Novel leukotriene b4 receptor inhibitors and use thereof
AssigneesEwha University-Industry Collaboration Foundation, Dongguk University Industry-Academic Cooperation Foundation
InventorsHyun Ae WOO, Hea-Young PARK, Jihye YOO, Darong KIM, Joohye KIM, Chang-Hoon LEE, Hyun Ji KIM
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Abstract
The present invention relates to N-phenylbenzoxazolo-2-amine and N-phenyloxazolopyridin-2-amine derivatives as novel leukotriene B4 receptor inhibitors, and use thereof.
Claims15
A compound represented by Formula 1 or a pharmaceutically acceptable salt thereof:
- in Formula 1,
- X is N or CR1,
- R1 to R4 are each independently hydrogen, halogen, nitro, C1-4 alkyl, or C1-4 alkoxy, and
- R5 to R9 are each independently hydrogen, amino, nitro, C1-4 alkoxy, hydroxy-C1-4 alkylcarbonylamino, C1-4 alkylcarbonyloxy-C1-4 alkylcarbonylamino, amino-C1-4 alkylcarbonylamino, or tert-butoxycarbonylamino-C1-4 alkylcarbonylamino.
A method of producing a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, the method comprising a 1 step of preparing a compound represented by Formula 3 by a cydization reaction of a hydroxyphenyl-thiourea derivative compound represented by Formula 2:
- in Formula 1,
- X is N or CR1,
- R1 to R4 are each independently hydrogen, halogen, nitro, C1-4 alkyl, or C1-4 alkoxy, and
- R5 to R9 are each independently hydrogen, amino, nitro, C1-4 alkoxy, hydroxy-C1-4 alkylcarbonylamino, C1-4 alkylcarbonyloxy-C1-4 alkylcarbonylamino, amino-C1-4 alkylcarbonylamino, or tert-butoxycarbonylamino-C1-4 alkylcarbonylamino.
A pharmaceutical composition for preventing or treating diseases related to LTB4 receptor activity, the composition comprising a compound of Formula 1 or a pharmaceutically acceptable salt thereof, as an active ingredient:
- in Formula 1 above,
- X is N or CR1,
- R1 to R4 are each independently hydrogen, halogen, nitro, C1-4 alkyl, or C1-4 alkoxy, and
- R5 to R9 are each independently hydrogen, amino, nitro, C1-4 alkoxy, hydroxy-C1-4 alkylcarbonylamino, C1-4 alkylcarbonyloxy-C1-4 alkylcarbonylamino, amino-C1-4 alkylcarbonylamino, or tert-butoxycarbonylamino-C1-4 alkylcarbonylamino.
Dependencies are inferred from the claim text.