Abstract:
PURPOSE: A 2-substituted 6-(biphenyl-4-carboxamido)quinoxaline derivative is provided to suppress MCH1R and to prevent and treat obesity. CONSTITUTION: A 2-substituted 6-(biphenyl-4-carboxamido)quinoxaline derivative is denoted by chemical formula 1. A MCH1R inhibitor composition contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing and treating obesity contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.
Abstract:
본 발명은 클로로이미다졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료용 약학적 조성물에 관한 것으로서, 상기 유도체는 TAZ 단백질을 조절하므로, 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료에 유용하게 사용될 수 있다. 클로로이미다졸 유도체, TAZ, 골다공증, 비만, 당뇨, 고지혈증
Abstract:
본 발명은 화학식 1로 표시되는 2-설파닐-벤즈이미다졸-4-카르복스아미드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 폴리(ADP-리보스)폴리머라제-1(PARP-1)의 과활성에 의해 유발되는 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명의 상기 유도체들은 과활성화시에 다량의 ATP를 소비하여 세포 손상 및 세포 사멸을 초래하는 효소인 PARP-1를 강력히 억제하는 바, 심근경색, 협심증, 부정맥, 심부전증, 뇌졸중, 뇌외상 또는 신부전증을 포함하는 허혈성 질환과 파킨슨씨 질병, 알츠하이머 질병 또는 다발성 경화증을 포함하는 신경퇴행성 질환의 예방 또는 치료 용도로, 또한 관동맥우회술 또는 관동맥경피성형술을 포함하는 수술요법과 혈전용해제를 이용한 재관류 요법과 같은 약물요법 시술시에 심장보호용도로 유용하게 사용될 수 있다. [화학식 1]
(상기 식에서, R 1 , R 2 , X 및 n은 명세서에 정의된 바와 같다.) 2-설파닐-벤즈이미다졸-4-카르복스아미드 유도체, PARP-1 억제제, 허혈성 질환, 신경퇴행성 질환
Abstract:
PURPOSE: A pharmaceutical composition containing phenyltetrazole derivatives for preventing or treating osteoporosis, obesity, diabetes or hyperlipidemia is provided to control TAZ(transcriptional coactivator with PDZbinding motif) protein. CONSTITUTION: A pharmaceutical composition for preventing or treating osteoporosis contains a compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing or treating obesity, diabetes or hyperlipidemia contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. The compound is phenyltetrazole derivatives.
Abstract:
본 발명은 하기 화학식 1의 아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체, 이의 제조 방법 및 이를 포함하는 약학적 조성물에 관한 것으로, 본 발명의 아마이드로 치환된 벤조퓨란 및 벤조싸이오펜 유도체는 허혈성 세포사를 현저히 감소시킬 수 있으므로, 이를 유효성분으로 함유하는 조성물은 허혈성 세포사에 의해 매개되는 허혈성 질환의 예방 및 치료제 또는 장기 보호제로 유용하게 활용될 수 있다.
상기 식에서, R 1 , B, n, Y, Z, X, W 및 A는 명세서 중에 정의한 바와 같다.
Abstract:
Benzofuran and bezothiophene derivatives substituted with amide, a preparation process thereof, and a pharmaceutical composition containing the same are provided to prevent and treat ischemic diseases such as cerebral ischemia mediated by ischemic cell death. Benzofuran and bezothiophene derivatives substituted with amide are represented by the chemical formula 1. The benzofuran and bezothiophene derivatives substituted with amide of the chemical formula 1 is obtained by reacting a compound of the chemical formula 2 and a compound of the chemical formula 3. The benzofuran and bezothiophene derivatives substituted with amide or their pharmaceutically acceptable salts is contained as an active ingredient of a pharmaceutical composition for preventing and treating ischemic diseases.
Abstract:
An imidazol derivative having an aryl piperidine substituent is provided to prevent and cure diseases relating to MCH by acting on an antagonist to a melanin-concentrating hormone receptor. An imidazole derivative or a salt pharmaceutically allowable is indicated as a chemical formula 1. In the chemical formula 1: R1 is a group 1 or a group 2; X is H, halogen, OR4, C1~C4 of straight-chain or side chain alkyl, CF3, phenyl, CN, NO2, -CO2R5 or -CONR6R7; R4, R5, R6 and R7 are independently H, halogen, C1~C3 of straight-chain or side chain alkyl or phenyl; R2 is H, halogen, C1~C3 of straight-chain or side chain alkyl, phenyl, OR4, NO2, CN, pyridyl or -CONR6R7; R3 is C1~C3 of straight-chain or side chain alkyl and phenyl substituted into halogen or methyl; A is CH or N; and n is an integer of 2 - 5.
Abstract:
An aminothiophene derivative is provided to decrease ischemic apoptosis, thereby being used as a composition for preventing and treating ischemic diseases mediated by the ischemic apoptosis or for protecting organs. A composition for preventing or treating ischemic diseases comprises an aminothiophene derivative represented by a formula(1) or (2), or a pharmaceutically acceptable salt thereof as an effective ingredient, wherein the ischemic disease is cerebral ischemia, cardiac ischemia, diabetic cardiovascular diseases, cardiac failure, cardiac hypertrophy, retinal ischemia, ischemic colitis, ischemic acute renal failure, stroke, cerebral wound, Alzheimer's disease, Parkinson's disease, hypoxia in newborn, glaucoma and diabetic neuropathy. In the formulae, R^1 is H, CO2R^2, CH2OR^2, CONR^2R^3, or a group(1); each R^2 and R^3 is independently H, or C1-6 linear or branched alkyl, or halogen or hydroxy substituted alkyl; B is H, phenyl, or C1-3 alkyl or halogen substituted phenyl; n is an integer from 0 to 2; Y is S, O, SO or SO2; Z is H, halogen, NO2, NH2, C1-3 linear or branched alkyl or OR^4; R^4 is H or C1-3 linear or branched alkyl; and A is CH, N or N-O. Further, the ischemic diseases are selected from cerebral ischemic damage, Ischemic Heart Failure, cardiac failure, retinal ischemia or Alzheimer's disease.
Abstract translation:提供氨基噻吩衍生物以减少缺血性细胞凋亡,从而用作预防和治疗由缺血性细胞凋亡或保护器官介导的缺血性疾病的组合物。 用于预防或治疗缺血性疾病的组合物包含由式(1)或(2)表示的氨基噻吩衍生物或其药学上可接受的盐作为有效成分,其中缺血性疾病是脑缺血,心脏缺血,糖尿病心血管疾病, 心脏衰竭,心脏肥大,视网膜缺血,缺血性结肠炎,缺血性急性肾衰竭,中风,脑伤,阿尔茨海默病,帕金森病,新生儿缺氧,青光眼和糖尿病性神经病变。 在式中,R 1是H,CO 2 R 2,CH 2 OR 2,CONR 2 R 3,或基团(1); 每个R 2和R 3独立地是H或C 1-6直链或支链烷基,或卤素或羟基取代的烷基; B是H,苯基或C 1-3烷基或卤素取代的苯基; n为0〜2的整数; Y是S,O,SO或SO2; Z是H,卤素,NO 2,NH 2,C 1-3直链或支链烷基或OR 4; R 4是H或C 1-3直链或支链烷基; A是CH,N或N-O。 此外,缺血性疾病选自脑缺血性损伤,缺血性心力衰竭,心力衰竭,视网膜缺血或阿尔茨海默病。
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.