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41.发明公开
公开(公告)号：KR1020070087953A
公开(公告)日：2007-08-29
申请号：KR1020060017372
申请日：2006-02-22
IPC: C07D231/04 , C07D237/04
CPC classification number: Y02P20/55 , C07D231/04 , C07D237/04 , C07D243/02 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D417/12
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。
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公开(公告)号：KR1020070074250A
公开(公告)日：2007-07-12
申请号：KR1020060002175
申请日：2006-01-09
IPC: C07D277/06 , C07D417/12 , A61P3/04 , A61P35/00
CPC classification number: C07D277/20 , C07D417/12
Abstract: A rhodanine derivative or a pharmaceutically acceptable salt is provided to inhibit the activity of phosphatase, thereby being usefully used for treating diseases such as autoimmune diseases, diabetes, damaged glucose resistance, insulin resistance, obesity, cancer, and malignant diseases. The rhodanine derivative is represented by the formula(1), wherein R1 is alkoxy, arylalkoxy, substituted arylalkoxy, heteroaryl alkoxy, substituted heteroaryl alkoxy, heteroaryl alkyl alkoxy, aryl oxy alkoxy, substituted aryl oxy alkoxy, heteroaryl oxy alkoxy, substituted heteroaryl oxy alkoxy, heterocyclic alkoxy, amino alkoxy, substituted amino alkoxy, heterocyclic oxy alkoxy, cyclic amino alkoxy, heterocyclic amino alkoxy, alkenyl alkoxy, cyclic amino, heterocyclic amino, substituted heterocyclic amino, nitro, sulfonyl, benzene sulfonyl, or substituted benzenesulfonyl; R2 is H or Br; R3 is H, halo, hydroxy, alkoxyl, substituted alkoxy, substituted aryl oxy, alkyl amino alkoxy, cyclic amino alkoxy, heterocyclic amino alkoxy, substituted heterocyclic amino alkoxy, alkyl amino aryl, alkyl amido alkoxy, aryl amido alkoxy, sulfonyl amino alkoxy, or substituted aryl oxy amido alkoxy; R4 is H, halo, nitro, heterocyclo, alkoxy, aryl alkoxy, or substituted aryl alkoxy; and R5 is H or a group represented by the structural formula(a). The method comprises the steps of: (a) preparing an intermediate represented by the formula(3) from a compound represented by the formula(2) as a starting material; and (b) reacting the intermediate of the formula(3) with rhodanine of the formula(4) in the presence of sodium acetate and acetic acid to prepare the rhodanine derivative of the formula(1).
Abstract translation: 提供绕丹宁衍生物或药学上可接受的盐以抑制磷酸酶的活性，从而有效地用于治疗诸如自身免疫性疾病，糖尿病，葡萄糖耐药性，胰岛素抵抗，肥胖，癌症和恶性疾病等疾病。 所述绕丹宁衍生物由式（1）表示，其中R 1是烷氧基，芳基烷氧基，取代的芳基烷氧基，杂芳基烷氧基，取代的杂芳基烷氧基，杂芳基烷基烷氧基，芳氧基烷氧基，取代的芳氧基烷氧基，杂芳氧基烷氧基，取代的杂芳基氧基烷氧基 杂环烷氧基，氨基烷氧基，取代氨基烷氧基，杂环氧基烷氧基，环状氨基烷氧基，杂环氨基烷氧基，烯基烷氧基，环状氨基，杂环氨基，取代的杂环氨基，硝基，磺酰基，苯磺酰基或取代的苯磺酰基。 R2是H或Br; R 3是H，卤素，羟基，烷氧基，取代的烷氧基，取代的芳基氧基，烷基氨基烷氧基，环氨基烷氧基，杂环氨基烷氧基，取代的杂环氨基烷氧基，烷基氨基芳基，烷基氨基烷氧基，芳基氨基烷氧基，磺酰氨基烷氧基， 或取代的芳基氧基酰胺基烷氧基; R4是H，卤素，硝基，杂环基，烷氧基，芳基烷氧基或取代的芳基烷氧基; R5为H或结构式（a）所示的基团。 该方法包括以下步骤：（a）由式（2）表示的化合物作为原料制备由式（3）表示的中间体; 和（b）在乙酸钠和乙酸的存在下，使式（3）的中间体与式（4）的绕丹宁反应以制备式（1）的绕丹宁衍生物。
