51660-15-2Relevant academic research and scientific papers
Cyclopentyl-pyrimidine based analogues as novel and potent IGF-1R inhibitor
Aware, Valmik,Gaikwad, Nitin,Chavan, Sambhaji,Manohar, Sonal,Bose, Julie,Khanna, Smriti,B-Rao, Chandrika,Dixit, Neeta,Singh, Kishori Sharan,Damre, Anagha,Sharma, Rajiv,Patil, Sambhaji,Roychowdhury, Abhijit
supporting information, p. 246 - 256 (2015/05/26)
A series of novel 2-amino-4-pyrazolecyclopentylpyrimidines have been prepared and evaluated as IGF-1R tyrosin kinase inhibitors. The in vitro activity was found to depend strongly on the substitution pattern in the 2-amino ring, 4-pyrazolo moieties and size of fused saturated ring with the central pyrimidine core. A stepwise optimization by combination of active fragments led to discovery of compound 6f and 6k, two structures with IGF-1R IC50 of 20 nM and 10 nM, respectively. 6f was further profiled for its anti cancer activity across various cell lines and pharmacokinetic studies in Sprague Dawley rats.
HETEROARYL INHIBITORS OF PDE4
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Paragraph 0898, (2014/05/24)
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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Page/Page column 205, (2012/06/15)
The invention is directed 10 Compound's of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
BENZOXAZEPINES BASED P13K/MT0R INHIBITORS AGAINST PROLIFERATIVE DISEASES
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Page/Page column 197, (2010/12/18)
The invention is directed to compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Carboxylic acid derivatives, their preparation and use in treating cancer
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, (2008/06/13)
This invention provides a method for treating cancer in an individual, wherein the cancer is a tumor in which endothelin is upregulated (e.g. tumors of the prostate, lung, liver, breast, brain, stomach, colon, endometrium, testicle, thyroid, pituatary, bladder, kidney, pancreas and meninges) by administering to the individual an effective amount of a compound of Formula I or Formula Ia, as describe herein.
