78686-83-6Relevant articles and documents
AZAQUINOLONE BASED COMPOUNDS EXHIBITING PROLYL HYDROXYLASE INHIBITORY ACTIVITY, COMPOSITIONS, AND USES THEREOF
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, (2008/12/06)
Compounds of Formula (I) are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein.
QUINOLONES AND AZAQUINOLONES THAT INHIBIT PROLYL HYDROXYLASE
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, (2008/12/08)
Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
Inhibitors of protein tyrosine phosphatase 1B
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Page/Page column 13; 33, (2008/06/13)
Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
2-(Alkylamino)nicotinic Acid and Analogs. Potent Angiotensin II Antagonists
Winn, Martin,De, Biswanath,Zydowsky, Thomas M.,Altenbach, Robert J.,Basha, Fatima Z.,et al.
, p. 2676 - 2688 (2007/10/02)
A series of pyridines and other six-membered ring heterocycles connected to a biphenyltetrazole with a-CH2-NR'-link (1) were discovered to be potent angiotensin II antagonists.In the pyrimidine carboxylic acid series (W = CR, X = N, Y = CH, Z = COOH), compounds with an alkyl group (R') on the exocyclic nitrogen were much more potent than compounds with an alkyl group (R) on the heterocyclic ring.The corresponding pyridine, pyridazine, pyrazine, and 1,2,4-triazine carboxylic acids also showed potent in vitro angiotensin II antagonism.The pyridine (W, X, Y = CH, Z = COOH, R' = n-C3H7) demonstrated potent in vitro activity (pA2 = 10.10, rabbit aorta, and Ki = 0.61 nM, receptor binding in rat liver) as well as exceptional oral antihypertensive activity and bioavailability.Any nonacidic replacement for the carboxylic acid was detrimental for activity.
Angiotensin II receptor antagonists
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, (2008/06/13)
Compounds are disclosed having the formula: STR1 The compounds of the invention are angiotensin II receptor antagonists.
Some Methyl 2,5- and 5,6-Dihalonicotinates
Setliff, Frank L.,Hule, W. Reeves
, p. 332 - 333 (2007/10/02)
The preparation of the methyl esters of eight dihalonicotinic acids is described.The esters were synthesized either by the methanolysis of their respective acid chlorides or by treatment of the appropriate acid with diazomethane in ether.Experimental and spectral data for the methyl dihalonicotinates are presented.