Abstract: The current invention is directed to a novel compound and compositions having said compound, wherein said compound is a compound according to formula I or formula II, or an acceptable salt thereof. The invention also relates to specific uses of said compound, particularly as antimicrobial agent.

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

Abstract: Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 dependent condition more specifically, by contacting the MRGPR X2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

Abstract: Disclosed herein are compounds which can act modulators of the aryl hydrocarbon receptor (AHR). Further disclosed herein are methods for treating diseases and disorders, such as cancer and viral infections, using the compounds disclosed herein.

Abstract: The present invention relates to a process for the preparation of olaparib. The present invention also relates to a novel crystalline form of olaparib, and a process for its preparation. Further, the present invention also relates to a pharmaceutical composition containing a therapeutically effective amount of the novel crystalline form of olaparib. Also, the present invention relates to improved processes for the preparation of crystalline form H and crystalline form A of olaparib.

Abstract: The present invention provides a process for obtaining 5-fluoro-4-imino-3-methyl-1-(phenyl-4-sulfonyl)-3, 4-dihydro-1H-pyrimidin-2-one having formula (I): The present invention also provides a method for isolating a compound having the formula (I). The present invention also provides a monomethylsulfate salt of the compound having formula (I). The present invention also provides a method for crystallizing or recrystallizing a compound having formula (I) using an anti-solvent. The present invention also provides a method of isolating a compound having formula (II).

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or an enriched composition comprising a compound of formula (I), by reacting a compound of formula (II), with hydroxylamine or its salt, a base, a chiral catalyst, and an organic solvent, wherein said base is an anion exchange resin.

Abstract: Described herein is the preparation of a P2X3 antagonist and chemical intermediates used in the synthetic process.

Abstract: Provided are deuterated analogs of MDMA, including deuterated empathogens. In some embodiments, such compounds are monoamine releasers or inhibit monoamine transporters. In some aspects, features of the compounds provide stability, such as metabolic stability, and efficacy. Also provided are methods for the preparation of deuterated empathogens and pharmaceutical compositions comprising the same. Methods of using the deuterated empathogens, alone or in combination with other therapeutic agents, are provided. In some embodiments, deuterated empathogens are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders.

Abstract: The present invention relates to the compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as maxi-K potassium channel openers, which makes them suitable for use in therapy, particularly in the treatment or prevention of fragile X associated disorders, such as fragile X syndrome.

Abstract: The present invention relates to the compounds of formula (I) wherein the variables are defined as given in the description and claims. The invention further relates to their use and composition.

Abstract: Provided herein are compounds, tautomers, or pharmaceutically acceptable salts thereof, having a structure of formula (I): wherein X1, Y, Z1, Z2, (R1)n, (R2)m, and ring A are as described herein. Also provided are pharmaceutical compositions comprising compounds, tautomers, or pharmaceutically acceptable salts having a structure of formula (I). Further provided are a method of inhibiting cyclin dependent kinase 19 (CDK19) a method of treating breast cancer with the disclosed compounds.

Abstract: Disclosed are a compound serving as a PARP7 inhibitor, and a use thereof in preparing a drug for treating relevant diseases. Specifically disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The compound can be used for treating cancer.

Abstract: The present invention relates to novel crystalline forms of (R)—N—((S)-1-(4-(3,3-dimethyl-2-oxoindolin-1-yl)piperidin-1-yl)-1-oxo-4-phenylbutan-2-yl)piperidine-3-carboxamide hydrochloride (HCl-salt), and to pharmaceutical compositions thereof, process for preparation or isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of various diseases or disorders which are mediated by motilin receptor activity.

Abstract: The present invention belongs to the technical field of antibacterial drugs, and discloses a pyrrolylacylpiperidylamine compound and use thereof. The present invention in particular relates to a pyrrolylacylpiperidylamine compound and a pharmaceutically acceptable salt thereof, and use thereof in the preparation of a medicament for resisting infections with bacteria, mycoplasma or chlamydia.

Abstract: The present invention relates to a pyrimidine-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating cancer, comprising the same as an active ingredient. The pyrimidine-2,4-diamine derivative exhibits a high inhibitory ability against EGFR and HER2 mutations, and thus can be advantageously used in the treatment of cancer in which EGFR and HER2 mutations have occurred. In addition, the pyrimidine-2,4-diamine derivative exhibits a significant synergistic effect when administered in combination, and thus may be advantageously used in combination therapy.

