摘要:
This invention relates to 3-amino piperadine derivatives, their intermediates and methods of manufacture. As such, the present invention includes methods of making a compound of the formulas (la) and (lb) wherein R,, R2, R3, R4, R,4, and n are herein defined. The present invention also relates to the compounds used in such processes, as well as the compounds made by the processes.
摘要:
The present invention relates to inhibitors of aspartic proteinases, particularly, BACE. The present invention also relates to compositions thereof and methods therewith for inhibiting BACE activity in a mammal, and for treating Alzheimer's Disease and other BACE-mediated diseases.
摘要:
N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要:
The present invention provides a novel process for the preparation of substituted piperidin-4-ones useful as intermediates in the preparation of pharmaceuticals.
摘要:
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
摘要:
The present invention provides a novel process for the preparation of substituted piperidin-4-ones useful as intermediates in the preparation of pharmaceuticals.
摘要:
A compound of formula (I) wherein R is hydrogen or an electron withdrawing group; one of X to X is a CR R group wherein at least one of R and R is C to C6 aliphatic group, an aromatic group, a heterocyclic group, a basic group or R CONH wherein R is a C1 to C6 aliphatic group, an aromatic group or a heterocyclic group and any remaining R or R is hydrogen; at least one of X to X is a CHR group wherein R comprises a hydrogen bond donor or acceptor; the remaining X to X groups are CH2, O or NR wherein R is hydrogen, a C1 to C6 aliphatic group, an aromatic group or a heterocyclic group; and y is 0 or 1, or a pharmaceutically acceptable salt thereof.
摘要:
Compounds of structure (1) are obtained by reduction of compounds of the structures (2a), (2b), (4a), (4b). Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inter alia paroxetine.
摘要:
Novel 1,4-substituted cyclic amine derivatives which have serotonin antagonism and serve as drugs having high clinical usefulness, especially an agent for the remedy/alleviation/prevention of spastic paralysis or a central muscle relaxant for alleviating myotonia. The derivatives are represented by general formula (I) or pharmacologically acceptable salts thereof, wherein A, B, C, D, T, Y, and Z each represents a methine group or a nitrogen atom; R , R , R , R , and R each represents a substituent; n is an integer of 0 to 3; m is an integer of 0 to 6; and p is an integer of 1 to 3.
摘要:
The invention concerns a method of preparing norbenzomorphane in the central intermediate stage in the preparation of pharmaceutically useful benzomorphane derivatives of general formula (1), in particular (-)-(1R,5S,2"R)-3'-hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzomorphane or [(-)-(2R,6S,2'R)-3-(2-methoxypropyl)-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-methanobenzo[ alpha ]oxacin-9-ol] (BIII 277).