounds may be derived from modified amino acids. Related treatment compositions, premix compositions, precursor compounds, and methods of making and using such materials and compositions.

Abstract: The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds.

Abstract: Provided are substituted 8-methylquinazolin-4(3H)-one compounds useful as PARP inhibitors for the treatment of cancer and asthma, as well as pharmaceutical compositions comprising them and methods for their synthesis.

Abstract: The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.

Abstract: The present disclosure relates, in general, to improved processes for the preparation of 4-{8-amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)-benzamide, particularly large-scale processes for manufacturing 4-{8-amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide and intermediates used in such processes.

Abstract: Activators of BAX and their uses in cancer therapy are disclosed.

Abstract: A pharmaceutical composition containing forskolin and retinoic acid as active ingredients which is suitable for preventing or treating sensorineural hearing loss is disclosed. A pharmaceutical composition containing forskolin and retinoic acid as active ingredients has an excellent effect of preventing, alleviating or treating hearing loss caused by ototoxic drugs during anticancer treatment, and thus is useful as a pharmaceutical composite preparation capable of reducing side effects of anticancer drugs and, additionally, as an agent for preventing or treating sensorineural hearing loss.

Abstract: Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

Abstract: The present invention relates to processes for preparing a Compound (1): or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

Abstract: A compound 3-(4-chlorophenyl)-5-{[5-methyl-2-(propan-2-yl)phenoxy]methyl}-1,2,4-oxadiazole compound, its synthesis, and its use as an anticancer and/or antimicrobial agent.

Abstract: Pharmaceutical combinations of LTV-17 (I), a lactivicin derivative, and ?-lactamase inhibitors are provided, wherein the combinations comprise antibacterial agents suitable for use in the treatment or prevention of bacterial infections.

Abstract: Thiazole tethered organoselenide compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The thiazole tethered organoselenide compounds are identified as being capable of inhibiting 5-lipoxygenase (5-LO).

Abstract: Pharmaceutical intermediates and methods for efficiently preparing muscimol mono-BOC and derivatives thereof in the synthesis of muscimol and congeners and derivatives thereof.

Abstract: Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.