- INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
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Page/Page column 492
(2021/09/11)
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- DIHYDROBENZOFURAN AND INDEN ANALOGS AS CARDIAC SARCOMERE INHIBITORS
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Provided are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, Z, B, R1, R2, R3, G1, G2, and G3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt, thereof for use in methods of treatment heart diseases through cardiac sarcomere inhibtion.
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Paragraph 0265
(2019/08/08)
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- PYRIDINE COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
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The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
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Paragraph 00429; 00460
(2018/08/12)
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- TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
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The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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Paragraph 0964; 0965
(2017/01/23)
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- FUROPYRIDINES AS INHIBITORS OF PROTEIN KINASES
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The invention relates to furo[3,2-b]pyridines substituted at least in position 5 as inhibitors of protein kinases, regulators or modulators, methods of preparation thereof, pharmaceutical compositions containing the compounds, and pharmaceutical use of the compounds and compositions in the treatment of the diseases such as, for example, cancer or neurodegenerative diseases. (Formula (I))
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Page/Page column 67
(2015/11/23)
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- Synthesis of novel 7-substituted pyrido[2′,3′:4,5]furo[3,2-d] pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases
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The efficient synthesis of 7-substituted pyrido[2′,3′:4,5] furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues is described. 3,5-Dibromopyridine was converted into 3-amino-6-bromofuro[3,2-b]pyridine-2- carbonitrile intermediate which was formylated with DMFDMA. Functionalization at position 7 of the tricyclic scaffold was accomplished, before or after cyclisation step, by palladium-catalyzed Suzuki-Miyaura cross-coupling while the pyrimidin-4-amines and N-aryl counterparts were synthesized by microwave-assisted formamide degradation and Dimroth rearrangement, respectively. The final products were evaluated for their potent inhibition of a series of five Ser/Thr kinases (CDK5/p25, CK1δ/ε, CLK1, DYRK1A, GSK3α/β). Compound 35 showed the best inhibitory activity with an IC50 value of 49 nM and proved to be specific to CLK1 among the panel of tested kinases.
- Deau, Emmanuel,Loidreau, Yvonnick,Marchand, Pascal,Nourrisson, Marie-Renee,Loaec, Nadege,Meijer, Laurent,Levacher, Vincent,Besson, Thierry
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p. 6784 - 6788
(2014/01/06)
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- A convenient route to functionalized 3-amino-6-bromofuro[3,2-b]pyridine-2-carboxamides
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An efficient synthesis of 3-amino-6-bromofuro[3,2-b]pyridine-2-carboxamides is described via the formation of 3-amino-6-bromofuro[3,2-b]pyridine-2-carbonitrile. Functionalization of the amino group at position 3 of the heterocycle will be discussed.
- Bretéché, Anne,Marchand, Pascal,Nourrisson, Marie-Renée,De Nanteuil, Guillaume,Duflos, Muriel
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experimental part
p. 4490 - 4494
(2010/07/06)
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- COMPOUNDS
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Bicyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 27; 75-76
(2008/12/08)
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