3109-99-7Relevant academic research and scientific papers
REGIMENS OF ESTROGEN RECEPTOR ANTAGONISTS
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Paragraph 0087; 0098-0099, (2021/01/29)
Provided herein are methods of administering estrogen receptor antagonists for use in treatment of cancer. The antagonists (such as a hexahydro pyrido[3,4-b]indole, AZD9496, RAD-1901, ARN-810, endoxifen, or fulvestrant) may be an inhibitor of both activating function 1 and activating function 2 of the estrogen receptor. Also provided are combinations of above inhibitors with a secondary agent, which is a CDK 4/6 inhibitor (such as, palbocociclib, ribociclib, abemaciclib, lerociclib, and trilaciclib).
METHODS OF TREATING ESTROGEN RECEPTOR-ASSOCIATED DISEASES
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Paragraph 0194, (2021/09/11)
The present disclosure provides methods of treating estrogen receptor-associated diseases, disorders, and conditions.
IMIDAZO[1,2-B]PYRIDAZINE IL-17A INHIBITORS
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Page/Page column 19; 48, (2020/07/25)
The invention provides certain difluorocyclohexyl-imidazopyridazinyl-imidazolidinone compounds of formula II as IL-17A inhibitors, pharmaceutical compositions thereof, and methods of using a compound of formula II to treat certain symptoms of psoriasis, rheumatoid arthritis or multiple sclerosis.
NOVEL SALTS OF SELECTIVE ESTROGEN RECEPTOR DEGRADERS
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Paragraph 0148, (2020/07/14)
Provided herein are compounds, salts, crystalline forms, and pharmaceutical compositions that are related to Selective Estrogen Receptor Degraders, as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, crystalline forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as breast cancer.
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.
INDAZOLE DERIVATIVES THAT DOWN-REGULATE THE ESTROGEN RECEPTOR AND POSSESS ANTI-CANCER ACTIVITY
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Page/Page column 136-137, (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.
ESTROGEN RECEPTOR MODULATORS
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Paragraph 0129, (2017/11/04)
Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS
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Paragraph 00331-00332, (2017/07/28)
The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.
Synthesis method of 2-fluoro-2-methyl-1-propyl alcohol
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Paragraph 0011; 0024; 0028, (2017/07/20)
The invention discloses a synthesis method of 2-fluoro-2-methyl-1-propyl alcohol as a novel antitumor drug intermediate. According to the technological route, the 2-fluoro-2-methyl-1-propyl alcohol is prepared from methyl-2-hydroxyisobutyrate as a starting material through esterification, fluorination and reduction reaction. Halogenating reaction and a specific rectification method are adopted in the purification step, so that the purity of a product is improved and the stability of the product is improved. The used raw materials are cheap and available; the technological route is simple; the production cost is reduced; meanwhile, the production security and the purity of the product are improved; and industrial production is facilitated.
BICYCLIC HETEROARYL AMIDES AS CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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Page/Page column 50, (2016/03/13)
The present invention relates to substituted bicyclic heteroaryl amide derivatives that are inhibitors of cathepsin K proteases and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of these enzymes. In addition, the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of bone diseases such as osteoporosis and osteoarthritis as well as other diseases and conditions. The compounds have the general formula: [Formula should be inserted here]
