- Pyrrolotriazine compounds and applications thereof
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The invention belongs to the field of medical chemistry, and particularly relates to a class of lactam-based histone deacetylase inhibitors and a preparation method thereof, a pharmaceutical composition containing the histone deacetylase inhibitor, and applications of the inhibitors in drugs for preventing and/or treating diseases related to histone deacetylase activity out-of-control.
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Paragraph 0094; 0100-0101
(2020/05/01)
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- PYRROLOTRIAZINE COMPOUNDS AND METHODS OF INHIBITING TAM KINASES
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat cancer. (II), or a pharmaceutically acceptable salt thereof, wherein: R1 is pyridin-3-yl, pyridin-4-yl, pyrazol-4-yl, cyclohexyl, or 8-azabicyclo[3.2.1]oct-2- ene-3-yl, wherein R1 is optionally substituted with up to four independently selected substituents; R2 is cyclohexyl substituted with hydroxy and optionally substituted with one or two additional substituents independently selected from C1-C4 alkyl and fluoro, or is 4,5,6,7- tetrahydro-lH-indazolyl optionally substituted with one to three substituents independently selected from C1-C4 alkyl and fluoro; and R3 is -C3-C8 alkyl, -(C2-C6 alkylene)-0-(C1-C6 alkyl), C3-C6 cycloalkyl, or -(C2-C6 alkylene)-C3-C6 cycloalkyl, wherein R3 is optionally substituted with 1-5 substituents inde endentl selected from deuterium, halo, and -OH.
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Paragraph 0160-0161
(2019/05/06)
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- Azabicyclo derivatives, preparation methods thereof, and pharmaceutical applications thereof
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The invention relates to azabicyclo derivatives, preparation methods thereof, and pharmaceutical applications thereof. Specifically, the invention discloses compounds represented by a formula (I), or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. The invention also provides preparation methods of the derivatives, and applications of the derivatives in EGFR inhibitors. The definitions of the groups in the formula are defined in the specifications.
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Paragraph 0171; 0174
(2016/10/09)
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- PYRROLOTRIAZINE INHIBITORS OF IRAK4 ACTIVITY
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The present invention relates to pyrrolotriazine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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Page/Page column 33
(2016/09/26)
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- Discovery and process synthesis of novel 2,7-pyrrolo[2,1- f ][1,2,4]triazines
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The synthesis of a new kinase inhibitor template 2-anilino-7-aryl- pyrrolo[2,1-f][1,2,4]triazine is described which includes a late stage orthogonally reactive key intermediate amenable to rapid diversification as well an optimized in situ triflate displa
- Thieu, Tho,Sclafani, Joseph A.,Levy, Daniel V.,McLean, Andrew,Breslin, Henry J.,Ott, Gregory R.,Bakale, Roger P.,Dorsey, Bruce D.
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supporting information; experimental part
p. 4204 - 4207
(2011/10/04)
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- PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS
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The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
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Page/Page column 335
(2010/08/05)
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