Abstract:
PURPOSE: Phenylamidine derivatives having anti-oxidant activity and a pharmaceutical composition containing the same are provided. The compounds have improved anti-oxidant activity and lower toxicity. CONSTITUTION: Phenylamidine derivatives are characterized by the formula 1, wherein X1 and X2 are independently hydrogen, or linear or branched chain alkyl having C1-C9 saturated or unsaturated carbon; Y is CH2 or CH=CH(C=O); and Ar is phenyl, thiopen or pyrrole. An anti-oxidant is characterized by containing the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof. The pharmaceutical composition for prevention of aging and treatment of cancer, diabetes, epilepsy, apoplexy, Parkinson's disease, Huntington's disease and dementia contains the phenylamidine derivatives of the formula 1 and pharmaceutically acceptable salts thereof.
Abstract:
PURPOSE: A 4-hydroxycinnamamide derivative, pharmaceutically acceptable salt thereof and preparation thereof are provided. A pharmaceutical composition containing them as an active ingredient for use in anti-aging, and treating cancers, diabetes, epilepsy and neurodegenerative diseases is also provided. CONSTITUTION: The 4-hydroxycinnamamide derivative has the formula 1, wherein each of X1 and X2 is independently hydrogen or a C1-C15 saturated or unsaturated, linear or branched alkyl group; each of Y1, Y2, Y3 and Y4 is independently hydrogen, halogen, hydroxy group, amino group, phenyl group, C1-C8 alkyl group or C1-C8 alkoxy group; and n is an integer between 0 and 9. The 4-hydroxycinnamamide derivative and pharmaceutically acceptable salt thereof have excellent anti-oxidant activity and low toxicity compared to other conventional anti-oxidants.
Abstract:
PURPOSE: Provided is a quinone compound having excellent antioxidant activity, which can be used for preventing aging and curing cancer, diabetes, epilepsy, imbecility, Parkinson's disease, and etc. CONSTITUTION: The quinone compound is represented by the formula 1 and produced from a compound represented by the formula 3, wherein R1 and R2 are independently methyl or methoxy or R1 and R2 are connectively -CH=CH-CH=CH-, R3 is -NH-(CH2)m-R5, -CO2R6, -OH, and etc., R5 is methyl, phenyl, benzyl, and etc., R6 is hydrogen atom or C1-C4 alkyl, X is CH2 or C=O, and n and m are each 0 or an integer of 1-10.
Abstract:
본 발명은 하기 화학식 1로 표시되는 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체 또는 이의 약제학적으로 허용 가능한 염, 이를 유효성분으로 함유하는 신경퇴행성 질환의 예방 및 치료용 약제학적 조성물 및 이를 유효성분으로 함유하는 베타-세크리테아제(BACE)의 활성 억제제 조성물에 관한 것이다. [화학식 1]
본 발명에 따른 4-(벤즈이미다졸-2-일아미노)피롤리딘 유도체는 베타-세크리테아제(BACE)의 활성을 억제하여 신경세포를 손상시키는 베타-아밀로이드 단백질의 생성을 억제함으로써 알츠하이머, 다운증후군 등의 신경퇴행성 질환을 치료하거나 예방하는데 효과적으로 사용될 수 있다.
