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1. 发明授权

US5567698A Pyridinium thiomethyl substituted chepholosporin derivatives 失效
标题翻译：吡啶硫代甲基取代的chepholosporin衍生物
公开(公告)号：US5567698A
公开(公告)日：1996-10-22
申请号：US454058
申请日：1995-05-30
申请人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
发明人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36 , A61K31/43 , C07D501/60
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译：由通式表示的新型头孢烯衍生物，其中酰基取代基是式IMA的组，其中Ar是亲脂性任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基为革兰氏阳性抗菌剂，特别可用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病（ MRSA）。

2. 发明授权

US5559108A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5559108A
公开(公告)日：1996-09-24
申请号：US445628
申请日：1995-05-22
申请人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco, Jr. , John A. Wichtowski , Joanne J. Bronson , Stanley V. D'Andrea , Thomas W. Hudyma
发明人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco, Jr. , John A. Wichtowski , Joanne J. Bronson , Stanley V. D'Andrea , Thomas W. Hudyma
IPC分类号： C07D501/40 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/44 , C07D501/46 , C07D501/38
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## where Ar is a substituted phenyl or optionally substituted naphthyl or benzthiazolyl group and A is a substituted-pyridinium group are gram-positive antibiotics, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
摘要翻译：由通式“IMAGE”表示的新型头孢烯衍生物，其中酰基取代基是式IMAMA的基团，其中Ar是取代的苯基或任选被取代的萘基或苯并噻唑基，A是取代的吡啶鎓基是革兰氏阳性抗生素，特别适用于治疗由耐甲氧西林金黄色葡萄球菌引起的疾病。

3. 发明授权

US5734047A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5734047A
公开(公告)日：1998-03-31
申请号：US761738
申请日：1996-12-05
申请人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco , John A. Wichtowski
发明人： Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco , John A. Wichtowski
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
摘要翻译：由通式 + TR 表示的新型头孢烯衍生物，其中Ar是任选取代的亲脂性苯基，萘基，苯并噻唑基或吡啶基; R 1表示式（VIII）的基团，其中R 8和R 9各自独立地为氢，C 1 -C 6烷基或（C 1 -C 6）烷氧基羰基，所述C 1 -C 6烷基任选被1-5个羟基或C 1 -C 6 烷氧基 m为0或1; A是任选被1-5个羟基取代的C 2 -C 10烷基; 且R 2和R 3各自独立地为氢或C 1 -C 6烷基。衍生物是革兰氏阳性抗菌剂，特别适用于治疗耐甲氧西林金黄色葡萄球菌引起的疾病。

4. 发明授权

US5668284A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5668284A
公开(公告)日：1997-09-16
申请号：US644751
申请日：1996-05-08
申请人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
发明人： Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36 , C07D211/84 , C07F9/58
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译：由通式表示的新型头孢烯衍生物，其中酰基取代基是式IMA的组，其中Ar是亲脂性任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基是革兰氏阳性抗菌剂，特别可用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病（ MRSA）。

5. 发明授权

US5668290A Substituted 4-thio pyridones 失效
标题翻译：取代的4-硫代吡啶酮
公开(公告)号：US5668290A
公开(公告)日：1997-09-16
申请号：US697384
申请日：1996-08-23
申请人： Joanne J. Bronson , Stanley V. D'Andrea , Shelley E. Hoeft , John D. Matiskella , Peter F. Misco, Jr. , Bing Yu Luh , Dane M. Springer , Yasutsugu Ueda , John A. Wichtowski
发明人： Joanne J. Bronson , Stanley V. D'Andrea , Shelley E. Hoeft , John D. Matiskella , Peter F. Misco, Jr. , Bing Yu Luh , Dane M. Springer , Yasutsugu Ueda , John A. Wichtowski
IPC分类号： C07D501/00 , C07D501/36 , C07D213/44
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).
摘要翻译：由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团：其中Ar是亲脂性任选取代的苯基，萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基，其中R9和R10各自独立地为氢或C1-C6烷基，所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断，并且R 2和R 3各自独立地为氢，烷基或氨基烷基为革兰氏阳性抗菌剂，特别可用于治疗由甲氧西林抗性引起的疾病金黄色葡萄球菌（以下也称为MRSA或耐甲氧西林金黄色葡萄球菌）。

