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11.发明授权히스톤 디아세틸라제 저해활성을 갖는 알킬카바모일나프탈렌일옥시 옥테노일 하이드록시아마이드 유도체 및그의 제조방법 失效具有针对脱乙酰壳多糖的抑制活性的亚苄基氨基甲酰氧基酰胺衍生物及其制备方法
公开(公告)号：KR100696139B1
公开(公告)日：2007-03-20
申请号：KR1020050103693
申请日：2005-11-01
Applicant: 한국화학연구원 , 크리스탈지노믹스(주)
IPC: C07C237/32
CPC classification number: C07C259/06 , C07C2601/14 , C07C2601/16 , C07D207/12 , C07D207/14 , C07D211/58 , C07D213/75 , C07D233/54 , C07D233/61 , C07D295/185 , C07D307/66 , C07D333/20
Abstract: Provided are an alkylcarbamoyl naphthalenyloxyoctenoylhydroxyamide derivative which inhibits the enzymatic activity of histone diacetylase effectively, its preparation method, and an antitumor pharmaceutical composition containing the derivative. The alkylcarbamoyl naphthalenyloxyoctenoylhydroxyamide derivative is represented by the formula 1, wherein R1 is independently a C1-C2 alkyl group substituted or unsubstituted with at least one substituent selected from the group consisting of a C1-C3 alkyl group, a hydroxyalkyl group of C1-C2, a haloalkyl group of C1-C2, a piperidinyl group, a morpholinyl group, a cyanomethyl group, a piperazinyl group, a di(C1-C2)alkylamino(C1-C2)alkyl group, a piperidinyl(C1-C2)alkyl group, a morpholinyl(C1-C2)alkyl group, a piperazino(C1-C2)alkyl group, a pyrrolidinyl group and a (C1-C2)alkylpyrrolidinyl group; and R2 is H or a methyl group.
Abstract translation: 提供了有效抑制组蛋白二乙酰化酶的酶活性的烷基氨基甲酰基萘氧基辛酰基羟基酰胺衍生物，其制备方法和含有该衍生物的抗肿瘤药物组合物。 烷基氨基甲酰基萘氧基辛烯酰羟基酰胺衍生物由式1表示，其中R1独立地为被至少一个选自C1-C3烷基，C1-C2羟烷基，C1-C2烷基， C1-C2的卤代烷基，哌啶基，吗啉基，氰基甲基，哌嗪基，二（C1-C2）烷基氨基（C1-C2）烷基，哌啶基（C1-C2）烷基， 吗啉基（C1-C2）烷基，哌嗪基（C1-C2）烷基，吡咯烷基和（C1-C2）烷基吡咯烷基; R2为H或甲基。
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公开(公告)号：KR100441901B1
公开(公告)日：2004-07-27
申请号：KR1020010039222
申请日：2001-07-02
IPC: C07D501/57
Abstract: PURPOSE: Provided is an improved process for the preparation of cephalosporin derivatives from (cis)-3-acetoxypropen-cephalosporinic acid in higher yield. CONSTITUTION: The improved process for the preparation of cephalosporin derivative of the formula(1) comprises the steps of: radical reaction of a compound of the formula(5) with benzenthiol and azobisisobutyronitrile as a radical initiator in an organic solvent to convert it into a trans form; continuous reaction of the reaction product with a compound of the formula(10) to obtain a compound of the formula(3); and reaction of the compound of the formula(3) with an acylated compound of the formula(8) and a silylated compound of the formula(9).
Abstract translation: 目的：提供一种由（顺式）-3-乙酰氧基丙烯酸头孢菌素酸以较高产率制备头孢菌素衍生物的改进方法。 构成：制备式（1）头孢菌素衍生物的改进方法包括以下步骤：将式（5）化合物与苯硫醇和偶氮二异丁腈作为自由基引发剂在有机溶剂中进行自由基反应，将其转化为 转变; 使反应产物与式（10）化合物连续反应，得到式（3）化合物; 和式（3）化合物与式（8）酰化化合物和式（9）甲硅烷基化化合物的反应。
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公开(公告)号：KR1020030002925A
公开(公告)日：2003-01-09
申请号：KR1020010039222
申请日：2001-07-02
IPC: C07D501/57
Abstract: PURPOSE: Provided is an improved process for the preparation of cephalosporin derivatives from (cis)-3-acetoxypropen-cephalosporinic acid in higher yield. CONSTITUTION: The improved process for the preparation of cephalosporin derivative of the formula(1) comprises the steps of: radical reaction of a compound of the formula(5) with benzenthiol and azobisisobutyronitrile as a radical initiator in an organic solvent to convert it into a trans form; continuous reaction of the reaction product with a compound of the formula(10) to obtain a compound of the formula(3); and reaction of the compound of the formula(3) with an acylated compound of the formula(8) and a silylated compound of the formula(9).
