54966-20-0Relevant academic research and scientific papers
Synthetic Cathinone Analogues Structurally Related to the Central Stimulant Methylphenidate as Dopamine Reuptake Inhibitors
Yadav-Samudrala, Barkha J.,Eltit, Jose M.,Glennon, Richard A.
, p. 4043 - 4050 (2019/09/07)
Synthetic cathinones are, primarily, stimulant drugs of abuse that act at monoamine transporters (e.g., the dopamine transporter or DAT) as releasing agents or as reuptake inhibitors. In the past few years, the emergence of >150 new synthetic cathinones has attracted considerable attention from medical and law enforcement communities. threo-Methylphenidate (tMP), used clinically for the treatment of ADHD and narcolepsy, is also a DAT reuptake inhibitor. tMP is somewhat structurally similar to abused cathinone stimulants, and the structure-activity relationships (SAR) of tMP have been well-defined. Hence, available tMP literature might assist in understanding the SAR of synthetic cathinones, about which less is known. In the present study, we synthesized and examined eight 2-benzoylpiperidine analogues (4, 6-12) to determine if tMP SAR might be applicable to cathinone SAR. The benzoylpiperidine analogues were evaluated in a competition assay using live-cell imaging against APP+ in HEK293 cells stably expressing hDAT and in cells coexpressing DAT and voltage-gated Ca2+ channels. All compounds were found to be DAT reuptake inhibitors, and a significant correlation was obtained between the potency of the benzoylpiperidines and tMP binding data (r = 0.91), suggesting that the SAR of tMP analogues might be directly applicable to certain synthetic cathinones as DAT reuptake inhibitors.
HEPATITIS B CAPSID ASSEMBLY MODULATORS
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Paragraph 0358; 0359; 0376; 0377, (2019/12/30)
Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
New indolizine compound, preparation method thereof and pharmaceutical compositions containing them (by machine translation)
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Paragraph 0103; 0104; 0105, (2016/10/09)
The invention of the formula (I) compound, Wherein R a, R b, R c, R d, T, R 3, R 4, R 5, X, Y and Het as defined in the description. The invention also relates to a medicament containing the above-mentioned compounds. (by machine translation)
INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0072-0074, (2016/07/27)
Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
PHOSPHATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0071-0073, (2015/02/19)
Compounds of formula (I): wherein X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T and R5 are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
INDOLIZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0058 - 0060, (2015/02/25)
Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
NEW ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 50; 51, (2015/02/19)
Compounds of formula (I): (I) wherein Het, R3, R4, R5, R7, R8, R9, T, p, p', q, and q' are as defined in the description are pro-apoptotic agents useful in the treatment of cancers and of a
Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads
West, Nicholas P.,Cergol, Katie M.,Xue, Millie,Randall, Elizabeth J.,Britton, Warwick J.,Payne, Richard J.
supporting information; experimental part, p. 5166 - 5168 (2011/06/10)
The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.
New chiral lewis bases derived from l-pipecolinic acid showing stereocontrol highly dependent on the catalyst design in the hydrosilylation of N-phenyl ketimines
Collados, Juan F.,Quiroga-Feijoo, Maria L.,Alvarez-Ibarra, Carlos
experimental part, p. 3357 - 3367 (2011/02/26)
Chiral L-pipecolinic acid based catalysts, the N-functionalized pipecolinamides 4a-h and 5a-e, have been obtained in a straightforward two-step synthesis starting from BOC-Lpipecolinic acid. The catalysts form, a complex with trichlorosilane, which proved
