223375-01-7Relevant academic research and scientific papers
Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of aldehyde dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy
Buchman, Cameron D.,Buckanovich, Ronald J.,Chtcherbinine, Mikhail,Debnath, Bikash,Felton, Jeremy,Grimley, Edward,Huddle, Brandt C.,Hurley, Thomas D.,Larsen, Scott D.,Li, Siwei,Mao, Shuai,McGonigal, Stacy C.,Neamati, Nouri,Pan, Shu,Sun, Duxin,Takahashi, Cyrus,Wen, Bo
, (2020/12/21)
There is strong evidence that inhibition of one or more Aldehyde Dehydrogenase 1A (ALDH1A) isoforms may be beneficial in chemotherapy-resistant ovarian cancer and other tumor types. While many previous efforts have focused on development of ALDH1A1 select
Electrophile-Directed Diastereoselective Oxonitrile Alkylations
Chepyshev, Sergiy V.,Pitta, Bhaskar Reddy,Vangala, Saidi Reddy,Lujan-Montelongo, J. Armando,Steward, Omar W.,Fleming, Fraser F.
supporting information, p. 2850 - 2853 (2018/02/09)
Diastereoselective alkylation of prochiral oxonitrile dianions with secondary alkyl halides efficiently installs two contiguous stereogenic centers. The confluence of nucleophilic trajectory and the electrophile chirality causes distinct steric differences that allow efficient discrimination for one of the six possible conformers. Numerous oxonitrile-derived dianions efficiently displace secondary alkyl halides propagating the electrophile chirality to efficiently install two contiguous tertiary centers. The prevalence of chiral, secondary electrophiles makes the interdigitated alkylation of chiral electrophiles a particularly attractive route because the resulting oxonitriles are readily transformed into bioactive heterocycles.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00330; 00331, (2013/08/28)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
PROCESSES AND INTERMEDIATES FOR PREPARING CYSTEINE PROTEASE INHIBITORS
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Page/Page column 54-55, (2010/10/20)
The present invention is directed to a novel process for preparing certain cysteine protease inhibitors.
HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 54-55, (2008/06/13)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 41-42, (2010/02/11)
The application is directed to haloalkyl-substituted compounds of Formula (I), wherein R1, R1a, R2, R3, R4’ and E are as defined in the claims. The compounds are inhibitors of cysteine proteases, in p
AMIDINO COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page/Page column 38, (2010/02/09)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceu
CYSTEINE PROTEASE INHIBITORS
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Page/Page column 41-42, (2010/02/07)
The present invention is directed to compounds that are inhibitors of cysteine protease, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceut
PEPTIDIC COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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Page 61, (2010/11/30)
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
