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1. 发明授权

US5773421A Antifungal fusacandins 失效
标题翻译：抗真菌菌素
公开(公告)号：US5773421A
公开(公告)日：1998-06-30
申请号：US548803
申请日：1995-12-21
申请人： Lisa A. Alder , Marianna Jackson , Neal S. Burres , James B. McAlpine , Jill E. Hochlowski , Larry L. Klein , Paul A. Lartey , Clinton Yeung
发明人： Lisa A. Alder , Marianna Jackson , Neal S. Burres , James B. McAlpine , Jill E. Hochlowski , Larry L. Klein , Paul A. Lartey , Clinton Yeung
IPC分类号： C12P17/06 , A01N43/16 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , A61P31/10 , C07H15/10 , C07H17/04 , C12R1/645 , A61K31/71 , C07H15/00 , C12P19/44
CPC分类号： C07H15/10 , A01N43/16
摘要： Novel antifungal agents having the formula: ##STR1## wherein R is hydrogen or --C(O)--R.sub.1 wherein R.sub.1 is alkenyl, C.sub.2 -C.sub.12 -alkyl, aryl, arylalkenyl, arylalkyl, aryl-aryl-, arylalkoxy-aryl-, aryloxyl-aryl-, aryl-aryl-aryl- or arylalkoxy-aryl-aryl-, or pharmaceutically acceptable salts, esters or prodrugs thereof, as well as (i) pharmaceutical compositions comprising such compounds, (ii) methods of treatment using such compounds, and (iv) methods and fungal cultures useful in making the same.
摘要翻译：具有下式的新型抗真菌剂：其中R是氢或-C（O）-R1，其中R 1是烯基，C 2 -C 12烷基，芳基，芳基烯基，芳基烷基，芳基 - 芳基 - ，芳基烷氧基芳基 - 芳基 - 芳基 - 芳基 - 芳基 - 芳基 - 或芳基烷氧基 - 芳基 - 芳基 - 或其药学上可接受的盐，酯或前药，以及（i）包含这些化合物的药物组合物，（ii）使用这种化合物的治疗，以及（iv）可用于制备该化合物的方法和真菌培养物。

2. 发明授权

US5654411A Process for preparing 4-deoxyerythromycin derivatives 失效
标题翻译： 4-脱氧红霉素衍生物的制备方法
公开(公告)号：US5654411A
公开(公告)日：1997-08-05
申请号：US435900
申请日：1995-05-04
申请人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
发明人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/08 , A61P1/10 , A61P31/04 , C07D233/22 , C07H17/08 , C07H1/00
CPC分类号： C07H17/08
摘要： 4"-Deoxy derivatives of erythromycin having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.
摘要翻译： 4'' - 具有式（I）的红霉素的脱氧衍生物及其药学上可接受的盐，其是胃动力的增强剂，但是具有最小的抗菌活性，以及含有它们的药物组合物以及它们的方法使用和准备。

3. 发明授权

US5834438A 4"-deoxyerythromycin derivatives 失效
公开(公告)号：US5834438A
公开(公告)日：1998-11-10
申请号：US435903
申请日：1995-05-04
申请人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
发明人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/08 , A61P1/10 , A61P31/04 , C07D233/22 , C07H17/08
CPC分类号： C07H17/08
摘要： 4"-Deoxy derivatives of erythromycin having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.

4. 发明授权

US5075289A 9-R-azacyclic erythromycin antibiotics 失效
标题翻译： 9-R-抗坏血酸抗菌药物
公开(公告)号：US5075289A
公开(公告)日：1991-12-24
申请号：US203400
申请日：1988-06-07
申请人： Richard J. Pariza , Paul A. Lartey , Clarence J. Maring , Larry L. Klein
发明人： Richard J. Pariza , Paul A. Lartey , Clarence J. Maring , Larry L. Klein
IPC分类号： A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61P31/00 , A61P31/04 , C07H17/08 , C07H19/04
CPC分类号： C07H17/08
摘要： Semisynthetic antibiotics with improved therapeutic properties are disclosed. In particular, 9-R-azacyclic derivatives of erythromycin, its derivatives, and their salts and esters show superior antimicrobial activity compared to other macrolide compounds.

