884738-96-9Relevant articles and documents
COMPOUNDS USEFUL FOR TREATING DISORDERS RELATED TO RET
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, (2018/02/21)
Described herein are compounds of formula (I) that inhibit wild- type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
HETEROARYL COMPOUNDS AND THEIR USE AS MER INHIBITORS
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Paragraph 1126; 1943, (2018/04/27)
Compounds of formula (I) [Formula should be inserted here] and a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, R24, X, L, n and p are as defined in the specification, are useful for treating or preventing Mer tyrosine kinase receptor modulated disease or conditions. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
PYRIMIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
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, (2013/10/22)
The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
Discovery of SB-705498: A potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development
Rami, Harshad K.,Thompson, Mervyn,Stemp, Geoffrey,Fell, Steve,Jerman, Jeffrey C.,Stevens, Alexander J.,Smart, Darren,Sargent, Becky,Sanderson, Dominic,Randall, Andrew D.,Gunthorpe, Martin J.,Davis, John B.
, p. 3287 - 3291 (2007/10/03)
Small molecule antagonists of the vanilloid receptor TRPV1 (also known as VR1) are disclosed. Pyrrolidinyl ureas such as 8 and 15 (SB-705498) emerged as lead compounds following optimisation of the previously described urea SB-452533. Pharmacological studies using electrophysiological and FLIPR-Ca2+-based assays showed that compounds such as 8 and 15 were potent antagonists versus the multiple chemical and physical modes of TRPV1 activation (namely capsaicin, acid and noxious heat). Furthermore, 15 possessed suitable developability properties to enable progression of this compound into in vivo studies and subsequently clinical development.
Substituted amine derivatives and methods of use
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, (2008/06/13)
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Substituted amine derivatives and methods of use
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, (2008/06/13)
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.