91564-21-5Relevant academic research and scientific papers
AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Paragraph 0195, (2021/08/05)
The present invention relates to new compounds that show pharmacological activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the μ-opiod receptor (MOR or mu-opioid). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.
Pd(II)-Catalyzed Direct ?-C(sp3)-H Arylation between Free β2-Amino Esters and β3-Amino Esters and Aryl Iodides Using a Catalytic Transient Directing Group
Wang, Zhaohui,Fu, Yangjie,Zhang, Qiyu,Liu, Hong,Wang, Jiang
, p. 7683 - 7693 (2020/07/15)
Pd(II)-catalyzed direct ?-C(sp3)-H arylation coupling with free β2-amino esters and β3-amino esters using a commercially available catalytic transient directing group has been developed. This approach features high efficiency, broad substrate tolerance, easily accessible starting materials, and mild reaction conditions.
NOVEL COMPOUNDS
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Page/Page column 33, (2008/06/13)
This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
Fatty acid analogs and prodrugs
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, (2008/06/13)
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which x is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5.
Fatty acid analogs and prodrugs
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, (2008/06/13)
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5,
Dipeptides as renin inhibitors
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, (2008/06/13)
Dipeptides are described which are represented by the formula STR1 wherein the various substituents are defined hereinbelow. These compounds have a strong inhibitory efect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin-associated hypertension.
NOVEL PHENYLALANINE ANALOGUES AS PUTATIVE INHIBITORS OF ENZYMES ACTING ON PHENALALANINE
Zon, Jerzy,Laber, Bernd
, p. 711 - 714 (2007/10/02)
Two analogues of phenylalanine, (+/-)-2-aminomethyl-3-phenylpropanoic acid and (E)-2-aminomethyl-3-phenylpropenoic acid, were synthesized and found to inhibit buckwheat phenylalanine ammonia-lyase (PAL) competitively with Ki values of 16.5 and
