- Heterocyclic compound as FGFR inhibitor, synthesis method and applications thereof
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The present invention discloses a heterocyclic compound as an FGFR inhibitor, and a synthesis method thereof, and applications of the heterocyclic compound in preparation of drugs for treating cancers. According to the present invention, the heterocyclic compound as the FGFR inhibitor or the pharmaceutically acceptable salt thereof has high FGFR inhibitory action, and the pharmaceutical composition prepared from the heterocyclic compound has good anticancer effect and wide application range.
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Paragraph 0165; 0168-0171
(2019/10/01)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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- New bicyclic compounds as crac channel modulators
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The present invention relates to novel compounds which are inhibitors of CRAC channel activity. This invention also relates to pharmaceutical compositions containing them, process for their preparation and their use in therapy.
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- ISOTOPICALLY LABELED BIARYL UREA COMPOUNDS
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The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers.
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Page/Page column 14; 15
(2014/01/07)
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- NOVEL 6-AZAINDOLE AMINOPYRIMIDINE DERIVATIVES HAVING NIK INHIBITORY ACTIVITY
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The present invention relates to a compound of formula I: wherein: R1 is C1-6 alkyl, C3-8 cycloalkyl, aryl, heterocyclyl, or -COR1x, where the C1-6 alkyl, C3-8 cycloalkyl, aryl, and heterocyclyl may be substituted; and R1x is C3-8 cycloalkyl, aryl, or heterocyclyl, any of which may be substituted; R2, R3, R4, R5, R6, and R7 are each independently hydrogen, halogen, C1-6 alkyl, or aryl, where the C1-6 alkyl or aryl may be substituted; R8 is hydrogen, C1-6 alkyl, aryl, or heterocyclyl, any of which may be substituted; or a pharmaceutically acceptable salt or ester thereof.
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Page/Page column 42; 43
(2010/04/28)
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- Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: Exploration of 5-6 fused rings as alternative S1 moieties
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A series of cis-1,2-diaminocyclohexane derivatives were synthesized with the aim of optimizing previously disclosed factor Xa (fXa) inhibitors. The exploration of 5-6 fused rings as alternative S1 moieties resulted in two compounds which demonstrated improved solubility and reduced food effect compared to the clinical candidate, compound A. Herein, we describe the synthesis and structure-activity relationship (SAR), together with the physicochemical properties and pharmacokinetic (PK) profiles of some prospective compounds.
- Yoshikawa, Kenji,Yokomizo, Aki,Naito, Hiroyuki,Haginoya, Noriyasu,Kobayashi, Shozo,Yoshino, Toshiharu,Nagata, Tsutomu,Mochizuki, Akiyoshi,Osanai, Ken,Watanabe, Kengo,Kanno, Hideyuki,Ohta, Toshiharu
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experimental part
p. 8206 - 8220
(2010/04/06)
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