27065-94-7Relevant academic research and scientific papers
Phenanthro [9,10-d] imidazole derivatives containing indoles as well as synthesis and application of phenanthro [9,10-d] imidazole derivatives containing indoles
-
Paragraph 0017; 0018; 0019, (2017/08/23)
The invention discloses phenanthro [9,10-d] imidazole derivatives containing indoles as well as a preparation method and application of the phenanthro [9,10-d] imidazole derivatives containing the indoles and belongs to the field of biological organic synthesis. The phenanthro [9,10-d] imidazole derivatives containing the indoles, disclosed by the invention, are characterized in that an indole pharmacophore with anticancer activity is introduced on phenanthro imidazole to increase conjugate area and improve biological activities of molecules, thereby improving an antitumor effect. The preparation method of the phenanthro [9,10-d] imidazole derivatives containing the indoles, disclosed by the invention, is characterized in that by taking indole-3-formaldehyde as a starting point, different chains (halides) are modified at N-positions, and are finally condensed with 9,10-phenanthrenequinone to synthesize the phenanthro [9,10-d] imidazole derivatives containing the indoles which have a restraining force for the growth of tumor cells in vitro.
Supported TBD-assisted solution phase diversification of formyl-aza-heterocycles through alkylation-knoevenagel one pot sequences
Maatougui, Abdelaziz El,Crespo, Abel,Silva, Artur M.S.,Coelho, Alberto
experimental part, p. 570 - 582 (2012/07/31)
An efficient solution-phase parallel procedure to perform the structural diversification of some formyl-nitrogen heterocycles (A) using the reusable TBD supported base is described. The library synthesis is based in a consecutive Alkylation-Knoevenagel functionalisation that uses alkyl halides (B), Michael acceptors (C) and activated methylene compounds (D) as diversity elements.
Solid-liquid phase alkylation of n-heterocycles: Microwave-assisted synthesis as an environmentally friendly alternative
Milen, Matyas,Gruen, Alajos,Balint, Erika,Dancso, Andras,Keglevich, Gyoergy
experimental part, p. 2291 - 2301 (2010/09/17)
The solid-liquid phase alkylation of a variety of five-membered N-heterocycles (carbazole, imidazole, benzimidazole, and indole-3-carbaldehyde) was carried out under different conditions. The use of alkali carbonate in dimethylformamide or in MeCN (in the latter case, in the presence of a phase-transfer catalyst) is a suitable method to prepare the corresponding N-alkylated products in an efficient way. In most cases, the solventless, microwave-assisted reaction is an environmentally friendly alternative to traditional methods. Copyrigh
ORGANIC COMPOUNDS
-
Page/Page column 162-163, (2008/06/13)
3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that cla
3,4,(5)-SUBSTITUTED TETRAHVDROPYRIDINES
-
Page/Page column 162-163, (2008/06/13)
Organic Compounds 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)- substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)- substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)- substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.
PHARMACEUTICAL PREPARATIONS COMPRISING INSULIN, ZINC IONS AND A ZINC-BINDING LIGAND
-
Page/Page column 229-230, (2008/06/13)
Novel preparations comprising branched ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The preparations have a prolonged action designed for flexible injection regimes.
PHAMACEUTICAL PREPARATIONS COMPRISING INSULIN
-
Page/Page column 224-225, (2010/02/15)
Novel preparations comprising ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer wherein the ligand is extended by protamine that are capable of prolonging the ac-tion of insulin preparations.
Efficient consecutive alkylation-Knoevenagel functionalisations in formyl aza-heterocycles using supported organic bases
Coelho, Alberto,El-Maatougui, Abdelaziz,Ravi?a, Enrique,Cavaleiro, José A. S.,Silva, Artur M. S.
, p. 3324 - 3328 (2008/09/17)
An efficient solution-phase parallel procedure to perform the structural diversification of some formyl aza-heterocycles employing supported organic bases (PS-BEMP, PS-TBD or Si-TBD) is described. The library synthesis is based on a consecutive alkylation-Knoevenagel functionalisation that employs alkyl halides, Michael acceptors, and malonic acid derivatives as diversity elements. Georg Thieme Verlag Stuttgart.
Stabilised insulin compositions
-
Page/Page column 120, (2008/06/13)
The present invention provides pharmaceutical compositions comprising insulin and novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The resulting preparations have improved physical and chemical stability.
PHARMACEUTICAL PREPARATIONS COMPRISING ACID-STABILISED INSULIN
-
Page/Page column 225-226, (2010/02/08)
Novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer that are capable of prolonging the action of insulin preparations are disclosed.
