16173-99-2Relevant academic research and scientific papers
Asymmetric Synthesis of Heterocyclic Chloroamines and Aziridines by Enantioselective Protonation of Catalytically Generated Enamines**
McLean, Liam A.,Ashford, Matthew W.,Fyfe, James W. B.,Slawin, Alexandra M. Z.,Leach, Andrew G.,Watson, Allan J. B.
supporting information, (2022/02/25)
We report a method for the synthesis of chiral vicinal chloroamines via asymmetric protonation of catalytically generated prochiral chloroenamines using chiral Br?nsted acids. The process is highly enantioselective, with the origin of asymmetry and catalyst substituent effects elucidated by DFT calculations. We show the utility of the method as an approach to the synthesis of a broad range of heterocycle-substituted aziridines by treatment of the chloroamines with base in a one-pot process, as well as the utility of the process to allow access to vicinal diamines.
COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS
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Paragraph 00230-00231, (2021/02/05)
Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.
P300/CBP HAT INHIBITORS
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Paragraph 00117; 00246-00247, (2019/09/04)
Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).
Inhibitors of the renal outer medullary potassium channel
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Page/Page column 31, (2016/12/07)
This invention relates to compounds of Formula I having the following general structure: [in-line-formulae]Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 [/in-line-formulae] wherein R
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 38, (2016/11/07)
The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
HETEROARYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 47, (2016/07/05)
The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
Discovery of a potent and selective ROMK inhibitor with pharmacokinetic properties suitable for preclinical evaluation
Walsh, Shawn P.,Shahripour, Aurash,Tang, Haifeng,Teumelsan, Nardos,Frie, Jessica,Zhu, Yuping,Priest, Birgit T.,Swensen, Andrew M.,Liu, Jessica,Margulis, Michael,Visconti, Richard,Weinglass, Adam,Felix, John P.,Brochu, Richard M.,Bailey, Timothy,Thomas-Fowlkes, Brande,Alonso-Galicia, Magdalena,Zhou, Xiaoyan,Pai, Lee-Yuh,Corona, Aaron,Hampton, Caryn,Hernandez, Melba,Bentley, Ross,Chen, Jing,Shah, Kashmira,Metzger, Joseph,Forrest, Michael,Owens, Karen,Tong, Vincent,Ha, Sookhee,Roy, Sophie,Kaczorowski, Gregory J.,Yang, Lihu,Parmee, Emma,Garcia, Maria L.,Sullivan, Kathleen,Pasternak, Alexander
supporting information, p. 747 - 752 (2015/07/15)
A new subseries of ROMK inhibitors exemplified by 28 has been developed from the initial screening hit 1. The excellent selectivity for ROMK inhibition over related ion channels and pharmacokinetic properties across preclinical species support further pre
Phosphine-catalyzed Aza-MBH reactions of vinylpyridines: Efficient and rapid access to 2,3,5-triarylsubstituted 3-pyrrolines
Chen, Jing,Li, Jianjun,Wang, Jiazhe,Li, Hao,Wang, Wei,Guo, Yuewei
supporting information, p. 2214 - 2217 (2015/05/13)
Vinylpyridines have been developed in aza-Morita-Baylis-Hillman (MBH) reaction to construct triarylsubstituted 3-pyrrolines. The first electron-deficient aromatic ring is marked as an activating mode for the vinyl group in the MBH reaction. This method provides efficient and rapid access to a range of triarylpyrrolines in good yields and at an excellent level of diastereoselectivity. Moreover, the synthetic potential of this protocol is further enhanced by the straightforward synthesis of unsymmetrical tri- and polyarylsubstituted pyrroles.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 44, (2013/05/22)
This invention relates to compounds of Formula I-VI having the following general structure: wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with (CH2)n1- and (CH2)n2-, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 30, (2013/05/22)
This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diureti
