Diaryl Derivatives of - 1.5 - 4.5 - dihydro 1h pyrazole - 3 - carboxamidina as CB1 cannabinoid receptor antagonist, method for its preparation, and Pharmaceutical composition comprising the same
KWEE HYUN SUH,TAE HEE HA,NAM DU KIM,YOUNG HEE JUNG,JONG OUK BAEK,HEE SOOK OH,DONG JIN HONG,MOON SUB LEE
申请号：
ARP140102438
公开号：
AR101053A1
申请日:
2014.06.30
申请国别(地区):
AR
年份:
2016
代理人:
摘要：
The present compound exhibits activity as a CB1 cannabinoid receptor antagonist with high selectivity for peripheral tissues, thereby exhibiting anti-obesity effects, and thus being useful in the prevention or treatment of obesity or related metabolic diseases. with obesity. Claim 1: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein A is selected from the group consisting of C₁₋₇-alkyl,aryl C₆₋₁₀,C₄₋₁₀ heteroaryl,cycloalkyl C₃₋₆,and C₃₋₆ heterocycloalkyl,a. Among the alternatives, each alternative consists of at least one alternative selected from the hydrogen group, c83218c832626 linear or branched, alcoxi c83218331 linear or branched, halo, dihalo, Trihalo, CN, oh, no832222；- (C 3DO) -R SH SR SOR SO R NHNHR NRR - (C 3DO) -NH- (C = O) -NHR, and - (C = O) -NRR； B and C are each independently C₆₋₁₀ aryl or C₄₋₁₀ heteroaryl,a. Among the alternatives, each alternative consists of at least one alternative selected from the hydrogen group, c83218c832626 linear or branched, alcoxi c83218331 linear or branched, halo, dihalo, Trihalo, CN, oh, no832222；- (C 3DO) -R SH SR SOR SO R NHNHR NRR - (C 3DO) -NH- (C = O) -NHR, and - (C = O) -NRR； R and R are each independently linear or branched C₁₋₆-alkyl； and R¹ and R² are each independently hydrogen or C₁₋₆ alkyl,and optionally, each of which is independently substituted with at least one substituent selected from the group consisting of hydrogen, linear or branched C₁₋₆-alkyl, linear or branched C₁₋₆-alkoxy, halo, CN, OH NO₂,And SH.El compuesto de la presente muestra actividad como antagonista del receptor de canabinoides CB1 con una alta selectividad por los tejidos periféricos, exhibiendo de este modo efectos anti-obesidad, y de este modo es útil en la prevención o tratamiento de la obesidad o enfermedades metabólicas relacionadas con la obesidad. Reivindicación 1: Un compuesto representado por la fórmula (1) o una de sus sales aceptables desde el punto de vista farmacéutico, en donde
