신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1H-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물
    51.
    发明公开
    신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1H-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-(3,4-二甲氧基苯基) - 乙基] -1H-吡唑化合物,其制备方法和包含其的药物组合物

    公开(公告)号:KR1020080065722A

    公开(公告)日:2008-07-15

    申请号:KR1020070002715

    申请日:2007-01-10

    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 translation: 提供了一种新型化合物,以显示对PDE-4酶的优异活性和对其他PDE酶的高选择性,从而被用作炎症相关疾病,关节炎,特应性皮炎,白血病,各种癌症和退行性脑病的治疗剂 效果。 1-(1-(3,4-二烷氧基苯基) - 烷基] -1H-吡唑化合物由式(1)表示,通过式(2)表示的卤代苄基化合物与吡唑化合物 由公式(3)表示。 在式(1)中,每个R 1和R 2独立地为H,可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基,C 3-7环烷基,(C 3-7)环烷基(C 1-7) 烷基,芳基或杂芳基,芳(C 1-5)烷基或芳(C 1-5)烷氧基,或者R 1和R 2可以被C 1-3亚烷基相互连接; 每个R 3,R 4和R 5独立地为H,苯基,吡啶基,N-氧代吡啶基,直链或支链饱和和不饱和C 1-7烷基,C 3-7环烷基,(C 3-10)环烷基(C 1-7)烷基,卤素,氰基 ,硝基,氨基,单或二(C1-7)烷基氨基,单或二(C1-7)烷基氨基羰基,C3-7环烷基氨基,3至7元饱和或不饱和杂环,包括O,N或S,胍基 (C 1-7)烷基,羟基(C 1-7)烷基,羧基或(C 1-7)烷氧基羰基;(C 1-7)烷氧基, R6是直链或支链饱和和不饱和的C1-7烷基,C3-7环烷基,(C3-10)环烷基(C1-7)烷基,苯基,苯氧基,苄基,苄氧基,C1-7烷氧基或(C1-7) 烷氧基(C 1-7)烷基。 用于治疗或预防与气道炎症,关节炎,特应性皮炎,白血病,癌症或退行性脑疾病相关的疾病的药物组合物包括1- [1-(3,4-二烷氧基苯基) - 烷基] -1H-吡唑衍生物作为有效的 成分。

    퓨란-2-카복실산 유도체 및 그의 제조 방법
    52.
    发明公开
    퓨란-2-카복실산 유도체 및 그의 제조 방법 失效
    呋喃-2-羧酸衍生物及其制备方法

    公开(公告)号:KR1020080012621A

    公开(公告)日:2008-02-12

    申请号:KR1020060073717

    申请日:2006-08-04

    CPC classification number: C07D307/68

    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 translation: 提供呋喃-2-羧酸衍生物以抑制糖或脂质的形成,并通过活化AMPK(AMP(腺苷一磷酸)活化的蛋白激酶)促进糖的吸收,使得呋喃-2-羧酸衍生物可用于预防 和代谢综合症的治疗,包括糖尿病,肥胖症,高脂血症,高胆固醇血症,脂肪肝和脂肪性肝炎。 由式(1)表示的呋喃-2-羧酸衍生物,其中X是氢或卤素,n是1,2或3,m是0,1或2,R是氢或C 1-4烷基,是由 将式(2)表示的化合物与式(3)表示的化合物在有机溶剂中,在Y是三苯基溴化鏻盐,三苯基碘化鏻盐或苯并噻唑-2-磺酰基的碱存在下反应。 用于预防或治疗代谢综合征的组合物包括由式(1)表示的呋喃-2-羧酸衍生物。

    7-(3,4-디알콕시페닐)-피라졸로[1,5-a]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물
    53.
    发明授权
    7-(3,4-디알콕시페닐)-피라졸로[1,5-a]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물 失效
    7-(3,4-디알콕시페닐) - 피라졸로[1,5-α]피리미딘화합물을포함하는관절염,아토피피부염,백혈병을포함한암및알쯔하이머,우울증또는기억력감소등의뇌질환의치료및 예방을위약제제학적조성

    公开(公告)号:KR100753017B1

    公开(公告)日:2007-08-30

    申请号:KR1020060046860

    申请日:2006-05-25

    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 translation: 用于治疗或预防关节炎,特应性皮炎,肿瘤和退行性脑疾病,其包括7-(3,4-二烷氧基) - 吡唑并提供[1,5-a]嘧啶化合物抑制PDE-4的活性(phosphodiesterase-的药物组合物 4)并通过减少HARBS(高亲和力咯利普兰结合位点)亲和力来减少副作用,例如呕吐。 用于治疗或预防关节炎,特应性皮炎,肿瘤和退行性脑疾病的药物组合物包含7-(3,4-二烷氧基) - 吡唑并[1,5-a]嘧啶化合物由式(1)表示,其中R1和R2 (C 1 -C 7)烷基,含有卤素原子的直链或支链饱和或不饱和(C 1 -C 7)烷基,(C 3 -C 7)环烷基,含有3至7元杂环烷基的3元至7元杂环烷基 (C4-C10)环烷基(C1-C7)烷基,在杂环中含有氧,氮或硫的3元至7元杂环烷基(C1-C7)烷基,苯基 ,苄基或烯丙基; (C 1 -C 7)烷基,(C 1 -C 7)烷氧基,(C 1 -C 7)烷氧基(C 1 -C 7)烷基,(C 1 -C 7)烷氧基, (C 1 -C 7)烷基,羧酸,羧基(C 1 -C 7)烷基酯,羧基(C 1 -C 7)烷基酰胺,氨基或单或二(C 1 -C 7)烷基氨基羰基; (C 1 -C 7)烷基,(C 3 -C 7)环烷基,(C 1 -C 7)烷氧基,(C 1 -C 7)烷氧基(C 1 -C 7)烷基,羟基(C 1 -C 7)烷基, C1-C7)烷基酮,(C1-C10)烷基羧酸,羧基(C1-C10)烷基酯,羧基(C1-C10)烷基酰胺,氨基,单或二(C1-C7)烷基氨基,单或二(C1-C7 )烷基氨基羰基,(C3-C7)环烷基胺,吗啉,氧化吗啉,哌啶,哌嗪,哌嗪氧化物或芳基。

