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    신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법
    4.
    发明公开
    신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법 有权
    新型抗坏血酸酶抑制剂化合物及其制备方法

    公开(公告)号：KR1020110023190A

    公开(公告)日：2011-03-08

    申请号：KR1020090080865

    申请日：2009-08-31

    Applicant: 일동홀딩스(주)

    Inventor： 강재훈 ,  이홍섭 ,  이희열 ,  안경미 ,  정주영

    IPC: C07D487/12 ,  C07D487/14 ,  C07D233/70

    Abstract: PURPOSE: A novel peptide deformylase inhibitor compound is provided to be used as a therapeutic agent for respiratory diseases and a therapeutic agent for respiratory diseases. CONSTITUTION: A novel peptide deformylase inhibitor compound is denoted by chemical formula I. The compound of chemical formula I and pharmaceutically acceptable salt thereof are prepared by reacting a compound of chemical formula III with a compound of chemical formula IVa or IVb or salt thereof. The reaction is performed under the presence of tetrahydrofuran, dichloromethane, N,N-dimethyl formaldehyde. An antibacterial composition contains therapeutically effective amount of novel peptide deformylase inhibitor compound or salt thereof and pharmaceutically acceptable carrier.

    Abstract translation: 目的：提供一种新的肽去甲酰化酶抑制剂化合物，用作呼吸系统疾病的治疗剂和呼吸系统疾病的治疗剂。 构成：化学式I表示新的肽失活酶抑制剂化合物。化学式I化合物及其药学上可接受的盐通过化学式III化合物与化学式IVa或IVb化合物或其盐反应制备。 反应在四氢呋喃，二氯甲烷，N，N-二甲基甲醛存在下进行。 抗菌组合物含有治疗有效量的新型肽失活酶抑制剂化合物或其盐和药学上可接受的载体。

    펩티드 데포르밀라제 저해제로서 신규의 히드록사믹 산유도체 및 그 제조방법
    5.
    发明公开
    펩티드 데포르밀라제 저해제로서 신규의 히드록사믹 산유도체 및 그 제조방법 失效
    一种新型羟基酸衍生物作为肽类抗坏血酸酶抑制剂及其制备方法

    公开(公告)号：KR1020060111744A

    公开(公告)日：2006-10-30

    申请号：KR1020050034057

    申请日：2005-04-25

    Applicant: 일동홀딩스(주)

    Inventor： 강재훈 ,  유승우 ,  이희열 ,  조봉환 ,  안경미

    IPC: C07D211/58

    CPC classification number: C07D211/58 ,  Y02P20/55

    Abstract: A novel hydroxamic acid derivative as a peptide deformylase inhibitor and a manufacturing method thereof are provided to inhibit proliferation of pathogenic bacteria by inhibiting their protein biosynthesis and polypeptide maturation catalyzed by the peptide deformylase. The hydroxamic acid derivative represented by the formula(I) or its pharmaceutically acceptable salt is provided, wherein A is -C(=O)NHOH or -N(CHO)OH; R1 is hydrogen, C1-3 alkyl, C4-6 cycloalkyl, halogen or hydroxy; R2 is hydrogen, linear or branched C1-6 alkyl, linear or branched C1-6 alkene, C4-6 cycloalkyl, C4-6 heterocycle containing N or O, or benzyl; R3 is hydrogen, methyl, linear or branched C1-6 alkyl, linear or branched C1-6 alkene, C4-6 cycloalkyl, phenyl or benzyl; R4 is hydrogen, linear or branched C1-4 alkyl, C1-4 alkene, or hydroxy substituted C1-4 alkyl; Y is represented by the formula(IIa), formula(IIb) or formula(IIc); n is 0 or 1; and R5, R6, R7, R8 and R9 are each independently hydrogen, linear or branched C1-3 alkyl, hydroxy, alkoxy, acyl, acyloxy, halogen, cyano, nitro, amino, N,N-dimethylamino, phenyl, morpholine or formyl. The hydroxamic acid derivative represented by the formula(I) or its pharmaceutically acceptable salt is prepared by reacting compounds of the formula(III) with hydroxylamine or N- or O-protected hydroxylamine, and removing the protecting group.

