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1. 发明授权

US5599816A Quinolizinone type compounds 失效
标题翻译：喹诺酮类化合物
公开(公告)号：US5599816A
公开(公告)日：1997-02-04
申请号：US482249
申请日：1995-06-07
申请人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner , Zhenkun Ma , Wei-Bo Wang
发明人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner , Zhenkun Ma , Wei-Bo Wang
IPC分类号： A61K38/00 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/16 , C07D519/00 , C07K5/06 , A61K31/495 , A61K31/44 , A61K31/505 , A61K31/535 , C07D471/02 , C07D487/00 , C07D498/02
CPC分类号： C07D471/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07K5/06026 , A61K38/00
摘要： Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds whereinA is.dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要翻译：具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其选择的优选实例包括其中A = CR 6 - 的那些化合物; R1是3至8个碳原子的环烷基或取代的苯基; R2选自 R3是卤素; R4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R5为氢，低级烷基，卤代（低级烷基）或-NR13R14; 并且R6是卤素，低级烷基，卤代（低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基或氨基（低级烷基），以及含有这些化合物的药物组合物及其用于治疗细菌感染。

2. 发明授权

US5726182A Quinolizinone type compounds 失效
标题翻译：喹诺酮类化合物
公开(公告)号：US5726182A
公开(公告)日：1998-03-10
申请号：US484632
申请日：1995-06-07
申请人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner , Zhenkun Ma , Wei-Bo Wang
发明人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner , Zhenkun Ma , Wei-Bo Wang
IPC分类号： A61K38/00 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/16 , C07D519/00 , C07K5/06 , C07D491/00 , A61K31/44 , C07D498/00
CPC分类号： C07D471/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07K5/06026 , A61K38/00
摘要： Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is .dbd.CR.sup.6 --; R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; and R.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要翻译：具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其选择的优选实例包括其中A = CR 6 - 的那些化合物; R1是3至8个碳原子的环烷基或取代的苯基; R2选自 R3是卤素; R4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R5是氢，低级烷基，卤代（低级烷基）或-NR13R14; 并且R6是卤素，低级烷基，卤代（低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基或氨基（低级烷基），以及含有这些化合物的药物组合物及其用于治疗细菌感染。

3. 发明授权

US5668164A Process for synthesis of chiral cis-and trans-3-amino-4 substituted pyrrolidine compounds 失效
标题翻译：合成手性顺式和反式-3-氨基-4-取代的吡咯烷化合物的方法
公开(公告)号：US5668164A
公开(公告)日：1997-09-16
申请号：US764418
申请日：1996-12-12
申请人： Zhenkun Ma , Curt S. Cooper , Anthony K. L. Fung , Daniel T. Chu
发明人： Zhenkun Ma , Curt S. Cooper , Anthony K. L. Fung , Daniel T. Chu
IPC分类号： C07D207/14 , C07D413/06
CPC分类号： C07D207/14
摘要： Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas: ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas: ##STR2## with the assistance of a streochemically directing chiral oxazolidinone moiety having the formula: ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated add chloride, reaction with N-benzyl-N-(methoxymethyl)trimethyl-silylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.
摘要翻译：具有下式的手性顺式-3,4-取代的吡咯烷化合物的方法：具有下式的具有下式的具有下式的手性3,4-反式取代的吡咯烷化合物：在具有磺酰化引导的手性恶唑烷酮部分的帮助下，通过化合物或其后的中间体与α，β-不饱和氯化物的顺序反应，与N-苄基-N-（甲氧基甲基）三甲基甲硅烷基甲基胺和通过色谱法分离异构体，恶唑烷酮部分的水解去除，与二苯基磷酰基叠氮化物和三乙胺的反应和脱苄基化; 和这个过程的新中间体。