Abstract translation: 目的：提供从（顺式）-3-乙酰氧基丙基 - 头孢菌酸制备头孢菌素衍生物的较高产率的改进方法。 构成：制备式（1）的头孢菌素衍生物的改进方法包括以下步骤：将式（5）化合物与苯并二酚和偶氮二异丁腈作为自由基引发剂在有机溶剂中进行自由基反应，将其转化为 转变; 反应产物与式（10）化合物的连续反应，得到式（3）化合物; 和式（3）的化合物与式（8）的酰化化合物和式（9）的甲硅烷基化合物的反应。
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公开(公告)号：KR1020020079654A
公开(公告)日：2002-10-19
申请号：KR1020020052421
申请日：2002-09-02
IPC: C07D265/22
Abstract: PURPOSE: Provided are azetidinone compound of the formula(I) as an intermediate useful for the manufacture of carbapenem antibiotics and a process for the preparation thereof. CONSTITUTION: The azetidine compound is represented by the formula(I). It is useful as an intermediate for the manufacture of beta-methylcarbapenem antibiotics and manufactured by reacting 4-acetoxy-azetidine compound of the formula(II) and alpha-halo propionic acid amide compound of the formula(III).
Abstract translation: 目的：提供式（I）的氮杂环丁酮化合物作为制备碳青霉烯类抗生素的中间体及其制备方法。 构成：氮杂环丁烷化合物由式（I）表示。 通过使式（II）的4-乙酰氧基 - 氮杂环丁烷化合物与式（III）的α-卤代丙酸酰胺化合物反应制备β-甲基碳青霉烯类抗生素的中间体是有用的。
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15.发明授权
公开(公告)号：KR101116754B1
公开(公告)日：2012-03-13
申请号：KR1020090105097
申请日：2009-11-02
Applicant: 한국화학연구원
IPC: C07C239/14 , C07C231/14 , A61K31/165 , A61P35/00
Abstract: 본 발명은 신규한 6-아미노-
N -하이드록시헥산아마이드 화합물 및 약학적으로 허용 가능한 이의 염, 이 화합물의 제조방법, 그리고 이 화합물을 유효성분으로 하는 약학조성물에 관한 것이다.
본 발명의 6-아미노-
N -하이드록시헥산아마이드 화합물 및 약학적으로 허용 가능한 이의 염은 히스톤 디아세틸라제의 효소활성을 저해하므로 종양세포의 증식 억제하는 약물로 유용하게 사용될 수 있다.
히스톤 디아세틸라제, 항암, 6-아미노-N-하이드록시헥산아마이드-
Patent Agency Ranking16.发明公开
公开(公告)号：KR1020110048336A
公开(公告)日：2011-05-11
申请号：KR1020090105096
申请日：2009-11-02
Applicant: 한국화학연구원
IPC: C07C239/14 , C07C231/14 , A61K31/165 , A61P35/00
Abstract: PURPOSE: A 6-amido-n-hydroxyhexanamide compound is provided to selectively induce the terminal differentiation of tumor cell by effectively inhibiting enzyme activity of histone deacetylase, and to inhibit the proliferation of tumor cell. CONSTITUTION: A compound is selected from a 6-amido-n-hydroxyhexanamide compound represented by chemical formula 1 and pharmaceutically acceptable salts thereof. In chemical formula 1, X is selected from a single bond or the group of C1-6 alkylenyl; R is amino, C1-6 alkylamino, di(C1-6 alkyl)amino, 5-9-membered aryl, 5-9-membered aryl C1-6 alkyl, 5-9-membered aryl C1-6 alkyloxy, 5-9-membered heteroaryl including 1-3 hetero atoms selected from N and O, and 5-7-membered heterocycloalkyl including 1-3 hetero atoms selected from N and O.
