Abstract:
A pharmaceutical composition is provided to prevent and cure diseases relating to MCH using an aryl piperidine group-containing imidazole derivative as an active ingredient. A pharmaceutical composition includes an aryl piperidine group-containing imidazole derivative represented by a formula to an active ingredient. In the formula: R1 is group1, and group2 or group3; R4 is H, halogen, C1~C3 of a straight-chain or a side-chain alkyl, or C1~C3 of a straight-chain or a side-chain alkoxy; W is CH or N; Y is O, S or NR8; R8 is H or C1~C3 of a straight-chain or a side-chain alkyl; M is an integer of 1-2; R2 is H, halogen, C1~C3 of a straight-chain or a side-chain alkyl, or C1~C3 of a straight-chain or a side-chain alkoxy, NO2; R3 is C1~C3 of a straight-chain or a side-chain alkyl; A is CH; and N is an integer of 2-5.
Abstract:
A composition is provided to decrease ischemic apoptosis significantly, thereby being usefully utilized as a prophylactic or therapeutic agent of ischemic diseases mediated by the ischemic apoptosis, or an organ protecting agent. A composition for preventing or treating an ischemic disease selected from the group consisting of cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, cardiac failure, hypertrophy, retinal ischemia, ischemic colitis, ischemic acute cardiac failure, stroke, traumatic brain injury, Alzheimer's disease, Parkinson's disease, newborn hypoxia, glaucoma and diabetic neurosis mediated by ischemic apoptosis comprises an N-phenyl amide derivative represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein the ischemic apoptosis is induced under low oxygen condition. In the formula(1), R^1 is H, -CO2R^5, -CH2OR^5, -CONR^5R^5, or a structural formula(1)(wherein each R^5 and R^6 is independently H or methyl); each R^2, R^3 and R^4 is independently H, C1-3 alkyl or alkoxy, or halogen; B is H or phenyl; n is 0 or 1; Y is S; Z is H, halogen or C1-3 alkoxy; and A is CH or N.
Abstract translation:提供了显着降低缺血性凋亡的组合物,从而有效地用作由缺血性细胞凋亡介导的缺血性疾病或器官保护剂的预防或治疗剂。 用于预防或治疗缺血性疾病的组合物,其选自脑缺血,心脏缺血,糖尿病心血管疾病,心力衰竭,肥大,视网膜缺血,缺血性结肠炎,缺血性急性心力衰竭,中风,创伤性脑损伤,阿尔茨海默氏病, 由缺血性细胞凋亡介导的帕金森病,新生儿缺氧,青光眼和糖尿病性神经症包括由式(1)表示的N-苯基酰胺衍生物或其药学上可接受的盐作为有效成分,其中在低氧条件下诱导缺血性凋亡。 在式(1)中,R 1是H,-CO 2 R 5,-CH 2 OR 5,-CONR 5 R 5或结构式(1)(其中每个R 5和R 6独立地是H 或甲基); 每个R 2,R 3和R 4独立地是H,C 1-3烷基或烷氧基或卤素; B是H或苯基; n为0或1; Y是S; Z是H,卤素或C 1-3烷氧基; A是CH或N.
