20291-99-0Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12C
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Page/Page column 103, (2021/01/23)
Provided are heterocyclic compounds as inhibitors of the KRAS G12C and uses thereof. Specifically, provided are the compounds of any of formula I to XI or stereoisomers, enantiomers, atropoisomerics or pharmaceutically acceptable salts thereof. Definition of each group in the formula can be found in the specification for details.
Synthesis of an enantiopure thioester as key substrate for screening the sensitivity of penicillin binding proteins to inhibitors
Simon, Justine F.,Bouillez, André,Frère, Jean-Marie,Luxen, André,Zervosen, Astrid
, p. 22 - 31 (2016/10/31)
The synthesis of the enantiopure thioester (R)-2-(2-benzamidopropanoylthio)acetic acid was developed. After the exploration of several activation methods, reaction conditions were found for the formation of the thioester bond in the presence of propylphosphonic anhydride with high enantioselectivity (ee > 99%). The thioester activity of Penicillin Binding Proteins is helpful in research programs looking for new lead structures to overcome the problem of bacterial resistance.
Novel sirtuin inhibitory warheads derived from the Nε-acetyl-lysine analog l-2-amino-7-carboxamidoheptanoic acid
He, Yanhua,Yan, Lingling,Zang, Wenwen,Zheng, Weiping
supporting information, p. 10442 - 10450 (2015/11/10)
Built upon the catalytic mechanism-based pan-SIRT1/2/3 inhibitory warhead l-2-amino-7-carboxamidoheptanoic acid (l-ACAH, a close structural analog of Nε-acetyl-lysine) that our laboratory discovered recently, in the current study, its carboxami
HETEROCYCLIC AMIDES AS ROCK INHIBITORS
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, (2011/10/03)
The present invention relates to new kinase inhibitors of formula (I), more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: Structure-activity relationships and selective binding patterns
Moore, Susanna,Jaeschke, Holger,Kleinau, Gunnar,Neumann, Susanne,Costanzi, Stefano,Jiang, Jian-Kang,Childress, John,Raaka, Bruce M.,Colson, Anny,Paschke, Ralf,Krause, Gerd,Thomas, Craig J.,Gershengorn, Marvin C.
, p. 3888 - 3896 (2007/10/03)
The substituted thieno[2,3-d]pyrimidine 3 (Org 41841), a partial agonist for the luteinizing hormone/choriogonadotropin receptor (LHCGR) and the closely related thyroid-stimulating hormone receptor (TSHR), was fundamentally altered, and the resulting anal
1-dethia-2-thia-cephalosporanic acids
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, (2008/06/13)
Novel 1-dethia-2-thia-cephalosporanic acid derivatives of the formula STR1 wherein R is selected from the group consisting of STR2 Ra is an organic radical, Ri and Rj are individually selected from the group consisting of hydrogen, aliphatic, aromatic and heterocycle or taken together with the nitrogen atom to which they are attached form an optionally substituted cycle or Rb NH--, Rb is optionally substituted carbocyclic or heterocyclic aryl, R1 and --COM are as defined in the specification, R4 is hydrogen or methoxy, n2 is 0, 1 or 2 and their non-toxic, pharmaceutically acceptable acid addition salts in racemic or optically active form having antibiotic activity and their preparation and novel intermediates.
Benzimidazole compounds
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, (2008/06/13)
Novel imidazoles of the formula STR1 and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.
The Synthesis of Substituted thio>acetic Acids
Woulfe, Steven R.,Miller, Marvin J.
, p. 3133 - 3139 (2007/10/02)
The synthesis of substituted thio>acetic acids (6, thiamazins) is described.Various substituted 3(S)-(acylamino)-2-azetidinones were sulfenylated with tert-butyl (phtalimidothio)acetate.Deprotection of the tert-butyl ester with trifluoroacetic acid provided the title compounds.In sharp contrast to their oxygen analogues (oxamazins), the thiamazins were devoid of biological activity.
