摘要:
The present invention provides a compound of formula (I) processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and a method of treating disorders resulting from an excess of cholesterol or cancer or a fungal infection.
摘要:
Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the SlP receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
摘要:
A process for the production of amines which is characterized by reacting an imine with a nucleophilic compound (except trialkylsilyl vinyl ethers) in the presence of a phosphoric acid derivative represented by the general formula (1): (1) (wherein A is a spacer; X and X are each independently a divalent nonmetal atom or a divalent nonmetal atomic group; and Y is oxygen or sulfur). The invention provides a process by which amines (particularly optically active amines) useful as intermediates of drugs, agricultural chemicals, or the like can be produced without special post-treatment in high yield at high optical purity; and phosphoric acid derivatives (particularly optically active phosphoric acid derivatives) useful in the production of the amines.
摘要翻译:一种制备胺的方法,其特征在于在通式(1)表示的磷酸衍生物存在下使亚胺与亲核化合物(三烷基甲硅烷基乙烯基醚除外)反应:(1)(其中A 1 是间隔基; X 1和X 2各自独立地为二价非金属原子或二价非金属原子团; Y 1为氧或硫)。 本发明提供了一种可以在高光学纯度下以高产率而不用特殊后处理而用作药物,农药等中间体的胺(特别是光学活性胺)的方法。 和可用于制备胺的磷酸衍生物(特别是光学活性磷酸衍生物)。
摘要:
A process for producing a reaction product of a diazo compound, which process comprises: a. continuously supplying to a first reactor a precursor of a diazo compound; a water-miscible solvent; a base and water; b. mixing the precursor of a diazo compound; the water-miscible solvent; the base and water to generate a diazo compound; c. continuously removing from the first reactor, through a hydrophobic membrane, into a second reactor the formed diazo compound; d. continuously removing from the first reactor all reaction products that have not passed into the second reactor; e. continuously supplying to the second reactor a substrate in a non-water-miscible solvent; f. mixing the above components to generate a reaction product of a diazo compound; and g. continuously removing from the second reactor the non-water-miscible solvent and the reaction product of the diazo compound, and apparatus suitable for carrying out such a process.
摘要:
A method for identifying a solid support in combinatorial synthesis or determining the structure of a compound in combinatorial synthesis. The method involves attaching, detaching and identifying at least one tag by detaching the tag from the solid support and reacting the detached tag with a fluoroalkanoyl acid or its alcohol-reactive equivalent. A preferred linker/tag is of formula -C(=O)C6H3(OCH3)-OR1 in which R1 is C13 to C33 alkane or ether.
摘要:
Therapeutic agents and methods for the treatment of immunologically mediated diseases and malignancies of myeloid cell or lymphoid cell origin. These particular methods utilize the characterization of particular activation mechanisms important to the progression of these pathologies in humans. Selective inhibition of cell types responsible for precipitating these disorders in humans are provided with therapeutic agents which include peptides capable of inhibiting dipeptidyl peptidase-I activation of proenzymes present primarily in cytotoxic T-cells and myeloid cells, such as Gly-Phe-CHN2. Antisense oligonucleotides are also characterized which are specific for human dipeptidyl peptidase-I gene which may be used in the treatment of the described disorders.
摘要:
A method for identifying a solid support in combinatorial synthesis or determining the structure of a compound in combinatorial synthesis. The method involves attaching, detaching and identifying at least one tag by detaching the tag from the solid support and reacting the detached tag with a fluoroalkanoyl acid or its alcohol-reactive equivalent. A preferred linker/tag is of formula -C(=O)C6H3(OCH3)-OR1 in which R1 is C13 to C33 alkane or ether.
摘要:
Novel alkyl ketone compounds having potent cytotoxic activity are described as antitumor agents and are particularly effective against leukemia and breast tumor cells. The compounds of the invention have formula (I), wherein R1-R4, X and p have the meanings given in the description.
摘要:
Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding alpha -keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.
摘要:
A process for producing a diazomethane derivative by oxidizing a hydrazone derivative in a two-phase system containing: a) an aqueous solution of a mixture of a caustic alkali and an alkali metal hypochlorite in respective concentrations of 4-14 w/w % and 3-10 w/w % based on the total weight of the solution; b) a hydrophobic organic solvent; c) an inorganic iodine compound, and d) a phase-transfer catalyst.