Abstract:
본 발명은 하기 화학식 Ⅰ로 표시되는 (3R)-아미노-(4R)-아릴피페리딘 화합물 또는 이의 약제학적으로 허용 가능한 염에 관한 것이고, 또한 상기 3R)-아미노-(4R)-아릴피페리딘 화합물 또는 이의 약제학적으로 허용 가능한 염을 유효성분으로 함유하는 알쯔하이머 또는 다운증후군의 예방 또는 치료용 조성물, 또는 베타-세크리테아제(BACE)의 활성 억제제 조성물에 관한 발명이다. [화학식 Ⅰ]
본 발명에 따른 3R)-아미노-(4R)-아릴피페리딘 화합물은 베타-세크리테아제(BACE)의 활성을 억제하여 신경세포를 손상시키는 베타-아밀로이드 단백질의 생성을 억제함으로써 알츠하이머 질환을 치료하거나 예방하는데 효과적으로 사용될 수 있다. 알츠하이머 질환, 피페리딘 화합물, 베타-세크리테아제, 노화, 신경퇴행성 질환, 베타-아밀로이드
Abstract:
A novel piperazine derivative is provided to show excellent antagonism against a dopamine receptor D4, thereby being effective as a therapeutic agent for schizophrenia. A piperazine derivative having a cycloalkyl bicyclic heterocycle group is represented by a formula(1), where R1 is a group represented by the structural formula(1) or (2); X is H, halogen, nitro, cyano, C1-6 alkyl, or C1-6 alkoxy; Y is NH, S or O; R2 is phenyl or pyridine, which may be substituted or unsubstituted by a substituent selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, and cyano; n is an integer from 1 to 3. A method for preparing a piperazine compound represented by the formula(1b) comprises the steps of: (a) subjecting cyclopentanone carboxylic acid coupled to a Wang resin and represented by the formula(3) with a piperazine to a reducing amination to obtain a compound represented by the formula(3a); and (b) applying microwave to the compound of the formula(3a) with an amine compound represented by the formula(3b) to synthesize the compound of the formula(1b), where R2, X, Y, and n are the same as defined above, and A is Wang resin. A therapeutic agent for schizophrenia comprises the compound of the formula(1) or a pharmaceutically acceptable salt thereof.
Abstract:
Huperzine-tacrine hybrids and preparing process thereof is provided to improve inhibiting activity of acetylcholine esterase(AChE) associated with occurrence of neurodegenerative disease, and enhance their production yield. The huperzine-tacrine hybrid derivatives represented by the formula(1) having neurodegenerative disease-treating effect are provided, wherein X is hydrogen, halogen group or C1-C6 alkyl group, m is 1 to 3 and n is 1 or 2; and the neurodegenerative disease is dementia. The precursors of the huperzine-tacrine hybrid derivatives represented by the formula(6) are provided. The process for preparing the huperzine-tacrine hybrid derivatives comprises the steps of: (1) treating chloro acrydine represented by the formula(2) with hydroxylamine to prepare hydroxy compounds represented by the formula(3); (2) oxidizing the compounds of the formula(3) with an oxidizing agent selected from pyridinium chlorochromate(PCC), pyridinium dichromate(PDC), Jone's reagent and manganese dioxide to prepare aldehyde compounds represented by the formula(4); (3) condensing the aldehyde compounds of the formula(4) with pyridineamine represented by the formula(5) by using a molecular sieve to prepare immine, and reducing it to prepare compounds represented by the formula(6); and (4) deprotecting the compounds of the formula(6) by using trimethylsilyl iodide(TMSI).
Abstract:
본 발명은 다음 화학식 1로 표시되는 후퍼진(huperzine) B 유도체와 이의 제조방법에 관한 것으로서, 더욱 상세하게는 다음 화학식 2로 표시되는 카르복실산 화합물을 출발물질로 사용하고, C5 위치의 카르복실기를 아민화 및 N -알켄일화하여 다음 화학식 4로 표시되는 화합물을 반응 중간체로 합성한 후에, 이 중간체 화합물을 복분해반응(Ring Closing Metathesis, RCM)한 후에 메틸보호기를 제거하는 일련의 제조과정을 거쳐 합성하게 되는, 다음 화학식 1로 표시되는 후퍼진 B 유도체와 이의 제조방법에 관한 것이다. 본 발명에 따른 상기 화학식 1로 표시되는 화합물은 치매치료 효과가 있는 것으로 잘 알려져 있는 후퍼진 B 화합물의 유도체로서 화합물 그 자체의 의약적 활성이 기대된다.