109801-72-1Relevant academic research and scientific papers
Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742
Gege, Christian
, p. 737 - 744 (2016)
Retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt or RORC2) is a key transcription factor for the differentiation of na?ve proinflammatory CD4+ T cells and the production of T helper-17 (TH17) cells. Inhibiting RORγt activity is thought to be beneficial in targeting a variety of inflammatory and autoimmune disorders, however current candidates remain to be validated in the clinic. Recently Vitae Pharmaceuticals successfully finished its Phase 1 single ascending dose clinical study with their proprietary RORγt inverse agonist VTP-43742. On the basis of the reported promising results, Vitae Pharmaceuticals could currently be considered as having the leading clinical candidate in the RORγt inverse agonist category. This prompts the interest on the exact chemical structure of their clinical candidate. The first relevant patent application (WO2014179564) from Vitae Pharmaceuticals describes RORγt inverse agonists with a 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole core, while in the second and latest patent application (WO2015116904) this element has changed towards a 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine core. By combining information from Vitae’s patent applications and trustworthy online information, the potential elucidation of the chemical structure of clinical candidate VTP-43742 is described.
Thioamide-substituted dihydropyrrolopyridine compounds as ROR[gamma] inhibitors
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Paragraph 0128; 0130; 0153-0157, (2019/01/24)
The invention relates to thioamide-substituted dihydropyrrolopyridine compounds as ROR[gamma] inhibitors. The compounds represented by the formula (I) or pharmaceutically acceptable salts thereof havegood ROR[gamma] inhibitory activity and are expected to
DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
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Paragraph 0083, (2016/05/24)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
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Paragraph 0099; 0100, (2016/06/01)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
Dihydropyrrolopyridine inhibitors of ROR-gamma
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Page/Page column 19; 20, (2016/11/21)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions co
DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
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Paragraph 0097, (2015/09/23)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
Synthesis of tetrasubstituted symmetrical pyrazines from β-keto γ-amino esters: A mild strategy for self-dimerization of peptides
Kumar, Mothukuri Ganesh,Thombare, Varsha J.,Bhaisare, Rupal D.,Adak, Anindita,Gopi, Hosahudya N.
, p. 135 - 141 (2015/02/02)
A facile synthesis of highly symmetrical tetrasubstituted pyrazines through simple aerial oxidation of β-keto γ-amino esters is reported. The scope of the reaction was examined by use of various amino acid side-chain functional groups andpeptides. The mil
Exploring β-hydroxy γ-amino acids (statines) in the design of hybrid peptide foldamers
Bandyopadhyay, Anupam,Malik, Ankita,Kumar, Mothukuri Ganesh,Gopi, Hosahudya N.
, p. 294 - 297 (2014/01/23)
The synthesis and characterization of syn and anti β-hydroxy γ-amino acid (statine) diastereoisomers, their utilization in the design of hybrid peptide foldamers, and their single crystal conformations are studied.
Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity
Fukui, Yurie,Narita, Koichi,Dan, Singo,Yamori, Takao,Ito, Akihiro,Yoshida, Minoru,Katoh, Tadashi
, p. 301 - 313 (2014/03/21)
The bicyclic depsipeptide histone deacetylase (HDAC) inhibitors burkholdacs A and B were efficiently synthesized in a highly convergent and unified manner. The synthesis features the amide coupling of a d-valine-d-cysteine- or d-allo-isoleucine-d-cysteine-containing segment with a d-methionine-containing segment to directly assemble the corresponding seco-acids, key precursors for macrolactonization. Using the same methodology, 5,6,20-tri-epi-burkholdac A was also synthesized. HDAC inhibitory assays and cell-growth inhibition analyses of the synthesized depsipeptides demonstrated the potency order of this class of bicyclic depsipeptides as compared to the clinically approved depsipeptide FK228 (romidepsin). Novel structure-activity relationships within this class of compounds were also revealed.
A facile transformation of amino acids to functionalized coumarins
Bandyopadhyay, Anupam,Gopi, Hosahudya N.
experimental part, p. 8089 - 8095 (2012/01/04)
The synthesis of novel chiral coumarins functionalized with proteinogenic amino acid side chains via N-protected γ-amino-β-keto esters and their incorporation into the cell permeable HIV-1 TAT peptide through the modified solid phase peptide synthesis are
