Abstract:
PROBLEM TO BE SOLVED: To obtain, efficiently and safely in a short process, and further with high purity and in high yield, 3,5-diisopropylphenol or the like which are important as a synthetic intermediate for medicines and agrochemicals. SOLUTION: 3,5-bisalkylphenol (2) and a carbinol compound (1) are obtained by the following reaction formula. [wherein, R1 represents H, an alkali metal atom, an alkali earth metal atom or a hydroxyl protecting group (except a methyl group); R2 may represent a 1-5C lower alkyl group or a phenyl group which may have a substitute; R3 and R4 may represent the same or different lower alkyl, aralkyl or aryl groups].
Abstract:
PROBLEM TO BE SOLVED: To provide an ApoC1_mRNA expression inhibitor.SOLUTION: A composition containing a compound represented by formula (1) or its salt or their solvate as an active ingredient.
Abstract:
PROBLEM TO BE SOLVED: To provide a therapeutic and/or preventive agent of neoplastic diseases.SOLUTION: This agent is a compound expressed by formula (I). In formula, Rto Reach represents a specific substituent group.
Abstract:
PROBLEM TO BE SOLVED: To provide a novel compound that exhibits an effect for promoting insulin secretion from a pancreas β cell and is useful as a preventive and/or therapeutic agent for diseases caused by hyperglycemia, for example, diabetes. SOLUTION: The novel compound is a substituted pyrimidine derivative represented by general formula (1) [wherein the ring A is an optionally substituted 5 to 10-membered heteroaryl group; Q is an oxygen atom or the like; R 1 is a methyl group or the like; R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently a hydrogen atom or the like; m is an integer of 0-2; and n is an integer of 1-3] or a salt thereof, or a solvate thereof. COPYRIGHT: (C)2011,JPO&INPIT
Abstract translation:待解决的问题:提供一种具有促进胰腺β细胞胰岛素分泌的作用的新型化合物,可用作高血糖引起的疾病例如糖尿病的预防和/或治疗剂。 解决方案:新化合物是由通式(1)表示的取代嘧啶衍生物[其中环A是任选取代的5至10元杂芳基; Q是氧原子等; R 1是甲基等; R 2 SP>,R 3 SP>,R 4 SP>,R 5 SP>,R R 7,R SP< SP>,< SP> 9< SP>和R< SP> 10< SP>各自独立地为氢原子等; m是0-2的整数; n为1-3的整数)或其盐或其溶剂合物。 版权所有(C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a method of production by which the number of acid addition of an acid adduct salt of a polyacidic base compound or a water adduct thereof can simply be adjusted to a desired number. SOLUTION: The method for producing the acid adduct salt of the polyacidic base compound or water adduct thereof includes reacting the polyacidic base compound having a basic site stronger than pyridine with an acid salt of the pyridine. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide a low-molecular compound which has such an action as to decrease the amount of PCSK9 protein and increase the amount of LDL receptor, and to provide a medicine including the low-molecular compound as an active ingredient.SOLUTION: The medicine includes (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetate which is substantially optically-pure or a salt thereof, or solvates of them as an active ingredient.
Abstract:
PROBLEM TO BE SOLVED: To obtain a new anilide compound having organ-selective ACAT- inhibiting and intracellular cholesterol transport-inhibiting actions and useful for preventing or curing, etc., of hyperlipidemia or arterial sclerosis, being as a specific anilide compound having a benzo-azole group. SOLUTION: This new anilide compound is expressed by the formula [Ar is a (substituted) aryl; R4 and R5 are each H, a lower alkyl, a lower alkoxy or R4 forms a lower alkylene in which one or more than two intermediate methylene groups may be substituted by O or S, together with R5 in one body; X is NH, O or S; Y is NH, O, S, SO or SO2 ; Z is a single bond or NR6 (R6 is H or a lower alkyl); (n) is an integer of 0-15] and is useful as an acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitor, an intracellular cholesterol transport inhibitor, a depressor of cholesterol in blood or a macrophage foaming suppressor, etc., and is effective for preventing or curing, etc., of hyperlipidemia, arterial sclerosis, cerebrovascular disease, ischemic heart disease or aortic aneurysm.
Abstract:
PURPOSE:To obtain the subject compound in high yield in a short process and under a modest condition by using diethyl-(3-pyridyl)borane and 2,4-disubstituted bromobenzene as starting raw materials, a specific solvent and a specific base and subjecting to a heating reaction in the presence of Pd catalyst. CONSTITUTION:Readily available diethyl-(3-pyridyl)borane and 2,4-disubstituted bromobenzene expressed by formula I [R is nitro or NHCOR (R is lower alkyl or N-protected amino lower alkyl); R is lower alkoxy] are reacted together with potassium carbonate and a base of tetraalkylammonium halide in dimethylformamide solvent in an inert gas atmosphere such as N2 gas in the presence of Pd catalyst preferably under a heating condition at 50-120 deg.C to industrially advantageously afford the objective compound expressed by formula II useful as an intermediate for production of medicine. The compound of formula II can also be isolated and purified by conventional method.
Abstract:
PURPOSE:To produce the title compound in high yield, industrially and advantageously by using one of 4-mesyloxy-2-nitrotoluene, 3-(2,4-dinitrophenyl)pyridine and 3-(4-ethoxyphenyl)pyridine as a raw material. CONSTITUTION:A compound shown by formula II is made into an ethyl ether compound, which is then reacted with pyrrolidine and N, N-dimethylformamide and then subjected to pyridine ring formation reaction to give a compound shown by formula V, which is reduced to give the title compound shown by formula I. A compound shown by formula VI is partially reduced to give a compound shown by formula VII, which is subjected to diazo hydrolysis reaction to give a compound shown by formula VIII. This compound is further ethyl etherified to give a compound shown by formula V, which is reduced to give the compound shown by formula I. A compound shown by formula IX is brominated to give a compound shown by formula X, which is further reacted with benzylamine to give a compound shown by formula XI, which is finally debenzylated to give the compound shown by formula I.