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公开(公告)号：KR1020070027939A
公开(公告)日：2007-03-12
申请号：KR1020050079915
申请日：2005-08-30
IPC: C07C245/10
Abstract: Provided are pentacene precursors, which are synthesized by a Diels-Alder reaction, have high solubility in organic solvent, and produce pentacene via a retro Diels-Alder reaction by pyrolysis without using vacuum devices. The pentacene precursor is a Diels-Alder reaction product of an aromatic azine compound and a benzyne equivalent and comprises at least one -N=N- bridge on a 2 to 4-positioned benzene ring of the following formula(I). The aromatic azine compound is selected from phthalazine, pyridazine, or tetrazine. The benzyne equivalent is selected from tetrabromobenzene, 2,3-dibromonaphthalene, or phthalic anhydride.
Abstract translation: 通过Diels-Alder反应合成的并五苯前体在有机溶剂中具有很高的溶解度，并且通过热解而不使用真空装置通过复古Diels-Alder反应产生并五苯。 并五苯前体是芳族吖嗪化合物和苯并对等物的Diels-Alder反应产物，并且在下述式（I）的2至4位苯环上包含至少一个-N = N-桥。 芳族吖嗪化合物选自酞嗪，哒嗪或四嗪。 苯并对当量选自四溴苯，2,3-二溴萘或邻苯二甲酸酐。
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公开(公告)号：KR100622667B1
公开(公告)日：2006-09-19
申请号：KR1020040069245
申请日：2004-08-31
Applicant: 한국화학연구원
IPC: C07C63/337
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-
公开(公告)号：KR100547193B1
公开(公告)日：2006-01-31
申请号：KR1020030035444
申请日：2003-06-02
Applicant: 한국화학연구원 , 씨제이 주식회사 , 제일파마홀딩스 주식회사
IPC: C07D403/06
Abstract: 본 발명은 하기 화학식 1의 신규한 시아노-피라졸린 유도체와 이의 약학적으로 허용가능한 염 및 이의 제조 방법에 관한 것이다. 본 발명의 시아노-피라졸린 유도체는 디펩티딜 펩티다제-IV(DPP-IV)의 활성을 억제하므로 이를 포함하는 약학 조성물은 DPP-IV에 의해서 매개되는 인슐린 의존성, 비인슐린 의존성 당뇨병, 관절염, 비만, 골다공증 및 손상된 글루코스 내성과 같은 질환의 치료제로서 매우 유용하다:
상기 식에서, A는 또는 이고,
상기 식에서, R
1 은 서로 같거나 다른 하나 또는 두 개의 C
1 -C
4 알킬, C
1 -C
4 알콕시, 할로겐, 트리플루오르메틸, 시아노 또는 니트로로 치환된 피리디닐, 피리미디닐 또는 페닐 잔기이고;
R
2 는 서로 같거나 다른 하나 또는 두 개의 C
1 -C
4 알킬, C
1 -C
4 알콕시, 할로겐, 트리플 루오르메틸, 시아노 또는 니트로로 치환된 피리디닐, 피리미디닐, 페닐 또는 치환되지 않거나 서로 같거나 다른 하나 또는 두 개의 할로겐, 트리플루오르메틸, 시아노 또는 니트로로 치환된 벤조일 잔기이고;
R
3 은 치환된 아다만틸이고;
R
4 는 서로 같거나 다른 하나 또는 두 개의 수소, 하이드록시, C
1 -C
4 알킬, C
1 -C
4 알콕시, 또는 할로겐이다.Abstract translation: 本发明涉及式（I）的新型氰基 - 吡唑啉衍生物，其药学上可接受的盐及其制备。 本发明吡唑啉衍生物的氰基的二肽基肽-IV包括相同的，所以抑制（DPP-IV）的活性的药物组合物是胰岛素依赖由DPP-IV介导的，非胰岛素依赖型糖尿病，关节炎， 肥胖，骨质疏松和葡萄糖耐量降低。
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Patent Agency Ranking
公开(公告)号：KR100524699B1
公开(公告)日：2005-11-01
申请号：KR1020030024557
申请日：2003-04-18
