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公开(公告)号:US5306722A
公开(公告)日:1994-04-26
申请号:US939232
申请日:1992-09-02
申请人: Choung U. Kim , Bing Y. Luh , Peter F. Misco
发明人: Choung U. Kim , Bing Y. Luh , Peter F. Misco
IPC分类号: A61K31/505 , A61P31/12 , C07D405/04 , C07H19/06 , C07D403/04
CPC分类号: C07H19/06
摘要: Thymidine kinase inhibitor of formula I ##STR1## in which R is C.sub.1-6 alkyl or AR(CH.sub.2).sub.n --, wherein Ar represents phenyl optionally substituted with one to five same or different halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; and n equals one to six.A further aspect of the present invention provides a method of inhibiting viral thymidine kinase. Yet another aspect of the invention relates to treating herpes simplex viral infections in mammals. Yet another aspect of the invention provides a pharmaceutical formulation.
摘要翻译: 式I的胸苷激酶抑制剂(*化学结构*)I其中R是C 1-6烷基或AR(CH 2)n - ,其中Ar表示任选被1至5个相同或不同的卤素,C 1-6烷基或C 1 -C 6烷基取代的苯基, 6烷氧基; n等于1到6。 本发明的另一方面提供了抑制病毒胸苷激酶的方法。 本发明的另一方面涉及治疗哺乳动物中的单纯疱疹病毒感染。 本发明的另一方面提供一种药物制剂。
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公开(公告)号:US5208221A
公开(公告)日:1993-05-04
申请号:US619856
申请日:1990-11-29
申请人: Choung U. Kim , John C. Martin , Bing Y. Luh , Peter F. Misco
发明人: Choung U. Kim , John C. Martin , Bing Y. Luh , Peter F. Misco
IPC分类号: A61K31/675 , A61P31/12 , A61P31/18 , C07F9/40 , C07F9/6512 , C07F9/6561
CPC分类号: C07F9/65616 , C07F9/4006 , C07F9/65121
摘要: The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.
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3.
公开(公告)号:US5386030A
公开(公告)日:1995-01-31
申请号:US16401
申请日:1993-02-11
申请人: Choung U. Kim , John C. Martin , Bing Y. Luh , Peter F. Misco
发明人: Choung U. Kim , John C. Martin , Bing Y. Luh , Peter F. Misco
IPC分类号: A61K31/675 , A61P31/12 , A61P31/18 , C07F9/40 , C07F9/6512 , C07F9/6561 , C07F9/02
CPC分类号: C07F9/65616 , C07F9/4006 , C07F9/65121
摘要: The present invention concerns nucleotide analogs and their compositions and use. In particular it relates to novel (phosphonomethoxy) methoxy purine/pyrimidine derivatives.
摘要翻译: 本发明涉及核苷酸类似物及其组合物和用途。 特别涉及新型(膦酰基甲氧基)甲氧基嘌呤/嘧啶衍生物。
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4.
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)。 -
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.
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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。 -
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.
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公开(公告)号:US5734047A
公开(公告)日:1998-03-31
申请号:US761738
申请日:1996-12-05
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。 -
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)。 -
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。
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