495-52-3

Usage

Uses

s-Hydrindacene is a useful building block for organic synthesis.

Upstream product

• 14927-64-1 3,5,6,7-tetrahydro-2H-s-indacen-1-one 
• 6555-87-9 3,6-Dihydrobenzo<1,2:4,5>dicyclopentene 
• 4228-10-8 1-indan-5-yl-ethanone 
• 30084-91-4 indan-5-carbaldehyde 
• 113364-52-6 3-(3-oxo-2,3-dihydro-1H-inden-5-yl)propanoic acid 
• 113364-54-8 1-(2-indan-5-yl-2-oxo-ethyl)-pyridinium; iodide 
• 35288-49-4 p-phenylenediacrylic diacid dichloride 
• 86031-43-8 methyl 5-indanecarboxylate 
• 23291-98-7 3-(2.3-Dihydro-1H-inden-5-yl)-propanoic acid 
• 65898-38-6 indan-5-carboxylic acid 
• 7549-44-2 dimethyl-1,4-phenylenediacrylate 
• 4251-21-2 3,3'-(1,4-phenylene)dipropanoic acid 
• 496-11-7 INDANE 
• 56635-88-2 3-(5-Indanyl)-prop-2-ensaeure 

Downstream Products

• 65935-69-5 Benzyl-(1,2,3,5,6,7-hexahydro-s-indacen-4-ylmethyl)-methyl-amine 
• 68293-39-0 2-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)acetic acid 

Relevant academic research and scientific papers

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 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 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.

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.

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.

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.

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 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.

Electron Paramagnetic Resonance Spectra of the Radical Cations of Some Benzocyclobutenes, Benzocyclopentenes and Benzocyclohexenes

1,2,4,5-Tetrahydrobenzodicyclobutene, 1,2,3,5,6,7-hexahydrobenzodicyclopentene and 1,2,3,4,6,7,8,9-octahydrobenzodicyclohexene, and their dimethyl derivatives, and tetramethylbenzocyclo-butene, -pentene and -hexene have been prepared.All except the first compound have been oxidised to their corresponding radical cations, and the EPR spectra have been analysed by assigning McConnell-type Q-values to the substituents in the benzene ring.It is suggested that the ordering of the orbital energy levels (ΨA above ΨS) in 3,6-dimethylbenzobiscyclobutene and -pentene is a manifestation of the Mills-Nixon effect, and results from rehybridisation of the strained molecular framework.In the radical cations of 5,10-dimethyl-1,2,3,4,6,7,8,9-octahydrobenzodicyclohexene and 5,6,7,8-tetramethyl-1,2,3,4-tetrahydrobenzocyclohexene the total unpaired electron density, as implied by the McConnell type of relationship, appears to be less than unity.Various possible causes of this are examined.