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1. 发明申请

US20100009957A1 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：US20100009957A1
公开(公告)日：2010-01-14
申请号：US12442816
申请日：2007-09-24
申请人： Timothy A. Blizzard , Helen Y. Chen , Jane Yang Wu , Seongkon Kim , Sookhee Ha , Christopher J. Mortko , Narayan Variankaval , Anna Chiu
发明人： Timothy A. Blizzard , Helen Y. Chen , Jane Yang Wu , Seongkon Kim , Sookhee Ha , Christopher J. Mortko , Narayan Variankaval , Anna Chiu
IPC分类号： A61K31/397 , C07D205/12 , A61P31/04
CPC分类号： C07D487/04
摘要： A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：在双环的两个位置被杂环基氨基羰基或碳环基氨基羰基取代的一类7-氧代-2,6-二氮杂双环[3.2.0] - 庚烷-6-磺酸化合物是β-内酰胺酶抑制剂。化合物及其前药和药学上可接受的盐可用于与β-内酰胺抗生素联合治疗细菌感染。特别地，由于β-内酰胺酶的存在，这些化合物适用于β-内酰胺抗生素（例如亚胺培南和头孢他啶）对抗β-内酰胺抗生素的微生物。

2. 发明申请

US20110294777A1 BETA-LACTAMASE INHIBITORS 有权
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：US20110294777A1
公开(公告)日：2011-12-01
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Sookhee Ha , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： A61K31/4545 , C07D487/08 , C07D519/00 , A61K31/55 , A61K31/454 , A61P31/04 , A61K31/439 , A61K31/553 , A61K31/496 , C07D401/12 , A61P31/00 , C07D471/08 , A61K31/4439
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于治疗与β-内酰胺抗生素组合的细菌感染。特别地，由于β-内酰胺酶的存在，这些化合物可以与抗β-生物抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

3. 发明授权

US08487093B2 β-lactamase inhibitors 有权
标题翻译： β-内酰胺酶抑制剂
公开(公告)号：US08487093B2
公开(公告)日：2013-07-16
申请号：US12812763
申请日：2009-01-15
申请人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
发明人： Timothy A. Blizzard , Helen Chen , Candido Gude , Jeffrey D. Hermes , Jason Imbriglio , Seongkon Kim , Jane Y. Wu , Christopher J. Mortko , Ian Mangion , Nelo Rivera , Rebecca T. Ruck , Michael Shevlin
IPC分类号： C07D243/00 , A61K31/551
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于与β-内酰胺抗生素联合治疗细菌感染。特别地，由于β-内酰胺酶的存在，该化合物可与β-内酰胺抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

4. 发明授权

US6008212A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US6008212A
公开(公告)日：1999-12-28
申请号：US168422
申请日：1998-10-08
申请人： Ronald W. Ratcliffe , Timothy A. Blizzard
发明人： Ronald W. Ratcliffe , Timothy A. Blizzard
IPC分类号： C07D477/14 , A61K31/395 , C07D487/04
CPC分类号： C07D477/14
摘要： Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
摘要翻译：公开了式I化合物及其药学上可接受的盐。 R2是H，R3是C1-3烷基，R2和R3组合表示C1-3亚烷基。还包括药物组合物和治疗方法。该化合物可用于耐甲氧西林葡萄球菌（MRSA）。

5. 发明授权

US5114930A Avermectin derivatives with a spacer inserted between the disaccharide and the aglycone useful as antiparasitic agents 失效
标题翻译：异麦芽糖衍生物与异丙肾上腺素之间插入的抗体衍生物作为抗原药物有用
公开(公告)号：US5114930A
公开(公告)日：1992-05-19
申请号：US522709
申请日：1990-05-14
申请人： Timothy A. Blizzard , Gaye Margiatto
发明人： Timothy A. Blizzard , Gaye Margiatto
IPC分类号： A01N43/90 , A61K31/70 , A61K31/7028 , A61P33/10 , C07D493/18 , C07H15/26 , C07H19/01 , C12P17/18 , C12R1/465
CPC分类号： C07H19/01 , A01N43/90 , C07H15/26
摘要： There are disclosed avermectin derivatives which incorporate a spacer between the disaccharide and the aglycone. The synthetic spacer-containing analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.

