Abstract:
The present invention relates to a novel 5-sulfonylamino-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one compound having an inhibitory activity for 5-HT6, which is one of serotonin subtypes, and a pharmaceutical composition comprising the compound as an active ingredient. Since the novel compound of the present invention has 5-HT6 inhibitory activities, the compound can be used for diagnosing, preventing, and treating central nervous system (CNS) diseases such as Alzheimer′s disease (AD), attention deficit disorder (ADHD), epilepsy, depression, obesity, schizophrenia, sleep disorders, and pain disorders.
Abstract:
본 발명은 칼슘이온 채널 조절제로서 유효한 피라졸릴메틸아민-피페라진 유도체 및 이의 약제학적으로 허용 가능한 염, 이들 화합물의 제조방법, 그리고 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다. 피라졸릴메틸아민-피페라진 유도체, 칼슘이온 채널 조절제, 뉴런, 탈분극화, 급성통증, 만성통증, 신경병증성 통증, 고혈압치료제
Abstract:
PURPOSE: A pyrazolylmethylamine-piperazine derivative which is effective as a calcium ion channel modulator is provided to ensure effective activation as an T-type calcium ion channel antagonist and to use as an agent for preventing and treating brain diseases, heart diseases and pain diseases. CONSTITUTION: A pyrazolylmethylamine-peperazine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases, heart diseases or pain diseases by T-type calcium ion channel antagonism contains the pyrazolylmethylamine-peperazine derivative of chemical formula 1 or its pharmaceutically acceptable salt an active ingredient. The brain disease is epilepsy, depression, Parkison's disease, dementia or somnipathy. The heart disease is hypertension, cardiac arrhythmia, myocardial infarction, or congestive failure. The pain disease is chronic pain, acute pain, or neurogenic pain. The pyrazolylmethylamine-peperazine derivative is prepared by binding pyrazolylmethylamine compound of chemical formula 3 with piperazine acetyl halide compound of chemical formula 2.
Abstract:
본 발명은 신규한 피라졸릴카르복스아미도알킬피페라진 유도체와 이의 제조방법 및 이 화합물이 갖는 칼슘이온 채널 억제 효과에 의한 질환 치료제로 사용하는 의약적 용도에 관한 것이다. 피라졸릴카르복스아미도알킬피페라진 유도체, 칼슘이온 채널 억제제, 뉴런, 틸분극화, 급성통증, 만성통증, 신경병증성 통증, 항암제, 고혈압치료제
Abstract:
A novel compound having antagonism in 5-HT7 receptor is provided to be usefully used for relax and treatment of disease mediated in 5-HT7 or symptom and to have good pharmaceutical properties. A novel compound having antagonism in 5-HT7 receptor is represented by a chemical formula (I). In the chemical formula (I), R1 is substitution radical selected from a group consisting of alkyl of C1~C4 substituted for halogen or nitro and alkoxy of C1~C4 or phenyl or benzyl; R2 is anisole naphthalene or quinoline; R3 is H, C1~C4 alkyl, halogen or C1~C4 alkoxy; R4 is H or C1~C3 alkyl not substituted for cyclo C5~C7 alkyl or phenyl.
Abstract:
A composition for blocking T-type calcium channel comprising morpholin-2-one derivatives is provided to block the T-type calcium channel in the same level as the conventional T-type calcium channel blocker, mibefradil, without side effects. A composition for blocking T-type calcium channel comprises morpholin-2-one derivatives represented by the formula(1), or pharmaceutically acceptable salts thereof, wherein R^1 and R^2 are each independently hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy; and R^3 and R^4 are each independently hydrogen, C1-C6 alkyl, C1-C6 thioalkyl, amino or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy. The composition prevents or treats diseases caused by overexpression of T-type calcium channel including angina pectoris, hypertension, myocardiac infarction, pain and epilepsy.
Abstract:
A novel piperazinylalkylpyrazole derivative is provided to be able to selectively block T-type calcium ion channels, thereby showing better pain, hypertension, and epilepsy therapeutic effect compared to conventional medicines. The piperazinylalkylpyrazole derivative is represented by the formula(1), where R1 is phenyl, X1-substituted phenyl(where X1 is nitro, methyl, chloro, or methoxy, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), 1,1-diphenylmethyl or X2-substituted diphenylmethyl(where X2 is chloro or methyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), R2 is H, methyl or ethyl, R3 is methyl, propyl, isobutyl, phenyl, cyclohexyl, substituted phenyl(methyl, chloro, or methoxy as a substituent), naphthyl, piperidinyl, R4 is H, C1-6 alkyl, 2-furyl, phenyl or X3-substituted phenyl(where X3 is chloro, methyl, cyclohexyl or piperidinyl, the substitution position is ortho, meta, or para, and mono, di, tri, tetra or all are able to be substituted), and n is an integer from 0 to 3.