    Abstract translation: 提供了一种新颖的异羟肟酸衍生物作为肽变性酶抑制剂及其制备方法，通过抑制其由肽变性酶催化的蛋白质生物合成和多肽成熟来抑制致病菌的增殖。 提供由式（I）表示的异羟肟酸衍生物或其药学上可接受的盐，其中A是-C（= O）NHOH或-N（CHO）OH; R1是氢，C1-3烷基，C4-6环烷基，卤素或羟基; R2是氢，直链或支链C1-6烷基，直链或支链C1-6烯烃，C4-6环烷基，含有N或O的C4-6杂环或苄基; R 3是氢，甲基，直链或支链C 1-6烷基，直链或支链C 1-6烯烃，C 4-6环烷基，苯基或苄基; R4是氢，直链或支链C 1-4烷基，C 1-4烯烃或羟基取代的C 1-4烷基; Y由式（IIa），式（IIb）或式（IIc）表示; n为0或1; R 5，R 6，R 7，R 8和R 9各自独立地为氢，直链或支链C 1-3烷基，羟基，烷氧基，酰基，酰氧基，卤素，氰基，硝基，氨基，N，N-二甲基氨基，苯基，吗啉或甲酰基 。 由式（I）表示的异羟肟酸衍生物或其药学上可接受的盐通过使式（III）的化合物与羟胺或N-或O-保护的羟胺反应并除去保护基来制备。

    신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법
    7.
    发明公开
    신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법 有权
    新型抗坏血酸酶抑制剂化合物及其制备方法

    公开(公告)号：KR1020080107570A

    公开(公告)日：2008-12-11

    申请号：KR1020070055482

    申请日：2007-06-07

    Applicant: 일동홀딩스(주)

    Inventor： 강재훈 ,  유승우 ,  이희열 ,  조봉환 ,  안경미

    IPC: C07D211/58 ,  C07D401/12 ,  A61K31/435

    CPC classification number: C07D211/58 ,  C07D401/12 ,  C07D405/12

    Abstract: A novel compound, a method for preparing the compound, and an antibacterial composition containing the compound are provided to obtain a compound useful as a peptide deformylase inhibitor and showing an activity against the bacterial having tolerance to the already-known antibiotics. A novel peptide deformylase inhibitor compound is represented by the formula I, wherein A is -C(=O)NHOH or -N(CHO)OH; R1 is H, a C1-C3 alkyl group, a C4-C6 cycloalkyl group, a halogen atom, or a hydroxyl group; R2 is H, a linear or branched C1-C6 alkyl group, a linear or branched C2-C6 alkenyl group, a C4-C6 cycloalkyl group, a phenyl group, or a benzyl group; X is H or NR4R5; R4 and R5 are independently H, a linear or branched C1-C3 alkyl group, a t-butoxycarbonyl group, or a benzyloxycarbonyl group; and W is C or N.

    Abstract translation: 提供新化合物，制备该化合物的方法和含有该化合物的抗菌组合物，以获得可用作肽变性酶抑制剂的化合物，并显示对已知抗生素具有耐受性的细菌活性。 一种新的肽失活酶抑制剂化合物由式I表示，其中A是-C（= O）NHOH或-N（CHO）OH; R1是H，C1-C3烷基，C4-C6环烷基，卤素原子或羟基; R2是H，直链或支链C 1 -C 6烷基，直链或支链C 2 -C 6烯基，C 4 -C 6环烷基，苯基或苄基; X为H或NR4R5; R4和R5独立地为H，直链或支链C1-C3烷基，叔丁氧基羰基或苄氧基羰基; W为C或N.

    펩티드 데포르밀라제 저해제로서 신규의 엔-포르밀히드록실아민 화합물 및 그 제조방법
    8.
    发明公开
    펩티드 데포르밀라제 저해제로서 신규의 엔-포르밀히드록실아민 화합물 및 그 제조방법 失效
    新型N-甲基羟甲基胺化合物作为肽类抗坏血酸酶的抑制剂及其制造方法

    公开(公告)号：KR1020080052854A

    公开(公告)日：2008-06-12

    申请号：KR1020060124557

    申请日：2006-12-08

    Applicant: 일동홀딩스(주)

    Inventor： 강재훈 ,  유승우 ,  이희열 ,  조봉환 ,  안경미

    IPC: C07D215/50 ,  C07D401/04

    Abstract: A new N-formyl hydroxylamine compound as an inhibitor of peptide deformylase is provided to improve safety of use, treat respiratory disease by inhibiting growth of Streptococcus pneumonia, and show anti-bacterial activity against antibiotic-resistance bacteria. A anti-bacterial N-formyl hydroxylamine compound represented by the formula(1) or pharmaceutically acceptable salts thereof is provided as an inhibitor of peptide deformylase, wherein R1 is hydrogen, C1-3 alkyl, C4-6 cycloalkyl, halogen or hydroxyl; R2 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkene, C4-6 cycloalkyl, C4-6 heterocycle having N or O, or benzyl; R3 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkene, C4-6 cycloalkyl, phenyl or benzyl; A is selected from compounds represented by the formula(IIa), formula(IIb) and formula(IIc); R4 is hydrogen, linear or branched C1-6 alkyl, C3-6 cycloalkyl, phenyl or halogen-substituted phenyl; R5 and R6 are each independently hydrogen or halogen; Q is O or N-R7 or CH-R7; R7 is hydrogen or C1-3 alkyl; and n is 0 or 1.

