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1. 发明授权

US5252574A Angiotensin II antagonists incorporating a substituted thiophene or furan 失效
标题翻译：加入取代噻吩或呋喃的血管紧张素II拮抗剂
公开(公告)号：US5252574A
公开(公告)日：1993-10-12
申请号：US846152
申请日：1992-03-11
申请人： Eric E. Allen , Nancy Kevin , Tomasz W. Glinka , Ralph A. Rivero
发明人： Eric E. Allen , Nancy Kevin , Tomasz W. Glinka , Ralph A. Rivero
IPC分类号： A61K31/41 , A61K31/505 , A61P9/12 , A61P27/02 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D471/04 , C07D239/88 , C07D239/93 , C07D239/95
CPC分类号： C07D405/14 , C07D409/10 , C07D409/14
摘要： Substituted heterocycles attached through a methylene bridge to novel substituted phenyl thiophene or phenyl furan derivative of the Formula I are useful as angiotensin II antagonists. ##STR1##

2. 发明授权

US6087355A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US6087355A
公开(公告)日：2000-07-11
申请号：US730042
申请日：1996-10-11
申请人： In-Seop Cho , Scott J. Hecker , Tomasz W. Glinka , Ving J. Lee , Zhijia J. Zhang
发明人： In-Seop Cho , Scott J. Hecker , Tomasz W. Glinka , Ving J. Lee , Zhijia J. Zhang
IPC分类号： C07D277/20 , A61K31/00 , A61K31/545 , A61K31/546 , A61P31/00 , A61P31/04 , C07D277/40 , C07D277/44 , C07D277/46 , C07D501/00 , C07D501/24 , C07D501/59
CPC分类号： C07D501/00
摘要： The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR2## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-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：本发明包括新的式A化合物，其中A，B，D和E选自碳，氮和硫，R99选自硫，SO，SO 2，NH，N-烷基，氧，C = C（顺式或反式）和C 3BOND C，R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐，包括对β-内酰胺抗生素具有抗性的生物体，作为抗菌剂是有用的。本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

3. 发明授权

US5607926A Cephalosporin antibiotics 失效
公开(公告)号：US5607926A
公开(公告)日：1997-03-04
申请号：US413714
申请日：1995-03-29
申请人： Scott J. Hecker , In-Seop Cho , Burton G. Christensen , Tomasz W. Glinka
发明人： Scott J. Hecker , In-Seop Cho , Burton G. Christensen , Tomasz W. Glinka
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-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.

4. 发明授权

US08044230B2 Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof 失效
标题翻译：氯霉素，甲砜霉素及其类似物的水溶性前药
公开(公告)号：US08044230B2
公开(公告)日：2011-10-25
申请号：US11953972
申请日：2007-12-11
申请人： Tomasz W. Glinka
发明人： Tomasz W. Glinka
IPC分类号： C07C229/00 , C07D211/78 , C07D285/14 , C07D413/00 , A61K31/44 , A61K31/41 , A61K31/225
CPC分类号： C07C317/32 , C07D233/60
摘要： The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
摘要翻译：本发明公开了氯霉素或甲砜霉素或其类似物的某些新型前药，包括氯霉素或硫代霉酚或其类似物的药学上可接受的盐的前药，包括这些化合物的两个醇基的含氮酯。在某些实施方案中，这些新型前药具有足够的水溶性，以满足氯霉素或甲砜霉素或其类似物的前药所需的功能。在一个实施方案中，化合物的某些亚类还具有将前药保持在受试者系统的溶液中所需的水解稳定性，直到前药可以水解，释放所讨论的活性化合物时才存在适当的条件。

5. 发明授权

US07713950B2 Antibacterial 1-(4-mono-and di-halomethylsulphonylphenyl)-2-acylamino-3-fluoroproponals and preparation thereof 失效
标题翻译：抗菌1-（4-单 - 和二 - 卤代甲基磺酰基苯基）-2-酰基氨基-3-氟丙酮及其制备方法
公开(公告)号：US07713950B2
公开(公告)日：2010-05-11
申请号：US12038105
申请日：2008-02-27
申请人： Dale E. Shuster , Scott J. Hecker , Tomasz W. Glinka , Rajeshwar Singh , Zhuoyi Su
发明人： Dale E. Shuster , Scott J. Hecker , Tomasz W. Glinka , Rajeshwar Singh , Zhuoyi Su
IPC分类号： A61K31/165 , C07F9/09
CPC分类号： C07F9/094 , A61K31/165 , A61K31/661 , C07C317/32 , C07F9/091 , Y02A50/475
摘要： Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CHX1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.
摘要翻译：具有化学结构的新型氟苯尼考化合物：或其药学上可接受的盐或其溶剂合物或其前药，其中R 1为CHCl 2，CHClF，CHF 2，CHBrCl，CH 3，CH 2 N 3，CH 2 CN，CH（R 2）NH 2或CHX 1 X 2; 其中R2是H，CH3或CH2OH，X1和X2是独立选择的卤素; 和R 3是CH 2 Cl，CH 2 F，CHF 2，CHCl 2或CH 2 OH。该化合物可用于治疗和/或预防广泛范围的患者中的细菌感染，例如但不限于鸟类，鱼类，贝类和哺乳动物。