Applicant: 한국화학연구원
IPC: C07D265/02
Abstract: 본 발명은 사이클로펜타[
d ][1,2]-옥사진 유도체에 관한 것으로서, 더욱 상세하게는 신규 구조를 가지는 사이클로펜타[
d ][1,2]-옥사진 유도체와, 상기한 신규 화합물이 PTP1B(protein tyrosine phosphatase 1B), Prl-3, CD45, LAR(Leukocyte Antigen-Related), Cdc25A, Cdc25B, Cdc25C, Yop, PP1, VHR(vaccina human-related)과 같은 단백질 포스파타제(protein phosphatase, PPase)에 대한 약리학적 억제활성이 우수하므로 신규 화합물 또는 이들의 약제학적으로 허용 가능한 염을 자가면역 질병, 급성 및 만성 염증, 제1형 및 제2형 당뇨병, 손상된 글루코스 내성, 인슐린 저항성, 비만, 암 및 악성질병 등과 관련된 질병의 치료 및 예방제로 사용하는 용도에 관한 것이다.-
公开(公告)号：KR1020040104054A
公开(公告)日：2004-12-10
申请号：KR1020030035443
申请日：2003-06-02
Applicant: 한국화학연구원 , 씨제이 주식회사 , 제일파마홀딩스 주식회사
IPC: C07D231/04 , A61P3/10 , C07D213/81 , C07D213/83
Abstract: PURPOSE: Pyrazolidine derivatives comprising acyl group and pharmaceutical acceptable salts thereof, and a method for the preparation thereof are provided, which derivatives have improved DPP-IV(dipeptidyl peptidase-IV) inhibiting activity, so that they are useful for treatment of disease associated with DPP-IV, such as insulin or non-insulin dependent diabetes, arthritis, obeseness, osteoporosis and damaged glucose resistance. CONSTITUTION: The pyrazolidine derivatives comprising acyl group represented by formula (1) or pharmaceutical acceptable salts thereof are provided, wherein R1 is the same or different, and hydrogen, halogen, cyano, nitro, hydroxy, amino, CO2H, CONH2, CSNH2, amidine, C1-C4 alkyl, C1-C4 haloalkyl, C1-C7 alkoxy, C1-C4 alkylamino, C1-C4 alkylthio, C1-C4 alkylamide, C1-C4 acylamide, C1-C4 acyloxy, C1-C4 alkylsulfoneamide, C1-C4 alkylsulfonate, imidic acid C1-C4 alkylester, thioimidic acid C1-C4 alkylester, methyl substituted with hydroxy, amino, cyano, morpholine, acetate, acetamide or methanesulfonamide, phenyl substituted with C1-C4 haloalkyl, C1-C4 alkoxy or halogen, or benzyloxy substituted with C1-C4 haloalkyl, C1-C4 alkoxy or halogen; m is 1 or 2; n is 0 or 1; X is O, S or N-CN; ACO is a group of formula (2) or formula (3); R2 is a substituent present in alanine, arginine, aspartic acid, cysteine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, hydroxyproline, serine, threonine, tryptophane, tyrosine, valine, cyclohexylglycine, threonine, isoleucine-isoleucine, isoleucine-valine, valine-isoleucine, proline-isoleucine or isoleucine-proline; and R3 is C1-C6 alkyl, hydrogen or benzoylamide substituted C5-C8 cycloalkyl, hydrogen or hydroxy substituted adamantyl, morpholine or C1-C4 alkyl substituted piperazine, hydroxy or C1-C4 alkyl substituted piperazine, or ethylamino pyridine substituted with cyano, halogen, nitro or C1-C4 haloalkyl.
