- Pharmaceutical composition for the treatment or prevention of stroke and systemic embolism
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The present invention relates to a prodrug useful for treating or preventing a stroke and systemic embolism and suitable for being effectively used in the oral delivery of dabigatran, and to a compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, and a hydrate thereof or a solvate thereof. The compound represented by the chemical formula 1, the pharmaceutically acceptable salt thereof, and the hydrate thereof or the solvate thereof are useful for treating or preventing a stroke and systemic embolism, and is suitable for being effectively used in oral delivery since the absorption rate, that is, bioavailability of dabigatran is improved.(AA) DSC curve of dabigatran pivoxyl (+)-(1S)- campo-10-sulfonateCOPYRIGHT KIPO 2015
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Paragraph 0272-0276
(2016/11/17)
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- COMPOUND HAVING TAFIA INHIBITORY ACTIVITY
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Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula -(CH2)-, the formula -(CH2)2-, an oxygen atom, a nitrogen atom or a single bond; Y is the formula -(CH2)3-NH-R3, the formula -(CH2)4-NH-R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula -CO2R4; R4 is a C1-6 alkyl group, the formula -CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; a R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.
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