wherein R 1 is an eicosapentaenoyl or docosahexaenoyl; R 2 and R 3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R 4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, -C(=O)NH-(CH 2 ) n -NH- wherein n is 2 or 3, or a bivalent group of the following formula
wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.
摘要:
A 3,4,5,6-tetrahydrophthalamide derivative and a 3,4,5,6-tetrahydroisophthalimide derivative, both having an excellent efficay as the active ingredient of a herbicide, and an industrial process for efficiently producing these higher-performance, herbicidally active compounds. A tetrahydrophthalamide derivative represented by general formula (I) is produced by the reaction of a tetrahydrophthalimide derivative, prepared by the reaction of a halogenated 5-cycloalkyloxyaniline derivative with 3,4,5,6-tetrahydrophthalic anhydride, or of the tetrahydroisophthalimide derivative of the invention with various amines. These tetrahydrophthalamide and tetrahydroisophthalimide derivatives have an excellent herbicidal effect in the treatment of lowland and upland soils and foliage treatment. The tetrahydroisophthalimide derivative is useful also as an intermediate for producing the tetrahydrophthalamide derivative and the like.
摘要:
A human prourokinase-like polypeptide having an amino acid sequence represented by the following formula: (Met).Ser1-X156.Y157.Z158- (wherein Met represents an optionally existing methionine, Ser represents serine present at 1-position of the N-terminal, X represents arginine or other amino acid present at 156-position, Y represents proline, glycine, alanine or valine present at 157-position, Z represents lysine or arginine present at 158-position, and the solid line represents the same amino acid sequence as that of corresponding part of natural human prourokinase or human urokinase-like polypeptide wherein lysine at 135-position is replaced by other amino acid than basic amino acids) or having an amino acid sequence substantially the same as this is disclosed. In addition, a DNA segment which codes the above-described polypeptide; a plasmid containing said DNA segment; E. coli transformed by said plasmid; a process for preparing said polypeptide by culturing said E. coli; a medicine containing said polypeptide; use of said polypeptide for prophylaxis or treatment for formation of thrombus; and use of said polypeptide for preparing the medicine for the above purpose are also disclosed.
摘要:
The invention relates to a process for producing a 2-oxo-3-aromatic carboxylic acid derivative, which comprises reacting an aromatic pyruvic acid derivative with an electrophilic compound in a protic solvent in the presence of a base. This process can provide in good yields the 2-oxo-3-aromatic carboxylic acid derivatives which can be easily converted to aromatic amino acid derivatives or 2-aromatic alkanoic acid derivatives which are important intermediates for synthesizing medicines, agrochemicals, etc.
摘要:
A polyester type polyfunctional macromonomer represented by the general formula (I):
wherein R¹ represents a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms, X represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having from 1 to 6 carbon atoms or a phenyl group, A represents an aliphatic polyester chain, m is 0 or 1, and p, which may be the same or different in each branched chains, represents an integer of from 0 to 6; a polyester type gel which is obtained by polymerization of the polyester type polyfunctional macromonomer; and a drug release controlling material responsive to changes in temperature comprising the polyester type gel are disclosed. The polyester type gel possesses mechanical properties suitable to various utilities, in particular, as a biodegradable polymeric material having a high tensile elongation. The drug release controlling material has an on-off control function of drug release responsive to changes in temperature depending upon the gel transition of the aliphatic polyester type gel.
摘要:
New L-phenylalanine dehydrogenases produced by a microorganism belonging to the genus Bacillus , new microorganisms capable of L-phenylalanine dehydrogenase and belonging to the genus Bacillus , a process for production of L-phenylalanine dehydrogenase using the microorganisms, and processes for production of L-amino acids using the enzymes or the microorganisms.