5. 发明授权

US5578579A 4"-deoxyerythromycin derivatives 失效
标题翻译： 4“ - 脱氧红霉素衍生物
公开(公告)号：US5578579A
公开(公告)日：1996-11-26
申请号：US284730
申请日：1994-08-02
申请人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
发明人： Paul A. Lartey , Larry L. Klein , Ramin Faghih , Hugh N. Nellans
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/08 , A61P1/10 , A61P31/04 , C07D233/22 , C07H17/08
CPC分类号： C07H17/08
摘要： 4"-Deoxy derivatives of erythromycin having the Formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are enhancers of gastric motility but have minimal antibacterial activity, as well as pharmaceutical compositions containing the same and methods for their use and preparation.
摘要翻译： 4'' - 具有式（I）的红霉素的脱氧衍生物及其药学上可接受的盐，其是胃动力的增强剂，但是具有最小的抗菌活性，以及含有它们的药物组合物以及它们的方法使用和准备。

6. 发明授权

US5789591A Process for preparing 1-substituted 8-chloro-7-fluoro-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid ethyl ester compounds 失效
标题翻译：制备1-取代的8-氯-7-氟-9-甲基-4-氧代-4H-喹嗪-3-羧酸乙酯化合物的方法
公开(公告)号：US5789591A
公开(公告)日：1998-08-04
申请号：US735625
申请日：1996-10-23
申请人： Daniel T. Chu , David Allen Degoey , David J. Grampovnik , Larry Lewis Klein , Paul A. Lartey , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung
发明人： Daniel T. Chu , David Allen Degoey , David J. Grampovnik , Larry Lewis Klein , Paul A. Lartey , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung
IPC分类号： C07D455/02
CPC分类号： C07D455/02
摘要： A process for preparing a compound having the formula: ##STR1## wherein R is selected from the group consisting of C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylmethyl, C.sub.1 -C.sub.6 -alkyl, allyl and 2-methoxyethyl, by reacting: ##STR2## under defined conditions with subsequent stepwise reactions of the respective intermediate compounds with a malonic acid diester, POCl.sub.3, and by heating the final intermediate in a high boiling solvent.
摘要翻译：制备具有下式的化合物的方法：其中R选自C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基甲基，C 1 -C 6 - 烷基，烯丙基和2-甲氧基乙基，通过以下反应：在定义的条件下，将各种中间体化合物与丙二酸二酯POCl 3的后续逐步反应，并通过在高沸点溶剂中加热最终的中间体，在图像> 下进行。

7. 发明授权

US5696084A Amino-lipopetide antifungal agents 失效
标题翻译：氨基脂肽抗真菌剂
公开(公告)号：US5696084A
公开(公告)日：1997-12-09
申请号：US698610
申请日：1996-08-16
申请人： Paul A. Lartey , Leping Li , Larry Lewis Klein , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung , David Allen Degoey , David J. Grampovnik
发明人： Paul A. Lartey , Leping Li , Larry Lewis Klein , Christina Louise Leone , Sheela Albert Thomas , Ming Clinton Yeung , David Allen Degoey , David J. Grampovnik
IPC分类号： A61K38/00 , C07K7/56 , A61K38/12 , C07K5/00
CPC分类号： C07K7/56 , A61K38/00
摘要： Disclosed are novel antifungal agents having the formula: ##STR1## or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R.sub.1 is selected from the group consisting of --NH.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R.sub.3 is selected from the group consisting of --CH.sub.2 (p-C.sub.6 H.sub.4).sub.3 O(CH.sub.2).sub.3 CH.sub.3, --CH.sub.2 (p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --COO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(Piperazinyl)(p-C.sub.6 H.sub.4).sub.2 OCH.sub.3, --CO(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.4 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)O(CH.sub.2).sub.6 CH.sub.3, --CO(p-C.sub.6 H.sub.4)(Piperazinyl)(p-C.sub.6 H.sub.4)OCH.sub.3, and --CO(p-C.sub.6 H.sub.4)(Piperazinyl)O(CH.sub.2).sub.6 CH.sub.3 ; and R.sub.4 is selected from the group consisting of --CH(OH)CH.sub.3, --CH.sub.2 OH, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2)NH.sub.2, --CH.sub.2 NH.sub.2, --CH.sub.2 (CH.sub.2).sub.2 (NH)C.dbd.(NH)--NH.sub.2, --CH.sub.3, --CH.sub.2 (Ph)OH, hydrogen, --CH.sub.2 CH.sub.2 COOH, and --CH.sub.2 COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.
摘要翻译：公开了具有下式的新型抗真菌剂：其中优选的化合物包括那些其中R 1选自-NH 2;或其药学上可接受的酸，酯或前药。 R2选自氢，氟和羟基; R 3选自-CH 2（对-C 6 H 4）3 O（CH 2）3 CH 3，-CH 2（对-C 6 H 4）O（CH 2）6 CH 3，-COO（对-C 6 H 4）O（CH 2）6 CH 3，-CO（哌嗪基）（对-C 6 H 4）2 OCH 3，-CO（p-C 6 H 4）O（CH 2）6 CH 3，-CO（p-C 6 H 4）（哌嗪基）（对-C 6 H 4）O（CH 2）4 CH 3，-CO（p-C 6 H 4）（哌嗪基）（p-C6H4）O（CH2）6CH3，-CO（对-C6H4）（哌嗪基）（对-C 6 H 4）OCH 3和-CO（对-C 6 H 4）（哌嗪基）O（CH 2）并且R 4选自-CH（OH）CH 3，-CH 2 OH，-CH 2 CH 3，-CH 2 CH 2 CH 2 NH 2，-CH 2（CH 2）NH 2，-CH 2 NH 2，-CH 2（CH 2）2（NH）C =（NH） NH 2，-CH 3，-CH 2（Ph）OH，氢，-CH 2 CH 2 COOH和-CH 2 COOH。还公开了含有这些化合物的药物组合物及其在治疗真菌感染中的用途。

