88304-58-9Relevant academic research and scientific papers
HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00189, (2016/04/09)
The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject
UREA COMPOUNDS AND THEIR USE AS FAAH ENZYME INHIBITORS
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Page/Page column 39; 59, (2015/02/25)
A compound having Formula (I): wherein: R1 is selected from hydrogen, halogen, hydroxyl and C1-4 alkoxy; R2 is selected from hydrogen, halogen, hydroxyl and C1-4 alkoxy; R3 is C1-4 alkyl; R4 is aryl which is substituted with a group selected from OSO2NH2, NHCONH2, NHSO2NH2, NHSO2C1-4 alkyl and CONH2; and n is 0 or 1; or a pharmaceutically acceptable salt thereof; provided that the compound is not N-(1-benzylpiperidin-4-yl)-N-methyl-4-(4-(sulfamoylamino)phenyl)-1H-imidazole-1-carboxamide or N-(1-benzylpiperidin-4-yl)-N-methyl-4-(3-(methylsulfonamido)phenyl)-1H-imidazole-1-carboxamide. The compound may be used as an inhibitor of fatty acid amide hydrolase.
IDO inhibitors
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Page/Page column 204; 206, (2015/11/27)
Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for mod
Synthesis and histamine H3 and H4 receptor activity of conformationally restricted cyanoguanidines related to UR-PI376
Geyer, Roland,Buschauer, Armin
scheme or table, p. 775 - 785 (2012/03/12)
Recently, we identified highly potent agonists of the human histamine H4 receptor (hH4R) among a series of imidazolylbutylcyanoguanidines. Aiming at improved selectivity for the hH 4R relative to the H3 receptor
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase
Kumar, Sanjeev,Jaller, Daniel,Patel, Bhumika,LaLonde, Judith M.,DuHadaway, James B.,Malachowski, William P.,Prendergast, George C.,Muller, Alexander J.
experimental part, p. 4968 - 4977 (2009/07/11)
Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathological immune suppression. With the goal of developing more potent IDO in
Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
, p. 2390 - 2410 (2007/10/03)
A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.
CARBENIC REACTIONS OF 4-DIAZO-4H-IMIDAZOLE WITH BENZENE DERIVATIVES
Amick, T. J.,Shechter, H.
, p. 901 - 904 (2007/10/02)
The electrophilic behavior of 4H-imidazolylidene is greatly modified by coordinating groups in benzene derivatives undergoing substitution.
(Imidazolylphenyl)formamidines. A structurally novel class of potent histamine H2 receptor antagonists
Donetti,Cereda,Bellora,Gallazzi,Bazzano,Vanoni,Del Soldato,Micheletti,Pagani,Giachetti
, p. 380 - 386 (2007/10/02)
Structure-activity considerations of N(α)-guanylhistamine, the first compound found with detectable H2-antagonist activity, led to the synthesis of a series of conformationally rigid guanylhistamine analogues, namely (imidazolylphenyl)guanidine