Abstract:
A novel pyrazole compound is provided to show excellent inhibitory activity on PDE-4 enzyme, thereby being used in order to prevent and treat asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases. A 1-(3,4-dialkoxybenzyl)-1H-pyrazole compound is represented by the formula(1), wherein each R1 and R2 is independently H, linear or branched C1-7 alkyl, linear or branched C1-7 C1-7 alkyl including halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, phenyl, benzyl or allyl, or R1 and R2 may be linked to each other with C1-3 alkylene or C1-3 alkylene including halogen; R3 is H, formyl, halogen, linear or branched C1-10 alkyl, C1-10 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, (C1-10)alkylcarboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl; (C3-7)cycloalkylamino, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide, cyano, nitro, carboxylic acid guanidine, urea, phenoxy, benzyloxy, or an Aryl represented by the group(I); each R4 and R5 is independently H, halogen, formyl, linear or branched C1-10 alkyl, C1-10 alkoxy, (C1-10)alkoxy(C1-10)alkyl, C1-7 alkylketone, hydroxy(C1-10)alkyl, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, carboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, phenyl, phenoxy, benzyl, benzyloxy, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkoxy including O, N or S in a hetero-cycle, cyano, nitro, (C3-7)cycloalkylamino, guanidine, or urea. A method for preparing the compound of the formula(1) comprises a step of reacting a halobenzyl compound represented by the formula(3) with a pyrazole compound represented by the formula(4), each R1, R2, R3, R4, and R5 are same as defined above, and X is halogen. A pharmaceutical composition for preventing and treating inflammation related diseases such as asthma and chronic obstructive pulmonary diseases comprises the compound of the formula(1) as an effective ingredient.
Abstract:
본 발명은 목단피(Moutan Cortex Radicis) 추출물, 옥시패오니플로린(oxypaeoniflorin), 패오니플로린(paeoniflorin), 메틸패오니플로린(methylpaeoniflorin) 또는 패오니다닌(paeonidanin)을 유효성분으로 함유하는 혈압강하용 조성물에 관한 것이다. 본 발명에 따른 조성물은 혈관 평활근 이완작용을 통해 우수한 혈압강하효과를 나타내므로 고혈압 및 고혈압의 합병증으로 인한 각종 심혈관계질환의 예방 및 치료를 위한 약학 조성물뿐만 아니라 식품첨가물로도 유용하게 사용될 수 있다.
chinensis ) 추출물, 또는 이로부터 분리된 (-)-소서네올[(-)-saucerneol], 소서네올 C(saucerneol C), 마나산틴 A(manassantin A) 또는 마나산틴 B를 유효성분으로 함유하는 건강증진용 식품에 관한 것이다. 본 발명에 따른 식품은 비정상적인 B 세포 및 T 세포의 증식을 효과적으로 억제하여 우수한 면역억제효과를 나타내므로 장기이식거부반응, 자가면역질환, 알러지, 아토피 등과 같은 면역과민반응으로 야기되는 질환의 예방을 위한 건강증진용 식품으로서 유용하게 사용될 수 있다.
Abstract:
본 발명은 3,5-위치가 치환된 퓨란-2-카르보닐구아니딘 유도체, 그의 제조방법 및 이를 포함하는 약학적 조성물에 관한 것이다. 본 발명의 3,5-위치가 치환된 퓨란-2-카르보닐구아니딘 유도체는 나트륨/수소 교환통로인 NHE-1에 대하여 강력한 억제작용을 나타내고, 적출 허혈심장모델에서 허혈/재관류에 의한 심장기능 손상의 회복을 증진시키며, in vivo 허혈동물모델에서 심근경색의 크기를 유의성있게 감소시켜 우수한 심장보호효과를 나타낸다. 따라서, 본 발명의 조성물은 심근경색, 부정맥, 협심증 등의 허혈성 심장질환의 예방 및 치료에 유용하게 사용될 수 있으며, 관동맥우회술, 관동맥경피성형술 등 심장시술 시 또는 혈전용해제 등 재관류요법에 대한 심장보호제 등으로 사용될 수 있다.
Abstract:
본 발명은 퓨란카보닐구아니딘 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것이다. 본 발명의 퓨란카보닐구아니딘 유도체는 나트륨/수소 교환통로인 NHE-1 (sodium-hydrogen exchanger isoform 1)을 억제하여 허혈/재관류 손상에 대하여 심장기능 회복을 증진시키고 심근경색율을 감소시켜 심근세포 손상을 보호함으로써, 심근경색, 부정맥, 협심증 등의 허혈성 심장질환의 예방 및 치료제로 사용할 수 있으며, 또한 관동맥우회술, 관동맥경피성형술 등 심장시술시 또는 혈전용해제 등 재관류요법에 대한 심장보호제 등으로 사용할 수 있다.