    Abstract translation: 提供新的N-甲酰羟胺化合物作为肽脱甲酰酶的抑制剂，以提高使用的安全性，通过抑制肺炎链球菌的生长来治疗呼吸道疾病，并显示对抗生素抗性细菌的抗菌活性。 提供由式（1）表示的抗菌N-甲酰基羟胺化合物或其药学上可接受的盐作为肽变性酶抑制剂，其中R1是氢，C1-3烷基，C4-6环烷基，卤素或羟基; R 2为氢，直链或支链C 1-6烷基，直链或支链C 2-6烯烃，C 4-6异氰酸酯，C 3-6杂环或N或O，或苄基; R 3是氢，直链或支链C 1-6烷基，直链或支链C 2-6烯烃，C 4-6环烷基，苯基或苄基; A选自由式（IIa），式（IIb）和式（IIc）表示的化合物; R4是氢，直链或支链C 1-6烷基，C 3-6环烷基，苯基或卤素取代的苯基; R5和R6各自独立地为氢或卤素; Q是O或N-R7或CH-R7; R7是氢或C1-3烷基; n为0或1。

    펩티드 데포르밀라제 저해제로서 신규의 엔-포르밀히드록실아민 유도체 및 그 제조방법
    9.
    发明授权
    펩티드 데포르밀라제 저해제로서 신규의 엔-포르밀히드록실아민 유도체 및 그 제조방법 失效
    新型N-甲醛羟基胺衍生物作为肽变位酶的抑制剂及其制备方法

    公开(公告)号：KR100774728B1

    公开(公告)日：2007-11-08

    申请号：KR1020060047172

    申请日：2006-05-25

    Applicant: 일동홀딩스(주)

    Inventor： 강재훈 ,  유승우 ,  이희열 ,  조봉환 ,  안경미

    IPC: C07D235/18 ,  C07D235/26 ,  C07D235/30

    Abstract: Novel N-formyl hydroxylamine derivatives are provided to inhibit growth of Streptococcus pneumoniae and antibiotic-resistant bacteria by inhibiting activity of peptide deformylase(PDF) associated with protein biosynthesis and polypeptide maturation, thereby treating respiratory disease. The N-formyl hydroxylamine derivatives represented by the formula(I) are provided, wherein A is -C(=O)NHOH or -N(CHO)OH; R1 is hydrogen, C1-3 alkyl, C4-6 cycloalkyl, halogen or hydroxyl; R2 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, N or O-containing C4-6 heterocycle or benzyl; R3 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, phenyl or benzyl; Y is a compound represented by the formula(IIa) or formula(IIb). In the formula(IIa) or formula(IIb), R4 is hydrogen, linear or branched C1-6 alkyl, linear or branched C2-6 alkenyl, C4-6 cycloalkyl, phenyl or benzyl; and R5 is hydrogen, halogen, amino, C1-6 alkyl substituted amino, aryl substituted amino, furan or a compound represented by the formula(III). In the formula(III), R6-R10 is independently hydrogen, linear or branched C1-3 alkyl, linear or branched halogen substituted C1-4 alkyl, hydroxy, acyl, acyloxy, halogen(fluoro, chloro, bromo, iodo), cyano, nitro, amino, N,N-dimethylamino, phenyl, morpholinyl or formyl.

    Abstract translation: 提供新的N-甲酰羟胺衍生物，通过抑制与蛋白质生物合成和多肽成熟相关的肽形成酶（PDF）的活性来抑制肺炎链球菌和抗生素抗性细菌的生长，从而治疗呼吸道疾病。 提供由式（I）表示的N-甲酰基羟胺衍生物，其中A为-C（= O）NHOH或-N（CHO）OH; R1是氢，C1-3烷基，C4-6环烷基，卤素或羟基; R 2是氢，直链或支链C 1-6烷基，直链或支链C 2-6烯基，C 4-6环烷基，含N或O的C 4-6杂环或苄基; R 3是氢，直链或支链C 1-6烷基，直链或支链C 2-6烯基，C 4-6环烷基，苯基或苄基; Y是由式（IIa）或式（IIb）表示的化合物。 在式（IIa）或式（IIb）中，R 4是氢，直链或支链C 1-6烷基，直链或支链C 2-6烯基，C 4-6环烷基，苯基或苄基; R 5为氢，卤素，氨基，C 1-6烷基取代的氨基，芳基取代的氨基，呋喃或式（III）表示的化合物。 在式（III）中，R 6 -R 10独立地为氢，直链或支链C 1-3烷基，直链或支链卤素取代的C 1-4烷基，羟基，酰基，酰氧基，卤素（氟，氯，溴，碘） ，硝基，氨基，N，N-二甲基氨基，苯基，吗啉基或甲酰基。

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