C07D453/02

HEPATITIS B CORE PROTEIN MODULATORS

The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

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NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

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RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND PREPARATION METHOD AND USE THEREOF

The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).

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RHO-ASSOCIATED PROTEIN KINASE INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND PREPARATION METHOD AND USE THEREOF

The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).

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METHODS FOR EXTRACTION, PROCESSING, AND PURIFICATION OF A SELECTED FAMILY OF TARGET COMPOUNDS FROM CANNABIS

Disclosed are methods for separating, recovering, and purifying cannabidiolic acid (CBDA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in C5-C7 hydrocarbon solvents, adding thereto a selected amine to thereby precipitate a CBDA-amine salt therefrom, dissolving the recovered CBDA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified CBDA-amine salt therefrom. The recrystallized CBDA-amine salt may be decarboxylated to form a mixture of cannabidiol (CBD) and amine. The CBD amine mixture may be acidified to separate the amine from CBD. Also disclosed are CBDA-amine salts produced with certain amines selected from groups of secondary amines, tertiary amines, diamines, amino alcohols, amino ethers, and highly basic amines.

QUINUCLIDINONE ANALOGUES AS ANTICANCER AGENTS
20230089530 · 2023-03-23 ·

The disclosure includes compounds of Formula (I) and Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, m, n, k, and L are defined herein. Also disclosed are methods for treating a neoplastic disease, autoimmune disease, or an inflammatory disorder with these compounds.

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QUINUCLIDINONE ANALOGUES AS ANTICANCER AGENTS
20230089530 · 2023-03-23 ·

The disclosure includes compounds of Formula (I) and Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, m, n, k, and L are defined herein. Also disclosed are methods for treating a neoplastic disease, autoimmune disease, or an inflammatory disorder with these compounds.

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2-HETEROARYL AMINOQUINAZOLINONE DERIVATIVE

Provided is a 2-heteroaryl aminoquinazolinone derivative, which is a compound represented by formula (1):

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or a pharmaceutically acceptable salt thereof wherein X.sup.1 represents CR.sup.1 or N, X.sup.2 represents CR.sup.2 or N, X.sup.3 represents CR.sup.3 or N, X.sup.4 represents CR.sup.4 or N, Y represents optionally substituted C.sub.1-6 alkyl, an optionally substituted C.sub.3-10 alicyclic group, an optionally substituted 4- to 10-membered nitrogen-containing non-aryl heterocycle, optionally substituted C.sub.6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl, Z represents optionally substituted 6- to 10-membered heteroaryl, and R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each independently represent a hydrogen atom, halogen, cyano, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.1-6 alkoxy, or the like.

TRICYCLIC DEGRADERS OF IKAROS AND AIOLOS

Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.