Abstract: The present invention relates to a novel method for preparing an intermediate of Chemical Formula 3, wherein the intermediate can be effectively used in the synthesis of a xanthine oxidase inhibitor.

Abstract: The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. Disclosed herein is a compound according to Formula (I) or an optically pure stereoisomer, pharmaceutically acceptable salt, solvate, or prodrug thereof. Further disclosed herein is a compound according to Formula (II) or an optically pure stereoisomer, pharmaceutically acceptable salt, solvate, or prodrug thereof.

Abstract: The present disclosure relates to a heterocyclic compound represented by Chemical Formula 1, an organic light emitting device including the same, and a composition for an organic material layer: in Chemical Formula 1, each substituent has the same definition as described in the detailed description.

Abstract: A salt of 2-[3-({1-[2-(dimethylamino)ethyl]-2-(2,2-dimethylpropyl)-1H-1,3-benzodiazol-5-yl}sulfonyl)azetidin-1-yl]ethan-1-ol with an acid, wherein the acid is selected from the group consisting of hydrochloric acid (HCl), maleic acid, and methanesulfonic acid; a crystalline form of the salt; a pharmaceutical composition comprising the salt; a pharmaceutical composition comprising the crystalline form; a method for preventing or treating a disorder or condition comprising administering the salt; and a process for preparing a pharmaceutically acceptable salt.

Abstract: Prodigiosin analogs which reactivate the p53 pathway are provided, as well as compositions of these compounds, and methods for reactivation of the p53 pathway using these compounds are provided. The prodigiosin analogs may be used to treat cancer in which p53 mutation plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.

Abstract: The present disclosure relates to synthesizing and utilizing fluorescent dye compounds or pharmaceutically acceptable salts thereof. Conjugation of amino acid groups to the fluorescent dyes increase specificity and detection of the compound. Methods of manufacture and synthesis of the compounds for use thereof in diagnostic imaging are contemplated.

Abstract: The present invention provides processes for preparing a compound of formula I and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula II wherein each R3 independently represents a tertiary alkyl group, preferably wherein each R3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula I and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula I and their use in the treatment of proliferative disorders.

Abstract: The present disclosure provides an organic compound, a light extraction layer material, and an organic electronic device. The organic compound has a structure represented by formula (1). X1 and X2 are independently selected from O, S, or NR1; L1 and L2 are independently selected from a single bond, a substituted or unsubstituted aromatic group having 6 to 30 ring atoms, or a substituted or unsubstituted heteroaromatic group having 5 to 30 ring atoms; M1 and M2 are independently selected from a substituted or unsubstituted aromatic group having 6 to 60 ring atoms, a substituted or unsubstituted heteroaromatic group having 5 to 60 ring atoms, or a substituted or unsubstituted amino group.

Abstract: In order to prevent deterioration inside an organic EL element and significantly improve the light extraction efficiency, an object of the present invention is to provide a compound that absorbs light rays with wavelengths of 400 to 410 nm of sunlight, thereby preventing them from affecting a material inside the element, and has a high refractive index in a wavelength range of 450 to 750 nm. The present invention provides an amine compound having a specific benzazole ring structure having a high refractive index. An organic EL element having excellent light emission efficiency is obtained by using the compound of the present invention as a material constituting a capping layer.

Abstract: Substituted 1,2,4-thiadiazolyl nicotinamides, salts or N-oxides thereof and their use as herbicidally active substances The present invention relates to substituted 1,2,4-thiadiazolyl nicotinamides of the general formula (I), salts or N-oxides thereof, where the radicals in the general formula (I) correspond to the definitions given in the description, and to their use as herbicides, in particular for controlling broad-leaved weeds and/or weed grasses in crops of useful plants and/or as plant growth regulators for influencing the growth of crops of useful plants.

Abstract: The present invention relates to new macrocyclic ligands substituted with at least one picolinate group, to the radioactive complexes thereof and to the uses thereof in medical imaging and/or in therapy, in particular in interventional radiology. The present invention also relates to a new process for preparing ligands according to the invention, and also to the preparation intermediates thereof.

