877133-56-7Relevant articles and documents
TETRAHYDROBENZO-QUINOLINE SULFONAMIDES DERIVATIVE COMPOUNDS
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Page/Page column 12, (2021/07/02)
The present invention relates to tetrahydrobenzo-isoquinoline sulfonamides derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses,
DIHYDROCYCLOPENTA-ISOQUINOLINE-SULFONAMIDE DERIVATIVES COMPOUNDS
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Page/Page column 25-26, (2021/07/02)
The present invention relates to dihydrocyclopenta-isoquinoline-sulfonamide derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FcεRI receptor.
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR
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Page/Page column 53, (2020/09/03)
Disclosed are heterocyclic compounds as inhibitors of FGFR-4 represented by formula (I). Also disclosed is a pharmaceutical composition that includes an inhibitor of FGFR-4. The compounds maybe used to treat diseases mediated with abnormality of FGFR-4 and /or FGF19, such as hepatocellular carcinoma and other forms of cancer.
Heterocyclic compound as FGFR inhibitor, synthesis method and applications thereof
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Paragraph 0071; 0074-0077, (2019/10/01)
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.
CONDENSED TRICYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 73, (2017/03/14)
There is provided compounds of formula I, (I) wherein R1, R2, R3 R4, R5, R6, R7a and R7b have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. CDK8 and/or Haspin kinase) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
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Paragraph 0674; 0675; 0676, (2016/12/01)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
1-(HET)ARYLSULFONYL-(PYRROLIDINE OR PIPERIDINE)-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
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Paragraph 01232; 01233; 01234, (2016/09/22)
The invention is concerned with the compounds of formula I and salts thereof and other compounds of formulas II-IX as disclosed herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formulas I-IX as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain or asthma.
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors
Zak, Mark,Yuen, Po-Wai,Liu, Xiongcai,Patel, Snahel,Sampath, Deepak,Oeh, Jason,Liederer, Bianca M.,Wang, Weiru,O'Brien, Thomas,Xiao, Yang,Skelton, Nicholas,Hua, Rongbao,Sodhi, Jasleen,Wang, Yunli,Zhang, Lei,Zhao, Guiling,Zheng, Xiaozhang,Ho, Yen-Ching,Bair, Kenneth W.,Dragovich, Peter S.
, p. 8345 - 8368 (2016/10/03)
NAMPT inhibitors may show potential as therapeutics for oncology. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for potent cellular NAMPT inhibition. However, when combined with a benzyl group in the center of the inhibitors, such pyridine-like moieties also led to consistent and potent inhibition of CYP2C9. In an attempt to reduce CYP2C9 inhibition, a parallel synthesis approach was used to identify central benzyl group replacements with increased Fsp3. A spirocyclic central motif was thus discovered that was combined with left-hand pyridines (or pyridine-like systems) to provide cellularly potent NAMPT inhibitors with minimal CYP2C9 inhibition. Further optimization of potency and ADME properties led to the discovery of compound 68, a highly potent NAMPT inhibitor with outstanding efficacy in a mouse tumor xenograft model and lacking measurable CYP2C9 inhibition at the concentrations tested.
COMPOUNDS AND METHODS OF USE
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Paragraph 0178, (2015/07/16)
This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.