- 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; 0097; 0099
(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
(2019/05/06)
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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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- 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; 0173
(2016/10/09)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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Page/Page column 172
(2012/11/13)
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- HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
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Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
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Page/Page column 32
(2011/08/06)
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- COMPOUNDS AND METHODS FOR THEIR USE
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The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
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Page/Page column 22
(2010/03/31)
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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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- N-(substituted amino)pyrrole derivatives, and herbicidal compositions
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This invention is to provide an N-(substituted amino)pyrrole derivative represented by the formula (I): which is used as an effective ingredient of herbicidal compositions: STR1 wherein R2, R3, R4 and R5 is independently hydrogen atom, halogen atom, C1 -C4 alkyl group, (C1 -C4 alkyl)carbonyl group, (C3 -C6 cycloalkyl) carbonyl group, (C1 -C4 haloalkyl)carbonyl group, (C3 -C5 alkenyl)carbonyl group, benzoyl group which may be substituted with 1-3 halogen atoms and/or C1 -C4 alkyl groups, N,N-[(di-C1 -C4 alkyl)amino]carbonyl group, (C1 -C4 alkoxy)carbonyl group, etc., X1 and X2 are independently hydrogen atom, halogen atom, C1 -C4 alkyl group, C1 -C4 alkoxy group, etc., and Z is nitrogen atom or CH.
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- Studies on the Synthesis of Phytochrome and Related Tetrapyrroles. Dihydropyrromethenones by Photochemical Rearrangement of N-Pyrrolo Enamides
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Dihydropyrromethenone 67b, a potential precursor for the synthesis of phytochrome 1, has been prepared in enantiomerically pure form beginning with N-aminopyrrole 64 and the acetylenic acid 62b. The key step involved a 3,5-sigmatropic rearrangement of N-pyrrolo enamide 66b.
- Jacobi, Peter A.,Buddhu, Subhas C.,Fry, Douglas,Rajeswari
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p. 2894 - 2906
(2007/10/03)
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- A NOVEL SYNTHESIS OF PYRROMETHENONES
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Pyrromethenones are prepared by a process involving acylation of an N-aminopyrrole with a suitable acetylenic acid, followed by sequential 5-exo-dig cyclization and 3,5-sigmatropic shift.
- Jacobi, Peter A.,Buddhu, Subhas C.
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p. 4823 - 4826
(2007/10/02)
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