19179-73-8Relevant academic research and scientific papers
MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS
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Paragraph 0912, (2020/08/13)
Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R 1a, R 1b, L 1, L 2, L 3, X, A, B and C are as defined as set forth
MODULATORS OF HEMOGLOBIN
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Paragraph 0237; 0243-0244, (2020/06/08)
The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of hemoglobin, and methods for their use in treating disorders mediated by hemoglobin.
Unnatural amino acid synthesis by thermostable O-phospho-L-serine sulfhydrylase from hyperthermophilic archaeon Aeropyrum pernix K1
Nakamura, Takashi,Kunimoto, Kohei,Yuki, Toru,Ishikawa, Kazuhiko
supporting information, p. 1789 - 1792 (2017/11/23)
O-Acetyl-L-serine sulfhydrylase (OASS) from plants and bacteria synthesizes cysteine and unnatural amino acids that are important building blocks for active pharmaceuticals and agrochemicals. A thermostable O-phospho-L-serine sulfhydrylase from hyperthermophilic archaeon Aeropyrum pernix K1 (OPSSAp) exhibits a function similar to OASS. In the present study, we examined the synthesis of various unnatural amino acids using OPSSAp and demonstrated OPSSAp could efficiently synthesize various sulfur-containing amino acids. OPSSAp would be useful for industrial production of biologically important unnatural amino acids.
Thiazine amide derivative thereof in the preparation of medicaments for preventing neurodegenerative diseases, the use of the
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Paragraph 0021; 0025-0027, (2017/02/23)
The invention relates to a compound shown as the formula I, pharmaceutically acceptable salts of the compound, and/ or solvates and/ or hydrates of the compound. The invention also relates to a preparation method of the compound, a medicinal composition c
Thiazine Amide Derivative and Pharmaceutical Composition and Use Thereof
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Paragraph 0059-0061, (2015/07/27)
The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hy
THIAZINE AMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0041; 0042, (2015/07/15)
The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hy
Synthesis of novel chiral NiII complexes of dehydroalanine Schiff bases and their reactivity in asymmetric nucleophilic addition reactions. Novel synthesis of (S)-2-carboxypiperazine
Saghiyan, Ashot S.,Stepanyan, Lala A.,Manasyan, Luiza L.,Geolchanyan, Arpine V.,Djamgaryan, Silva M.,Ajvazyan, Hrant R.,Panosyan, Henry A.,Maleev, Viktor I.,Saveleva, Tatiana F.
scheme or table, p. 2638 - 2645 (2011/02/16)
New chiral NiII complexes of Schiff bases of dehydroalanine with modified chiral auxiliaries (S)-2-N-[N′-(3,4-dichlorobenzyl)prolyl] aminobenzophenone (3,4-DCBPB), (S)-2-N-[N′-(3,4-dimethylbenzyl)prolyl] aminobenzophenone (3,4-DMBPB), (S)-2-N-[N′-(2-chlorobenzyl)prolyl] aminobenzophenone (2-CBPB), and (S)-2-N-[N′-(2-fluorobenzyl)prolyl]- aminobenzophenone (2-FBPB) have been synthesized. Asymmetric Michael addition reactions of primary and secondary amines and thiols to the dehydroalanine moieties of the complexes were studied. (S)-2-FBPB was found to be the best chiral auxiliary in terms of both selectivity of the reactions (de ～92-96%) and reactivity of the complexes. A novel synthetic route toward (S)-2-carboxypiperazine was developed based on the auxiliary.
N-SUBSTITUTED THIOMORPHOLINE DERIVATIVES AS THE INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND THE PHARMACEUTICAL USES THEREOF
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Page/Page column 5-6, (2009/12/24)
The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system.
Stereochemistry of reactions of the inhibitor/substrates L- And D-β-chloroalanine with β-mercaptoethanol catalysed by L-aspartate aminotransferase and D-amino acid aminotransferase respectively
Adams, Benjamin,Lowpetch, Kreingkrai,Thorndycroft, Faye,Whyte, Sheena M.,Young, Douglas W.
, p. 3357 - 3364 (2007/10/03)
Two members of the α-family of PLP-dependent enzymes, L-aspartate aminotransferase and D-amino acid aminotransferase, have been shown to catalyse β-substitution of L- and D-β-chloroalanine respectively with β-mercaptoethanol, reactions typical of the β-family of PLP-dependent enzymes. The reaction catalysed by L-aspartate aminotransferase has been shown to occur with retention of stereochemistry, a typical outcome for reactions catalysed by β-family enzymes. There are also indications that the reaction catalysed by D-amino acid aminotransferase may involve retention of stereochemistry. Both enzymes have been shown to catalyse exchange at C-3 when the appropriate enantiomer of β-chloroalanine is the substrate. The Royal Society of Chemistry 2005.
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates
Levin,Chen,Laakso,Du,Du,Venkatesan,Sandanayaka,Zask,Xu,Xu,Zhang,Skotnicki
, p. 4345 - 4349 (2007/10/03)
The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing a butynyloxy P1′ group was explored. In particular, compound 5k has excellent in vitro potency against TACE enzyme and in cells, and oral activity in an in vivo model of TNF-α production and a collagen-induced arthritis model.
