Abstract:
The present invention relates to a 2-(substituted ethynyl)quinoline derivative having activity as an mGluR5 antagonist and to a pharmaceutically acceptable salt of the same. The compound of the present invention can be used as a medicine to treat and prevent mGluR5 acceptor-mediated diseases, for example; Alzheimer′s, senile dementia, Parkinson′s disease, L-dopa-induced dyscinesia, Huntington′s chorea, amyotrophic lateral sclerosis, disseminated sclerosis, schizophrenia, anxiety disorders, dysthymia, neuropathic pains, drug dependence, fragile X syndrome, autism, migraine, and gastroesophageal reflux disease (GERD).
Abstract:
본 발명은 테트라베나진 (TBZ)과 다이하이드로테트라베나진 (DTBZ)의 제조방법에 관한 것으로, 더욱 상세하게는 6,7-다이메톡시-1,2,3,4-테트라하이드로아이소퀴놀린과 4-메틸-2-(3-(트리메틸실릴)프로프-1-엔-2-일)펜탄을 출발물질로 사용하여, 알킬화 반응, 산화제 존재 하에서의 아자-프린스 고리화 반응, 산화반응을 순차적으로 수행하는 간결하고 짧은 반응공정에 의해 테트라베나진 (TBZ)과 다이하이드로테트라베나진 (DTBZ)을 제조하는 방법에 관한 것이다.
Abstract:
본 발명은 3,4-다이메틸렌옥세페인 화합물과 이의 제조방법에 관한 것으로서, 더욱 상세하게는 알렌닐 알코올 화합물과 알데하이드 화합물을 특정의 루이스산과 특정의 용매 존재하에서 프린스 고리화 반응을 수행하여 제조된, 입체선택성을 가지는 하기 화학식 1로 표시되는 3,4-다이메틸렌옥세페인 화합물과 이 화합물의 제조방법에 관한 것이다. [화학식 1]
상기 화학식 1에서, R 1 은 수소원자; C 1-6 알킬기; 또는 페닐기를 나타내고, R 2 는 C 1-6 알킬기; 할로, 나이트로, C 1-6 알킬, 및 C 1-6 알콕시 중에서 선택된 1 내지 3개의 치환기로 치환 또는 비치환된 페닐기; 퓨란일기; 또는 티오펜일기를 나타낸다.
Abstract:
PURPOSE: A methylidene-heterocyclic compound and a pharmaceutical composition containing the same are provided to strongly suppress IkappaB kinase-b(IKK-b) and to treat various inflammatory diseases. CONSTITUTION: A methylidene-heterocyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating inflammatory diseases contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, juvenile arthritis, asthma, spondyloarthopathies, gout, osteoarthritis, allergic rhinitis, atopic dermatitis, systemic lupuserythematosus, psoriasis, ulcerative colitis, SIRS, sepsis, or polymyositis. A method for preparing the compound of chemical formula 1 comprises: a step of cyclizing an aniline compound of chemical formula 2 and preparing a 3-phenyl rhodanine compound of chemical formula 3; and a step of condensing the compound of chemical formula 3 with aldehyde compound of R2-C(O)H under an acidic condition. [Reference numerals] (AA) Step 1; (BB) Step 2
Abstract:
PURPOSE: A pharmaceutical composition containing 1,4-diazepane pyrazole compound and a pharmaceutically acceptable salt thereof is provided to be used as an agent for preventing or treating brain diseases, heart diseases, cancer, epilepsy, and pain. CONSTITUTION: A 1,4-diazepane pyrazole compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating brain diseases such as epilepsy, depression, Parkinson's diseases, dementia, sleep disorders, or heart diseases such as hypertension, cardiac arrhythmia, or myocardial infarction, or pain contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound of chemical formula 1 comprises a step of reacting pyrazolemethyl amine of chemical formula 2 with chloroacetyl chloride.
Abstract:
PURPOSE: A pharmaceutical composition containing pyrazoyl piperidine compounds and pharmaceutically acceptable salt thereof is provided to prevent or treat brain diseases, heard diseases, cancer, and pain. CONSTITUTION: A pyrazoyl piperidine compound is denoted by chemical formula 1. A pharmaceutical composition for treating cerebral diseases, cardiac diseases, cancer, or pain contains the compound of chemical formula 1 as an active ingredient. A method for preparing the compound comprises: a step of reacting piperidine acetate of chemical formula 2 and pyrazole methyl amine of chemical formula 3 of a step of reacting piperidine compound of chemical formula 4 with an aldehyde compound of chemical formula 5 by reduction-amination. [Reference numerals] (AA) Reductive amination