- MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS
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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
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Paragraph 0912
(2020/08/13)
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- MODULATORS OF HEMOGLOBIN
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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.
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Paragraph 0237; 0243-0244
(2020/06/08)
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- Unnatural amino acid synthesis by thermostable O-phospho-L-serine sulfhydrylase from hyperthermophilic archaeon Aeropyrum pernix K1
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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.
- Nakamura, Takashi,Kunimoto, Kohei,Yuki, Toru,Ishikawa, Kazuhiko
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supporting information
p. 1789 - 1792
(2017/11/23)
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- Thiazine amide derivative thereof in the preparation of medicaments for preventing neurodegenerative diseases, the use of the
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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
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Paragraph 0021; 0025-0027
(2017/02/23)
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- Thiazine Amide Derivative and Pharmaceutical Composition and Use Thereof
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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
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Paragraph 0059-0061
(2015/07/27)
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- THIAZINE AMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
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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
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Paragraph 0041; 0042
(2015/07/15)
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- Synthesis of novel chiral NiII complexes of dehydroalanine Schiff bases and their reactivity in asymmetric nucleophilic addition reactions. Novel synthesis of (S)-2-carboxypiperazine
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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.
- 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.
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scheme or table
p. 2638 - 2645
(2011/02/16)
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- N-SUBSTITUTED THIOMORPHOLINE DERIVATIVES AS THE INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND THE PHARMACEUTICAL USES THEREOF
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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.
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Page/Page column 5-6
(2009/12/24)
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- 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
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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.
- Adams, Benjamin,Lowpetch, Kreingkrai,Thorndycroft, Faye,Whyte, Sheena M.,Young, Douglas W.
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p. 3357 - 3364
(2007/10/03)
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- Substituted 6?membered n?heterocyclic compounds and their uses as neurological regulator
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This invention relates to substituted 6-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R1, R2, X, Y, and Z are as defined in the description; their pre
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Page/Page column 5
(2008/06/13)
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- Synthesis of Amino Acids with Modified Principal Properties 3: Sulfur-Containing Amino Acids
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The synthesis and characterization of seven medium-sized, medium-polar, sulfur-containing amino acids are presented.The compounds were prepared with the objective of finding amino acids which possess physical and chemical properties such that their principal properties would be clearly different from those of previously known amino acids.The principal properties are determined as latent variables in principal component analysis of molecular property descriptors.The following amino acids were prepared in homochiral form from L-cysteine: (2R)-2-amino-3-(2-hydroxyethylsulfanyl)propanoic acid, (2R)-2-amino-3-(2-hydroxyethylsulfonyl)propanoic acid, (3R)-perhydro-1,4-thiazine-3-carboxylic acid and (3R)-1,1-dioxoperhydro-1,4-thiazine-3-carboxylic acid. (3R)-1-Oxoperhydro-1,4-thiazine-3-carboxylic acid was prepared in N,C protected form, but all attempts to obtain the free amino acid failed.The principal properties of this amino acid were determined on the racemic diastereomers obtained by oxidation of the racemic perhydro-1,4-thiazine-3-carboxylic acid prepared from 2-aminoethanethiol and ethyl 3-bromo-2-oxopropanoate.With the exception of (3R)-perhydro-1,4-thiazine-3-carboxylic acid for which the synthesis has been previously described, the amino acids described are new compounds.An improved synthesis of (3R)-perhydro-1,4-thiazine-3-carboxylic acid via the cyclization of (2R)-benzyl-2-amino-3-(2-hydroxyethylsulfanyl)propanoate under Mitsunobu conditions is presented.Full experimental details for the syntheses are given.The principal property scores of the synthesized sulfur-containing amino acids and of the structurally related 3-(2-aminoethyl)cysteine which was commercially available are given.
- Larsson, Ulf,Carlson, Rolf
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p. 517 - 525
(2007/10/02)
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