6940-57-4Relevant articles and documents
ADENOSINE RECEPTOR BINDING COMPOUNDS
-
Paragraph 00261, (2020/02/06)
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
FUSED RING HETEROARYL COMPOUNDS AS ALK4/5 INHIBITORS
-
Paragraph 0149; 0150, (2020/08/05)
The invention provides novel substituted heterocyclic compounds represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of ALK5 and/or ALK4 and are useful in the treatment of pulmonary fibrosis, NASH, obesity, diabetes, cancers and other inflammation.
NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
-
Paragraph 0943; 1201-1205, (2016/07/05)
There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)
Effects of structural modifications on the metal binding, anti-amyloid activity, and cholinesterase inhibitory activity of chalcones
Fosso, Marina Y.,LeVine, Harry,Green, Keith D.,Tsodikov, Oleg V.,Garneau-Tsodikova, Sylvie
supporting information, p. 9418 - 9426 (2015/09/15)
As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synthesis, and biochemical evaluation of a series of chalcones, and assesses the relationship between their structures and their ability to bind metal ions and/or Aβ species, and inhibit AChE/BChE activity. Several chalcones were found to exhibit potent disaggregation of pre-formed N-biotinyl Aβ1-42 (bioAβ42) aggregates in vitro in the absence and presence of Cu2+/Zn2+, while others were effective at inhibiting the action of AChE.
A two-in-one pincer ligand and its diiron(II) complex showing spin state switching in solution through reversible ligand exchange
Samanta, Subhas,Demesko, Serhiy,Dechert, Sebastian,Meyer, Franc
supporting information, p. 583 - 587 (2015/03/04)
A novel pyrazolate-bridged ligand providing two {PNN} pincer-type compartments has been synthesized. Its diiron(II) complex LFe2(OTf)3(CH3CN) (1; Tf=triflate) features, in solid state, two bridging triflate ligands, with a terminal triflate and a MeCN ligand completing the octahedral coordination spheres of the two high-spin metalions. In MeCN solution, 1 is shown to undergo a sequential, reversible, and complete spin transition to the low-spin state upon cooling. Detailed UV/Vis and 19F NMR spectroscopic studies as well as magnetic measurements have unraveled that spin state switching correlates with a rapid multistep triflate/MeCN ligand exchange equilibrium. The spin transition temperature can be continuously tuned by varying the triflate concentration in solution.
Zinc complexes bearing N,N′-bidentate entiopure ligands: Synthesis, structure and catalytic activity toward ring opening polymerisation of rac-lactide
Nayab, Saira,Lee, Hyosun,Jeong, Jong Hwa
experimental part, p. 55 - 62 (2012/09/22)
Dichloro zinc complexes with (S)-1-phenyl-N-[(S)-1-(pyridin-2-yl)ethyl] ethanamine (PMMA) and (S)-1-(6-methylpyridin-2-yl)-N-[(S)-1-phenylethyl] ethanamine (MPMMA) were prepared and characterised by X-ray diffraction. The catalytic activity of the dimethyl complexes, generated in situ, was high in the ring opening polymerization of rac-lactide. Specifically, the dimethyl derivative of (PMMA)ZnCl2 yielded a highly stereocontrolled polylactide with Pr = 0.84.
PYRAZOLE DERIVATIVE
-
Page/Page column 35-36, (2008/06/13)
Not available
Novel fused heteroaromatic compounds as transforming growth factor (TGF) inhibitors
-
, (2008/06/13)
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
NOVEL TRIAZOLE AND OXAZOLE COMPOUNDS AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITOR
-
Page 54, (2008/06/13)
Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor ("TGF")-β signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
Lanthanide complexes of a new sterically hindered potentially hexadentate podand ligand based on a tris(pyrazolyl)borate core; crystal structures, solution structures and luminescence properties
Reeves, Zoe R.,Mann, Karen L. V.,Jeffery, John C.,McCleverty, Jon A.,Ward, Michael D.,Barigelletti, Francesco,Armaroli, Nicola
, p. 349 - 355 (2007/10/03)
The new podand ligand hydrotris[3-(6-methyl)pyridin-2-ylpyrazol-1-yl]borate [L1]- was prepared which contains three bidentate pyrazolyl/pyridine arms attached to a {BH}- head-group. This ligand differs from an earlier ligand hydrotris[3-(2-pyridyl)pyrazol-1-yl]borate [L2]- by the presence of methyl groups attached to the C6 positions of the pyridyl rings, which would interfere with each other sterically if the ligand co-ordinated in a fully hexadentate manner. Instead, crystallographic analysis of the complexes [M(L1)(NO3)2(H2O)] (M = Eu, Tb or Gd) showed that partial dissociation of the podand occurs to relieve this potential steric problem: either one or two of the pyridyl groups are not co-ordinated, such that [L1]- is penta- or tetra-dentate, but instead are involved in intramolecular N...H-O hydrogen-bonding interactions with the co-ordinated water molecule. The presence of both structural forms in single crystals of the gadolinium and europium complexes shows that interconversion between them in solution must be facile. Variable-temperature 1H NMR spectra of the diamagnetic lanthanum(III) analogue shows that, whereas all three ligand arms are equivalent on the NMR timescale at high temperatures, at -80°C there is mirror symmetry in the complex such that two arms are equivalent and the third is different from the other two; this is consistent with the crystalline form in which [L1]- is tetradentate with two pendant pyridyl arms, which has pseudo-mirror symmetry. Luminescence studies showed that whereas the ligand-based luminescence is retained in the gadolinium(III) complex, in the europium(III) and terbium(III) complexes the ligand-centred emission is quenched by ligand-to-metal energy transfer, resulting in the usual metal-centred emission spectra. The intensity of the emission from the europium(III) and terbium(III) complexes of [L1]- is substantially reduced compared to the emission from the analogous complexes [M(L2)(NO3)2] (M = Eu or Tb) which we ascribe to the sterically induced poorer co-ordination of the podand ligand, resulting in (i) less efficient ligand-to-metal energy transfer, and (ii) co-ordination of labile solvent molecules (H2O) to the metal centres.
