- Campestarenes: New building blocks with 5-fold symmetry
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Campestarene is a planar, shape-persistent macrocycle with 5-fold symmetry. A range of derivatives bearing peripheral functional groups suitable for generating supramolecular interactions has been designed and synthesised for potential applications in creating 2D quasicrystal molecular assemblies. The new campestarene derivatives bear ester, carboxylic acid, methoxy, bromo, 4-pyridyl, 4-cyanophenyl and 4-phenyl carboxylic acid groups, including further derivatives of the latter two bearing alkyl chains on the phenyl groups to improve solubility. The campestarene derivatives were prepared by reductive condensation of phenol precursors bearing nitro and formyl groups using Na2S2O4. The target functional groups were installed either by pre-cyclisation derivatisation or by synthesis of methoxy-substituted campestarene and subsequent derivatisation. The cyclisation reaction is tolerant of the functional groups introduced. The ten new campestarene derivatives were characterised by NMR spectroscopy and MALDI-TOF MS, although the poor solubility of some examples precluded their detailed characterisation.
- Nam, Seong,Ware, David C.,Brothers, Penelope J.
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p. 6460 - 6469
(2018/10/02)
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- 3-substituted coumarin derivative and application and GPR35 receptor agonist
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The invention discloses a 3-substituted coumarin derivative and a pharmaceutically acceptable salt, a solvate, a hydrate or a crystal form. The compound of the invention generally exhibits high agonistic activity against human G protein-coupled receptor 35 (GPR35) and is specific agonists of the human GPR35 receptor. The compound provided by the invention is an active ligand of the novel GPR35 receptor, and the compound and the pharmaceutically acceptable salt, the solvate, the hydrate or the crystal form thereof generally exhibit higher activity and good selectivity to the human GPR35. The 3-substituted coumarin derivative is the specific agonist of the GPR35 receptor and can be used in the preparation of a medicament for treating, preventing and inhibiting a disease mediated by the GPR35receptor.
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Paragraph 0060-0061
(2018/06/04)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000244
(2015/04/15)
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- Crystal structures, spectroscopic, electrochemical, and antibacterial properties of a series of new copper(II) Schiff base complexes
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Two new and two previously reported Schiff base ligands as well as four corresponding new Cu(II) complexes (CuL1-4) were synthesized and characterized. The Schiff base ligands were synthesized from condensation of 5-bromo-2-hydroxy-3-nitrobenza
- Imani, Nasibeh,Behzad, Mahdi,Rudbari, Hadi Amiri,Bruno, Giuseppe,Jahromi, Hamideh Samari,Khaleghian, Ali
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p. 2296 - 2306
(2015/07/15)
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- Extended release formulation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one
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The present invention relates to an extended release formulation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one or a pharmaceutically acceptable salt thereof or a hydrate of said pharmaceutically acceptable salt thereof. The invention further relates
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Page/Page column 2
(2008/06/13)
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- 1-[2H-1-BENZOPYRAN-2-ONE-8-YL]-PIPERAZINE DERIVATIVES FOR THE TREATMENT OF PAIN
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The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl]--piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT1A-agonistic as well
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Page/Page column 17-18
(2008/06/13)
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- 1-[2H-1-BENZOPYRAN-2-ONE-8-YL]-PIPERAZINE DERIVATIVES FOR THE TREATMENT OF MOVEMENT DISORDERS
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The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT1A receptor agonistic
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Page/Page column 16-17
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF 3-AMINO-8-(1-PIPERAZINYL) -2H-1-BENZOPYRAN-2-ONE AND SALTS AND HYDRATES THEREOF
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The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relat
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Page/Page column 12-13
(2008/06/13)
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- Total synthesis of the marine alkaloid halitulin
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The structure of the strongly cytotoxic marine alkaloid halitulin (1) has been confirmed by total synthesis and its absolute configuration determined as (15S). The synthesis follows a strategy previously reported by one of us and uses an efficient prepara
- Heinrich, Markus R.,Steglich, Wolfgang,Banwell, Martin G.,Kashman, Yoel
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p. 9239 - 9247
(2007/10/03)
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