Abstract: Embodiments relate to novel pan caspase inhibitors and method of manufacture of the same. Additionally, embodiments provide pharmaceutical compositions using novel pan caspase inhibitors, and methods for the use thereof as caspase inhibitors and for the treatment of disorders caused by excessive apoptotic activity.

Abstract: Disclosed herein are compounds and compositions for inhibiting, treating or preventing respiratory infections, illnesses, diseases, and other respiratory conditions such as those caused by viruses including RSV, coronavirus, and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus. Methods of inhibition, treatment or prevention of infections and diseases caused by these viruses are also provided.

Abstract: The present disclosure encompasses solid state forms of Vericiguat, in embodiments crystalline polymorphs of Vericiguat, processes for preparation thereof, and pharmaceutical compositions thereof.

Abstract: The present invention provides a compound represented by Formula (I): wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.

Abstract: Provided are compounds as potent inhibitors of cyclin-dependent kinase (CDK), or pharmaceutically acceptable salts thereof. Corresponding compositions are also provided.

Abstract: The invention provides deuterium-enriched piperidinyl-methyl-purine amines and related compounds, pharmaceutical compositions, their use for inhibiting NSD2, and their use in the treatment of a disease or condition, such as cancer.

Abstract: Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.

Abstract: Disclosed are compounds that bind to embryonic ectoderm development (EED) protein and proteolysis-targeting chimeric (PROTAC) derivatives thereof that induce degradation of EED. The disclosed compounds may be characterized as substituted [1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds. The disclosed PROTAC derivatives thereof typically include a first targeting moiety that binds to EED (MEED) which may be derived from the disclosed[1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds that bind to EED. The first targeting moiety typically is linked via a bond or a linker (L) to a second targeting moiety that binds to an E3 ubiquitin ligase (ME3). As such, the disclosed PROTACS may be described as having a formula MEED-L-ME3 or ME3-L-MEED.

Abstract: Provided are compounds of formula (la) and (lb), and pharmaceutically acceptable salts thereof. Additionally provided are compositions and pharmaceutical compositions comprising the compounds, therapeutic methods using same for modulating (e.g., inhibiting) CREB binding protein (CBP)/?-catenin mediated signaling in treating a condition, disease or disorder (e.g., fibrosis, cancer, neurological conditions, metabolic disorders (e.g., diabetes, etc.), and skin conditions (dermatitis, psoriasis, scarring, alopecia, etc.) mediated by aberrant CBP/?-catenin signaling, and cosmetic methods for treating skin conditions (e.g., aging, etc.). Additionally provided are methods for enhancing vaccine efficacy using the compounds and compositions. Further provided are methods for efficiently synthesizing an antagonist of CBP/catenin signaling pathway, comprising use, in a penultimate, or last reaction step, of an intermediate 2-propynyl-compound to form a pyrazole derivative (e.g., via 3+2 cycloaddition).

Abstract: The disclosure relates to compounds that act as inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Abstract: The present invention relates to a group of IMB-C5 series compounds having anti-coronavirus activity and the application thereof. The structure of the IMB-C5 series compounds is as shown in formula (1). The application is an application of the IMB-C5 series compounds in preparing a drug. The drug is a drug for inhibiting coronavirus, and is preferably a drug for treating human coronavirus infection. The coronavirus is preferably human ?-coronavirus or human ?-coronavirus, especially novel coronavirus (SARS-COV-2).

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: Provided herein are methods of treating painful diabetic peripheral neuropathy, such as advanced painful DPN, in a patient by administering to the patient an effective amount of NYX-2925 or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of 3-hydroxy-2-(5-isobutyryl-1-oxo-2,5-diazaspiro [3,4] octan-2-yl) butanamide.

Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

Abstract: The present invention relates to compounds of formula (I) (shown below) useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.

Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The disclosure is directed to compounds of Formula I pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

Abstract: A compound of Formula (1) is provided that has been shown to be useful for treating a disease caused by a viral infection: wherein R1, R2, R3, A, L, m, n, p and q are as defined herein.

Abstract: The disclosure relates thieno[2,3-d]pyrimidin-4-one derivatives as modulators of NMDA receptors and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for managing conditions related to cognition, typically prevention or treatment of neurological conditions related to the NMDA receptor.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: The present invention relates hydroxypyridoxazepine compounds, methods of making them, pharmaceutical compositions containing them and their use as Nrf2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, or a tautomer thereof, or a hydrate thereof.