105901-10-8Relevant academic research and scientific papers
Investigating the Reactivity of 1,4-Anthracene-Incorporated Cycloparaphenylene
Li, Penghao,Wong, Bryan M.,Zakharov, Lev N.,Jasti, Ramesh
, p. 1574 - 1577 (2016)
Cycloparaphenylenes (CPPs) and their derivatives are unique conjugated macrocycles with novel optoelectronic and host-guest properties. A better understanding of their reactivity is essential for creating new functional materials utilizing these strained
And its manufacturing method hydroxytriarylamine compd., and its use
-
Paragraph 0125; 0126, (2016/11/17)
PROBLEM TO BE SOLVED: To provide an effective material in an organic EL element using a phosphorescent material. SOLUTION: An amine compound expressed by general formula (1) is used in at least one layer among an emission layer, a hole-transport layer and a hole-injection layer, where in formula (1), the rings A, B and C each represents an aromatic ring or a heteroaromatic ring; R1, R2, R3and R4each represents a hydrogen atom, aliphatic hydrocarbon group, alkoxy group, cyano group, aryl group, aryloxy group or heteroaryl group; and Ar1and Ar2each represents an aryl group or heteroaryl group which may have substituents. COPYRIGHT: (C)2012,JPOandINPIT
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors
Liu, Tao,Zhan, Wenhu,Wang, Yanming,Zhang, Liangren,Yang, Bo,Dong, Xiaowu,Hu, Yongzhou
, p. 167 - 176 (2014/01/17)
A series of diphenylmethylamine derivatives were rationally designed, synthesized and biologically evaluated. Most of them exhibited moderate to good Akt1 inhibitory activities, as well as promising anti-proliferative efficacy against cancer cell lines. Besides, molecular docking studies were carried out to probe their binding modes with Akt1. Further kinase selectivity studies of compound 22c were performed, indicating its excellent selectivity against Aurora A, Drak, IKKβ, GSK3β, SYK and JAK2, and moderate selectivity against PKC and BRAF. Finally, a refined pharmacophore model was generated using the most active compounds 2, 12c and 22c via application of HipHop program.
PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS
-
, (2010/07/08)
The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing f
Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design
Donald, Alastair,McHardy, Tatiana,Rowlands, Martin G.,Hunter, Lisa-Jane K.,Davies, Thomas G.,Berdini, Valerio,Boyle, Robert G.,Aherne, G. Wynne,Garrett, Michelle D.,Collins, Ian
, p. 2289 - 2292 (2008/02/03)
6-Phenylpurines were identified as novel, ATP-competitive inhibitors of protein kinase B (PKB/Akt) from a fragment-based screen and were rapidly progressed to potent compounds using iterative protein-ligand crystallography with a PKA-PKB chimeric protein.
PHARMACEUTICAL COMPOUNDS
-
Page/Page column 137, (2008/06/13)
The invention provides a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N-C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4 alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated.
ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS
-
Page/Page column 140, (2008/06/13)
The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N-C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents as defined in the claims.
PHARMACEUTICAL COMPOUNDS
-
Page/Page column 111, (2010/11/25)
The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length
