163423-99-2Relevant articles and documents
2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
Mochizuki, Akiyoshi,Nagata, Tsutomu,Kanno, Hideyuki,Suzuki, Makoto,Ohta, Toshiharu
experimental part, p. 1623 - 1642 (2011/04/21)
We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
NEW HALOALKYLSULFONANILIDE DERIVATIVE, HERBICIDE, METHOD FOR USING THE SAME AND INTERMEDIATE THEREFOR
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Page/Page column 57, (2008/06/13)
PROBLEM TO BE SOLVED: To provide a herbicide excellently safe for humans and animals, having high selectivity for crops, exhibiting high herbicidal effects with a low dose and having wide applicability, persistence of the effects and excellent selectivity between crops and weeds and especially excellent performances as a paddy herbicide. SOLUTION: A haloalkylsulfonanilide derivative is represented by general formula (I) [wherein, R1 denotes a halo(1-6C)alkyl; R2 and R5 denote each an H, a (1-6C)alkyl, a (substituted) phenyl(1-6C)alkyl or the like; R3, R4, R6 and R7 denote each an H, a (1-6C)alkyl, a (3-6C)cycloalkyl, a halogen, a CN or the like; R3 and R4 may mutually be bound to form a 3- to a 7-membered ring; R6 and R7 may mutually be bound to form a 3- to a 7-membered ring; A denotes O or S; G denotes O, S or a CR8, R9 {wherein, R8 and R9 denote each H, a (1-6C)alkyl or the like}; Q denotes a (1-6C)alkyl, a (substituted) (3-6C)cycloalkyl or the like; a and b denotes each 0 or 1; and X denotes H, a halogen, a (1-6C)alkyl, a (substituted) phenyl, a (substituted) heterocyclic ring or the like]. The herbicide comprises the haloalkylsulfonanilide derivative or its salts as an active ingredient. COPYRIGHT: (C)2006,JPO&NCIPI
Aniline derivatives possessing an inhibitory effect of nitric oxide synthase
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, (2008/06/13)
Compounds represented by the general formula (1): ? (where R1is SR6or NR7R8, where R6is typically an alkyl group having 1-6 carbon atoms, R7is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2and R3are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3and Y4which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof. The compounds possess a potent nitric oxide synthase inhibiting activity and are useful as therapeutics of cerebrovascular diseases.