Abstract: A new analgesic has been developed for T-type calcium channels as therapeutic targets. The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1): wherein each of R1 and R2 independently represents —H or —OH; R3 represents —OH; R4 represents —OH or —H; R5 represents a straight or branched alkyl or cycloalkyl-alkyl group having one to ten carbon atoms or a straight or branched alkenyl or cycloalkyl-alkenyl group having two to ten carbon atoms, or a pharmaceutically acceptable salt or solvate thereof. The present invention also provides this T-type calcium channel inhibitor, a medicament containing the T-type calcium channel inhibitor, and a therapeutic or prophylactic agent for a disease having an effective T-type calcium channel inhibitory action.

Abstract: Cannabinoids can be separated or extracted from plant material. Versions can include a process for separating trichomes from plant material, including mixing plant material with a fluid in a metered feed system and forming a slurry; pumping the slurry into a turbulent processor, agitating the slurry between rotating and static teeth and shearing trichomes from the plant material to form a mixture of fluid, trichomes and plant material; coarse filtering the mixture and removing portions of the plant material to form an interim mixture; and then second filtering the interim mixture and removing other plant material and some trichomes to form a resulting mixture comprising other trichomes and fluid.

Abstract: A system for processing cannabinoids and recovering solvent has a vessel for a mixture of cannabinoids and solvent. A pump forms a vacuum in the system to draw the mixture into a first heat exchanger to pre-heat the mixture. A falling film evaporator receives the mixture from the first heat exchanger, and boils the mixture to form a solvent vapor. The falling film evaporator collects the cannabinoids from the mixture as a crude oil. The first heat exchanger receives the solvent vapor. Heat is transferred to incoming mixture of the system, and cools and condenses the solvent vapor to form solvent condensate and vapor. A second heat exchanger receives and further cools the solvent condensate and vapor to form further condensed solvent and some solvent vapor. The pump receives the further condensed solvent and some solvent vapor and increases pressure to form solvent liquid and recovers solvent liquid for reuse.

Abstract: In some aspects, the present disclosure provides compounds of the formula: (I) or (II) wherein the variables are as defined herein. In some embodiments, these compounds may be used to treat cancer or other hyperproliferative diseases, as well as atherosclerosis and coronary artery disease.

Abstract: Provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea which are useful as bulk pharmaceutical crystals. Also provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea having excellent TrkA inhibitory effect, medicines and medicinal composition containing these crystals, and a method for producing these crystals.

Abstract: The present invention relates to herbicidal) active pyridyl-/pyrimidyl-pyrazine derivatives, as well as to processes and intermediates used for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, as well as to the use of such compounds and compositions in controlling undesirable plant growth: in particular the use in controlling weeds, in crops of useful plants.

Abstract: A method for preparing 1,1?-ethylene-2,2?-bipyridinium dichloride includes mixing an aqueous diquat dibromide solution with hydrochloric acid, adding dropwise to a mixture of an organic solvent, a bromine absorbent, and an oxidant, and reacting to produce 1,1?-ethylene-2,2?-bipyridinium dichloride.

Abstract: The present invention relates to novel compounds of formula (I) or formula (Ia) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof, and pharmaceutical compositions of these compounds which are useful for preventive and therapeutic use in human and veterinary medicine.

Abstract: The present disclosure discloses substituted quinazoline compounds having a capacity to cross the blood-brain barrier. The compound has the structural formula represented by formula (I): The quinazoline compounds, derivatives and pharmaceutically acceptable salts thereof of the present disclosure have the ability to cross the blood-brain barrier and are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a epidermal growth factor receptor and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, cancer with meningeal metastases, and neuroprotective diseases, and the like.

Abstract: Solid state forms of Neratinib and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof are disclosed.

Abstract: The present invention provides substituted pyrazole derivatives of formula (I) which are therapeutically useful as selective CDK12/13 inhibitors. These compounds are useful in the treatment and/or prevention of diseases and/or disorders associated with CDK12/13 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions with at least one of the substituted pyrazole derivatives of formula (I) or a pharmaceutically acceptable salt, an N-oxide or a stereoisomer thereof.

Abstract: Provided herein is a synthesis for omecamtiv mecarbil dihydrochloride hydrate and various intermediates.

Abstract: The technology relates in part to compounds that bind to multimeric ligand binding regions, referred to herein as “multimeric compounds.” In certain examples, the multimeric compounds provided herein bind to and multimerize polypeptides that bind to rimiducid, such as for example, chimeric polypeptides that comprise FKBP12 polypeptide variant regions. Multimeric compounds provided include those having a structure of Formula I. Where A, Z, Y, Z? and A? moieties are described herein.

Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

Abstract: Solid state forms of Ivosidenib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed.

Abstract: The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

Abstract: The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Abstract: Described are compounds and mixtures that are useful as hole transport layers of photovoltaic devices, such as perovskite solar cells. The compounds and mixtures include non-lithium containing or lithium-free electrolytes, such as imidazolium-based electrolytes, and small-molecule hole transport structures, such as N,N-di-p-methoxy phenyl amine-based structures. The hole transport structures and electrolytes may be covalently bonded or may be separate molecules. The hole transport structures and electrolytes may include cross-linkable groups and may be cross-linked. Devices employing the compounds and mixtures as hole transport layers are also described, such as photovoltaic devices. Synthetic methods of making small-molecule hole transport compounds are also described.

Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.

Abstract: A method for preparing an oxaspirocycle derivative and an intermediate thereof are described. The method reduces reaction steps, improves reaction yield, is simple and easy to operate, and is favorable for industrial large-scale production.

Abstract: The present disclosure relates to an improved process for the preparation of isochroman structured alpha2A adrenoceptor agonist, namely 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole of formula (I) and a pharmaceutically acceptable salts thereof, such as 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole hydrogensulfate of formula (Ia), and to a novel intermediate compound used in the process, namely N-(2-aminoethyl)-5-methoxyisochroman-1-carboxamide monohydrate of formula (V). Alpha2A agonists are useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases where alpha2A agonism is desired.

Abstract: The present invention relates to a new process for preparing quinoline compounds of the general formula (II): in which Q, A, R4, R3 and R3?, are as defined herein, as well as to the intermediate compounds of said new process.

Abstract: The present disclosure relates to certain compounds having binding affinity for Ku, and uses thereof. Specifically, the present disclosure relates to the use of Ku inhibitors as described herein in site-specific genome engineering technologies, including but not limited to CRISPR/Cas9, Zinc finger nuclease (ZFN), Transcription activator-like effector nuclease (TALEN), and meganuclease. The present disclosure also relates to kits useful for site-specific genome engineering that include at least one compound as described herein.

Abstract: The invention relates to substituted ureas, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.

Abstract: The present disclosure relates to biguanide derivatives of formula (I) and their rearrangement products. The present disclosure also relates to the use of these compounds in a method for treating cancer, in particular melanoma.

Abstract: The present invention provides compounds of Formula (Ia) and (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Abstract: The invention provides new heterocyclic compounds having the general formula (I) wherein A, L, X, m, n, R1, R2 and R3 are as described herein, pharmaceutically acceptable salts thereof, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Abstract: Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.

Abstract: The present invention relates to a novel compound useful as a TRPV4 antagonist, specifically the compound 1-(((5S,7R)-3-(5-cyclopropylpyrazin-2-yl)-7-hydroxy-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compound.

Abstract: The invention relates to methods of using compounds formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Abstract: New prodrugs of therapeutically active compounds, including oligomeric prodrugs of ethacrynic acid, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy. Also a method for the controlled administration of timolol to a patient in need thereof, such as a human, comprising administering a prodrug of timolol in a microparticle in vivo, wherein the timolol prodrug containing microparticle exhibits in vitro drug release kinetics in an aqueous solution at a pH between 6-8 at body temperature of a substantially consistent release of at least 60% timolol itself by molar ratio to the prodrug of timolol or an intermediate metabolite thereof over at least 100 days.

Abstract: The present disclosure relates to compounds, pharmaceutical compositions comprising such compounds, and use of such compounds in methods of treatment or in medicaments for treatment of inflammatory diseases and certain neurological disorders that are related to inflammatory signaling processes, including but not limited to misfolded proteins.

Abstract: There are disclosed certain novel compounds (including pharmaceutically acceptable salts thereof), that inhibit phosphatidylinositol 3-kinase gamma (PI3K?) and phosphatidylinositol 3-kinase gamma (PI3K?) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Abstract: A compound of Formula (Ia) or (Ib), or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Abstract: A compound of Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device including the same are disclosed: In Chemical Formula 1, each substituent is the same as defined in the detailed description.

Abstract: The present invention relates to fluorophenyl substituted muscarinic receptor ligands with selectivity for M3 over M2 and to the use of these compounds in the treatment of various diseases such as asthma, chronic obstructive pulmonary disease (COPD), bronchopulmonary dysplasia (BPD) and urinary incontinence.

Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

Abstract: Present invention provides bifunctional compounds that comprise an E3 Ubiquitin Ligase moiety that is linked to a moiety that inhibit EGFR, where the target protein can be proximate to the ubiquitin ligase to effect degradation of said protein. Present compounds are useful for the treatment of various cancers.

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.

Abstract: The present invention relates to small molecule compounds and their use as HDAC inhibitors and their use in the treatment of various diseases, such as cancer. The present invention further relates to methods for improvement of solubility by introducing basic substituents which offer the opportunity to create pharmaceutically acceptable salts. Moreover, it comprises methods of synthesizing the compounds and methods of treatment.

Abstract: Compounds having a structure according to formula (I) where R1 and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Abstract: Provided herein are co-crystal forms, and compositions thereof, useful as inhibitors of one or more protein kinases and which exhibit desirable characteristics for the same.

Abstract: The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt thereof, and the compound according to the present invention can be usefully used for the prevention or treatm ent of diseases which are associated with kinase inhibitory actions.

Abstract: The present invention relates to novel solid forms of compound (I), 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

Abstract: The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.

Abstract: The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.

Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.