Abstract:
The present invention relates to a novel anticancer composition and, more particularly, to a maleic acid derivative compound represented by Chemical Formula 1, a method for preparing the compound, and a pharmaceutical composition comprising the compound. The maleic acid derivative of the present invention selectively inhibits proliferation of a cancer cell line without affecting normal cells by inhibiting AIMP2-DX2 expression. Thus, the pharmaceutical composition containing the maleic acid derivative and a pharmaceutically acceptable salt thereof, as active ingredients, can be used for preventing and treating cancer.
Abstract:
본 발명은 신규한 2,4-피리미딘 유도체 및 이의 용도에 관한 것으로, 보다 상세하게는 전신성 홍반성 낭창에 효과가 있는 피리미딘 유도체, 이를 유효성분으로 포함하는 전신성 홍반성 낭창 예방 및 치료용 조성물 및 이를 스크리닝하는 방법에 관한 것이다. 본 발명자들은 gp96의 세포내 거류에 대한 분자 닻(anchor)인 AIMP1의 기능을 모방하여 gp96의 표면 전좌(translocation)를 저해하는 신규 물질을 찾았고, 이들 물질이 in vitro, in vivo상에서 자가면역질환 중 SLE 형질을 완화하여 SLE를 예방 및 치료하는 효과가 있음을 확인하였다. 따라서, 본 발명은 상기 기작을 이용하여 SLE의 치료제를 스크리닝하고, SLE를 예방 또는 치료하는 새로운 방법을 제공한다.
Abstract:
PURPOSE: A pharmaceutical composition containing novel chromeme derivative, pharmaceutically acceptable salts or isomers thereof is provided to prevent or treat blood clot-related diseases or cancer. CONSTITUTION: A chromene derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating PAR-1 activation-related diseases contains the chromene derivative, pharmaceutically acceptable salt, isomer as an active ingredient. A pharmaceutical composition for cardiovascular disease treatment aid contains the chromene derivative, pharmaceutically acceptable salt, or isomer as an active ingredient. A PAR-1 antagonist contains the chromene derivative, pharmaceutically acceptable salt, or isomer as an active ingredient.
Abstract:
A novel carbonitrile compound or its pharmaceutically acceptable salt, a method for preparing the compound, and a pharmaceutical composition containing compound are provided to prevent and treat osteoarthritis and various cancer without side effect. A carbonitrile compound is represented by the formula 1, wherein n is 1 or 2; R1 is H, halogen-substituted or unsubstituted linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C1-C10 alkoxy, C1-C10 alkylthio, hydroxy-C1-C10 alkyl, C1-C10 alkylcarbonyl, C1-C10 alkylthio-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C1-C10 alkoxy-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, or ar-C1-C10 alkoxy group; and R2 linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, C1-C10 alkoxycarbonyl, or ar-C1-C10 alkoxycarbonyl group.
Abstract:
A pharmaceutical composition for treating and preventing osteoporosis is provided to improve the selectivity and inhibitory activity to cathepsin K. A pharmaceutical composition for treating and preventing osteoporosis comprises a carbonitrile compound represented by the formula 1, wherein n is 1 or 2; R1 is H, F-substituted or unsubstituted linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C1-C10 alkoxy, C1-C10 alkylthio, C1-C10 hydroxyalkyl, C1-C10 alkylcarbonyl, C1-C10 alkylthio C1-C10 alkyl, C3-C7 cycloalkyl C1-C10 alkyl, C3-C7 cycloalkyl C1-C10 alkoxy, C1-C10 alkoxy C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, or ar-C1-C10 alkoxy group; and R2 is linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, C1-C10 alkoxycarbonyl, or ar-C1-C10 alkoxy group.
Abstract:
1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds are provided to inhibit activity of PDE-4(phosphodiesterase-4) with high activity and selectivity without side effects, so that the compounds are useful for treating inflammation diseases, neurodegenerative disease and cancers. 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds represented by the formula(1) are provided, wherein A is N or CH; R1 is linear or branched, saturated or unsaturated (C1-C7)alkyl or halogen-substituted linear or branched, saturated or unsaturated (C1-C7)alkyl; R2 is hydrogen atom, (C3-C7)cycloalkyl or (C3-C8)cycloalkylmethyl; R3, R4 and R5 are each independently hydrogen atom, phenyl, pyridinyl, N-oxypyridinyl, linear or branched, saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C3-C10)cycloalkyl(C1-C7)alkyl, halogen atom, cyano, nitro, amino, mono- or di(C1-C7)alkylamino, mono- or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamino, 3- to 7-membered saturated or unsaturated hetero ring containing oxygen, nitrogen or sulfur in hetero ring, guanidinyl, ureido, benzyl, benzyloxy, formyl, (C1-C7)alkanoyl, (C1-C7)alkoxy, (C1-C7)alkoxy(C1-C7)alkyl, hydroxy(C1-C7)alkyl, carboxyl or (C1-C7)alkoxycarbonyl; and R6 is pyridinyl or N-oxypyridinyl group.