- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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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.
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Page/Page column 445; 446
(2019/02/13)
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- Synthesis of New 1,3-Thiazolecarbaldehydes
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H-Lithiation and Br-lithiation reactions of 1,3-thiazole were studied in order to obtain new thiazole derivatives. Four isomeric chloromethyl derivatives of 1,3-thiazole containing a protected aldehyde group like 2-(1,3-dioxolan-2-yl)-5-(chloromethyl)-1,3-thiazole, 5-(1,3-dioxolan-2-yl)-2-(chloromethyl)-1,3-thiazole, 4-(1,3-dioxolan-2-yl)-2-(chloromethyl)-1,3-thiazole, and 2-(1,3-dioxolan-2-yl)-4-(chloromethyl)-1,3-thiazole were synthesized. Their nucleophilic substitution reactions with dimethylamine and sodium methylthiolate were studied. New aldehydes of 1,3-thiazole series of low-molecular weight were obtained.
- Sinenko,Slivchuk,Mityukhin,Brovarets
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p. 2766 - 2775
(2018/02/21)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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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.
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Page/Page column 185; 186
(2017/11/15)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Paragraph 1248
(2015/02/18)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
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Page/Page column 273; 274
(2015/02/02)
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- The characterization of a novel V1b antagonist lead series
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The SAR around a V1b antagonist HTS hit 3 was explored to produce a series of thiazole sulfonamides as a lead series with selectivity over the related V1 and oxytocin receptors.
- Smethurst, Chris A.,Borthwick, Jennifer A.,Gaines, Simon,Watson, Steve,Green, Andrew,Schulz, Mark J.,Burton, George,Buson, Alberto A.,Arban, Roberto
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scheme or table
p. 92 - 96
(2011/02/28)
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- Total synthesis of cystothiazole A by microwave-assisted olefin cross-metathesis
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A short and convergent synthesis of the myxobacterial antibiotic cystothiazole A by a microwave-assisted olefin crossmetathesis reaction and a sequential microwave-assisted cross-metathesis/Stille coupling is described. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Gebauer, Julian,Arseniyadis, Stellios,Cossy, Janine
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experimental part
p. 2701 - 2704
(2009/04/07)
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- BIARYL COMPOUNDS USEFUL AS AGONISTS OF THE GPR38 RECEPTOR
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The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal dis
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Page/Page column 30
(2008/06/13)
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- 4-[(4-(CARBOXYETHYL) PIPERIDINYL) METHYL] PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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3-Substituted pyrrolidines having a 4-carboxypiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- Asymmetric synthesis of (1R,2S,3R)-2-acetyl-4-(1,2,3,4- tetrahydroxybutyl)thiazole
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Two different methods for preparing the thiazole analogue 3 of the biologically active compound (1R,2S,3R)-2-acetyl-4(5)-(1,2,3,4- tetrahydroxybutyl)imidazole 1 are reported.
- Ung, Alison T.,Pyne, Stephen G.
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p. 1395 - 1407
(2007/10/03)
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- Pyrethrinoid esters of thiazole alcohols
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In all possible stereoisomer forms and mixtures thereof of the formula STR1 wherein one of R1, R2 or R3 is: STR2
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