214000-16-5Relevant articles and documents
MACROCYCLIC ACTIVIN-LIKE RECEPTOR KINASE INHIBITORS
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Page/Page column 100, (2016/10/04)
The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of Activin-like receptor kinases, more in particular ALK1 and/or ALK2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of ALK1-kinase and/or ALK2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
COMPOUND HAVING RADIOACTIVE TECHNETIUM BINDING SITE, AND RADIOACTIVE TECHNETIUM COMPLEX THEREOF
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Paragraph 0170; 0171, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a radioactive technetium complex which enables a hypoxia area in a living body to be visualized. SOLUTION: The present invention provides a compound represented by a predetermined structural formula and having a radioactive technetium binding site, or salt thereof, a radioactive technetium complex thereof, a radioactive pharmaceutical composition comprising the same, and a kit used for the preparation of the same. COPYRIGHT: (C)2015,JPO&INPIT
Chemoselective alkynylation of N-sulfonylamides versus amides and carbamates-Synthesis of tetrahydropyrazines
Aubineau, Thomas,Cossy, Janine
, p. 3303 - 3305 (2013/06/04)
The chemoselective alkynylation of N-sulfonylamides versus amides and carbamates using TMS-EBX as an alkynylating agent leads to the formation of non-symmetrical tetrahydropyrazines from orthogonally protected diamines. The Royal Society of Chemistry 2013
THERAPEUTIC AGENT FOR CEREBRAL INFARCTION
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, (2012/08/08)
The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.
Concise preparation of 8-trifluoromethyltetrahydro-6H-pyrido [1,2-a] pyrazine-6-one
Kothandaraman, Shankaran,Guiadeen, Deodialsingh,Butora, Gabor,Doss, George,Mills, Sander G.,MacCoss, Malcolm,Yang, Lihu
scheme or table, p. 4050 - 4053 (2009/10/11)
Methodology to rapidly and efficiently assemble 8-trifluoromethyltetrahydro-6H-pyrido [1,2-a] pyrazine-6-one (11) has been developed and its general applicability has been demonstrated.
AMINOCYCLOPENTYL PYRIDOPYRAZINONE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page/Page column 25, (2010/11/27)
Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
Artificial transfer hydrogenases based on the biotin-(strept)avidin technology: Fine tuning the selectivity by saturation mutagenesis of the host protein
Letondor, Christophe,Pordea, Anca,Humbert, Nicolas,Ivanova, Anita,Mazurek, Sylwester,Novic, Marjana,Ward, Thomas R.
, p. 8320 - 8328 (2007/10/03)
Incorporation of biotinylated racemic three-legged d6-piano stool complexes in streptavidin yields enantioselective transfer hydrogenation artificial metalloenzymes for the reduction of ketones. Having identified the most promising organometallic catalyst precursors in the presence of wild-type streptavidin, fine-tuning of the selectivity is achieved by saturation mutagenesis at position S112. This choice for the genetic optimization site is suggested by docking studies which reveal that this position lies closest to the biotinylated metal upon incorporation into streptavidin. For aromatic ketones, the reaction proceeds smoothly to afford the corresponding enantioenriched alcohols in up to 97% ee (R) or 70% (S). On the basis of these results, we suggest that the enantioselection is mostly dictated by CH/π interactions between the substrate and the η6-bound arene. However, these enantiodiscriminating interactions can be outweighed in the presence of cationic residues at position S112 to afford the opposite enantiomers of the product.
An efficient synthesis of N,N'-linked oligoureas
Wilson, Mark E.,Nowick, James S.
, p. 6613 - 6616 (2007/10/03)
This paper reports an efficient synthesis of N-alkyl-N,N'-linked oligourcas [-NR-CO-NH-CH2CH2](n), which involves the repetition of three steps: (1) main-chain extension by ring-opening of N-(2- nitrobenzenesulfonyl)-2-imidazolidone (1) by a secondary amine RR'NH to afford sulfonamide RR'N-CO-NH-CH2CH2-NH-SO2Ar (2) side-chain attachment by N-alkylation of the sulfonamide with alkyl halide R'X, and (3) removal of the sulfonyl group to give a new secondary amine RR'N-CO NH-CH2CH2-NHR'). A tetraurea was prepared in 10 steps and 58% overall yield by this method.
