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公开(公告)号：EP1432713A4
公开(公告)日：2005-05-11
申请号：EP02753353
申请日：2002-06-28
发明人： 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分类号： A61K31/519 , A61K31/525 , A61P31/04 , C07D401/12 , C07D471/04 , C07D475/08 , C07D487/02 , C07D487/04 , C07D519/00 , A61K31/517 , C07D239/95
CPC分类号： C07D401/12 , C07D471/04 , C07D475/08 , C07D487/04
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2.发明公开8/17 HETEROCYCLIC COMPOUNDS AND USES THEREOF AS D-ALANYL-D-ALANINE LIGASE INHIBITORS 审中-公开8/17杂环化合物和它们作为D-丙氨酰-D-丙氨酸连接酶抑制剂
公开(公告)号：EP1411949A4
公开(公告)日：2004-11-24
申请号：EP02759101
申请日：2002-06-28
发明人： 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分类号： A61K31/519 , A61K31/525 , A61P31/04 , C07D401/12 , C07D471/04 , C07D475/08 , C07D487/02 , C07D487/04 , C07D519/00 , A61K31/517
CPC分类号： C07D401/12 , C07D471/04 , C07D475/08 , C07D487/04
摘要： 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.
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3.发明公开STRUCTURE-BASED DRUG DESIGN METHODS FOR IDENTIFYING D-ALA-D-ALA LIGASE INHIBITORS AS ANTIBACTERIAL DRUGS 审中-公开主动设计工艺对结构基础一种判别D-ALA-D-ALA-连接酶抑制剂AS抗菌物质
公开(公告)号：EP1412516A2
公开(公告)日：2004-04-28
申请号：EP02749688.4
申请日：2002-06-28
发明人： 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分类号： C12Q1/37
CPC分类号： C12N9/93
摘要： 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.
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4.发明公开PRODRUGS OF A 7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID ANTIBIOTIC 审中-公开A 7酰氨基-3-杂-3-头孢烯抗生素CARBOXYLIC前药的
公开(公告)号：EP1320533A1
公开(公告)日：2003-06-25
申请号：EP01918879.6
申请日：2001-03-20
申请人： Essential Therapeutics, Inc. , Hecker, Scott J. , Cho, Aesop , Glinka, Tomasz W. , Calkins, Trevor , Lee, Ving J.
IPC分类号： C07D501/59 , A61K31/546 , A61P31/04
CPC分类号： C07D501/00
摘要： The present invention relates to prodrugs of the antibiotic compound (7R)-7-[(Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(hydroxylimino)acetamido]acetamidol]-3-{3-(2-aminoethylthiomethyl]-pyrid-4-ylthio}-3-cephem-4-carbocyllic acid, where the prodrugs are substantially more water soluble at or near neutral pH than the parent compound.
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公开(公告)号：EP1333836A4
公开(公告)日：2004-07-07
申请号：EP01968147
申请日：2001-08-23
发明人： GLINKA TOMASZ W
IPC分类号： C07D501/59 , A61K31/546 , A61P31/04 , C07D501/00 , A61K31/545 , A61P31/00
CPC分类号： C07D501/00
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6.发明公开MEDICINE FOR INHIBITING DRUG ELIMINATION PUMP 审中-公开MEDIKAMENT ZUM INHIBIEREN EINER PUMPE，MIT DER ARZNEIMITTEL ELIMINIERT WERDEN
公开(公告)号：EP1389463A1
公开(公告)日：2004-02-18
申请号：EP02722752.9
申请日：2002-04-24
发明人： NAKAYAMA, K., c/o Daiichi Pharmaceutical Co., Ltd , OHTSUKA, M., c/o Daiichi Pharmaceutical Co., Ltd. , KAWATO, H., c/o Daiichi Pharmaceutical Co., Ltd , OKUMURA, R., c/o Daiichi Pharmaceutical Co., Ltd. , HOSHINO, K., c/o Daiichi Pharmaceutical Co., Ltd. , WATKINS, W., c/o Essential Therapeutics, Inc. , ZHANG, Jason, c/o Essential Therapeutics, Inc. , PALME, Monica, c/o Essential Therapeutics, Inc. , CHO, Aesop, c/o Essential Therapeutics, Inc.