8. 发明授权

US5217960A Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：US5217960A
公开(公告)日：1993-06-08
申请号：US695176
申请日：1991-05-03
申请人： Paul A. Lartey , Ramin Faghih , Shari DeNinno
发明人： Paul A. Lartey , Ramin Faghih , Shari DeNinno
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： A61K31/70 , C07H17/08
摘要： Antibacterial compounds are disclosed having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is --NR.sup.4 R.sup.6, where R.sup.4 and R.sup.6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R.sup.4 and R.sup.6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R.sup.2 is selected from the group consisting of hydrogen, --OH and, when R.sup.3 is methylene, oxygen so as to form an epoxide; and R.sup.3 is selected from the group consisting of --CH.sub.2 OH, --NR.sup.4 R.sup.6, --(CH.sub.2).sub.n NR.sup.4 R.sup.6 and, when R.sup.2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R.sup.4 and R.sup.6 are as previously defined, with the proviso that when R.sup.2 is --OH, R.sup.3 may not be --NR.sup.4 R.sup.6 ; or R.sup.2 and R.sup.3 together are.dbd.CH.sub.2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.
摘要翻译：公开了具有下式的抗菌化合物及其药学上可接受的盐，其中R 1是-NR 4 R 6，其中R 4和R 6独立地选自氢，低级烷基和芳基烷基，或者R 4和R 6一起形成氮 - 在氮原子附着的杂环; R2选自氢，-OH，当R3为亚甲基时，为氧，形成环氧化物; 并且R 3选自-CH 2 OH，-NR 4 R 6， - （CH 2）n NR 4 R 6，并且当R 2为氧时，亚甲基以形成环氧化物，其中n为1-4，并且R 4和R 6如前所定义，条件是当R 2是-OH时，R 3可以不是-NR 4 R 6; 或R 2和R 3一起为= CH 2。还公开了可用于制备上述化合物的方法和中间体，以及含有其的组合物及其使用方法。

9. 发明授权

US4613589A D-manno-2-octulosonic acid derivatives, pharmaceutical compositions and method of use 失效
标题翻译： D-壬烯-2-辛酮酸衍生物，药物组合物和使用方法
公开(公告)号：US4613589A
公开(公告)日：1986-09-23
申请号：US767212
申请日：1985-08-19
申请人： William Rosenbrook , Paul A. Lartey , David A. Riley
发明人： William Rosenbrook , Paul A. Lartey , David A. Riley
IPC分类号： C07D309/10 , C07H7/033 , C07H15/04 , C07H15/14 , A61K31/70 , C07H3/08
CPC分类号： C07H15/14 , C07D309/10 , C07H15/04 , C07H7/033
摘要： Derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.
摘要翻译： 3-脱氧-D-manno-2-octulosonic acid（KDO）的衍生物是细菌酶和新型抗菌剂的有效抑制剂。

10. 发明授权

US4613590A Amino D-manno-2-octulopyranosidonate containing compounds, pharmaceutical compositions and method of use 失效
标题翻译：含氨基D-manno-2-octulopyranosidonate的化合物，药物组合物和使用方法
公开(公告)号：US4613590A
公开(公告)日：1986-09-23
申请号：US767297
申请日：1985-08-19
申请人： William Rosenbrook , Paul A. Lartey , David A. Riley
发明人： William Rosenbrook , Paul A. Lartey , David A. Riley
IPC分类号： C07D309/10 , C07H7/033 , C07H15/04 , A61K31/70 , C07H5/06
CPC分类号： C07H15/04 , C07D309/10 , C07H7/033
摘要： Aminodeoxy derivatives of 3-deoxy-D-manno-2-octulosonic acid (KDO) are potent inhibitors of bacterial enzymes and a novel class of antibacterial agents.
摘要翻译： 3-脱氧-D-manno-2-octulosonic acid（KDO）的氨基脱氧衍生物是细菌酶和新型抗菌剂的有效抑制剂。

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