Abstract: The present disclosure relates generally to compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, deuterated analog, tautomer, stereoisomer, or mixture of stereoisomers thereof and their use as LRRK2 inhibitors.

Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.

Abstract: Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5.

Abstract: Various crystalline and amorphous solid state forms of an apoptosis-inducing agent and preparations thereof are disclosed. Also discloses the use of crystalline forms for the preparation of amorphous form of apoptosis-inducing agent. Further discloses a process for preparation of the apoptosis-inducing agent.

Abstract: The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

Abstract: The invention relates to a KRAS mutant protein inhibitors of formula (I), a composition containing the inhibitors and the use thereof.

Abstract: The present invention provides N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide compositions, and the use thereof for treating a proliferative disorder.

Abstract: The invention relates to compounds of formula (I): or pharmaceutically acceptable sails or solvates thereof, to pharmaceutical compositions comprising them and to their use in the treatment and/or prevention of diseases or disorders mediated by histamine H4 receptor.

Abstract: The present invention relates to a sulfoximine compound represented by formula (I) as a bromodomain protein inhibitor and a pharmaceutically acceptable salt thereof and to a preparation method, pharmaceutical composition, and medical use thereof.

Abstract: The present invention relates to a compound of formula (I) wherein R4 is C1-6alkyl, halogen or cyano; R5 is halogen; R2 is 4,5,6,7-tetrahydropyrazolo[3,4-c]pyridinyl which is unsubstituted or substituted by C1-6alkyl or haloC1-6alkyl; 4,5,6,7-tetrahydropyrazolo[4,3-c]pyridinyl which is unsubstituted or substituted one or two times by C1-6alkyl; or 5,6-dihydro-4H-pyrrolo[3,4-c]pyrazolyl; R3 is C1-6alkyl; L is azetidinyl or piperidinyl; or a pharmaceutically acceptable salt thereof, for use as a TLR7, TLR8 and/or TLR9 antagonist for the treatment or prophylaxis of autoimmune diseases, such as e.g. systemic lupus erythematosus or lupus nephritis.

Abstract: The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as ?-lactamase inhibitors, notably in the treatment of a disease caused by gram negative bacteria, in particular enterobacteria, as well as pharmaceutical compositions containing such a compound and a process to prepare such a compound.

Abstract: The disclosure relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): wherein L1, L2, A, B, R1, R2, R3, and R4 are described herein.

Abstract: In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of aryl-cycloheptene scaffolds. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising an aryl-cycloheptene structure. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to modularly and scalably assemble common such cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. 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 disclosure.

Abstract: The invention concerns a method for isolation of cytisine from plant material. The method according to the invention, consists in extraction of the plant raw material by lower alcohol, acidified with mineral acid to pH within a range 1.5-3.5. The combined alcohol-aqueous extracts are concentrated under vacuum distillation till the alcohol is eliminated and after filtration they are extracted with chloroform, methylene chloride, butyl acetate or normal butanol in a ratio of 1:1. The purified from ballast substances acid aqueous concentrate is alkalized to pH 9-12 with alkaline hydroxide or ammonium hydroxide and the resulting alkaline aqueous concentrate is extracted at least twice with chloroform, methylene chloride, butyl acetate or normal butanol in a ratio of concentrate:extractant of 1:5 to 1:10. The combined organic extracts are evaporated to dryness, then acetone or ethyl acetate are added to obtain a suspension which is allowed to crystallize completely at 5-10° C., then it is filtered and dried.

Abstract: Disclosed are crystalline forms of sepiapterin free base selected from polymorphs A, B, C, D, E, F, and G, and combinations thereof, as well as crystalline polymorphs of salts of sepiapterin. Also disclosed are pharmaceutical compositions containing one or more such polymorphs and methods for preparing such polymorphs. Sepiapterin is useful in the treatment of a number diseases associated with low cellular levels of BH4, for example, phenylketonuria.

Abstract: Disclosed methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC AND TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

Abstract: There is described herein antagonists of ?4?7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are various substituents; stereocentres 1*, 2* and 3* are each independently selected from R and S; n is 1, 2, 3, or 4 and where n is 2-4, Z is an amino terminus of an amino acid; —C?O— adjacent L is the carboxy terminus of an amino acid; and L along with Z and —C?O— is a peptide.

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: Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.

Abstract: Novel cannabinoid ligands represented by the general formulas I, II, and III and methods for preparation and use within which one or more of a fluorescent ligand, nitroxide spin label, metal chelate, biotin moiety, or group with enhanced polarity may be incorporated. The compounds can bind to and modulate the cannabinoid CB1 and CB2 receptors and thereby considered specific ligands for these receptors. Some of the disclosed compounds that bind to cannabinoid CB1 and CB2 receptors can exhibit tight or irreversible binding characteristics for these receptors. Due to the presence of the imaging/diagnostic and/or therapeutic functional groups including fluorescent groups, nitroxide spin labels, metal chelates, biotin moieties, and groups with enhanced polarity, the disclosed compounds may be useful as imaging/diagnostic tools and/or therapeutic agents.

Abstract: Methods are disclosed including methods for crystallizing a material such as a drug. An example method may include combining a nucleation initiator, a surfactant solution, and an amorphous form of a drug to form a drug precursor dispersion/suspension. The method may also include incubating the drug precursor dispersion/suspension to allow the drug to convert from the amorphous form to a crystalline form.

