143707-72-6Relevant articles and documents
SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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Page/Page column 122; 128, (2020/12/11)
The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF LIVER CANCER
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Paragraph 0825-0826, (2020/09/09)
The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.
7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS AND DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF LIVER CANCER
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Page/Page column 78, (2019/09/18)
The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, for (use in) the treatment and/or prophylaxis of liver cancer.
Cortisol derivative as well as preparation method and application thereof
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Paragraph 0026, (2018/10/11)
The invention discloses a cortisol derivative and a preparation method thereof, a cortisol homogeneous enzyme immunoassay reagent as well as a preparation method and application method thereof. The cortisol derivative has a structure shown as a formula (I) shown in the description and is used for preparing a cortisol immunogen and an antibody thereof with high immunogenicity; the cortisol homogeneous enzyme immunoassay reagent prepared by using the antibody can achieve high throughput and rapid detection of cortisol on a fully automatic biochemical analyzer.
7-SUBSTITUTED SULFONIMIDOYLPURINONE COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF VIRUS INFECTION
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Page/Page column 30, (2018/03/25)
The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as TLR7 agonists for the treatment of viral infections.
Glucagon Receptor Modulators
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, (2012/07/13)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
HYDROXY-BISPHOSPHONIC ACID DERIVATIVES AS VECTOR TARGETING BONE TISSUE
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Page/Page column 6; 8, (2010/12/29)
The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: -n and m denote, independently of one another, an integer ranging from 1 to 4, —X denotes an oxygen atom or an N—R3 group, —R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and —R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.
Synthesis and activity of 5′-uridinyl dipeptide analogues mimicking the amino terminal peptide chain of nucleoside antibiotic mureidomycin A
Howard, Nigel I.,Bugg, Timothy D. H.
, p. 3083 - 3099 (2007/10/03)
A series of 5′-uridinyl dipeptides were synthesised which mimic the amino terminal chain of nucleoside antibiotic mureido omycin A. Aminoacyl-β-alanyl- and aminoacyl-N-methyl-β-alanyl- dipeptides were attached either via an ester linkage to the 5′-hydroxyl of uridine, or via an amide linkage to 5′-amino-5′-deoxyuridine. The most active inhibitor of Escherichia coli phospho-MurNAc-pentapeptide translocase (MraY) was 5′-O-(L-Ala-N-methyl-β-alanyl)-uridine (13l), which also showed 97% enzyme inhibition at 2.35 mM concentration, and showed antibacterial activity at 100 μg/mL concentration against Pseudomonas putida. Both the central N-methyl amide linkage and a 5′ uridine ester linkage were required for highest biological activity. Enzyme inhibition was shown to be competitive with Mg2+. It is proposed that the primary amino terminus of the inhibitor binds in place of the Mg2+ cofactor at the MraY active site, positioned via a cis-N-methyl amide linkage.
Synthesis and antinociceptive activity of orally active opioid peptides: Improvement of oral bioavailability by esterification
Ogawa, Tadashi,Araki, Mamoru,Miyamae, Tetsuhisa,Okayama, Toru,Hagiwara, Masaki,Sakurada, Shinobu,Morikawa, Tadanori
, p. 759 - 771 (2007/10/03)
To improve the oral bioavailability of a dermorphin tetrapeptide analog, Nα-1-iminoethyl-Tyr-D-MetO-Phe-MeβAla-OH (III), 1) which has a potent analgesic activity after oral administration, various derivatives were synthesized to incr
