162046-50-6Relevant articles and documents
Cannabinoid receptor light-operated ligand and preparation method and application thereof
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Paragraph 0066; 0073-0078, (2021/01/24)
The invention relates to the technical field of biology, in particular to a novel cannabinoid receptor light-operated ligand and a preparation method and application thereof. Disclosed is the cannabinoid receptor light-operated ligand or the isomer prodrug, the solvate and the pharmaceutically acceptable salt of the cannabinoid receptor light-operated ligand, wherein the structural formula of thecannabinoid receptor light-operated ligand is A-linker-B; A is a transmembrane domain ligand structure, and B is a light-operated element; Linker is a subunit which is linear and has no activity on acannabinoid receptor light-operated ligand. According to the invention, the cannabinoid receptor ligand is integrated with azobenzene through a proper connector, so that the ligand configuration is changed under an illumination condition, and the activation or inhibition state of the cannabinoid receptor is regulated and controlled.
General, Mild, and Metal-Free Synthesis of Phenyl Selenoesters from Anhydrides and Their Use in Peptide Synthesis
Temperini, Andrea,Piazzolla, Francesca,Minuti, Lucio,Curini, Massimo,Siciliano, Carlo
, p. 4588 - 4603 (2017/05/12)
A mild, practical, and simple procedure for phenyl selenoesters synthesis from several anhydrides and diphenyl diselenide was developed. This transition-metal-free method provides a straightforward entry to storable Fmoc-amino acid selenoesters which are effective chemoselective acylating reagents. An application to oligopeptide synthesis was illustrated.
2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
Mochizuki, Akiyoshi,Nagata, Tsutomu,Kanno, Hideyuki,Suzuki, Makoto,Ohta, Toshiharu
, 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.
NOVEL HETEROCYCLIC COMPOUNDS
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Page/Page column 69, (2009/09/05)
The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relat
Selective neuronal nitric oxide synthase inhibitors
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Page/Page column 30-31, (2009/01/24)
Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.
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
AMINE COMPOUNDS
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Page 234-235, (2010/02/07)
The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
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.