Abstract: The invention relates to compounds useful for inhibiting BTK and at least one other protein and to methods of treating diseases including cancer by administration of a compound(s) of Formula I-IV or pharmaceutically acceptable salts thereof as defined herein.

Abstract: Compounds of Formula (I) and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.

Abstract: Disclosed are degraders, pharmaceutical compositions containing them, and methods of making and using the degraders to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.

Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Ring B, A1, A2, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.

Abstract: The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

Abstract: This application discloses a new class of fused tricyclic heterocycles of formula (I), preparation methods thereof, pharmaceutical compositions comprising these compounds, and pharmaceutically acceptable salts, solvates, or prodrugs thereof, and their uses for the treatment of diseases in which modulation of STING is beneficial, for example, cancers, pre-cancerous disorders, and viral infections.

Abstract: The present invention relates to crystalline forms of cabotegravir sodium and to methods for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising one of said crystalline forms of cabotegravir sodium, preferably in a predetermined and/or effective amount, and at last one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prophylaxis of viral infections such as HIV infections.

Abstract: Provided are compounds of Formula (I?), including compounds of Formulas (I), (II), (III), (IIIA) and (IIIB), wherein L, R1, R3 and n are as defined herein, and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).

Abstract: The present invention relates to compounds of formula (I), ab (I), wherein R1 to R3 and L are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

Abstract: The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

Abstract: A multifunctional immunity-targeted micromolecule anti-cancer medicine Citrate Bestazomib and preparation method and application thereof. The structure of the multifunctional immunity-targeted micromolecule anti-cancer medicine Bestazomib Citrate is shown as follows: The multifunctional immunity-targeted micromolecule anti-cancer medicine Citrate Bestazomib has an activity-inhibiting effect on APN/CD13, also has an activity-inhibiting effect on tumor proteasome, and can be applied to the development of medicines for treating malignant tumors.

Abstract: The present disclosure encompasses solid state forms of Ixazomib Citrate and pharmaceutical compositions thereof. Also disclosed are processes for preparation of Ixazomib Citrate.

Abstract: A composition for an organic photoelectronic device, an organic photoelectronic device, and a display device, the composition comprising a first compound represented by Chemical Formula 1, and a second compound represented by Chemical Formula 2:

Abstract: Provided are certain silicon precursor compounds which are useful in the formation of silicon-containing films in the manufacture of semiconductor devices, and more specifically to compositions and methods for forming such silicon-containing films, such as films comprising silicon, silicon nitride, silicon oxynitride, silicon dioxide, a carbon-doped silicon nitride, or a carbon-doped silicon oxynitride film.

Abstract: The present invention provides: industrially desirable and novel optically-active cyclopentenone derivatives; and a novel industrial manufacturing method. The novel optically-active cyclopentenone derivatives and method for manufacturing the same are, respectively: an intermediate for industrially desirable and novel prostaglandin derivatives and the like; and a method for manufacturing the same. It is expected that the present invention will be commercialized and industrialized.

Abstract: The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II): processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

Abstract: A molybdenum compound and a method of manufacturing an integrated circuit device, the molybdenum compound being represented by the following General Formula (I):

Abstract: Provided are organoiridium compounds that are useful as emitters in OLEDs. The compounds have Formula I L1L2Ir-L-IrL3L4 where: L is a bis-bidentate ligand including two or more aromatic rings; one of the two or more aromatic rings is bonded to the two Ir atoms at the same time; and each of L1, L2, L3, and L4 is independently a bidentate N-heterocyclic carbene ligand or a substituted or unsubstituted acetylacetonate ligand with L1, L2, L3, and L4 each being the same or different. Also provided are formulations including these organoiridium compounds. Further provided are OLEDs and related consumer products that utilize these organoiridium compounds.

Abstract: Platinum complexes having ferrocene ligands for the catalysis of the alkoxycarbonylation of ethylenically unsaturated compounds.

Abstract: Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

Abstract: According to the present invention, there are provided a benzimidazole carbamate-sugar compound conjugate compound represented by the following Chemical Formula 1, a preparation method thereof, and a use thereof as an anti-cancer agent: Wherein, R1, R2, R3 and X are as defined in the specification and claims.

Abstract: A saccharide derivative represented by Chemical Formula (1) or (2), or a salt thereof, includes units of a monosaccharide linked to each other in a chainlike or cyclic manner through glycosidic bonding and has antimicrobial action. In the formulae, R1 represents an amino-containing structure; and n represents an integer of 3 or more. A saccharide derivative represented by Chemical Formula (5) or (6), or a salt thereof, includes units of a monosaccharide linked to each other in a chainlike or cyclic manner through glycosidic bonding and has antimicrobial activity enhancing action. In the formulae, R3 represents an amino-containing structure; R4 is selected from acetyl and propanoyl; and n represents an integer of 3 or more.

Abstract: Methods for preparing 3?-O-amino-2?-deoxyribonucleoside-5?-triphosphates with reduced 3?-hydroxy-2?-deoxyribonucleoside-5?-triphosphate contamination by converting 3?-(N-acetone-oxime)-2?-deoxynucleoside triphosphate to 3?-O-amine-2?-deoxynucleoside triphosphate by treatment with an aryl-oxyamine and compositions produced therefrom.

Abstract: The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, as well as methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.

Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, Meibomian gland dysfuntion or skin inflammatiom or a respiratory disease (e.g., asthma).