3810-12-6Relevant academic research and scientific papers
HETEROARYL INHIBITORS OF PAD4
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Paragraph 00200-00201, (2018/03/28)
The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
PROTEIN KINASE INHIBITORS
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Page/Page column 18, (2015/01/09)
The present invention provides a compound incorporating a group of formula (I) wherein: 1 of X, Y and Z is nitrogen and the other 2 are carbon; V is sulpur or carbon; R3 is oxygen or fluorine; R4 is an optionally present C1-3 alkyl group optionally substituted by fluorine; R5 is an optionally present cyclic group with 5-7 heavy atoms in the ring which may be carbocyclic or heterocyclic and aromatic or aliphatic and is optionally substituted, e.g. by a halogen, C1-2 alkyl or fluoroalkyl, OH, OR6, cyano, COOR6, CONHR6, sulfonamide or NHR6, in which R6 is a C1-2 alkyl or fluoroalkyl; at least one of R4 and R5 is present and R4 and R5 may both be present; m and n are each 1 or 2 depending on the identity of V and R3; when n=2 each R3 may be the same or different but are preferably the same, when m=2, each R4 and each R5 may be the same or different but are preferably the same; and W represents hydrogen, carbon, nitrogen, oxygen or sulphur; or incorporating a salt, hydrate or solvate of a group of formula (I); as well as therapeutic uses of these compounds, in particular as inhibitors of protein kinase activity and in the treatment of inflammation, inflammatory conditions and cancer.
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors
Wall, Mark J.,Chen, Jinsheng,Meegalla, Sanath,Ballentine, Shelley K.,Wilson, Kenneth J.,DesJarlais, Renee L.,Schubert, Carsten,Chaikin, Margery A.,Crysler, Carl,Petrounia, Ioanna P.,Donatelli, Robert R.,Yurkow, Edward J.,Boczon, Lisa,Mazzulla, Marie,Player, Mark R.,Patch, Raymond J.,Manthey, Carl L.,Molloy, Christopher,Tomczuk, Bruce,Illig, Carl R.
, p. 2097 - 2102 (2008/12/21)
A series of 3,4,6-substituted 2-quinolones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). The fully optimized compound, 4-(4-ethyl-phenyl)-3-(2-methyl-3H-imidazol-4-yl)-2-qui
Synthesis of aza analogues of the anticancer agent batracylin
Martínez-Viturro, Carlos M.,Domínguez, Domingo
, p. 4707 - 4710 (2008/03/13)
Three series of pyrido-fused pyrimido[2,1-a]isoindol-7-ones were prepared from readily available (aminopyridinyl)(aryl)methanones by reduction followed by a Mitsunobu reaction with phthalimide and acid-catalysed cyclodehydration. This approach provides a wide variety of aza analogues of the antitumour agent batracylin.
QUINOLINONE DERIVATIVES AS INHIBITORS OF C-FMS KINASE
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Page/Page column 26-27, (2010/02/10)
The invention is directed to compounds of Formulae I and II: (I) (II) wherein R1, R2, R3, R5, R6, Y1, Y2, Y3, Y4 and X are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.
Andres, J Ignacio,Alonso, Jose M,Fernandez, Javier,Iturrino, Laura,Martinez, Pedro,Meert, Theo F,Sipido, Victor K
, p. 3573 - 3577 (2007/10/03)
Following the program started at Johnson & Johnson Pharmaceutical Research & Development searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,4-c]-[2]benzazepine and 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,2-c]-[2]benzazepine. A new method for the synthesis of pyridobenzazepines is described as well. The affinities for several receptors as well as the mCPP antagonistic activity of the compounds synthesised are described.
Synthesis of ortho-substituted aminopyridines. Metalation of pivaloylamino derivatives
Estel,Linard,Marsais,Godard,Queguiner
, p. 105 - 112 (2007/10/02)
The three isomeric pivaloylaminopyridines were lithiated in more than 80% yields. Aminopyridine derivatives were treated by 2.5-3 equivalents of the complex BuLi-TMEDA at -10° in diethyl ether. Reaction of the lithiated species with various electrophiles afforded a number of ortho-substituted pivaloylaminopyridines in good yields. Secondary pyridine alcohols were oxidized to the corresponding aminopyridyl ketones. Pyridopyrimidines, benzonaphthyridines as well as an analogue of the natural antitumor alkaloid ellipticine has been synthesized showing the versatility of the method.
Directed Lithiation of 4-Halopyridines: Chemoselectivity, Regioselectivity and Application to Synthesis
Marsais, F.,Trecourt, F.,Breant, P.,Queguiner, G.
, p. 81 - 87 (2007/10/02)
4-Chloro and 4-fluoropyridines were ortho-lithiated by n-butyllithium-TMEDA chelate or lithium diisopropylamide at low temperature.The resulting 3-lithio 4-halopyridines were reacted with electrophiles which led to various 3,4-disubstituted pyridines.The versatility of this functionalization is enhanced by the 4-halogen reactivity towards nucleophiles such as water, methylate and amines.Some of the 3,4-disubstituted synthons were annelated to naphthyridine, xanthone and coumarin or condensed to Hantzsch-ester or to "chlotrimazol" analogues.Lithiation of 4-fluoropyridine led in one step to 3,4-pyridyne, which was trapped by cycloaddition with furans.
Synthesis of 4-Amino-3-pyridinyl and 4-Amino-5-pyrimidinyl Aryl Ketones and Related Compounds via an ortho-Lithiation Reaction
Radinov, Rumen,Haimova, Marietta,Simova, Ekaterina
, p. 886 - 891 (2007/10/02)
4-Chloropyridine and 4,6-dichloropyrimidine react regioselectively with lithium diisopropylamide to give 4-chloro-3-lithiopyridine and 4,6-dichloro-5-lithiopyrimidine, respectively.These intermediates react with benzaldehydes to give (4-chloro-3-pyridinyl
