58077-34-2Relevant academic research and scientific papers
COMPOUND HAVING γ TURN STRUCTURE AND LSD1 INHIBITOR USING THE SAME
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Paragraph 0185-0187; 0191-0193, (2017/12/27)
PROBLEM TO BE SOLVED: To provide a compound having LSD1 inhibitory activity and cancer cell growth inhibitory effect. SOLUTION: There is provided a compound represented by the formula (1) and a salt thereof. (1), where R1 is an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R2 is H, an alkyl group, a cycloalkyl group, an aryl group or a heteroaryl group, R3 is H, an alkyl group, a cycloalkyl group, an aralkyl group, an aryl group or a heteroaryl group, R4 is an aryl group or a heteroaryl group, each of the above described groups may be substituted, n is an integer of 2 to 10 and *1 and *2 are asymmetric carbons. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
5-Lipoxygenase inhibitors: Synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones
Bhatia, Pramila A.,Brooks, Clint D. W.,Basha, Anwer,Ratajczyk, James D.,Gunn, Bruce P.,Bouska, Jennifer B.,Lanni, Carmine,Young, Patrick R.,Bell, Randy L.,Carter, George W.
, p. 3938 - 3950 (2007/10/03)
Synthetic routes were developed to access a variety of novel 1-aryl- 2H,4H-tetrahydro-1,2,4-triazin-3-one analogs which were evaluated as 5- lipoxygenase (5-LO) inhibitors. The parent structure, 1-phenylperhydro- 1,2,4-triazin-3-one (4), was found to be a
2-,3-,4-,5-,6-,7-,8-,9- and/or 10-substituted dibenzoxazepine and dibenzthiazepine compounds, pharmaceutical compositions and methods of use
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, (2008/06/13)
The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
2-, 3-, 4-, 5-, 6-, 7-, 8-, 9- and/or 10-substituted dibenzoxazepine and dibenzthiazepine compounds, pharmaceutical compositions and methods of use
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, (2008/06/13)
The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
The Use of 2-Oxazolidinones as Latent Aziridine Equivalents. 2. Aminoethylation of Aromatic Amines, Phenols, and Thiophenols
Poindexter, Graham S.,Owens, Donald A.,Dolan, Peter L.,Woo, Edmund
, p. 6257 - 6265 (2007/10/02)
The utility of 2-oxazolidinones 1 as latent, carboxylated aziridine functionalities was examined.Reaction of 2-oxazolidinone (1a), 3-methyl2-oxazolidinone (1b), 3-(phenylmethyl)-2-oxazolidinone (1c), 3-phenyl-2-oxazolidinone (1d) 4,4-dimethyl-2-oxazolidinone (1e), and 5-ethyl-2-oxazolidinone (1f) with aromatic amine salts, phenol, or thiophenols at elevated temperatures (> 130 deg C) afforded aminoethylated adducts.The aminoethylation occurred with concomitant loss of carbon dioxide to furnish variously substituted N-aryl-1,2-ethanediamines 4, 1-(2-phenoxyethyl)-2-imidazolidinone (8), or 2-(arylthio)ethanamines 9 on reactions of 1 with aromatic amine salts, phenol, and thiophenols, respectively.Imidazolidinone 8 is believed to be a secondary reaction product resulting from the condensation of the initially formed 2-phenoxyethanamine with starting oxazolidinone 1a.The aminoethylation reaction did not proceed with aliphatic amine hydrochlorides or alkyl mercaptans.Preliminary mechanistic pathways for these ring openings were also investigated employing a specific, C-5 deuterium-labeled oxazolidinone 1b-d2.Ring-opening experiments of 1b-d2 with N-methylaniline hydrochloride suggest reaction can occur through either a dioxazolinium 5 and/or 5 intermediate.In contrast, reaction of 1b-d2 with thiophenol suggests ring-opening to proceed only via the dioxazolinium pathway.
Synthesis of 1,3-Disubstituted Diazolidines
Lambert, Joseph B.,Huseland, Dave E.,Wang, Gen-tai
, p. 657 - 658 (2007/10/02)
Symmetrical and unsymmetrical 1,3-diaminoethanes 1 are obtained by the reduction of N,N'-disubstituted oxamides 4 with lithium aluminum hydride.The oxamides 4 are readily produced by treatment of diethyl oxalate with primary amines.The 1,3-diaminoethanes 1 lead to 1,3-diazolidines 2 on treatment with formaldehyde.