6. 发明授权

US5620969A Cephalosporin derviatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5620969A
公开(公告)日：1997-04-15
申请号：US427778
申请日：1995-04-25
申请人： Joanne J. Bronson , Stanley V. D'Andrea , Shelley E. Hoeft , John D. Matiskella , Peter F. Misco, Jr. , Bing Y. Luh , Dane M. Springer , Yasutsugu Ueda , John A. Wichtowski
发明人： Joanne J. Bronson , Stanley V. D'Andrea , Shelley E. Hoeft , John D. Matiskella , Peter F. Misco, Jr. , Bing Y. Luh , Dane M. Springer , Yasutsugu Ueda , John A. Wichtowski
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).
摘要翻译：由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团：其中Ar是亲脂性任选取代的苯基，萘基或吡啶基; R1表示杂环氨基酸的残基或被羧基和式-NR9R10或基团取代的C2-C10烷基，其中R9和R10各自独立地为氢或C1-C6烷基，所述C 2 -C 10烷基任选被一个或多个氮原子或羰基中断，并且R 2和R 3各自独立地为氢，烷基或氨基烷基为革兰氏阳性抗菌剂，特别可用于治疗由甲氧西林抗性引起的疾病金黄色葡萄球菌（以下也称为MRSA或耐甲氧西林金黄色葡萄球菌）。

7. 发明授权

US5210081A Alkali metal 8,9-dehydroestrone sulfate esters 失效
标题翻译：碱金属8,9-脱氢雌酮硫酸酯
公开(公告)号：US5210081A
公开(公告)日：1993-05-11
申请号：US841694
申请日：1992-02-26
申请人： Panolil C. Raveendranath , John A. Wichtowski
发明人： Panolil C. Raveendranath , John A. Wichtowski
IPC分类号： A61K31/565 , A61P9/10 , A61P15/00 , C07J1/00 , C07J31/00
CPC分类号： C07J1/0059 , C07J31/006
摘要： This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.
摘要翻译：本发明提供了8,9-脱水雌酮的碱金属盐，其硫酸酯及其稳定的组合物，以及它们的生产方法。硫酸酯盐可用于雌激素替代疗法。

8. 发明授权

US06169082A Salts of 8,9-dehydroestrone sulfate ester 失效
标题翻译： 8,9-脱氢雌酮硫酸酯的盐
公开(公告)号：US06169082A
公开(公告)日：2001-01-02
申请号：US08019387
申请日：1993-02-18
申请人： Panolil C. Raveendranath , John A. Wichtowski
发明人： Panolil C. Raveendranath , John A. Wichtowski
IPC分类号： A61K3156
CPC分类号： C07J1/0059 , C07J31/006
摘要： This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.
摘要翻译：本发明提供了8,9-脱水雌酮的碱金属盐，其硫酸酯的盐及其稳定的组合物，以及它们在雌激素替代疗法和心血管保护中的生产和使用的方法。

9. 发明授权

US5288717A Alkali metal 8,9-dehydroestrone sulfate esters 失效
标题翻译：碱金属8,9-脱氢雌酮硫酸酯
公开(公告)号：US5288717A
公开(公告)日：1994-02-22
申请号：US984741
申请日：1992-12-03
申请人： Panolil C. Raveendranath , John A. Wichtowski
发明人： Panolil C. Raveendranath , John A. Wichtowski
IPC分类号： A61K31/565 , A61P9/10 , A61P15/00 , C07J1/00 , C07J31/00 , A61K31/56 , C07J53/00
CPC分类号： C07J1/0059 , C07J31/006
摘要： This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.
摘要翻译：本发明提供了8,9-脱水雌酮的碱金属盐，其硫酸酯及其稳定的组合物，以及它们的生产方法。硫酸酯盐可用于雌激素替代疗法。

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