905587-16-8Relevant articles and documents
2-(IMIDAZ0LYLAMIN0)-PYRIDINE DERIVATIVES AND THEIR USE AS JAK KINASE INHIBITORS
-
Page/Page column 65, (2010/04/03)
The present inv ention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Ring A is 5- or 6-membered heteroaryl, wherein said 5- or 6-membered heteroaryl is optionally substituted on carbon with one or more R6
CHEMICAL COMPOUNDS 000-1
-
Page/Page column 55, (2009/04/25)
The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors
Ioannidis, Stephanos,Lamb, Michelle L.,Davies, Audrey M.,Almeida, Lynsie,Su, Mei,Bebernitz, Geraldine,Ye, Minwei,Bell, Kirsten,Alimzhanov, Marat,Zinda, Michael
scheme or table, p. 6524 - 6528 (2010/05/18)
The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds.
PYRAZOLYL-AMINO-SUBSTITUTED PYRIMIDINES AND THEIR USE FOR THE TREATMENT OF CANCER
-
, (2008/12/08)
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.
PYRAZOLYL-AMINO-SUBSTITUTED PYRAZINES AND THEIR USE FOR THE TREATMENT OF CANCER
-
, (2008/12/04)
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.
5-AMINOPYRAZOL-3-YL-3H-IMIDAZO [4,5-B] PYRIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
-
, (2008/12/08)
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.
AMINO-THIAZOLYL- PYRIMIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
-
, (2009/01/20)
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.
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
-
, (2009/01/20)
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.
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases
Wang, Tao,Lamb, Michelle L.,Scott, David A.,Wang, Haixia,Block, Michael H.,Lyne, Paul D.,Lee, John W.,Davies, Audrey M.,Zhang, Hai-Jun,Zhu, Yanyi,Gu, Fei,Han, Yongxin,Wang, Bin,Mohr, Peter J.,Kaus, Robert J.,Josey, John A.,Hoffmann, Ethan,Thress, Ken,MacIntyre, Terry,Wang, Haiyun,Omer, Charles A.,Yu, Dingwei
experimental part, p. 4672 - 4684 (2009/07/25)
The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput screening identified a promising hit in the 4- aminopyrazolylpyrimidine chemotype. Initial optimization of the series led to more potent Trk inhibitors. Further optimization using two strategies resulted in significant improvement of physical properties and led to the discovery of 10z (AZ-23), a potent, orally bioavailable Trk A/B inhibitor. The compound offers the potential to test the hypothesis that modulation of Trk activity will be of benefit in the treatment of cancer and other indications in vivo.
CHEMICAL COMPOUNDS
-
, (2010/11/25)
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.