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:
Furan-2-carboxylic acid derivatives are provided to inhibit formation of sugars or lipids and promote absorption of sugars by activating AMPK(AMP(adenosine monophosphate)-activated protein kinase), so that the furan-2-carboxylic acid derivatives are useful for prevention and treatment of metabolic syndrome including diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver and steatohepatitis. Furan-2-carboxylic acid derivatives represented by the formula(1), wherein X is hydrogen or halogen, n is 1, 2 or 3, m is 0, 1 or 2 and R is hydrogen or C1-4 alkyl, are prepared by reacting compounds represented by the formula(2) with compounds represented by the formula(3) in organic solvent in the presence of base in which Y is triphenylphosphonium bromide salt, triphenylphosphonium iodide salt or benzothiazol-2-sulfonyl. A composition for prevention or treating metabolic syndrome comprises the furan-2-carboxylic acid derivatives represented by the formula(1).
Abstract:
A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.
Abstract:
A cyclic hydrazide derivative having a beta-amino group is provided to inhibit the activity of DPP-IV, thereby being useful for treating various diseases mediated by the DPP-IV. The cyclic hydrazide derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(a) or (b), R2 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, or a group represented by the structural formula(a), (b), (c), (d), (e), (f), (g), or (h)[wherein R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCH2O, OCF3, phenoxy, halogen, CN, NO2, CF3, COOR^b or NR^bR^c(wherein each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl), R^d is a group represented by the structural formula(a), (b), (i), (j), (k), (l), or (m), R^e is C1-6 alkyl, C3-6 cycloalkyl, or a group represented by the structural formula(a) or (b), R^f is halogen, NR^b, R^c, a group represented by the structural formula(n) or (o), -S-heteroayl, tetrahydroisoquinoline, thiazolidine, proline, piperidine-4-carboxylic acid or tetrahydropyrimidine(where X is O or S)], and n is an integer from 1 to 3. The method comprises the steps of: (a) performing a condensation reaction of an amino acid represented by the formula(2) and a cyclic hydrazine represented by the formula(3) to obtain a compound represented by the formula(4); (b) reacting the compound of the formula(4) with chloroacetyl chloride to obtain a compound represented by the formula(6); (c) reacting the compound of the formula(6) with an R2 substituted nucleophilic compound to obtain a compound represented by the formula(5); and (d) deprotecting the compound of the formula(5). In the reaction formula(2), BOC is a protecting group, and each R1, R2, and n is the same as defined above.
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).
Abstract:
본 발명은 하기의 화학식 1로 표시되는 신규한 4-(3,4-디알콕시페닐)-2-아미노티아졸 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 알쯔하이머를 포함한 중추신경계통 질환의 치료, 예방을 위한 약제학적 조성물에 관한 것이다. [화학식 1]
Abstract:
본 발명은 5-(1,3-디아릴-1H-피라졸-4-일메틸렌)-티아졸리딘-2,4-디온 유도체 또는 이의 약제학적으로 허용가능한 염과 이의 제조방법 및 이를 유효활성 성분으로 함유하는 항암제 조성물에 관한 것이다. 5-(1,3-디아릴-1H-피라졸-4-일메틸렌)-티아졸리딘-2,4-디온, 세포분열저해제, CDC25B, 탈인산화효소, 항암제
Abstract:
본 발명은 PTP1B(protein tyrosine phosphatase 1B), CD45, LAR(Leukocyte Antigen-Related), Cdc25A, Cdc25B, Cdc25C, Yop, PP1, VHR(vaccina human-related), Prl-3과 같은 단백질 포스파타제(protein phosphatase, PPase)에 대하여 우수한 약리학적 억제활성을 가지고 있어 자가면역 질병, 급성 및 만성 염증, 제1형 및 제2형 당뇨병, 손상된 글루코스 내성, 인슐린 저항성, 비만, 암 등 악성질병과 관련된 질병의 치료 및 예방에 유효한 다음 화학식 1로 표시되는 신규 나프틸옥시아세트산 유도체와 이의 약제학적으로 허용 가능한 염과, 이 화합물의 제조방법, 그리고 이 화합물을 유효성분으로 함유하는 약제조성물에 관한 것이다.
상기 화학식 1에서, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 및 R 8 은 각각 발명의 상세한 설명에서 정의한 바와 같다. 나프틸옥시아세트산, 단백질 포스파타제, 당뇨병
Abstract:
본 발명은 신규 2,2'-이중치환-3,4-디하이드로-7,8-이중치환-6-알킬아미노 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, 벤조피란, 유사약물 라이브러리