Abstract translation: 目的：提供6-氨基 - 正 - 羟基己酰胺化合物，通过有效抑制组蛋白脱乙酰酶的酶活性，抑制肿瘤细胞的增殖，选择性诱导肿瘤细胞的末端分化。 构成：化合物选自由化学式1表示的6-氨基 - 正 - 羟基己酰胺化合物及其药学上可接受的盐。 在化学式1中，X选自单键或C1-6亚烷基; R为氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基，5-9元芳基，5-9元芳基C 1-6烷基，5-9元芳基C 1-6烷氧基，5-9 包括1-3个选自N和O的杂原子的杂芳基和包含1-3个选自N和O的杂原子的5-7元杂环烷基。
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17.发明授权히스톤 디아세틸라제 저해활성을 갖는 알킬카바모일나프탈렌일옥시프로페닐 하이드록시벤즈아마이드 유도체,이의 제조방법 및 이를 유효성분으로 하는 항암제용 약학조성물 失效组蛋白脱乙酰酶抑制活性，二烷基氨基甲酰基具有萘基氧基丙烯基羟基 - 苯甲酰胺衍生物，其制备方法和药物组合物用于抗癌剂它们的方法，作为有效成分
公开(公告)号：KR100711944B1
公开(公告)日：2007-05-02
申请号：KR1020050103687
申请日：2005-11-01
Applicant: 한국화학연구원 , 크리스탈지노믹스(주)
IPC: C07C237/32
Abstract: 본 발명은 하기
화학식 1 의 알킬카바모일 나프탈렌일옥시프로페닐 하이드록시벤즈아마이드 유도체(alkylcarbamoyl naphthalenyloxyprophenyl hydroxybenzamide derivatives), 이의 제조방법 및 이를 유효성분으로 하는 항암제용 약학 조성물에 관한 것으로, 본 발명의 알킬카바모일 나프탈렌일옥시프로페닐 하이드록시벤즈아마이드 유도체는 히스톤 디아세틸라제(histone deacetylase)의 효소활성을 효과적으로 저해하며 종양세포의 증식을 억제하는데 유용하게 사용될 수 있다.
상기 식에서,
R
1 은 수소 또는 메틸이고;
R
2 는 각각 독립적으로 C
1-3 알킬, 하이드록시C
1-2 알킬, 할로C
1-2 알킬, 피페리디닐, 몰포리닐, 사이아노메틸, 피페라지닐, 다이C
1-2 알킬아미노C
1-2 알킬, 피페리디닐C
1-2 알킬, 몰포리노C
1-2 알킬 및 피페라지노C
1-2 알킬로 구성된 군으로부터 선택된 하나 이상의 치환체로 치환되거나 치환되지 않은 C
1
-
2 알킬이거나;
R
1 및 R
2 는 서로 연결되어 그들이 부착된 질소 원자와 함께 몰포리닐, 피페리디닐 또는 피페라지닐 고리를 형성한다.Abstract translation: 到本发明
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公开(公告)号：KR1020020013988A
公开(公告)日：2002-02-25
申请号：KR1020000046447
申请日：2000-08-10
IPC: C07D413/14
CPC classification number: C07D413/06 , C07D205/08 , C07D265/06 , C07D265/14 , C07D487/04 , C07F9/65611 , Y02P20/55
Abstract: PURPOSE: Provided is an intermediate, azetidinone compound which is useful in manufacturing beta-methylcarbapenem antibiotics. And its manufacturing method is provided. CONSTITUTION: The intermediate of carbapenem, azetidinone compound, is represented by the formula(1), wherein R is hydrogen or hydroxy protective group, R1 and R2 are individually C1-C15 alkyl, benzyl, represent 5-6 membered cyclic compound to which R1 and R2 are linked, or hetero cyclic group including at least one oxygen or sulfur atom; R3 is lower alkyl group or lower alkylester group; and R4 is benzene, halogen, lower alkyloxy group, or nitro group substituted benzene ring.
