74701-35-2Relevant academic research and scientific papers
SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
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Page/Page column 32, (2008/12/04)
Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 392 - 395 (2008/09/17)
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
A facile synthesis of α,α′-bis(substituted-benzylidene)-cycloalkanones and substituted-benzylidene heteroaromatics: utility of NaOAc as a catalyst for aldol-type reaction
Motiur Rahman,Jeong, Byeong-Seon,Kim, Dong Hyeon,Park, Jung Ki,Lee, Eung Seok,Jahng, Yurngdong
, p. 2426 - 2431 (2007/10/03)
Utility of NaOAc in glacial HOAc as a catalyst for aldol-type condensation reactions was examined. Reactions of cycloalkanones and selected heteroaromatics with various aldehydes in the presence of NaOAc in glacial HOAc provided α,α′-bis(substituted-benzylidene)cycloalkanones and substituted-benzylidene heteroaromatics, respectively, in good yields.
Synthesis, characterization and electroluminescence properties of new iridium complexes based on cyclic phenylvinylpyridine derivatives: Tuning of emission colour and efficiency by structural control
Takizawa, Shin-Ya,Sasaki, Yuka,Akhtaruzzaman,Echizen, Hidenori,Nishida, Jun-Ichi,Iwata, Takeshi,Tokito, Shizuo,Yamashita, Yoshiro
, p. 841 - 849 (2008/02/04)
A series of phosphorescent cyclometalated iridium(iii) complexes 4-6 with new ligands of bicyclic phenylvinylpyridines have been synthesized and systematically examined for their photophysical, electrochemical and electroluminescence (EL) properties. All
Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
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Page/Page column 21, (2010/02/05)
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines of the formula I, in which A, R1, R2, R3, R4, R5 and n have the meanings indicated in the claims. The compounds of fo
β-Amino Ketones as Key Intermediates in the Synthesis of Pyridines: A Novel and Efficient Route to Annelated Bi- and Terpyridines
Westerwelle, Ulrich,Esser, Achim,Risch, Nikolaus
, p. 571 - 576 (2007/10/02)
The hydrochlorides of β-amino ketones 1a-e (Mannich bases) are easily obtained starting compounds for a novel synthesis of pyridines.Condensation with the heteroaromatic ketones 8, 9, and 10 yields 5,6-dihydro-1,10-phenanthrolines 3a-d, 13 and 4,5-diazafluorenes 4a-d, which have not yet been described in literature.Symmetrical terpyridines 3e, 4e are formed in a one-step reaction of 8, 9 with dimethylmethylenammonium chloride in the presence of an ammonia source.
Polyaza Cavity Shaped Molecules. Annelated Derivatives of 2-(2'-Pyridyl)-1,8-naphthyridine and 2,2'-Bi-1,8-naphthyridine
Thummel, Randolph P.,Lefoulon, Francois,Cantu, David,Mahadevan, Ramanathan
, p. 2208 - 2212 (2007/10/02)
A two-step method is presented for the oxidation of the 2-methylene position of 2,3-cycloalkenopyridines.The pyridyl ketones thus obtained may be reacted with 2-aminonicotinaldehyde to yield 3,3'-annelated derivatives of 2-(2'-pyridyl)-1,8-naphthyridine.T
