摘要:
The invention pertain to novel photoacid generator compounds of the formula (I, II or III), Wherein R 1 is for example C 1 -C 18 alkylsulfonyl or phenylsulfonyl, phenyl-C 1 -C 3 alkylsulfonyl, , naphthylsulfonyl, anthracylsulfonyl or phenanthrylsulfonyl, all optionally substituted, or R 1 is a group (a, b or c); X 1 , X 2 and X 3 independently of each other are O or S; R' 1 is e.g. phenylenedisulfonyl, naphthylenedisulfonyl, diphenylenedisulfonyl, or oxydiphenylenedisulfonyl, all optionally substituted; R 2 is halogen or C 1 -C 10 haloalkyl; X is halogen; Ar 1 is for example biphenylyl or fluorenyl, or is substituted naphthyl; Ar' 1 is heteroarylene, optionally substituted; R 8 , R 9 , R 10 and R 11 for example are C 1 -C 6 alkyl which is unsubstituted or substituted by halogen; or R 8 , R 9 and R 10 are phenyl which is unsubstituted or substituted by C 1 -C 4 alkyl or halogen; or R 10 and R 11 together are 1,2-phenylene or C 2 -C 6 alkylene which is unsubstituted or substituted by C 1 -C 4 alkyl or halogen.
摘要:
A process is disclosed for the separation of an enantiomerically enriched 1-tosyloxy-2-acyloxy-3-butene and an enantiomerically enriched 1-tosyloxy-2-hydroxy-3-butene from a first mixture containing both compounds. The process includes the steps of: (a) forming a solution of the mixture in an organic solvent; (b) bringing the solution formed in (a) to a temperature wherein most of the enantiomerically enriched 1-tosyloxy-2-hydroxy-3-butene precipitates, leaving in solution most of the enantiomerically enriched 1-tosyloxy-2-acyloxy-3-butene; and (c) separating the precipitate formed in (b) from the solution.
摘要:
Amidino and benzamidino compounds, including compounds of formula (I), wherein R -R , R -R , Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of formula (I).
摘要:
Disclosed are compounds of the formula (I) and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, R N , and R C are defined herein. These compounds interact with and inhibit the activity of the enzyme beta- secretase. These compounds are therefore useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions and methods of treatment of these diseases are also disclosed.
摘要翻译:公开了式(I)化合物及其药学上可接受的盐,其中变量G,L,A,W,E,R2,R3,R4,R5,Rb,N, > C sb>在此定义。 这些化合物相互作用并抑制β-分泌酶的活性。 因此,这些化合物可用于治疗阿尔茨海默病和其他类似疾病。 还公开了治疗这些疾病的药物组合物和方法。
摘要:
The invention concerns a method for detecting and identifying and/or quantifying an enzymatic activity such as deaminase of a micro-organism, which consists in contacting an inoculum capable of containing a micro-organism with a deaminase activity with a culture medium for micro-organisms. The invention is characterised in that the culture medium comprises at least a detecting agent for determining, by forming a coloured product with a colour reagent, an enzymatic activity such as deaminase, said detecting agent comprising at least one compound of general formula (I): said detecting agent is an L-amino acid of general formula (I) in which R represents a cyclic amino acid radical, substituted by 1 to 3 groups X, identical or different; X represents a group limiting diffusion of alpha -keto acid produced by the deamination of the cyclic amino acid; the compound of formula (I) capable of being substituted by different groups not interfering with the function of group X. The invention also concerns a detection agent and a culture medium comprising at least a detecting agent.
摘要:
A process is disclosed for the isolation of an enantiomerically enriched alcohol from a first mixture of an enantiomerically enriched alcohol and an enantiomerically enriched ester. The process includes the steps of: (a) contacting the mixture with a reagent capable of reacting with the hydroxy function of the alcohol, without the loss of optical purity, so as to produce a second mixture containing a base-stable derivative of the enantiomerically enriched alcohol and the unreacted ester; (b) contacting the second mixture with a base capable of reacting with the ester so as to produce a third mixture containing a compound more volatile than the base-stable derivative of the alcohol; (c) removing the volatile compound from the third mixture; and (d) converting the base-stable derivative of the alcohol back to the enantiomerically enriched alcohol, without the loss of optical purity.
摘要:
This invention relates to novel precursors suitable for 18 F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18 F radiolabeling of glutamate derivatives wherein the obtained 18 F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.