Abstract translation: 目的：提供可用于制备β-甲基碳青霉烯类抗生素的中间体氮杂环丁酮化合物。 并提供其制造方法。 构成：碳青霉烯类氮杂环丁酮化合物的中间体由式（1）表示，其中R是氢或羟基保护基，R1和R2分别是C1-C15烷基，苄基，代表5-6元环状化合物，其中R1 或R 2连接，或包含至少一个氧原子或硫原子的杂环基; R3是低级烷基或低级烷基酯基; R4为苯，卤素，低级烷氧基或硝基取代苯环。
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19.发明公开히스톤 디아세틸라제 저해활성을 갖는 알킬아미노나프탈렌일옥시메틸 프로페닐 하이드록시벤즈아마이드유도체, 이의 제조방법 및 이를 유효성분으로 하는항암제용 약학 조성물 失效组蛋白乙酰基 - 二 - 烷基氨基 - 萘基氧基甲基丙烯基羟基 - 苯甲酰胺衍生物，具有环化酶抑制活性，并且对于抗癌剂，用于活性成分此药物组合物，它们的制备方法
公开(公告)号：KR1020070047024A
公开(公告)日：2007-05-04
申请号：KR1020050103689
申请日：2005-11-01
Applicant: 한국화학연구원 , 크리스탈지노믹스(주)
IPC: C07D295/155 , C07D295/112 , A61P35/00
Abstract: 본 발명은 하기
화학식 1 의 알킬아미노 나프탈렌일옥시메틸 프로페닐 하이드록시벤즈아마이드 유도체(alkylamino naphthalenyloxymethyl propenyl hydroxybenzamide derivatives), 이의 제조방법 및 이를 유효성분으로 하는 항암제용 약학 조성물에 관한 것으로, 본 발명의 알킬아미노 나프탈렌일옥시메틸 프로페닐 하이드록시벤즈아마이드 유도체는 히스톤 디아세틸라제(histone deacetylase)의 효소활성을 효과적으로 저해하여 종양세포의 증식을 억제하는데 유용하게 사용될 수 있다.
상기 식에서,
R
1 은 수소 또는 메틸이고;
R
2 는 각각 독립적으로 C
1-2 알킬, 하이드록시C
1-2 알킬, 할로C
1-2 알킬, 피페리디닐, 몰포리닐, 사이아노메틸, 피페라지닐, 다이C
1-2 알킬아미노C
1-3 알킬, 피페리디닐C
1-2 알킬, 몰포리노C
1-2 알킬 및 피페라지노C
1-2 알킬로 구성된 군으로부터 선택된 하나 이상의 치환체로 치환되거나 치환되지 않은 C
1
-
2 알킬이거나;
R
1 및 R
2 는 서로 연결되어 그들이 부착된 질소 원자와 함께 몰포리닐, 피페리디닐 또는 피페라지닐 고리를 형성한다.Abstract translation: 到本发明
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公开(公告)号：KR100377448B1
公开(公告)日：2003-03-26
申请号：KR1020000046447
申请日：2000-08-10
IPC: C07D413/14
CPC classification number: C07D413/06 , C07D205/08 , C07D265/06 , C07D265/14 , C07D487/04 , C07F9/65611 , Y02P20/55
Abstract: There is disclosed an azetidinone compound of the formula (I):wherein R is hydrogen, or a hydroxy protecting group, R1 and R2 are each independently alkyl of 1-15 carbon atoms, benzyl or cyclized together with the carbon atom to which they are attached to form a 5 or 6-membered cyclic hydrocarbon or a heterocyclic radical having one or two hetero ring atoms, said hetero ring atoms being selected from the group consisting of O and S; R3 is lower alkyl or -COO(lower alkyl) R4 is phenyl, or phenyl substituted with halogen, lower alkoxy or nitro which is useful as a synthetic intermediate to the 1'beta-methylcarbapenem-type antibacterial agent.
Abstract translation: 公开了式（I）的氮杂环丁酮化合物：其中R是氢或羟基保护基，R 1和R 2各自独立地是1-15个碳原子的烷基，苄基或与它们所连接的碳原子一起环化 连接形成5或6元环烃或具有一个或两个杂环原子的杂环基，所述杂环原子选自O和S; R3是低级烷基或-COO（低级烷基），R4是苯基或被卤素，低级烷氧基或硝基取代的苯基，它可用作1'β-甲基碳代青霉烯类抗菌剂的合成中间体。
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