454-07-9Relevant articles and documents
3-Acetamido-4-(cyclooctylamino)nitro-benzene
Gonzalez-Platas,Ruiz-Perez,Torres,Yanes
, p. 651 - 654 (1997)
The crystal and molecular structure of the title compound, N-(2-cyclooctylamino-4-nitrophenyl)acetamide, C16H23N3O3, has been determined as part of an investigation into substituted benzene derivatives having no
CARBAZOLE AND CARBOLINE COMPOUNDS FOR USE IN THE DIAGNOSIS, TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH AMYLOID OR AMYOLID-LIKE PROTEINS
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Page/Page column 142, (2015/08/06)
The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
Development of a scalable synthesis of a vascular endothelial growth factor receptor-2 kinase inhibitor: Efficient construction of a 6-etherified [1,2,4]triazolo[1,5-a]pyridine-2-amine Core
Ishimoto, Kazuhisa,Fukuda, Naohiro,Nagata, Toshiaki,Sawai, Yasuhiro,Ikemoto, Tomomi
, p. 122 - 134 (2014/05/20)
A practical and scalable synthesis of the vascular endothelial growth factor receptor-2 (VEGFR-2) kinase inhibitor 1 has been developed. The key features of the process development include facile preparation of the key raw material 3-amino-4- fluorophenol, chemoselective nucleophilic aromatic substitution of 5-chloro-2-nitropyridine with phenol, a safe one-pot synthesis of a substituted urea using an isothiocyanate generated in situ from inexpensive materials, and improvement of the yield of acylation in the end game. The optimized six-step synthesis afforded 1·H2O in 54% overall yield, twice as much as the yield of the original synthesis, without chromatographic purification. In addition, a robust recrystallization procedure to afford the desired crystal form of 1 was also developed.
Synthesis, optimization, and evaluation of novel small molecules as antagonists of WDR5-MLL interaction
Bolshan, Yuri,Getlik, Matthaeus,Kuznetsova, Ekaterina,Wasney, Gregory A.,Hajian, Taraneh,Poda, Gennadiy,Nguyen, Kong T.,Wu, Hong,Dombrovski, Ludmila,Dong, Aiping,Senisterra, Guillermo,Schapira, Matthieu,Arrowsmith, Cheryl H.,Brown, Peter J.,Al-Awar, Rima,Vedadi, Masoud,Smil, David
supporting information, p. 353 - 357 (2013/04/24)
The WD40-repeat protein WDR5 plays a critical role in maintaining the integrity of MLL complexes and fully activating their methyltransferase function. MLL complexes, the trithorax-like family of SET1 methyltransferases, catalyze trimethylation of lysine 4 on histone 3, and they have been widely implicated in various cancers. Antagonism of WDR5 and MLL subunit interaction by small molecules has recently been presented as a practical way to inhibit activity of the MLL1 complex, and N-(2-(4-methylpiperazin-1-yl)-5-substituted- phenyl) benzamides were reported as potent and selective antagonists of such an interaction. Here, we describe the protein crystal structure guided optimization of prototypic compound 2 (Kdis = 7 μM), leading to identification of more potent antagonist 47 (Kdis = 0.3 μM).
3 -CYANO- 5 -ARYLAMINO-7 -CYCLOALKYLAMINOPYRROLO [1, 5 -A] PYRIMIDINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS
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Paragraph 000151; 000152; 000153, (2013/10/21)
The invention relates to chemical compounds of Formula (I): or a salt thereof. In some embodiments, the invention relates to inhibitors of CK2. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and treatment of CK2-related conditions and diseases, e.g., cancer.
(R)-3-(N,N-DIMETHYLAMINO)PYRROLIDINE DERIVATIVES
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Page/Page column 94, (2010/04/27)
(R)-3-(N,N-Dimethyiamino)pyrrolidine derivatives of formula (I), wherein the meaning for Cy1 is as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors
QUINOLINES AND THEIR THERAPEUTIC USE
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Page/Page column 109, (2008/06/13)
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1- C6fluoroalkyl, cyclopropyl, halo, -S(O)nR6, -SO2NR7R8, -NR7R8, -NR7C(O)R6, -CO2R7, -C(O)NR7R8, -C(O)R6, -NO2, -CN or a group -OR9; wherein each R6 is independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group -SO2R6; A is -CHR10-, -C(O)-, -S(O)n-, -0-, or -NR10- wherein n is an integer from 0-2 and R10 is hydrogen, C1-C3alkyl, or C1-C6fluoroalkyl group; B is a direct bond, or a divalent radical selected from -CH2-, -CH2CH2-, -CHR11-, -CR11R12-, -CH2CHR11-, -CH2CR11R12-, -CHR11CHR12-, and divalent radicals of formula -(CR11R12)P-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -NH-, or -S(O)n-, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(=O)NHSO2R6or SO2NHC(=O)R6; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.
CARBONYL-AMINO SUBSTITUTED ACYL PHENYL UREA DERIVATIVES, METHOD FOR THE PRODUCTION AND USE THEREOF
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Page/Page column 33, (2008/06/13)
The invention relates to compounds of formula (I) wherein the radicals have the cited meaning, in addition to the physiologically compatible salts thereof. The compounds, for example, can be used as medicaments for preventing and treating type 2 diabetes.
A novel synthesis of 4H-1,4-benzoxazines
Kudo, Noriaki,Furuta, Satoru,Sato, Kazuo
, p. 1663 - 1668 (2007/10/03)
The reaction of methyl 2-chloro-5-ethoxycarbonylamino-4-fluorobenzoate (4a) and 1-bromo-3,3-dimethyl-2-butanone (2) in the presence of 2.2 eq of lithium bis(trimethylsilyl)amide afforded the 4H-1,4-benzoxazine (6a) in good yield instead of the expected 4-
Herbicidal aryl triazolinones
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, (2008/06/13)
Herbicidal compounds of the formula STR1 in which, for example, X is Br, Cl or F; Y is Cl or Br, R2 is CHF2, R3 is CH3, R is alkyl, dialkylamino, carboxymethyl, hydroxy, haloalkyl, or aryl, and R1 is H, Na, lower alkyl or --SO2 R.