公开(公告)号：JP2004507481A

公开(公告)日：2004-03-11

申请号：JP2002522829

申请日：2001-08-23

Applicant: エッセンシャル・セラピューティクス・インコーポレイテッドEssential Therapeutics, Inc.

Inventor： トーマス・ダブリュー・グリンカ

IPC: C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00

CPC classification number: C07D501/00

Abstract: 本発明は、新規なセファロスポリン抗生物質、そのプロドラッグおよびこれらの医薬的に許容しうる塩を提供する。 これらの化合物は、現在の臨床上のベータラクタム抗生物質に抵抗する広域スペクトルのバクテリアに対して活性である。

公开(公告)号：JP2004516847A

公开(公告)日：2004-06-10

申请号：JP2002555752

申请日：2001-09-27

Applicant: エッセンシャル・セラピューティクス・インコーポレイテッドEssential Therapeutics, Inc.

Inventor： ポール ケイ． ナカネ、

IPC: C12Q1/20 ,  A61P31/00 ,  C12Q1/18 ,  C12R1/19

CPC classification number: C12Q1/18

Abstract: 本発明は、抗生物質による酵素阻害を組織化学的に検出する方法を用いた、抗生物質に対する細菌の感受性を迅速に判定する方法に関する。

公开(公告)号：WO03001887A3

公开(公告)日：2003-08-21

申请号：PCT/US0220567

申请日：2002-06-28

Applicant: ESSENTIAL THERAPEUTICS INC ,  PLIVA D D ,  MOE SCOTT T ,  ALA PAUL J ,  PEROLA EMANUELE ,  FAERMAN CARLOS H ,  CLEMENT JACOB J ,  ALI JANID A ,  WILL PAUL M ,  MARCHESE SALVATORE A ,  MAGEE ANDREW S ,  GAZZANIGA JOHN V ,  FARADY CHRISTOPHER ,  NAVIA MANUEL A ,  CONNELLY PATRICK R

Inventor： MOE SCOTT T ,  ALA PAUL J ,  PEROLA EMANUELE ,  FAERMAN CARLOS H ,  CLEMENT JACOB J ,  ALI JANID A ,  WILL PAUL M ,  MARCHESE SALVATORE A ,  MAGEE ANDREW S ,  GAZZANIGA JOHN V ,  FARADY CHRISTOPHER ,  NAVIA MANUEL A ,  CONNELLY PATRICK R

IPC: A61K31/519 ,  A61K31/525 ,  A61P31/04 ,  C07D401/12 ,  C07D471/04 ,  C07D475/08 ,  C07D487/02 ,  C07D487/04 ,  C07D519/00 ,  A61K31/517

CPC classification number: C07D401/12 ,  C07D471/04 ,  C07D475/08 ,  C07D487/04

Abstract: The invention is based on the discovery of a new class of heterocyclic compounds having, for example, antibacterial properties. The D-Ala-D-Ala ligase enzyme is a critical pathway enzyme in the bacterial cell-wall synthesis. The compounds can bind to and inhibit the enzyme D-Ala-D-Ala ligase. The new compounds' activity combined with their ability to cross bacterial cell membranes makes them suitable for use as antibacterial drugs or other antibacterial applications.

Abstract translation: 本发明基于发现具有例如抗菌性质的新类型的杂环化合物。 D-Ala-D-Ala连接酶是细菌细胞壁合成中的关键途径酶。 该化合物可以结合并抑制酶D-Ala-D-Ala连接酶。 新化合物的活性与其交叉细菌细胞膜的能力相结合，使其适合用作抗菌药物或其他抗菌药物。

公开(公告)号：WO2003002064A2

公开(公告)日：2003-01-09

申请号：PCT/US2002/020479

申请日：2002-06-28

Applicant: ESSENTIAL THERAPEUTICS, INC. ,  MOE, Scott, T. ,  CLEMENT, Jacob, J. ,  FAERMAN, Carlos ,  PEROLA, Emanuela ,  NAVIA, Manuel, A. ,  ALA, Paul, J. ,  MAGEE, Andrew, S. ,  WILL, Paul, M. ,  MARCHESE, Salvatore, A. ,  GAZZANIGA, John, V.

