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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

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）。

4. 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）。

5. 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）。

6. 发明授权

US4665170A Carbapenem antibiotics 失效
公开(公告)号：US4665170A
公开(公告)日：1987-05-12
申请号：US822576
申请日：1986-01-27
申请人： Choung U. Kim , Peter F. Misco, Jr.
发明人： Choung U. Kim , Peter F. Misco, Jr.
IPC分类号： C07D295/088 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D295/088 , C07D477/20
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

7. 发明授权

US4640799A Carbapenem antibiotics 失效
标题翻译：卡巴布本抗生素
公开(公告)号：US4640799A
公开(公告)日：1987-02-03
申请号：US762735
申请日：1985-08-05
申请人： Choung U. Kim , Peter F. Misco, Jr.
发明人： Choung U. Kim , Peter F. Misco, Jr.
IPC分类号： C07D295/088 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D295/088 , C07D477/20
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.
摘要翻译：公开了新的碳青霉烯衍生物，其特征在于具有式“IMAGE”的2-取代基，其中A表示任选被一个或多个C 1 -C 4烷基取代的亚环戊基，亚环己基或C 2 -C 6亚烷基; R 5表示（a）任选取代的脂族，脂环族，脂环族 - 脂族，芳基，芳脂族，杂芳基，杂脂肪族基，杂环基或杂环基 - 脂族基团或（b）二价亚苯基或C1-C4亚烷基，环以形成桥连多环基团; 并且表示季铵化的含氮非芳族杂环。这些衍生物可用作有效的抗菌剂。

8. 发明授权

US4552696A Carbapenem antibiotics 失效
公开(公告)号：US4552696A
公开(公告)日：1985-11-12
申请号：US471379
申请日：1983-03-08
申请人： Choung U. Kim , Peter F. Misco, Jr.
发明人： Choung U. Kim , Peter F. Misco, Jr.
IPC分类号： A61K31/40 , C07D213/20 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/00 , C07D477/20 , C07D487/04
CPC分类号： C07D213/20 , C07C321/00 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/20
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.

9. 发明授权

US4642341A Carbapenem antibiotics 失效
公开(公告)号：US4642341A
公开(公告)日：1987-02-10
申请号：US766624
申请日：1985-08-19
申请人： Choung U. Kim , Peter F. Misco, Jr.
发明人： Choung U. Kim , Peter F. Misco, Jr.
IPC分类号： C07D213/20 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/00 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D213/20 , C07C321/00 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/20
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.

10. 发明授权

US4710568A Carbapenem antibiotics 失效
标题翻译：卡巴布本抗生素
公开(公告)号：US4710568A
公开(公告)日：1987-12-01
申请号：US925026
申请日：1986-10-30
申请人： Choung Un. Kim , Peter F. Misco, Jr.
发明人： Choung Un. Kim , Peter F. Misco, Jr.
IPC分类号： C07D213/20 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/00 , C07D477/20 , C07D487/04 , A61K31/40
CPC分类号： C07D213/20 , C07C321/00 , C07D213/30 , C07D213/65 , C07D213/70 , C07D213/73 , C07D233/84 , C07D477/20
摘要： Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups and ##STR2## represents a quaternized nitrogen-containing aromatic heterocycle. Such derivatives are useful as potent antibacterial agents. Also disclosed are processes for the preparation of such derivatives and novel intermediates utilized in these processes.
摘要翻译：公开了新的碳青霉烯衍生物，其特征在于式“IMAGE”的2-取代基，其中A代表亚环戊基，亚环己基或任选被一个或多个C 1 -C 4烷基取代的C 2 -C 6亚烷基，并且“IMAGE”代表季铵化的含氮芳香杂环。这些衍生物可用作有效的抗菌剂。还公开了制备这些衍生物的方法和在这些方法中使用的新型中间体。

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