IPC分类号： A61K31/549 , A61K45/00 , A61K31/5377 , A61K31/55 , A61K31/4709 , A61P31/04 , A61P31/00 , A61P43/00 , C12Q1/18 , C12Q1/02 , G01N33/15
CPC分类号： C07D417/06 , A61K31/427 , A61K31/4709 , A61K31/4745 , A61K31/496 , A61K31/5025 , A61K31/519 , A61K31/5377 , A61K31/549 , A61K31/55 , A61K45/06 , C07D417/12 , C07D471/04 , C12Q1/18
摘要： A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I):
wherein, R 1 and R 2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W 1 represents -CH=CH-, -CH 2 O-, -CH 2 CH 2 - or the like; R 3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R 4 represents hydrogen atom, a group of -OZ 0-4 R 5 (Z 0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R 5 represents a cyclic alkyl group, an aryl group or the like); W 2 represents a single bond or -C(R 8 )=C(R 9 )- (R 8 and R 9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W 2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.摘要翻译： 一种用于预防和/或治疗微生物感染的药物，其包含作为活性成分的由以下通式（I）表示的化合物：其中R 1和R 2表示氢原子， 卤素原子，羟基等，W 1表示-CH = CH-，-CH 2 O - ， - CH 2 CH 2 - 等; R 3表示氢原子，卤素原子，羟基或氨基; R 4表示氢原子，-OZO 4 R 5基团（Z 0-4表示亚烷基，氟取代的亚烷基或单键，R 5表示环状烷基， 芳基等）; W 2表示单键或-C（R 8）= C（R 9） - （R 8和R 9）表示氢原子，卤素原子，低级烷基或 Q表示酸性基团，但W 2和Q可以一起形成亚乙基二氮烷二酮或等价杂环; m和n表示0〜2的整数，q表示0〜3的整数。
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公开(公告)号：EP1227084A4
公开(公告)日：2003-08-20
申请号：EP00970155
申请日：2000-10-27
发明人： LEGER ROGER , WATKINS WILLIAM JOHN , ZHANG JASON ZHIJIA , RENAU THOMAS ERIC , LEE VING JACK , OHTA TOSHIHARU , NAKAYAMA KIYOSHI , ISHIDA YOHHEI , OHTSUKA MASAMI , KAWATO HARUKO
IPC分类号： A61K31/341 , A61K31/41 , A61K31/421 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4375 , A61K31/44 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/4738 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/5383 , A61P31/04 , C07D277/26 , C07D277/28 , C07D277/32 , C07D277/44 , C12Q1/18 , G01N33/68 , C07D213/30 , A61K31/425 , C07D215/14 , C07D215/56 , C07D263/56 , C07D307/52 , C07D513/04
CPC分类号： G01N33/6803 , A61K31/341 , A61K31/41 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4375 , A61K31/44 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/4738 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/5383 , C07D213/30 , C07D215/14 , C07D215/56 , C07D263/56 , C07D277/24 , C07D277/28 , C07D285/08 , C07D307/52 , C07D409/12 , C07D417/04 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07K2299/00 , C12Q1/18 , G01N2500/04
摘要： Drugs for preventing and/or treating microbial infectious diseases which contain, as the active ingredient, compounds represented by the formula (I), physiologically acceptable salts thereof or hydrates of the same and have an effect of making a microorganism having acquired tolerance to a drug non-tolerant. In said formula R?1 and R2¿ independently represent each hydrogen, halogeno, carboxy, etc.; J1 represents 5- or 6-membered heteroaryl; W1 represents -CH=CH-, -CH CH-, -CH¿2?CH2-, etc.; A?1¿ represents phenylene, pyridinedyl, furandyl, etc.; G1 represents oxygen, carbonyl, ethynyl, etc.; p is an integer of from 0 to 3; G2 represents phenylene, furandyl, tetrahydrofurandyl, etc.; G3 represents -CH¿2?- or a single bond; m and n represent each an integer of 0 or 1; and Q?1¿ represents an acidic group.
摘要翻译： 一种用于预防和/或治疗微生物感染的药物，所述微生物感染具有消除对抗微生物剂具有获得性抗性的微生物的抗性的活性，其包含作为活性成分的由以下通式（I）表示的化合物，生理学上 其可接受的盐或其水合物：
其中R 1和R 2独立地表示氢原子，卤素原子，羧基等; J 1表示5或6元杂芳环; W 1表示-CH = CH - ， - C≡C-，-CH 2 CH 2 - 等; A 1表示亚苯基，吡啶二基，呋喃二基等; G 1表示氧原子，羰基，乙炔基等; p表示0〜3的整数， G 2表示亚苯基，呋喃基，四氢呋喃基等; G 3表示-CH 2 - 或单键; m和n表示0或1的整数; Q 1表示酸性基团。 -
8.发明公开7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID ANTIBIOTICS AND PRODRUGS THEREOF 有权7-酰胺基-3-乙酰氨基-3-头孢菌素羧酸类抗生素及其制剂
公开(公告)号：EP1222194A1
公开(公告)日：2002-07-17
申请号：EP00966807.0
申请日：2000-09-21
IPC分类号： C07D501/59 , A61K31/546 , A61P31/04 , C07D213/70 , C07D285/08 , C07F9/6506
CPC分类号： C07D213/70 , C07D285/08 , C07D501/00 , C07F9/65062
摘要： The present invention includes novel (7R)-7-acylamino-3-heteroarylthio-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts and prodrugs thereof, which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to β-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
摘要翻译： 本发明包括对广谱的生物体具有抗生素活性的新型（7R）-7-酰氨基-3-杂芳硫基-3-头孢烯-4-羧酸或其药理学上可接受的盐和前药，所述生物体包括对 β-内酰胺抗生素并且可用作抗菌剂。 本发明还涉及可用于制备本发明新化合物的新颖中间体，并涉及制备该新化合物和中间体化合物的新方法。
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9.发明公开STRUCTURE-BASED DRUG DESIGN METHODS FOR IDENTIFYING D-ALA-D-ALA LIGASE INHIBITORS AS ANTIBACTERIAL DRUGS 审中-公开主动设计工艺对结构基础一种判别D-ALA-D-ALA-连接酶抑制剂AS抗菌物质
公开(公告)号：EP1412516A4
公开(公告)日：2004-09-08
申请号：EP02749688
申请日：2002-06-28
发明人： 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
CPC分类号： C12N9/93
摘要： 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.
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公开(公告)号：EP1432713A2
公开(公告)日：2004-06-30
申请号：EP02753353.8
申请日：2002-06-28
发明人： 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分类号： C07D487/04 , C07D471/04 , C07D239/95 , A61K31/519 , A61K31/517 , A61P31/04
CPC分类号： C07D401/12 , C07D471/04 , C07D475/08 , C07D487/04
摘要： 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.
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