177785-14-7Relevant articles and documents
Synthesis of a novel diazepine
Memoli, Kevin A.
, p. 927 - 928 (2007)
(Chemical Equation Presented) A novel pyrrolopyridodiazepine ring system was synthesized from methyl 2-methyl nicotinate.
INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
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Page/Page column 40; 57, (2022/02/05)
Provided herein are compounds of formula (V) that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.
Identifying Poly(ADP-ribose)-Binding Proteins with Photoaffinity-Based Proteomics
Dasovich, Morgan,Beckett, Morgan Q.,Bailey, Scott,Ong, Shao-En,Greenberg, Marc M.,Leung, Anthony K. L.
supporting information, p. 3037 - 3042 (2021/03/08)
Post-translational modification of proteins with poly(ADP-ribose) (PAR) is an important component of the DNA damage response. Four PAR synthesis inhibitors have recently been approved for the treatment of breast, ovarian, and prostate cancers. Despite the clinical significance of PAR, a molecular understanding of its function, including its binding partners, remains incomplete. In this work, we synthesized a PAR photoaffinity probe that captures and isolates endogenous PAR binders. Our method identified dozens of known PAR-binding proteins and hundreds of novel candidates involved in DNA repair, RNA processing, and metabolism. PAR binding by eight candidates was confirmed using pull-down and/or electrophoretic mobility shift assays. Using PAR probes of defined lengths, we detected proteins that preferentially bind to 40-mer versus 8-mer PAR, indicating that polymer length may regulate the outcome and timing of PAR signaling pathways. This investigation produces the first census of PAR-binding proteins, provides a proteomics analysis of length-selective PAR binding, and associates PAR binding with RNA metabolism and the formation of biomolecular condensates.
BENZAZEPINE DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0199; 0200, (2019/03/29)
Disclosed are a benzazepine derivative, a preparation method, a pharmaceutical composition and the use thereof. A compound as shown in formula (I) of the present invention, and an isomer, a prodrug, a stable isotope derivative or a pharmaceutically acceptable salt thereof have the following structure. The benzazepine derivative of the present invention has a good regulation effect on the TLR family and the related signalling pathway, and in particular, has a good regulation effect on TLR8, can effectively treat, relieve and/or prevent various diseases mediated by TLR family and the TLR-related signalling pathway, and in particular, can effectively treat, relieve and/or prevent various diseases mediated by TLR8, such as cancers, autoimmune diseases, infections, inflammations, transplantation rejections, graft-versus-host diseases, etc.
NITROGEN-CONTAINING FUSED HETEROCYCLIC COMPOUND, AS WELL AS PREPARATION METHOD, INTERMEDIATE, COMPOSITION AND APPLICATION THEREOF
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Paragraph 0209; 0210, (2019/01/25)
The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
SPIRODIAMINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 44, (2016/05/02)
The invention provides compounds having the general formula (I) pharmaceutical compositions containing the compounds and a process for their preparation. The compounds act as aldosterone synthase inhibitors and are for use in the treatment or prevention of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrom.
HERBICIDAL COMPOUNDS
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Page/Page column 41, (2015/12/23)
The present invention relates to 8H-thiopyrano[3,4-b]pyridine 7,7-dioxide derivatives, to processes and intermediates for making these compounds, to herbicidal compositions comprising these compounds and to methods of using these compounds to control plan
NEW 3,4-DIHYDRO-2H-ISOQUINOLINE-1-ONE AND 2,3-DIHYDRO-ISOINDOL-1-ONE COMPOUNDS
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Page/Page column 46, (2014/12/12)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, A, B, m, n and p are as described herein compositions including the compounds and methods of using the compounds.
NEW BICYCLIC DIHYDROISOQUINOLINE-1-ONE DERIVATIVES
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Page/Page column 152, (2013/06/27)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, A1, A2, A3, A4, A5 and n are as described herein,compositions including the compounds and methods of using the compounds as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrom.
INHIBITORS OF JANUS KINASES
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Page/Page column 51, (2010/04/03)
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
