Abstract:
The invention provides processes for the manufacture of a compound of formula (I A ). The invention further provides improved methods for the conversion of the compound of formula (I A ) into pregabalin.
Abstract:
Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I)
(wherein, X represents a hydrogen atom or a halogen atom; R 1 represents a hydrogen atom; R 2 represents a hydrogen atom or a C 1-7 alkyl group; R 3 represents -CHO, -C(=O)R 5 , -COOR 5 (wherein R 5 represents a C 1-7 alkyl group), -CH 2 OH or -COOH; and R 4 represents a C 1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C 2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C 2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
Abstract translation:以下新型化合物可用于预防或治疗原生动物引起的疾病。 至少一种由式(I)表示的化合物(其中,X表示氢原子或卤素原子; R 1表示氢原子; R 2表示氢原子或C 1-7烷基; R 3表示 -CHO,-C(= O)R 5,-COOR 5(其中R 5表示C 1-7烷基),-CH 2 OH或-COOH; R 4表示具有一个的C 1-16烷基 或更多的末端碳原子和/或非末端碳原子上的取代基,在末端碳原子和/或非末端碳原子上具有一个或多个取代基的C 2-16烯基,或 使用在末端碳原子和/或非末端碳原子上具有一个或多个取代基的C 2-16炔基,其旋光异构体和药学上可接受的盐。
Abstract:
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R?1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13¿ and X are as defined in the specification. Compounds of formula (I) are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.
Abstract:
An optically active tri-substituted methane compound having, as substituents, an aromatic ring group and a phenyl group having hydroxyl group at ortho or para position can be obtained by allowing a phenol compound unsubstituted at the ortho- or/and para-position to react with an optically active secondary carbinol compound having an aromatic ring group at the alpha-position in the presence of tri-substituted phosphine and diazodicarboxylate or diazodicarboxamide. These and other optically active tri-substituted methane compounds are useful as active ingredients for medicines or as intermediate compounds for preparing medicines.
Abstract:
A polyprenyl carboxylic acid derivative having the general formula (I): in which n is an integer of from 2 to 4, R 1 represents the hydrogen atom or a protecting group for the carboxylic acid group, and R 2 represents a hydroxymethyl, formyl or carboxyl group. A process for the preparation of the polyprenyl carboxylic acid derivative involving microbiological oxidation using a strain belonging to the genus Nocardia is disclosed. The polyprenyl carboxylic acid derivative also exhibits pharmacological activity and is useful in form of a pharmaceutical composition.