856767-09-4Relevant articles and documents
Aryl imidazole derivative and application thereof
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Paragraph 0496-0500, (2021/06/23)
The invention relates to an aryl imidazole derivative and application thereof. The aryl imidazole derivative is a compound shown as a formula (I) in the description or pharmaceutically acceptable salt thereof. The invention also discloses application of the aryl imidazole derivative in preparation of drugs for treating cancers. The invention further discloses application of the aryl imidazole derivative in preparation of drugs for treating diseases caused by EGFR mutation.
Tricyclic Indazoles - A Novel Class of Selective Estrogen Receptor Degrader Antagonists
Scott, James S.,Bailey, Andrew,Buttar, David,Carbajo, Rodrigo J.,Curwen, Jon,Davey, Paul R. J.,Davies, Robert D. M.,Degorce, Sébastien L.,Donald, Craig,Gangl, Eric,Greenwood, Ryan,Groombridge, Sam D.,Johnson, Tony,Lamont, Scott,Lawson, Mandy,Lister, Andrew,Morrow, Christopher J.,Moss, Thomas A.,Pink, Jennifer H.,Polanski, Radoslaw
supporting information, p. 1593 - 1608 (2019/02/14)
Herein, we report the identification and synthesis of a series of tricyclic indazoles as a novel class of selective estrogen receptor degrader antagonists. Replacement of a phenol, present in our previously reported tetrahydroisoquinoline scaffold, with an indazole group led to the removal of a reactive metabolite signal in an in vitro glutathione trapping assay. Further optimization, guided by X-ray crystal structures and NMR conformational work, varied the alkyl side chain and pendant aryl group and resulted in compounds with low turnover in human hepatocytes and enhanced chemical stability. Compound 9 was profiled as a representative of the series in terms of pharmacology and demonstrated the desired estrogen receptor α degrader-antagonist profile and demonstrated activity in a xenograft model of breast cancer.
METHODS AND COMPOUNDS FOR TREATING DISORDERS
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Page/Page column 120, (2019/08/26)
The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancers and viral infections.
HETEROCYCLIC COMPOUNDS WITH AN ROR(GAMMA)T MODULATING ACTIVITY
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Paragraph 0824, (2018/03/06)
The present invention relates to a compound that may have an ROR(gamma)t modulating activity and can thus be useful in the treatment of cancer.
PYRAZOLYL-SUBSTITUTED HETEROARYLS AND THEIR USE AS MEDICAMENTS
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Page/Page column 52, (2017/03/28)
The invention relates to new substituted heteroaryls of formula 1 or of formula 1' wherein A is either N or CH, wherein R2 is selected from the group consisting of -C1-3-alkyl, -C1-3-haloalkyl, F, Br, CI, wherein Y is selected from -O- or -CH2-, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
INDAZOLE DERIVATIVES THAT DOWN-REGULATE THE ESTROGEN RECEPTOR AND POSSESS ANTI-CANCER ACTIVITY
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Page/Page column 107, (2017/12/28)
The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
CHEMICAL COMPOUNDS
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Paragraph 0759; 0760, (2017/11/11)
The specification relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
IRAK4 INHIBITING AGENTS
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Page/Page column 75, (2017/09/24)
Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production. Formula (I) The compounds are IRAK-4 inhibitors useful for treating an inflammatory disease, an autoimmune disease, cancer, a cardiovascular disease, a disease of the central nervous system, a disease of the skin, an ophthalmic disease and condition, and a bone disease.
IRAK4 INHIBITING AGENTS
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Page/Page column 269, (2016/03/13)
Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
SPIRO AZETIDINE ISOXAZOLE DERIVATIVES AND THEIR USE AS SSTR5 ANTAGONISTS
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Paragraph 1387, (2014/09/29)
Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.