40472-88-6Relevant academic research and scientific papers
Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension
Hoyt, Scott B.,Taylor, Jerry,London, Clare,Ali, Amjad,Ujjainwalla, Feroze,Tata, Jim,Struthers, Mary,Cully, Doris,Wisniewski, Tom,Ren, Ning,Bopp, Charlene,Sok, Andrea,Verras, Andreas,McMasters, Daniel,Chen, Qing,Tung, Elaine,Tang, Wei,Salituro, Gino,Clemas, Joe,Zhou, Gaochao,MacNeil, Douglas,Duffy, Ruth,Xiong, Yusheng
, p. 2384 - 2388 (2017)
We report the discovery and hit-to-lead optimization of a structurally novel indazole series of CYP11B2 inhibitors. Benchmark compound 34 from this series displays potent inhibition of CYP11B2, high selectivity versus related steroidal and hepatic CYP targets, and lead-like physical and pharmacokinetic properties. On the basis of these and other data, the indazole series was progressed to lead optimization for further refinement.
Discovery of benzimidazole CYP11B2 inhibitors with in vivo activity in rhesus monkeys
Hoyt, Scott B.,Park, Min K.,London, Clare,Xiong, Yusheng,Tata, Jim,Bennett, D. Jonathan,Cooke, Andrew,Cai, Jiaqiang,Carswell, Emma,Robinson, John,MacLean, John,Brown, Lindsay,Belshaw, Simone,Clarkson, Thomas R.,Liu, Kun,Liang, Gui-Bai,Struthers, Mary,Cully, Doris,Wisniewski, Tom,Ren, Ning,Bopp, Charlene,Sok, Andrea,Cai, Tian-Quan,Stribling, Sloan,Pai, Lee-Yuh,Ma, Xiuying,Metzger, Joe,Verras, Andreas,McMasters, Daniel,Chen, Qing,Tung, Elaine,Tang, Wei,Salituro, Gino,Buist, Nicole,Kuethe, Jeff,Rivera, Nelo,Clemas, Joe,Zhou, Gaochao,Gibson, Jack,Maxwell, Carrie Ann,Lassman, Mike,McLaughlin, Theresa,Castro-Perez, Jose,Szeto, Daphne,Forrest, Gail,Hajdu, Richard,Rosenbach, Mark,Ali, Amjad
supporting information, p. 573 - 578 (2015/05/27)
We report the discovery of a benzimidazole series of CYP11B2 inhibitors. Hit-to-lead and lead optimization studies identified compounds such as 32, which displays potent CYP11B2 inhibition, high selectivity versus related CYP targets, and good pharmacokin
INDAZOLE COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 43; 44, (2014/07/08)
This invention relates to indazole compounds of the structural formula: (structure represented) or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment or amelioration of conditions that could be treated by inhibiting aldosterone synthase.
TRIAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 41, (2013/04/10)
This invention relates to triazolopyridyl compounds of the structural formula: [Formula should be inserted here] or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
PYRAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 39, (2013/04/10)
This invention relates to pyrazolopyridyl compounds of the structural formula: [Formula should be inserted here] or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone s
IMIDAZOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 36, (2013/04/10)
This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 69, (2012/11/13)
This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
PI3 KINASE/mTOR DUAL INHIBITOR
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Page/Page column 3, (2012/07/28)
The present invention provides an imidazo[4,5-c]quinolin-2-one compound, or a pharmaceutically acceptable salt thereof, that inhibits both PI3K and mTOR and, therefore, is useful in the treatment of cancer.
ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 38-39, (2012/02/05)
The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.
1H-IMIDAZO[4, 5-c]QUINOLINONE COMPOUNDS, USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Page/Page column 152-153, (2010/12/29)
The invention relates to the use of 1 H-imidazo[4,5-c]quinolinone compounds and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1 H-imidazo[4,5-c]quinolinone compounds for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1 H-imidazo[4,5-c]quinolinone compounds to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1 H-imidazo[4,5-c]quinolinone compounds, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H-imidazo[4,5-c]quinolinone compounds; and a process for the preparation of the novel 1 H-imidazo[4,5-c]quinolinone compounds.