Inventor： MOE, Scott, T. ,  CLEMENT, Jacob, J. ,  FAERMAN, Carlos ,  PEROLA, Emanuela ,  NAVIA, Manuel, A. ,  ALA, Paul, J. ,  MAGEE, Andrew, S. ,  WILL, Paul, M. ,  MARCHESE, Salvatore, A. ,  GAZZANIGA, John, V.

IPC: A61K

CPC classification number: C07D401/12 ,  C07D471/04 ,  C07D475/08 ,  C07D487/04

Abstract: This invention relates to novel heterocyclic compounds and to their use in the medical treatment or prophylaxis of bacterial infections, or their use as antiseptics, sterilizants, or disinfectants.

Abstract translation: 本发明涉及新颖的杂环化合物及其在治疗或预防细菌感染中的用途，或其用作防腐剂，灭菌剂或消毒剂的用途。

公开(公告)号：WO03002063A3

公开(公告)日：2003-02-20

申请号：PCT/US0220465

申请日：2002-06-28

Applicant: ESSENTIAL THERAPEUTICS INC ,  PLIVA D D ,  NAVIA MANUEL A ,  ALA PAUL J ,  GRIFFITH JAMES P ,  ALI JANID A ,  FAERMAN CARLOS H ,  MOE SCOTT T ,  MAGEE ANDREW S ,  CONNELLY PATRICK R ,  PEROLA EMANUELE

Inventor： NAVIA MANUEL A ,  ALA PAUL J ,  GRIFFITH JAMES P ,  ALI JANID A ,  FAERMAN CARLOS H ,  MOE SCOTT T ,  MAGEE ANDREW S ,  CONNELLY PATRICK R ,  PEROLA EMANUELE

IPC: C12N9/00 ,  C12Q1/37

CPC classification number: C12N9/93

Abstract: The invention is based on the discovery that certain small molecules can bind to the ATP binding site of D-Ala-D-Ala ligase, even in the absence of the enzyme's substrate, and can cause a conformational change in the enzyme structure similar to that which occurs upon binding of ATP and substrate to the enzyme. Without wishing to be bound by any theory, it is believed that such a conformational change is required for either activation or inhibition of the enzyme. The information obtained from this discovery has enabled identification of key interactions in the active site of the enzyme, as well as the design and opimization of inhibitors.

Abstract translation: 本发明基于以下发现，即使在不存在酶的底物的情况下，某些小分子也可以结合D-Ala-D-Ala连接酶的ATP结合位点，并且可以引起类似于酶结构的构象变化 其在ATP和底物与酶结合后发生。 不希望受任何理论束缚，据信这种构象变化是酶活化或抑制所必需的。 从该发现获得的信息使得能够鉴定酶的活性位点中的关键相互作用以及抑制剂的设计和优化。

公开(公告)号：WO2003002063A2

公开(公告)日：2003-01-09

申请号：PCT/US2002/020465

申请日：2002-06-28

Applicant: ESSENTIAL THERAPEUTICS, INC. ,  PLIVA, D., D. ,  NAVIA, Manuel, A. ,  ALA, Paul, J. ,  GRIFFITH, James, P. ,  ALI, Janid, A. ,  FAERMAN, Carlos, H. ,  MOE, Scott, T. ,  MAGEE, Andrew, S. ,  CONNELLY, Patrick, R. ,  PEROLA, Emanuele

Inventor： NAVIA, Manuel, A. ,  ALA, Paul, J. ,  GRIFFITH, James, P. ,  ALI, Janid, A. ,  FAERMAN, Carlos, H. ,  MOE, Scott, T. ,  MAGEE, Andrew, S. ,  CONNELLY, Patrick, R. ,  PEROLA, Emanuele

IPC: A61K

CPC classification number: C12N9/93

Abstract: The invention is based on the discovery that certain small molecules can bind to the ATP binding site of D-Ala-D-Ala ligase, even in the absence of the enzyme's substrate, and can cause a conformational change in the enzyme structure similar to that which occurs upon binding of ATP and substrate to the enzyme. Without wishing to be bound by any theory, it is believed that such a conformational change is required for either activation or inhibition of the enzyme. The information obtained from this discovery has enabled identification of key interactions in the active site of the enzyme, as well as the design and opimization of inhibitors.

