220107-35-7Relevant academic research and scientific papers
AGONISTS OF THE APELIN RECEPTOR AND METHODS OF USE THEREOF
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Paragraph 0361; 0362; 0363, (2015/12/31)
Provided herein are small molecule agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.
Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics
Stiff, Cory,Graber, David R.,Thorarensen, Atli,Wakefield, Brian D.,Marotti, Keith R.,Melchior, Earline P.,Sweeney, Michael T.,Han, Fusen,Rohrer, Douglas C.,Zurenko, Gary E.,Romero, Donna L.
scheme or table, p. 6293 - 6297 (2009/07/18)
The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein.
Cyclic derivatives as modulators of chemokine receptor activity
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Page/Page column 41, (2008/06/13)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 38; 39, (2010/02/11)
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
SUBSTITUTED AMINO PHENYLACETIC ACIDS, DERIVATIVES THEREOF, THEIR PREPARATION AND THEIR USE AS CYCLOOXYGENASE 2 (COX-2) INHIBITORS
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Page 52-53, (2008/06/13)
Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
Trifluoromethoxy substituted anilines: Metalation as the key step for structural elaboration
Leroux, Frederic,Castagnetti, Eva,Schlosser, Manfred
, p. 4693 - 4699 (2007/10/03)
Trifluoromethoxy-substituted anilines undergo hydrogen/lithium permutation ("metalation") with optional site selectivity depending on the N-protective group employed. N-tert-Butoxycarbonyl-2-and -4-(trifluoromethoxy)aniline react with tert-butyllithium at
Thiazolobenzoheterocycles, preparation and medicines containing same
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, (2010/01/31)
Disclosed are thiazolobenzoheterocycles of the general formula STR1Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them. Also disclosed are novel intermediates for preparing the foregoing compounds, these intermediates having the formula STR2
1,2-Didehydro-3- and -4-(trifluoromethoxy)benzene: The "aryne" route to 1- and 2-(trifluoromethoxy)naphthalenes
Schlosser, Manfred,Castagnetti
, p. 3991 - 3997 (2007/10/03)
Upon treatment of 1-bromo-2-(trifluoromethoxy)benzene with lithium diisopropylamide (LIDA) at -100°C, 3-bromo-2-(trifluoromethoxy)phenyllithium is generated. It can be trapped as such, but isomerizes to afford 2-bromo-6-(trifluoromethoxy)phenyllithium whe
