68293-39-0

Usage

Physical form

White solid
The appearance of the compound in its pure state.

Molar mass

216.27 g/mol
The mass of one mole of the compound, expressed in grams.

Use in pharmaceutical industry

Intermediate in drug synthesis
HHSIA is utilized as a precursor in the production of various drugs, particularly those targeting the central nervous system.

Potential properties

Anti-inflammatory and analgesic
HHSIA is known for its possible ability to reduce inflammation and relieve pain.

Structural uniqueness

Valuable building block for complex organic molecules
The compound's structure makes it an important component in the synthesis of intricate organic compounds.

Precautions

Health and environmental risks
HHSIA may pose dangers to human health and the environment if not handled and managed properly.

InChI:InChI=1/C14H16O2/c15-14(16)8-13-11-5-1-3-9(11)7-10-4-2-6-12(10)13/h7H,1-6,8H2,(H,15,16)

Upstream product

• 63089-56-5 1,2,3,5,6,7-hexahydro-s-indacen-4-yl-amine 
• 108722-46-9 4-bromo-1,2,3,5,6,7-hexahydro-s-indacene 
• 495-52-3 s-hydrindacene 
• 14927-64-1 3,5,6,7-tetrahydro-2H-s-indacen-1-one 
• 39105-39-0 3-chloro-1-(2,3-dihydro-1H-inden-5-yl)propan-1-one 
• 496-11-7 INDANE 
• 65935-64-0 4-(chloromethyl)-s-hydrindacene 
• 68293-35-6 (s-4-hydrindacen-4-yl)acetonitrile 

Downstream Products

• 68293-52-7 N,N-Dimethyl-1(s-hydrindacen-4-yl)-2-methyl-2-propylamin 

Relevant academic research and scientific papers

SULFONAMIDE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of Formula (I) or (II): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

NLRP3 INHIBITORS

The present application relates to compounds with NLRP3inhibitory activity and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present application further relates to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3inhibition.

Discovery of N-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors

NLRP3 inflammasome mediated release of interleukin-1β (IL-1β) has been implicated in various diseases. In this study, rationally designed mimics of sulfonylurea moiety were investigated as NLRP3 inhibitors. Our results culminated into discovery of series of unprecedented N-cyano sulfoximineurea derivatives as potent NLRP3 inflammasome inhibitors. Compound 15 (IC50 = 7 nM) and analogues were found to be highly potent and selective NLRP3 inflammasome inhibitor with good pharmacokinetic profile. These effects translate in vivo, as 15, 29, and 34 significantly inhibit NLRP3 dependent IL-1β secretion in mice.

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.

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 or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

NOVEL COMPOUNDS

The present invention relates to substituted 5-membered nitrogen containing heteroaryl compounds, such as sulfonyl triazoles, where the heteroaryl ring is further substituted, optionally via a linking group such as -NH-, with a cyclic group which in turn is substituted at the α-position. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

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.