97483-79-9Relevant academic research and scientific papers
ZINC-SELECTIVE FLUORESCENT PROBES FOR EMISSION-RATIOMETRIC IMAGING
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Paragraph 0116, (2019/01/07)
A compound according to Formula (I):, wherein Z is: (II).
Bicyclic aza-amides for treatment of psychiatric disorders
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Paragraph 0070; 0073, (2014/02/15)
The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
BICYCLIC AZA-AMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS
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Page/Page column 35, (2014/02/16)
The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza- amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
Increasing the efficiency of ligands for FK506-binding protein 51 by conformational control
Wang, Yansong,Kirschner, Alexander,Fabian, Anne-Katrin,Gopalakrishnan, Ranganath,Kress, Christoph,Hoogeland, Bastiaan,Koch, Uwe,Kozany, Christian,Bracher, Andreas,Hausch, Felix
supporting information, p. 3922 - 3935 (2013/06/27)
The design of efficient ligands remains a key challenge in drug discovery. In the quest for lead-like ligands for the FK506-binding protein 51 (FKBP51), we designed two new classes of bicyclic sulfonamides to probe the contribution of conformational energy in these ligands. The [4.3.1] scaffold had consistently higher affinity compared to the [3.3.1] or monocyclic scaffolds, which could be attributed to better preorganization of two key recognition motifs. Surprisingly, the binding of the rigid [4.3.1] scaffold was enthalpy-driven and entropically disfavored compared to the flexible analogues. Cocrystal structures at atomic resolution revealed that the sulfonamide nitrogen in the bicyclic scaffolds can accept an unusual hydrogen bond from Tyr113 that mimics the putative FKBP transition state. This resulted in the first lead-like, functionally active ligand for FKBP51. Our work exemplifies how atom-efficient ligands can be achieved by careful conformational control even in very open and thus difficult binding sites such as FKBP51.
HOMOLYTIC ALKOXYCARBONYLATION REACTIONS IN TWO-PHASE SYSTEMS 3. INTRODUCTION OF A SINGLE CARBOXYLIC ACID ESTER FUNCTION INTO CYANO- OR ALKOXYCARBONYL SUBSTITUTED N-HETEROAROMATICS
Heinisch, Gottfried,Loetsch, Gerhard
, p. 731 - 744 (2007/10/02)
Homolytic alkoxycarbonylation reactions with cyanopyridines 1a, 2a, 3a, alkyl pyridinecarboxylates 1b, 2b, 3b, 3c and ethyl 4-pyridazinecarboxylate 4 in presence of dichloromethane were studied.It is demonstrated that under these conditions multiple substitution in general is suppressed markedly.Thus, this experimentally simple procedure represents an efficient and versatile method for single-step preparations of alkyl cyanopyridinecarboxylates 7a, 8a, 9a, 10a.Furthermore, it provides convenient access to so far not available mixed esters 5b, 7b, 8b, 10b, 13, derived from 2,3-pyridine-, 2,4-pyridine-, 3,4-pyridine and 4,5-pyridazinedicarboxylic acid.
Site-Selectivity in the Cyanation of 3-Substituted Pyridine 1-Oxides with Trimethylsilanecarbonitrile
Sakamoto, Takao,Kaneda, Soh-ichi,Nishimura, Sumiko,Yamanaka, Hiroshi
, p. 565 - 571 (2007/10/02)
The cyanation of 3-halo-, 3-methoxy-, and 3-dimethylaminopyridine 1-oxide with trimethylsilanecarbonitrile gave predominantly the corresponding 3-substituted 2-pyridinecarbonitriles.The deoxygenation of nitropyridine 1-oxides to nitropyridines with the same reagent is also described.Keywords - site-selective reaction; trimethylsilanecarbonitrile; pyridine 1-oxide; 2-pyridine-carbonitrile; nitropyridine 1-oxide; deoxygenation; aromatic amine N-oxide; cyanation
