Discovery of disubstituted imidazo[4,5- b ]pyridines and purines as potent TrkA inhibitors
Trk receptor tyrosine kinases have been implicated in cancer and pain. A crystal structure of TrkA with AZ-23 (1a) was obtained, and scaffold hopping resulted in two 5/6-bicyclic series comprising either imidazo[4,5-b]pyridines or purines. Further optimization of these two fusion series led to compounds with subnanomolar potencies against TrkA kinase in cellular assays. Antitumor effects in a TrkA-driven mouse allograft model were demonstrated with compounds 2d and 3a.
Wang, Tao,Lamb, Michelle L.,Block, Michael H.,Davies, Audrey Molina,Han, Yongxin,Hoffmann, Ethan,Ioannidis, Stephanos,Josey, John A.,Liu, Zhong-Ying,Lyne, Paul D.,MacIntyre, Terry,Mohr, Peter J.,Omer, Charles A.,Sjoegren, Tove,Thress, Kenneth,Wang, Bin,Wang, Haiyun,Yu, Dingwei,Zhang, Hai-Jun
The present invention relates to pyridinyl and pyrazinyl-(aza)indolsulfonamides having GPR17 modulator activity. The compounds have utility in the treatment of a variety of GPR17-associated disorders.
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Page/Page column 59; 66
(2020/01/11)
IMIDAZOPYRIDINE DERIVATIVES AS PI3K INHIBITORS
New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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Page/Page column 107
(2012/11/13)
5-AMINOPYRAZOL-3-YL-3H-IMIDAZO [4,5-B] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These novel compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 67-68
(2008/12/08)
9- (PYRAZOL- 3 -YL) - 9H- PURINE-2 -AMINE AND 3- (PYRAZ0L-3-YL) -3H-IMIDAZ0 [4, 5-B] PYRIDIN-5-AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
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Page/Page column 64-65
(2009/01/20)
CHEMICAL COMPOUNDS
This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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Page/Page column 54
(2008/06/13)
PYRAZOLYLAMINOPYRIDINE DERIVATIVES USEFUL AS KINASE INHIBITORS
This invention relates to novel compounds having the Formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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Page/Page column 101
(2008/06/13)
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