Abstract:
본 발명은 하기의 화학식 1로 표시되는 신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1 H -피라졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 관절염, 아토피피부염, 백혈병과 각종 암 및 알쯔하이머 등의 퇴행성뇌질환의 예방 및 치료용 또는 기억력증진용 약제학적 조성물에 관한 것이다. [화학식 1]
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.
Abstract:
The present invention relates to a method for preparing 1-O-alkyl glycerol, and more specifically, to a method for efficiently preparing alkyl glycerol which is used as the intermediate of a reactant for pharmaceutical synthesis, polymer synthesis, and cosmetic and a biological active substance. The method for preparing 1-O-alkyl glycerol according to one embodiment of the present invention includes a step of hydrolyzing linear or branched (C12-C24) alkyl glycidyl ether using 1,4-dioxane as a solvent under the presence of an acid catalyst.
Abstract:
A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.
Abstract:
본 발명은 신규 6-알킬아미노-2-메틸-2'-( N- 메틸치환술폰아미도)메틸-2 H- 1-벤조피란 유도체와, 조합화학 합성기술 중 하나인 평형합성법을 이용하여 상기한 신규 화합물을 고효율로 합성하는 방법, 그리고 상기한 신규 화합물이 우수한 5-라이폭시게네이즈(5-LO) 저해효과를 나타내므로 관련 류코트리엔(LTA4, B4, C4, D4)의 활성으로 유발되는 염증질환, 류마티스성 관절염, 대장염(Colitis), 천식, 건선 등의 예방 및 치료제로 사용하는 용도에 관한 것이다. 조합화학 합성, 평형 합성, 5-라이폭시게네이즈, 항염증 질환 치료제, 약리학적 효능, 2'-술폰아미도메틸벤조피란, 유사약물 라이브러리
Abstract:
A novel 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative is provided to show excellent 5-lipoxygenase(5-LO) inhibition effect, thereby being used for preventing and treating inflammatory diseases induced by related leukotrien(LTA4, B4, C4, D4), rheumatoid arthritis, colitis, asthma, and psoriasis. The 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative is represented by the formula(1), where R^1 is C1-10 alkyl; phenyl; phenyl substituted by a substituent selected from the group consisting of C1-6 alkyl, C1-6 acyloxy, C1-10 alkoxyalkyl, and C1-10 dialkoxyalkyl; benzyl; benzyl substituted by a substituent selected from the group consisting of halogen, nitro, cyano, hydroxy, C1-6 alkyl and C1-6 alkoxy; phenethyl; pyridyl methyl; thiophene methyl; or thiophene methyl substituted by C1-6 alkyl, each R^2 and R^3 is independently H; or C1-6 alkyl, and R^4 is C1-10 alkyl; phenyl; phenyl substituted by a substituent selected from the group consisting of C1-6 alkyl and C1-6 alkoxy; or thiophene. The anti-inflammatory agent comprises the 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative represented by the formula(1).