    베타아미노기를 갖는 고리화된 히드라자이드 유도체, 이의 약학적으로 허용 가능한 염 및 이의 제조 방법
    54.
    发明公开
    베타아미노기를 갖는 고리화된 히드라자이드 유도체, 이의 약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有β型-AMINO组的环状氢化衍生物及其药物可接受的盐及其制备方法

    公开(公告)号:KR1020070087953A

    公开(公告)日:2007-08-29

    申请号:KR1020060017372

    申请日:2006-02-22

    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 translation: 提供具有β-氨基的环状酰肼衍生物以抑制DPP-IV的活性,从而可用于治疗由DPP-IV介导的各种疾病。 具有β-氨基的环状酰肼衍生物由式(1)表示,其中R 1是由结构式(a)或(b)表示的基团,R 2是H,C 1-6烷基,C 3-6环烷基 或者由结构式(a),(b),(c),(d),(e),(f),(g)或(h) a独立地是H,C 1-6烷基,C 3-6环烷基,C 1-6烷氧基,OCH 2 O,OCF 3,苯氧基,卤素,CN,NO 2,CF 3,COOR b或NR b R c c(其中每个R b和 (a),(b),(i),(j),(k),(j),(k) 1)或(m)R e是C 1-6烷基,C 3-6环烷基或由结构式(a)或(b)表示的基团,R f是卤素,NR b, c,由结构式(n)或(o)表示的基团,-S-杂芳基,四氢异喹啉,噻唑烷,脯氨酸,哌啶-4-甲酸或四氢嘧啶(其中X为O或S)],n为 从1到3的整数。该方法包括以下步骤:(a)pe (2)表示的氨基酸与式(3)表示的环状肼的缩合反应,得到式(4)表示的化合物。 (b)使式(4)的化合物与氯乙酰氯反应,得到式(6)表示的化合物; (c)使式(6)化合物与R2取代的亲核化合物反应得到式(5)表示的化合物; 和(d)使式(5)的化合物脱保护。 在反应式(2)中,BOC为保护基,R1,R2和n各自与上述相同。

    염증억제 활성을 가지는6-알킬아미노-2-메틸-2'-(N-메틸치환술폰아미도)메틸-2H-1-벤조피란 유도체
    56.
    发明公开
    염증억제 활성을 가지는6-알킬아미노-2-메틸-2'-(N-메틸치환술폰아미도)메틸-2H-1-벤조피란 유도체 失效
    6-氨基亚氨基-2-甲基-2' - (N-甲基取代的磺酰胺)甲基-2H-1-苯并噻吩衍生物作为抗炎抑制剂

    公开(公告)号:KR1020070024838A

    公开(公告)日:2007-03-08

    申请号:KR1020050080383

    申请日:2005-08-30

    CPC classification number: C07D311/58 C07D405/12 C07D409/12 C07D409/14

    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 translation: 提供新的6-烷基氨基-2-甲基-2-(N-甲基取代亚磺酰氨基)甲基-2H-1-苯并吡喃衍生物,以显示出优异的5-脂氧合酶(5-LO)抑制作用,从而用于预防和治疗 由相关白细胞介素(LTA4,B4,C4,D4),类风湿关节炎,结肠炎,哮喘和牛皮癣引起的炎性疾病。 6-烷基氨基-2-甲基-2-(N-甲基取代亚磺酰氨基)甲基-2H-1-苯并吡喃衍生物由式(1)表示,其中R 1是C 1-10烷基; 苯基; 被选自C 1-6烷基,C 1-6酰氧基,C 1-10烷氧基烷基和C 1-10二烷氧基烷基的取代基取代的苯基; 苄基; 被选自卤素,硝基,氰基,羟基,C 1-6烷基和C 1-6烷氧基的取代基取代的苄基; 苯; 吡啶基甲基; 噻吩甲基; 或被C 1-6烷基取代的噻吩甲基,每个R 2和R 3独立地为H; 或C 1-6烷基,R 4是C 1-10烷基; 苯基; 被选自C 1-6烷基和C 1-6烷氧基的取代基取代的苯基; 或噻吩。 抗炎剂包含式(1)表示的6-烷基氨基-2-甲基-2-(N-甲基取代亚磺酰氨基)甲基-2H-1-苯并吡喃衍生物。

    나프틸옥시아세트산 유도체
    59.
    发明授权
    나프틸옥시아세트산 유도체 失效
    萘氧基乙酸衍生物

    公开(公告)号:KR100622667B1

    公开(公告)日:2006-09-19

    申请号:KR1020040069245

    申请日:2004-08-31

    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

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