6. 发明授权

US07041670B2 Florfenicol-type antibiotics 有权
标题翻译：氟苯尼考型抗生素
公开(公告)号：US07041670B2
公开(公告)日：2006-05-09
申请号：US10410330
申请日：2003-04-08
申请人： Constantine G. Boojamra , Lee S. Chong , Scott J. Hecker , Tomasz W. Glinka , Dale E. Shuster
发明人： Constantine G. Boojamra , Lee S. Chong , Scott J. Hecker , Tomasz W. Glinka , Dale E. Shuster
IPC分类号： C07D237/06 , C07D239/24 , C07D253/065 , A61K31/44 , A61P31/04
CPC分类号： C07D213/40 , A61K31/50 , A61K31/506 , A61K31/53 , C07C233/18 , C07C233/31 , C07C233/47 , C07C255/60 , C07C311/46 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07D213/73 , C07D233/54 , C07D237/08 , C07D237/20 , C07D239/26 , C07D239/42 , C07D241/12 , C07D249/08 , C07D261/08 , C07D261/12 , C07D261/14 , C07D261/18 , C07D271/06 , C07D271/10 , C07D275/02 , C07D277/28 , C07D277/40 , C07D285/08 , C07D285/12 , C07D317/58 , C07D333/20 , Y02A50/475
摘要： The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.
摘要翻译：本发明涉及具有以下化学结构的新型氟苯尼考化合物：其中所述化合物可用于治疗和/或预防广泛范围的患者（例如但不限于鸟类，鱼类，贝类和哺乳动物）中的细菌感染。

7. 发明授权

US6030965A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US6030965A
公开(公告)日：2000-02-29
申请号：US940508
申请日：1997-09-30
申请人： In-Seop Cho , Scott J. Hecker , Tomasz W. Glinka , Ving J. Lee , Zhijia J. Zhang
发明人： In-Seop Cho , Scott J. Hecker , Tomasz W. Glinka , Ving J. Lee , Zhijia J. Zhang
IPC分类号： C07D501/00 , C07D501/59 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention includes novel compounds of formula where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, S0.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR1## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-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：本发明包括新的式A化合物，其中A，B，D和E选自碳，氮和硫，R99选自硫，SO，SO 2，NH，N-烷基，氧，C = C（顺式或反式）和C 3BOND C，R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐，包括对β-内酰胺抗生素具有抗性的生物体，作为抗菌剂是有用的。本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

8. 发明授权

US08906868B2 Aminoglycoside derivatives 有权
标题翻译：氨基糖苷衍生物
公开(公告)号：US08906868B2
公开(公告)日：2014-12-09
申请号：US13697302
申请日：2011-05-12
申请人： Tomasz W. Glinka , Olga Rodny
发明人： Tomasz W. Glinka , Olga Rodny
IPC分类号： A61K31/70 , C07H15/00 , C07H17/02 , C07H15/06 , C07H15/236
CPC分类号： C07H15/236
摘要： The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.
摘要翻译：本发明涉及抗微生物剂。一些实施方案包括化合物，组合物，制备方法和使用新的氨基糖苷类和氨基糖苷衍生物的治疗方法。

9. 发明授权

US08119667B2 Carbonates of fenicol antibiotics 失效
标题翻译：芬太尼抗生素碳酸盐
公开(公告)号：US08119667B2
公开(公告)日：2012-02-21
申请号：US11611997
申请日：2006-12-18
申请人： Tomasz W. Glinka , Dale Edward Shuster , Chander Shekher Celly , Robert D. Simmons , Jason Zhang
发明人： Tomasz W. Glinka , Dale Edward Shuster , Chander Shekher Celly , Robert D. Simmons , Jason Zhang
IPC分类号： A61K31/44 , A61K31/41 , A61K31/42 , A61K31/265 , C07D211/78 , C07D285/12 , C07D261/06 , C07C69/96
CPC分类号： C07C317/32 , A61K31/222 , A61K31/265 , A61K31/42 , A61K31/433 , A61K31/44 , A61K45/06 , C07B2200/07 , C07C233/18 , C07C2601/02 , C07C2601/14 , C07D213/40 , C07D213/84 , A61K2300/00
摘要： Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.
摘要翻译：提供了具有作为抗生素前药的有用性质的新型芬西醇化合物，以及制备和使用这些新化合物的方法。

10. 发明授权

US07572777B2 Florfenicol prodrug having improved water solubility 有权
标题翻译：氟苯尼考前药具有改善的水溶性
公开(公告)号：US07572777B2
公开(公告)日：2009-08-11
申请号：US11511810
申请日：2006-08-29
申请人： Scott J. Hecker , Sunil V. Pansare , Tomasz W. Glinka
发明人： Scott J. Hecker , Sunil V. Pansare , Tomasz W. Glinka
IPC分类号： A61K31/661
CPC分类号： C07F9/547 , C07F9/094
摘要： The present invention discloses methods of using phosphate esters of florfenicol (prodrugs) and florfenicol analogs having superior water solubility that are hydrolyzed to florfenicol or the respective florfenicol analog in vivo, upon administration to an animal.
摘要翻译：本发明公开了在施用于动物时使用氟苯尼考（前药）和具有优异水溶性的氟苯尼考类似物的磷酸酯的方法，其被水解成氟苯尼考或其体内相应的氟苯尼考类似物。

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