153625-24-2

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Relevant academic research and scientific papers

SULFONIMIDAMIDE COMPOUNDS AS NLRP3 MODULATORS

Described herein are compounds of Formula (I), Formula (I-A), and Formula (I-B), solvates thereof, tautomers thereof, and pharmaceutically acceptable salts of the foregoing, Further described herein are methods of inhibiting NLRP3 using said compounds, and methods of and compositions useful in treating NLRP3-dependent disorders.

AGENT FOR REACTING WITH ACROLEIN, AND USE THEREOF AND NOVEL COMPOUND

PROBLEM TO BE SOLVED: To provide a reaction agent reacting with acrolein for detecting acrolein generated in a cell in a disease related to oxidative stress such as cancer, Alzheimer's and cerebral infarction. SOLUTION: There is provided a compound having a chemical structure represented by formula (1), wherein R1 and R2 each independently represents a hydrogen atom, a halogen atom, or an alkyl group having 1 to 5 carbon atoms which may be substituted with at least one halogen atom, with the proviso that at least one of R1 and R2 is an alkyl group having 1 to 5 carbon atoms; n is an integer of 1 or more and 5 or less; and * is a binding site with a rhodamine-based dye such as 5-carboxytetramethyl rhodamine or 6-carboxytetramethyl rhodamine or derivatives thereof. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT

NLRP MODULATORS

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein, useful to treat connected to the modulation of NRLP3.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

NLRP MODULATORS

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured.The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured. The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.

Ligand variation in alkylidene complexes of the type Mo(CHR)(NR')(OR'')2

A variety of complexes of the type Mo(NR)2Cl2L2 (R=4-Br-2,6-i-Pr2-C6H2, 4-CN-2,6-i-Pr2-C6H2, 3,5-Me2-C6H3, 2-i-Pr-C6H4, 2-CF3-C6H4, 2-Ph-C6H4, and 1-adamantyl; L=1/2 DME or pyridine) have been synthesized by treating 2 with four equivalents of RNH2 in the presence of Me3SiCl and Et3N.They are readily alkylated by Grignard reagents to give complexes of the type Mo(NR)2(CH2R')2 (R=4-Br-2,6-i-Pr2-C6H2, 4-CN-2,6-i-Pr2-C6H2, 2,6-Me2-C6H3, 3,5-Me2-C6H3, 2-t-Bu-C6H4, 2-i-Pr-C6H4, 2-CF3-C6H4, 2-Ph-C6H4, 1-adamantyl, R'=t-Bu or PhMe2C) from which alkylidene complexes of the type Mo(NR)(CHR')(OTf)2(DME) are formed upon addition of triflic acid.Addition of various alkoxides to the triflate complexes yields four-coordinate complexes of the type Mo(NR)(CHR')(OR'')2 (combinations include R=2,6-i-Pr2-C6H3, 4-Br-2,6-iPr2-C6H2, 4-CN-2,6-i-Pr2-C6H2, 2,6-Me2-C6H3, 3,5-Me2-C6H3, 2-t-Bu-C6H4, 2-i-Pr-C6H4, 2-CF3-C6H4, 2-Ph-C6H4, and 1-adamantyl; OR''=OCMe3, OCEt3, O-1-adamantyl, OCHMe2, OCMe2(CF3), OCMe(CF3)2, OC(CF3)3, and OC(CF3)2CF2CF2CF3).