Abstract:
본 발명은 글리코젠 합성 카이네이즈 3β (glycogen synthase kinase 3β)에 대한 저해활성과 다양한 암 세포주에 대한 성장저해작용을 나타내는 신규 피라졸로피리미딘온 유도체 또는 이의 약제학적 허용 가능한 염과 이 화합물의 제조방법 및 이 화합물을 유효성분으로 하는 항암제 조성물에 관한 것이다. 피라졸로피리미딘온 유도체, 암 질환, 암 세포성장저해, 글리코젠 합성 카이네이즈 3β
Abstract:
A pharmaceutical composition comprising pyrazole derivative having antagonistic effects against serotonin 5-HT3A(5-hydroxytryptamine(serotonin) receptor 3A) is provided to improve the inhibitory activity and bonding activity about 5-HT3A, thereby being applicable to the therapeutic agent of the central nervous system disease. The pharmaceutical composition for prevention and treatment of the central nervous system disease associated with serotonin 5-HT3A receptor comprises the pyrazole derivative compound and pharmaceutically acceptable salts, wherein the central nervous system disease is selected from emesis. nausea, alcoholism, drugs abuse, depression, compulsion neurosis, anxiety, seizure, Alzheimer type dementia, Parkinson's disease, Huntington`s chorea, psychosis, schizophrenia, suicidal tendency, somnopathy(sleep disorders), appetite disorder and migraine.
Abstract:
3-(4-Chloro)-4-oxo-2-thioxo-1,2,3,4-tetrahydro-quinazoline derivatives as T-type calcium channel antagonists are provided to treat neurogenic pain, epilepsy, hypertension or angina pectoris by inhibiting the T-type calcium channel without side effects such as pharmacokinetic interactions. 3-(4-chloro)-4-oxo-2-thioxo-1,2,3,4-tetrahydro-quinazoline derivatives represented by the formula(I) is used as a pharmaceutical composition, wherein X is (3-piperidin-1-yl-propyl)-amide, [3-(2-ethyl-piperidin-1-yl)-propyl]-amide, [3-(4-methyl-piperidin-1-yl)-propyl]-amide, 2-(butyl-methyl-amino)-ethyl-amide, (3-pyrrolidin-1-yl-propyl)-amide, (3-azepan-1-yl-propyl)-amide, [3-(4-ethyl-piperazin-1-yl)-propyl]-amide, [3-(benzyl-methyl-amide)-propyl]-amide or (2-dimethylamino-ethyl)-amide, and the compound represented by the formula(I) includes 3-(4-chloro-benzyl)-7-(4-methyl-piperazine-1-carbonyl)-2-thioxo-2,3-dihydro-1H-quinazolin-4-one.
Abstract:
Novel 1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel are provided to treat brain diseases including epilepsy, hypertension and angina pectoris, heart disease and nerve system pain by inhibiting the T-type calcium channel as a representative low-voltage activated calcium channel. The 1,3-dioxoisoindole derivatives represented by the formula(1) or their pharmaceutically acceptable salts are provided, wherein R1 is phenyl group or benzyl group which is substituted or unsubstituted by halogen atom, C1-C6 alkoxy group, C1-C6 alkyl group, or cyano group; R2 is a hetero ring group selected from piperidinyl group, pyrolidinyl group, morpholinyl group and piperazinyl group which is substituted or unsubstituted by C1-C6 alkyl substituent; and n is 1 or 2, provided that a compound in which R2 is morpholinyl group when R1 is C1-C6 alkyl-substituted phenyl group is excluded.