914358-73-9Relevant academic research and scientific papers
HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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, (2016/05/02)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
5-Alkynyl-pyridines
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, (2013/03/26)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification
NEW 5-ALKYNYL-PYRIDINES
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, (2013/03/26)
5-alkynyl-pyridine of general formula (I) which are inhibitors of the activity of PI3K alpha, and their use in the treatment of diseases characterized by excessive or abnormal cell proliferation, such as cancer.
PYRAZOLOPIPERIDINE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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, (2012/07/13)
Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
NEW 5-ALKYNYL-PYRIDINES
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, (2012/08/08)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
NEW 5-ALKYNYL-PYRIDINES
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, (2012/08/08)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of P13Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
N1/N2-Lactam Acetyl-CoA carboxylase inhibitors
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, (2012/05/07)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors
D'Angelo, Noel D.,Kim, Tae-Seong,Andrews, Kristin,Booker, Shon K.,Caenepeel, Sean,Chen, Kui,D'Amico, Derin,Freeman, Dan,Jiang, Jian,Liu, Longbin,McCarter, John D.,San Miguel, Tisha,Mullady, Erin L.,Schrag, Michael,Subramanian, Raju,Tang, Jin,Wahl, Robert C.,Wang, Ling,Whittington, Douglas A.,Wu, Tian,Xi, Ning,Xu, Yang,Yakowec, Peter,Yang, Kevin,Zalameda, Leeanne P.,Zhang, Nancy,Hughes, Paul,Norman, Mark H.
, p. 1789 - 1811 (2011/05/16)
Phosphoinositide 3-kinase α (PI3K-α) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of multiple tumor types. Consequently, PI3K- has become a target of intense research for drug discovery. Our studies began with the identification of benzothiazole compound 1 from a high throughput screen. Extensive SAR studies led to the discovery of sulfonamide 45 as an early lead, based on its in vitro cellular potency. Subsequent modifications of the central pyrimidine ring dramatically improved enzyme and cellular potency and led to the identification of chloropyridine 70. Further arylsulfonamide SAR studies optimized in vitro clearance and led to the identification of 82 as a potent dual inhibitor of PI3K and mTOR. This molecule exhibited potent enzyme and cell activity, low clearance, and high oral bioavailability. In addition, compound 82 demonstrated tumor growth inhibition in U-87 MG, A549, and HCT116 tumor xenograft models.
N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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, (2011/05/16)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions there-of; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal
N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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, (2011/06/16)
The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
