170098-98-3Relevant articles and documents
Preparation of a first 18F-labeled agonist for M1 muscarinic acetylcholine receptors
Drewes, Birte,Kolks, Niklas,Neumaier, Bernd,Neumaier, Felix,Rüngeler, Till,Zlatopolskiy, Boris D.
, (2020/07/10)
M1 muscarinic acetylcholine receptors (mAChRs) are abundant in postsynaptic nerve terminals of all forebrain regions and have been implicated in the cognitive decline associated with Alzheimer’s disease and other CNS pathologies. Consequently,
AURORA AND FLT3 KINASES MODULATORS
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Paragraph 0193, (2015/02/18)
The invention provides a compound having the formula (1): and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer.
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3- d ]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells
Henry, James R.,Kaufman, Michael D.,Peng, Sheng-Bin,Ahn, Yu Mi,Caldwell, Timothy M.,Vogeti, Lakshminarayana,Telikepalli, Hanumaiah,Lu, Wei-Ping,Hood, Molly M.,Rutkoski, Thomas J.,Smith, Bryan D.,Vogeti, Subha,Miller, David,Wise, Scott C.,Chun, Lawrence,Zhang, Xiaoyi,Zhang, Youyan,Kays, Lisa,Hipskind, Philip A.,Wrobleski, Aaron D.,Lobb, Karen L.,Clay, Julia M.,Cohen, Jeffrey D.,Walgren, Jennie L.,McCann, Denis,Patel, Phenil,Clawson, David K.,Guo, Sherry,Manglicmot, Danalyn,Groshong, Chris,Logan, Cheyenne,Starling, James J.,Flynn, Daniel L.
supporting information, p. 4165 - 4179 (2015/06/08)
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clinical efficac
Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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Paragraph 1250, (2015/09/22)
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
Substituted phenylimidazopyrazoles and their use
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Paragraph 0698; 0699; 0700, (2013/07/31)
The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
AURORA AND FLT3 KINASES MODULATORS
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Page/Page column 43, (2013/08/28)
The invention provides a compound having the formula (1) useful as modulator of the activity of Aurora kinases and FLT3 kinases: and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer
2-AMINO, 6-PHENYL SUBSTITUTED PYRIDO [2, 3 - D] PYRIMIDINE DERIVATIVES USEFUL AS RAF KINASE INHIBITORS
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Page/Page column 10, (2013/09/26)
The present invention provides the compound l-(3,3-Dimethylbutyl) -3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in tr
RAF INHIBITOR COMPOUNDS
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Page/Page column 42, (2013/09/26)
This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
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, (2012/04/23)
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
Modulators of ATP-binding cassette transporters
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Page/Page column 407, (2008/06/13)
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.