Abstract translation: 本发明基于这样的发现，即即使在不存在酶底物的情况下，某些小分子也可以与D-Ala-D-Ala连接酶的ATP结合位点结合，并且可以引起构象 酶结构的改变与ATP和底物与酶结合后发生的结构相似。 不希望受任何理论束缚，据信这种构象变化对于酶的活化或抑制是必需的。 从这一发现中获得的信息使得能够鉴定酶的活性位点中的关键相互作用，以及抑制剂的设计和优化。

公开(公告)号：WO2003001887A2

公开(公告)日：2003-01-09

申请号：PCT/US2002/020567

申请日：2002-06-28

Applicant: ESSENTIAL THERAPEUTICS, INC. ,  PLIVA D.D. ,  MOE, Scott, T. ,  ALA, Paul, J. ,  PEROLA, Emanuele ,  FAERMAN, Carlos, H. ,  CLEMENT, Jacob, J. ,  ALI, Janid, A. ,  WILL, Paul, M. ,  MARCHESE, Salvatore, A. ,  MAGEE, Andrew, S. ,  GAZZANIGA, John, V. ,  FARADY, Christopher ,  NAVIA, Manuel, A. ,  CONNELLY, Patrick, R.

Inventor： MOE, Scott, T. ,  ALA, Paul, J. ,  PEROLA, Emanuele ,  FAERMAN, Carlos, H. ,  CLEMENT, Jacob, J. ,  ALI, Janid, A. ,  WILL, Paul, M. ,  MARCHESE, Salvatore, A. ,  MAGEE, Andrew, S. ,  GAZZANIGA, John, V. ,  FARADY, Christopher ,  NAVIA, Manuel, A. ,  CONNELLY, Patrick, R.

IPC: A61K31/519 ,  A61K31/525 ,  A61P31/04 ,  C07D401/12 ,  C07D471/04 ,  C07D475/08 ,  C07D487/02 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D401/12 ,  C07D471/04 ,  C07D475/08 ,  C07D487/04

Abstract: The invention is based on the discovery of a new class of heterocyclic compounds having, for example, antibacterial properties. The D-Ala-D-Ala ligase enzyme is a critical pathway enzyme in the bacterial cell-wall synthesis. The compounds can bind to and inhibit the enzyme D-Ala-D-Ala ligase. The new compounds' activity combined with their ability to cross bacterial cell membranes makes them suitable for use as antibacterial drugs or other antibacterial applications.

Abstract translation: 本发明基于发现具有例如抗菌性质的新类型的杂环化合物。 D-Ala-D-Ala连接酶是细菌细胞壁合成中的关键途径酶。 该化合物可以结合并抑制酶D-Ala-D-Ala连接酶。 新化合物的活性与其交叉细菌细胞膜的能力相结合，使其适合用作抗菌药物或其他抗菌药物。

公开(公告)号：NO20030931L

公开(公告)日：2003-04-29

申请号：NO20030931

申请日：2003-02-27

Applicant: ESSENTIAL THERAPEUTICS INC

Inventor： GLINKA THOMASZ W

IPC: C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  A61K

Abstract: The present invention relates to chemical compounds having the formula:or a pharmaceutically acceptable salt thereof. R1 is selected from the group consisting of:R2 is selected from the group consisting ofhydrogen, CH3-, FCH2-, F2CH-R3 is selected from the group consisting of:X is selected from the group consisting of hydrogen, halogen, cyano, -NH2, -N(CH3)2, -HSO2NH2, -SO2NH2 and -SCH3. The subscript n is 0 or 1.

公开(公告)号：NO20030931A

公开(公告)日：2003-04-29

申请号：NO20030931

申请日：2003-02-27

Applicant: ESSENTIAL THERAPEUTICS INC

Inventor： GLINKA THOMASZ W

IPC: C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  A61K

CPC classification number: C07D501/00

公开(公告)号：NO20030931D0

公开(公告)日：2003-02-27

申请号：NO20030931

申请日：2003-02-27

Applicant: ESSENTIAL THERAPEUTICS INC

Inventor： GLINKA THOMASZ W

IPC: C07D501/59 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  A61K

Abstract: The present invention relates to chemical compounds having the formula:or a pharmaceutically acceptable salt thereof. R1 is selected from the group consisting of:R2 is selected from the group consisting ofhydrogen, CH3-, FCH2-, F2CH-R3 is selected from the group consisting of:X is selected from the group consisting of hydrogen, halogen, cyano, -NH2, -N(CH3)2, -HSO2NH2, -SO2NH2 and -SCH3. The subscript n is 0 or 1.