4. 发明授权

US5618949A Process for synthesis of chiral cis- and trans-3-amino-4-substituted pyrrolidine compounds 失效
标题翻译：合成手性顺式和反式-3-氨基-4-取代的吡咯烷化合物的方法
公开(公告)号：US5618949A
公开(公告)日：1997-04-08
申请号：US679043
申请日：1996-07-12
申请人： Zhenkun Ma , Curt S. Cooper , Anthony K. L. Fung , Daniel T. Chu
发明人： Zhenkun Ma , Curt S. Cooper , Anthony K. L. Fung , Daniel T. Chu
IPC分类号： C07D207/14 , C07D207/09
CPC分类号： C07D207/14
摘要： Process for preparation of chiral cis-3,4-substituted pyrrolidine compounds having the formulas ##STR1## and chiral 3,4-trans-substituted pyrrolidine compounds having the formulas ##STR2## with the assistance of a stereochemically directing chiral oxazolidinone moiety having the formula ##STR3## wherein P, R and R.sup.1 are specifically defined, by sequential reaction of the compound or subsequent intermediates with an a,b-unsaturated acid chloride, reaction with N-benzyl-N-(methoxymethyl)trimethylsilylmethylamine and separating isomers by chromatography, hydrolytic removal of the oxazolidinone moiety, reaction with diphenylphosphoryl azide and triethylamine, and debenzylating; and novel intermediates of the process.
摘要翻译：具有式“IMAGE”的手性顺式-3,4-取代的吡咯烷化合物和具有式“IMAGE”的手性3,4-反式取代的吡咯烷化合物的方法在具有式（I）的立体化学引发的手性恶唑烷酮部分其中P，R和R1通过化合物或其后的中间体与a，b-不饱和酰氯的顺序反应而具体定义，与N-苄基-N-（甲氧基甲基）三甲基甲硅烷基甲胺反应，并通过色谱法分离异构体，水解除恶唑烷酮部分，与二苯基磷酰基叠氮化物和三乙胺反应，脱苄; 和新的中间体的过程。

5. 发明授权

US5580872A Quinolizinone type compounds 失效
标题翻译：喹诺酮类化合物
公开(公告)号：US5580872A
公开(公告)日：1996-12-03
申请号：US316319
申请日：1994-09-30
申请人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner
发明人： Daniel T. Chu , Qun Li , Curt S. Cooper , Anthony K. L. Fung , Cheuk M. Lee , Jacob J. Plattner
IPC分类号： A61K38/00 , C07D213/61 , C07D213/68 , C07D455/02 , C07D471/04 , C07D491/16 , C07D519/00 , C07K5/06 , A61K31/495 , A61K31/505 , C07D401/00 , C07D239/72
CPC分类号： C07D471/04 , C07D213/61 , C07D213/68 , C07D455/02 , C07K5/06026 , A61K38/00
摘要： Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds whereinA is .dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要翻译：具有式（I）的抗菌化合物及其药学上可接受的盐，酯和酰胺，其优选实例包括其中A = CR 6 - 的那些化合物; R1是3至8个碳原子的环烷基或取代的苯基; R2选自 R3是卤素; R4是氢，低级烷基，药学上可接受的阳离子或前药酯基; R5是氢，低级烷基，卤代（低级烷基）或-NR13R14; 并且R6是卤素，低级烷基，卤代（低级烷基），羟基取代的低级烷基，低级烷氧基（低级烷基），低级烷氧基或氨基（低级烷基），以及含有这些化合物的药物组合物及其用于治疗细菌感染。

6. 发明授权

US4762845A 7-(3-Substituted imino-1-pyrrolidinyl)-quinolone-3-carboxylic acids 失效
标题翻译： 7-（3-取代的亚氨基-1-吡咯烷基） - 喹诺酮-3-羧酸
公开(公告)号：US4762845A
公开(公告)日：1988-08-09
申请号：US866194
申请日：1986-05-21
申请人： Daniel T. Chu , Andre G. Pernet , Curt S. Cooper
发明人： Daniel T. Chu , Andre G. Pernet , Curt S. Cooper
IPC分类号： C07D215/56 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/47
CPC分类号： C07D401/04 , C07D215/56 , C07D401/14 , C07D405/14 , C07D409/14
摘要： New 7-substituted 6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids or esters having a substituted or unsubstituted phenyl radical, an aromatic heterocyclic radical, an alkyl or cycloalkyl radical in the 1-position are antibacterial agents.
摘要翻译：在1-位具有取代或未取代的苯基，芳族杂环基，烷基或环烷基的新的7-取代的6-氟-1,4-二氢-4-氧代喹啉-3-羧酸或酯是抗菌剂。

