154404-97-4Relevant academic research and scientific papers
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors
Fairhurst, Robin A.,Gerspacher, Marc,Imbach-Weese, Patricia,Mah, Robert,Caravatti, Giorgio,Furet, Pascal,Fritsch, Christine,Schnell, Christian,Blanz, Joachim,Blasco, Francesca,Desrayaud, Sandrine,Guthy, Daniel A.,Knapp, Mark,Arz, Dorothee,Wirth, Jasmin,Roehn-Carnemolla, Esther,Luu, Van Huy
, p. 3575 - 3581 (2015)
Abstract A cyclisation within a 4′,5-bisthiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors led to a novel 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole tricyclic sub-series. The synthesis and optimisation of this 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole sub-series and the expansion to a related tricyclic 4,5-dihydrothiazolo[4,5-h]quinazoline sub-series are described. From this work analogues including 11, 12, 19 and 23 were identified as potent and selective PI3Kα inhibitor in vivo tool compounds.
UREA DERIVATIVE HAVING PI3K INHIBITORY ACTIVITY
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Page/Page column 119-120, (2012/03/26)
Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
2-Carboxamide Cycloamino Ureas
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Page/Page column 16, (2011/01/12)
The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
McIntyre, Neil A.,McInnes, Campbell,Griffiths, Gary,Barnett, Anna L.,Kontopidis, George,Slawin, Alexandra M. Z.,Jackson, Wayne,Thomas, Mark,Zheleva, Daniella I.,Wang, Shudong,Blake, David G.,Westwood, Nicholas J.,Fischer, Peter M.
supporting information; experimental part, p. 2136 - 2145 (2010/08/07)
Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- and 2-amino-N-aryl-4,5-dihydr
THIAZOLYL-DIHYDRO-CHINAZOLINE
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Page/Page column 27, (2008/06/13)
Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
THIAZOLYL-DIHYDRO-QUINAZOLINE
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Page/Page column 14, (2008/06/13)
Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.
PI3 KINASES
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Page/Page column 129, (2008/06/13)
The invention relates to the novel compounds of formula (1), which, due to their pharmaceutical effect as PI3 kinase modulators, are suitable for use in the therapy and treatment of inflammatory or allergic diseases. Examples of these diseases are inflammatory and allergic respiratory diseases, inflammatory diseases of the gastro-intestinal system and of the locomotor apparatus, inflammatory and allergic skin diseases, inflammatory ophthalmic diseases, diseases of the nasal mucosa, inflammatory or allergic autoimmune reactive conditions, or renal inflammations.