Abstract translation: 目的：提供包含酰基的吡唑烷衍生物及其药学上可接受的盐及其制备方法，该衍生物具有改善的DPP-IV（二肽基肽酶-IV）抑制活性，因此它们可用于治疗与 DPP-IV，例如胰岛素或非胰岛素依赖性糖尿病，关节炎，肥胖，骨质疏松症和损伤的葡萄糖耐药性。 提供了包含式（1）表示的酰基的吡唑烷衍生物或其药学上可接受的盐，其中R 1相同或不同，氢，卤素，氰基，硝基，羟基，氨基，CO 2 H，CONH 2，CSNH 2，脒 ，C1-C4烷基，C1-C4卤代烷基，C1-C7烷氧基，C1-C4烷基氨基，C1-C4烷硫基，C1-C4烷基酰胺，C1-C4酰基酰胺，C1-C4酰氧基，C1-C4烷基磺酰胺，C1-C4烷基磺酸酯 ，亚氨酸C 1 -C 4烷基酯，硫代亚氨酸C 1 -C 4烷基酯，被羟基，氨基，氰基，吗啉，乙酸酯，乙酰胺或甲磺酰胺取代的甲基，被C 1 -C 4卤代烷基，C 1 -C 4烷氧基或卤素取代的苯基或苄氧基取代 与C 1 -C 4卤代烷基，C 1 -C 4烷氧基或卤素; m为1或2; n为0或1; X是O，S或N-CN; ACO是式（2）或式（3）的一组; R2是存在于丙氨酸，精氨酸，天冬氨酸，半胱氨酸，谷氨酸，甘氨酸，组氨酸，异亮氨酸，亮氨酸，赖氨酸，甲硫氨酸，苯丙氨酸，脯氨酸，羟脯氨酸，丝氨酸，苏氨酸，色氨酸，酪氨酸，缬氨酸，环己基甘氨酸，苏氨酸， 异亮氨酸 - 异亮氨酸，异亮氨酸 - 缬氨酸，缬氨酸 - 异亮氨酸，脯氨酸 - 异亮氨酸或异亮氨酸 - 脯氨酸; 氢或羟基取代的金刚烷基，吗啉或C 1 -C 4烷基取代的哌嗪，羟基或C 1 -C 4烷基取代的哌嗪或被氰基，卤素取代的乙基氨基吡啶， 硝基或C 1 -C 4卤代烷基。
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公开(公告)号：KR1020040090614A
公开(公告)日：2004-10-26
申请号：KR1020030024557
申请日：2003-04-18
Applicant: 한국화학연구원
IPC: C07D265/02
Abstract: PURPOSE: Cyclopenta(d)(1,2)-oxazine derivatives are provided. The compounds have improved inhibiting activity on protein phosphatase(PPase) such as PTP-1B(protein tyrosine phosphatase 1B), CD45, LAR(leukocyte antigen-related), Cdc25B, VHR(vaccina human-related), Cdc25A, Cdc25C, Yop and PP1, so that they are useful for prevention and treatment of autoimmune disease, acute and chronic inflammation, diabetes, damaged glucose resistance, obesity, cancer, malignant disease, etc. CONSTITUTION: The cyclopenta(d)(1,2)-oxazine derivatives represented by formula (1), or pharmaceutically acceptable salts or optical isomers thereof are provided, wherein A is hydrogen, hydroxy, C1-C15 alkoxy, acetoxy, alkylcarbomethoxy, hydroxyacetamide or 3-oxydihydro-furan-2-one; B is hydrogen, chlorine or bromine containing halogen, hydroxy, carboxy or C1-C5 alkoxycarbonyl; D is hydrogen, or R1-(CO); E is optionally substituted aryl, optionally substituted C1-C15 alkyl, or optionally substituted C1-C15 alkyl or optionally substituted C7 to C20 arylalkyl; R2 is hydrogen, benzyl, hydroxyethyl, or CO2R3; R3 is hydrogen or C1-C5 alkyl; and R4 and R5 are independently hydrogen, optionally substituted C1-C15 alkyl, optionally substituted C7-C20 arylalkyl or nitrogen or oxygen containing ring-linked heteroalkyl.
