31437-05-5Relevant articles and documents
The synthesis of 2-amino-4(3H)-quinazolinones and related heterocycles via a mild electrocyclization of aryl guanidines
Sales, Zachary S.,Mani, Neelakandha S.,Allison, Brett D.
supporting information, p. 1623 - 1626 (2018/03/29)
A new method for the preparation of 2-amino-4(3H)-quinazolinones and similar fused heterocycles is described. Simply warming a mixture of an aryl guanidine and carbonyl diimidazole in acetonitrile results in formation of a putative N-amidinoisocyanate intermediate which undergoes a 6π-electron electrocyclic reaction with the aryl ring to generate the quinazolinone ring system. The mild conditions are compatible with a variety of functional groups, and the reaction is shown to be successful on multigram scale.
NOVEL ANTIPRION COMPOUNDS
-
Paragraph 0648; 0649; 0704, (2013/03/28)
Described herein are novel compositions and methods of treatment addressing diseases such as neurodegenerative diseases, including prion diseases and Alzheimer's disease.
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION
-
Paragraph 0123; 0124; 0125, (2013/04/24)
Pharmaceutical compositions of the invention are presented which comprise substiuted aminothiazoles derivatives. The substiuted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
2-aminothiazoles as therapeutic leads for prion diseases
Gallardo-Godoy, Alejandra,Gever, Joel,Fife, Kimberly L.,Silber, B. Michael,Prusiner, Stanley B.,Renslo, Adam R.
experimental part, p. 1010 - 1021 (2011/04/25)
2-Aminothiazoles are a new class of small molecules with antiprion activity in prion-infected neuroblastoma cell lines (J. Virol. 2010, 84, 3408). We report here structure-activity studies undertaken to improve the potency and physiochemical properties of 2-aminothiazoles, with a particular emphasis on achieving and sustaining high drug concentrations in the brain. The results of this effort include the generation of informative structure-activity relationships (SAR) and the identification of lead compounds that are orally absorbed and achieve high brain concentrations in animals. The new aminothiazole analogue (5-methylpyridin-2-yl)-[4-(3-phenylisoxazol-5-yl)-thiazol-2-yl]-amine (27), for example, exhibited an EC50 of 0.94 μM in prion-infected neuroblastoma cells (ScN2a-cl3) and reached a concentration of ～25 μM in the brains of mice following three days of oral administration in a rodent liquid diet. The studies described herein suggest 2-aminothiazoles as promising new leads in the search for effective therapeutics for prion diseases.
THIAZOLE DERIVATIVES AND USE THEREOF
-
Page/Page column 50-51, (2010/11/25)
The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
Das, Jagabandhu,Furch, Joseph A.,Liu, Chunjian,Moquin, Robert V.,Lin, James,Spergel, Steven H.,McIntyre, Kim W.,Shuster, David J.,O'Day, Kathleen D.,Penhallow, Becky,Hung, Chen-Yi,Doweyko, Arthur M.,Kamath, Amrita,Zhang, Hongjian,Marathe, Punit,Kanner, Steven B.,Lin, Tai-An,Dodd, John H.,Barrish, Joel C.,Wityak, John
, p. 3706 - 3712 (2007/10/03)
A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound 3 is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma.
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential
Press, Neil J.,Taylor, Roger J.,Fullerton, Joseph D.,Tranter, Pamela,McCarthy, Clive,Keller, Thomas H.,Brown, Lyndon,Cheung, Robert,Christie, Julie,Haberthuer, Sandra,Hatto, Julia D.I.,Keenan, Mark,Mercer, Mark K.,Press, Nicola E.,Sahri, Helene,Tuffnell, Andrew R.,Tweed, Morris,Fozard, John R.
, p. 3081 - 3085 (2007/10/03)
The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.
INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
-
Page 33-34, (2008/06/13)
Compounds of formula (I) in free or salt form, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinos
Aminothaizoles and their use as adenosine receptor antagonists
-
, (2008/06/13)
Compounds of formula (I) in free or salt form, where A is a C6-C15 monovalent aromatic group. R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C
