- Cannabinoid receptor light-operated ligand and preparation method and application thereof
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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.
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Paragraph 0066; 0073-0078
(2021/01/24)
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- General, Mild, and Metal-Free Synthesis of Phenyl Selenoesters from Anhydrides and Their Use in Peptide Synthesis
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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.
- Temperini, Andrea,Piazzolla, Francesca,Minuti, Lucio,Curini, Massimo,Siciliano, Carlo
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p. 4588 - 4603
(2017/05/12)
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- 2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
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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.
- Mochizuki, Akiyoshi,Nagata, Tsutomu,Kanno, Hideyuki,Suzuki, Makoto,Ohta, Toshiharu
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experimental part
p. 1623 - 1642
(2011/04/21)
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- NOVEL HETEROCYCLIC COMPOUNDS
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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
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Page/Page column 69
(2009/09/05)
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- Selective neuronal nitric oxide synthase inhibitors
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Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.
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Page/Page column 30-31
(2009/01/24)
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- NEW HALOALKYLSULFONANILIDE DERIVATIVE, HERBICIDE, METHOD FOR USING THE SAME AND INTERMEDIATE THEREFOR
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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
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Page/Page column 57
(2008/06/13)
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- AMINE COMPOUNDS
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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.
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Page 234-235
(2010/02/07)
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- Aniline derivatives possessing an inhibitory effect of nitric oxide synthase
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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.
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