Abstract: A method for synthesizing a compound 2-[(2R,5S)-5-[2-methylfuro[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by taking 7-chloro-6-nitrofuro[3,2-b]pyridine as the starting material, and by nucleophilic substitution, palladium on carbon reduction and cyclization reactions. The present synthesis method has mild reaction conditions, high product yield and high purity, and is suitable for industrial production. A crystal form of the compound, crystal forms of the salts thereof and preparation methods thereof. The crystal form of the compound and the crystal forms of the salts thereof have good physical and chemical properties and are suitable for drug development.

Abstract: Provided are compounds of Formula (I): wherein all of the variables are as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. Disclosed are the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of disease and disorders mediated by NLRP3.

Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.

Abstract: Provided is a method for synthesizing 1H-furo[3,2-b]imidazo[4,5-d]pyridine compounds. The method comprises the following steps of: reacting compound 1 with compound 2 in a solvent in the presence of a base to obtain compound 3; subjecting the compound 3 to a reduction reaction to obtain compound 4; and subjecting the compound 4 to a ring-closing reaction with compound 5 or compound 5? to obtain compound 6 or a hydrate thereof, wherein R is methyl or ethyl, the methyl or ethyl is optionally substituted by hydroxyl, and X?O or CH2. The method for synthesizing the 1H-furo[3,2-b]imidazo[4,5-d]pyridine compound has the advantages of high yield, fewer impurities and is easy to control, saves the cost. The method is simple and convenient to operate, and is suitable for industrial scale.

Abstract: A method for synthesizing a compound 2-[(2R,5S)-5-[2-methylfuro[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitr ile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by taking 7-chloro-6-nitrofuro[3,2-b]pyridine as the starting material, and by nucleophilic substitution, palladium on carbon reduction and cyclization reactions. The present synthesis method has mild reaction conditions, high product yield and high purity, and is suitable for industrial production. A crystal form of the compound, crystal forms of the salts thereof and preparation methods thereof. The crystal form of the compound and the crystal forms of the salts thereof have good physical and chemical properties and are suitable for drug development.

Abstract: Methods relate to treat a central nervous system (CNS) disorder using a compound of Formulae (I)-(III), or a salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative. or prodrug thereof. Methods of treating a CNS disorder using a composition comprising such compounds are also provided herein. The present disclosure also provides a compound of Formula (A), or a salt, solvate, hydrate, polymorph, co-crystal, tautomer, stereoisomer, isotopically labeled derivative, or prodrug thereof.

Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.

Abstract: Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.

Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.

Abstract: A method for synthesizing a compound 2-[(2R,5S)-5-[2-methylfuro[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitr ile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by taking 7-chloro-6-nitrofuro[3,2-b]pyridine as the starting material, and by nucleophilic substitution, palladium on carbon reduction and cyclization reactions. The present synthesis method has mild reaction conditions, high product yield and high purity, and is suitable for industrial production. A crystal form of the compound, crystal forms of the salts thereof and preparation methods thereof. The crystal form of the compound and the crystal forms of the salts thereof have good physical and chemical properties and are suitable for drug development.

Abstract: Provided is a method for synthesizing a compound 2-[(2R,5S)-5-[2-[(R)-1-hydroxyethyl]furo[3,2-b]imidazo[4,5-d]pyridin-1-yl]tetrahydropyran-2-yl]acetonitrile as a selective JAK1/TYK2 kinase inhibitor. The compound is prepared by nucleophilic substitution, palladium on carbon reduction, and cyclization reaction using 7-chloro-6-nitrofuro[3,2-b]pyridine as a starting material. The synthesis method has mild reaction conditions, high product yield, and high purity, and is suitable for industrial production. Further provided are a crystal form of the compound, crystal forma of its salts, and their preparation methods. The crystal form of the compound and the crystal forms of its salts have good physical and chemical properties and are suitable for drug development.

Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.

Abstract: Provided are a compound as represented by structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder.

Abstract: The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.

Abstract: The new arylsulfonamide and arylsulfone derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities and lysosome functions such as acid-related disorders and cancer.

Abstract: The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic diseases or disorders.

Abstract: The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic diseases or disorders.

Abstract: The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.

Abstract: The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic diseases or disorders.

Abstract: The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic diseases or disorders.