- HETEROARYL COMPOUNDS
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Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
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Paragraph 00290
(2021/05/29)
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- Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer
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The neurotrophic receptor tyrosine kinase (NTRK) genes including NTRK1, NTRK2, and NTRK3 encode the tropomyosin receptor kinase (Trk) proteins TrkA, TrkB, and TrkC, respectively. So far, two TRK inhibitors, larotrectinib sulfate (LOXO-101 sulfate) and ent
- Liu, Zongliang,Yu, Pengfei,Dong, Lin,Wang, Wenyan,Duan, Sijin,Wang, Bingsi,Gong, Xiaoyan,Ye, Liang,Wang, Hongbo,Tian, Jingwei
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p. 10286 - 10296
(2021/07/31)
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- A Straightforward Synthesis of Six-Membered-Ring Heterocyclic α-Aminophosphonic Acids from N-Acyliminium Ions
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A convenient synthesis of phosphonic analogues of pipecolic acid and its heterocyclic analogues is reported. The major step of the elaborated procedure is the introduction of the phosphonate group into the skeleton of the appropriate cyclic amide through N-acyliminium ions. The former ones were obtained by preparation of the hemiaminals or their methyl ethers from the N-protected cyclic amides. Finally, the reaction with trimethyl phosphite in the presence of BF3·OEt2 afforded the desired phosphonates, which were converted into phosphonic acids by the hydrolysis of phosphonate moiety with simultaneous cleavage of the nitrogen protecting groups.
- Argüello-Velasco, Rubén Oswaldo,Sánchez-Mu?oz, Grecia Katherine,Viveros-Ceballos, José Luis,Ordó?ez, Mario,Kafarski, Pawel
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- COMPOUNDS
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Disclosed are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis(ALS).
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Page/Page column 177
(2017/02/09)
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- COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
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The invention relates to the compound 5-(4-isopropylsulfonylphenyl) -3-[3-[4-[(3R)-morpholin-3-yl]phenyl]isoxazol-5-yl]pyrazine-2-amine and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of ATR kinase.
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Paragraph 00197
(2013/04/13)
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- Analogs of the δ opioid receptor selective cyclic peptide [2-D- penicillamine,5-D-penicillamine]-enkephalin: 2',6'-Dimethyltyrosine and Gly3-Phe4 amide bond isostere substitutions
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In order to develop systemically-active opioid peptides, the δ-selective, opioid pentapeptide [D-Pen2,D-Pen5]-enkephalin (DPDPE) was modified by esterification and by substitution of 2',6'-dimethyltyrosine for tyrosine to yield 4. Co
- Chandrakumar,Stapelfeld,Beardsley,Lopez,Drury,Anthony,Savage,Williamson,Reichman
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p. 2928 - 2938
(2007/10/02)
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