Abstract translation: 目的：提供环戊二烯（d）（1,2） - 恶嗪衍生物。 该化合物对蛋白磷酸酶（PPase）如PTP-1B（蛋白酪氨酸磷酸酶1B），CD45，LAR（白细胞抗原相关），Cdc25B，VHR（人类相关抗原），Cdc25A，Cdc25C，Yop和 PP1，因此它们可用于预防和治疗自身免疫性疾病，急性和慢性炎症，糖尿病，葡萄糖耐量降低，肥胖，癌症，恶性疾病等。构成：环戊二烯（d）（1,2） - 恶嗪衍生物 其中A为氢，羟基，C 1 -C 15烷氧基，乙酰氧基，烷基甲氧基，羟基乙酰胺或3-氧代二氢 - 呋喃-2-酮;或其药学上可接受的盐或旋光异构体。 B是氢，含氯或溴的卤素，羟基，羧基或C 1 -C 5烷氧基羰基; D是氢或R1-（CO）; E是任选取代的芳基，任选取代的C 1 -C 15烷基或任选取代的C 1 -C 15烷基或任选取代的C 7至C 20芳烷基; R2是氢，苄基，羟乙基或CO 2 R 3; R3是氢或C1-C5烷基; 并且R 4和R 5独立地为氢，任选取代的C 1 -C 15烷基，任选取代的C 7 -C 20芳烷基或含氮或含氧环的杂烷基。
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49.发明授权
公开(公告)号：KR101533376B1
公开(公告)日：2015-07-02
申请号：KR1020140023133
申请日：2014-02-27
Applicant: 한국화학연구원
IPC: A61K31/343 , A61K31/10 , A61P3/10 , A61P3/00
Abstract: 본발명은 GLP-1 수용체의활성을증가시키는효과가우수한상기화학식 I로표시되는새로운비펩티드성작용제화합물 ID: 170026 화합물을유효성분으로포함하는제2형당뇨병치료용약학조성물을제공하며, 상기조성물은제2형당뇨병을치료하는데유용하게사용될수 있다.
Abstract translation: 本发明提供了一种用于治疗2型糖尿病的药物组合物，其包含以化学式1表示的新的非肽激动剂化合物（化合物ID：170026）作为活性成分，其能够显着增加胰高血糖素样肽的活性 -1（GLP-1）受体。 该组合物可用于治疗2型糖尿病。
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公开(公告)号：KR101524208B1
公开(公告)日：2015-05-29
申请号：KR1020130046522
申请日：2013-04-26
Applicant: 한국화학연구원
IPC: C07D413/12 , C07D413/14 , A61K31/423 , A61P3/00
Abstract: 본발명은신규한벤조옥사졸유도체, 이의제조방법및 이를유효성분으로포함하는비만및 비만관련대사질환특히, 당뇨병및 다양한당뇨관련질환의예방또는치료용의약학적조성물에관한것이다. 본발명의신규한벤조옥사졸유도체는당-의존적인슐린분비를증가시키고섭식과체중증가의억제효과가있는 GPR119(G protein-coupled receptor 119)의활성을효율적으로항진시킴으로써당 및지질대사를개선시켜, 당뇨뿐 아니라, 비만, 고지혈증, 당뇨병성혈관질환등 다양한당뇨병성합병증에대한효율적인예방및 치료용조성물로유용하게이용될수 있다
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