6. 发明授权

US4923867A Synthetic marcfortine derivatives useful as antiparasitic agents 失效
标题翻译：用作抗寄生虫剂的合成马可氟汀衍生物
公开(公告)号：US4923867A
公开(公告)日：1990-05-08
申请号：US235418
申请日：1988-08-24
申请人： Timothy A. Blizzard , Helmut Mrozik
发明人： Timothy A. Blizzard , Helmut Mrozik
IPC分类号： A01N43/90 , C07D491/22
CPC分类号： C07D491/22 , A01N43/90
摘要： There are disclosed synthetic marcfortine derivatives of the natural products marcfortine A, marcfortine B, and marcfortine C. The synthetic derivatives are described in the following formula: ##STR1## wherein: n is 0 or 1R.sub.1 is hydrogen, loweralkyl, benzyl, lower alkanoyl, benzenesulfonyl in which the benzene ring is substituted with from 0 to 3 substituents selected from lower alkyl groups, lower alkoxy groups and halogen atoms, lower alkylamino-carbonyl, lower alkoxy-carbonyl;R.sub.24 is hydrogen, halogen or lower alkoxy (provided that R.sub.24 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position),R.sub.25 is hydrogen or halogen (provided that R.sub.25 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position);R.sub.29 is hydrogen, lower alkyl, alkoxyalkyl, haloalkyl, lower alkenyl, lower alkynyl, benzyl, lower alkanoyl, substituted benzenesulfonyl, lower alkylamino-carbonyl, not hydrogen or methyl if R.sub.1 is hydrogen; and the broken line represents a single or double bond between carbons 24 and 25.The compounds are active antiparasitic agents useful in particular against insect and nematode pests, and compositions for that use are disclosed.
摘要翻译：公开了天然产物马可氟汀A，马可氟汀B和马可氟汀C的合成马可氟汀衍生物。合成衍生物描述于下式中：其中：n为0或1，R1为氢，低级烷基，苄基，低级烷酰基苯磺酰基，其中苯环被0-3个选自低级烷基，低级烷氧基和卤素原子的取代基取代，低级烷基氨基 - 羰基，低级烷氧羰基; R24是氢，卤素或低级烷氧基（只要虚线表示24,25位的单键，R24不是氢），R25是氢或卤素（只要R25不是氢，只要是虚线代表24,25位的单键）; 如果R1是氢，R29是氢，低级烷基，烷氧基烷基，卤代烷基，低级烯基，低级炔基，苄基，低级烷酰基，取代的苯磺酰基，低级烷基氨基 - 羰基，不是氢或甲基; 并且虚线表示碳24和25之间的单键或双键。化合物是有效的抗寄生虫剂，特别适用于昆虫和线虫害虫，并且公开了该用途的组合物。

7. 发明申请

US20090012061A1 A Method of Treating Cancer 审中-公开
标题翻译：一种治疗癌症的方法
公开(公告)号：US20090012061A1
公开(公告)日：2009-01-08
申请号：US11662396
申请日：2005-09-09
申请人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
发明人： Timothy A. Blizzard , Carolyn A. Buser-Doepner , Douglas E. Frantz , Kelly Hamilton , Myle Hoang , Ling Lee , Christopher R. Moyes , Jerry A. Murry , Arash Soheili
IPC分类号： G01N33/574 , C12N9/99 , A61K31/403 , A61K31/428 , C07C271/06 , A61K31/27 , A61K31/47 , C07D215/38 , C07C39/12 , A61K31/05 , C07C275/28 , A61K31/17 , A61K31/165 , A61K31/415 , A61K31/44 , A61K31/5415 , A61K31/551 , A61P35/00
CPC分类号： C12Q1/42 , G01N33/6893 , G01N2500/00
摘要： The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要翻译：本发明涉及一种治疗细胞增殖性疾病，特别是癌症的方法，其包括施用有丝分裂驱动蛋白KSP活性的调节剂，其中KSP调节剂的活性取决于微管的存在。相信本方法中使用的KSP调节剂以先前未报道的方式结合KSP蛋白质，因为化合物相对于微管或ATP（KSP的底物）竞争性结合。在本方法中有用的调节剂还不能抵抗KSP的非微管刺激活性。可以使用本文公开的方法治疗的细胞增殖性疾病是例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。

8. 发明授权

US5756725A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5756725A
公开(公告)日：1998-05-26
申请号：US825786
申请日：1997-04-08
申请人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
发明人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
IPC分类号： C07D20060101 , C07D477/14 , C07D519/00 , C07D521/00 , C07D487/04 , A61K31/395
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式I表示：还包括药物组合物和使用方法。

9. 发明授权

US5496816A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5496816A
公开(公告)日：1996-03-05
申请号：US359770
申请日：1994-12-20
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
IPC分类号： C07D477/00 , A61K31/397 , A61K31/42 , A61K31/425 , A61K31/495 , A61P31/04 , C07D477/20 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20
摘要： Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：以下公式的碳青霉烯类似物：作为有用的抗菌剂被公开。还公开了药物组合物和使用方法。

10. 发明授权

US06294528B1 Carbapenem antibacterial compounds, compositions containing such compounds and method of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06294528B1
公开(公告)日：2001-09-25
申请号：US09338644
申请日：1999-06-23
申请人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
摘要翻译：公开了式I化合物及其药学上可接受的盐和可用作碳青霉烯类抗菌剂的组合物。

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