7. 发明授权

US5137892A Quinoline, naphthyridine and pyridobenzoxazine derivatives 失效
标题翻译：喹啉，萘啶和吡唑并噻嗪衍生物
公开(公告)号：US5137892A
公开(公告)日：1992-08-11
申请号：US626602
申请日：1990-12-12
申请人： Daniel T. Chu , Curt S. Cooper
发明人： Daniel T. Chu , Curt S. Cooper
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/535 , A61P31/04 , C07D401/04 , C07D471/04 , C07D491/06 , C07D491/10 , C07D491/113 , C07D519/00
CPC分类号： C07D401/04 , C07D471/04 , C07D491/10
摘要： Novel antibacterial compounds are disclosed having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof,wherein R.sup.1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl;R.sup.2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group;R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl;R.sup.5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; andA is N or C--R.sup.6, wherein R.sup.6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R.sup.1 and R.sup.6 taken together with the atoms to which they are attached form a 6-membered ring which may contain an oxygen or sulfur atom and which may be substituted with lower alkyl; as well as pharmaceutical compositions comprising such novel compounds and the thereapeutic use thereof.
摘要翻译：公开了具有式（I）的新型抗菌化合物及其药学上可接受的盐，酯，酰胺和前药，其中R 1选自（a）低级烷基，（b）卤代（低级烷基），（c）低级烷基（炔基），（d）低级环烷基，（e）低级烷基氨基，（f）含氮芳族杂环，（g）双环烷基和（h） R2选自氢，低级烷基，药学上可接受的阳离子和前药酯基; R 3和R 4独立地选自氢，卤素，氨基和低级烷基; R5是含氮杂环或含氮螺环双环杂环; 并且A是N或C-R6，其中R6选自氢，卤素，低级烷基和低级烷氧基，或者R1和R6与它们所连接的原子一起形成6元环，其中可以含有氧原子或硫原子，并可以被低级烷基取代; 以及包含这些新化合物的药物组合物及其治疗用途。

8. 发明授权

US4880814A 7-cycloalkyl naphthyridines 失效
标题翻译： 7-环烷基萘啶
公开(公告)号：US4880814A
公开(公告)日：1989-11-14
申请号：US119885
申请日：1987-11-13
申请人： Daniel T. Chu , Terry J. Rosen , Curt S. Cooper
发明人： Daniel T. Chu , Terry J. Rosen , Curt S. Cooper
IPC分类号： C07D215/56 , C07D471/04 , C07D498/06
CPC分类号： C07D215/56 , C07D471/04
摘要： The present invention includes compounds represented by the formula: ##STR1## wherein R.sub.1 is a hydroxy, a C.sub.1 to C.sub.6 alkoxy, benzoxy, or an alkylcarbonyloxymethoxy group, or R.sub.3 together with R.sub.1 forms a group of the formula --Y--NH-- where Y is oxygen or sulfur; or R.sub.3 is hydrogen; A is nitrogen or CR.sub.2, where R.sub.2 is hydrogen, or halogen, or R.sub.2 together with R forms a group of the formula --X--CH.sub.2 --CH(R.sub.6)-- or --X--CH.sub.2 --CH.dbd.CH.sub.2, wherein X is CH.sub.2, O, S, NH, or NCH.sub.3, and R.sub.6 is hydrogen, alkyl, or C.sub.1 -C.sub.3 haloalkyl; or R is (1) a C.sub.1 to C.sub.4 alkyl, (2) lower cycloalkyl, (3) alkylamino, (4) haloalkyl, (5) an aromatic heterocyclic ring or (6) a substituted phenyl group; and Z is a carbocyclic group;or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as antibacterial agents. 1
摘要翻译：本发明包括由下式表示的化合物：其中R1是羟基，C1至C6烷氧基，苯氧基或烷基羰氧基甲氧基，或R3与R1一起形成式-Y-NH-的基团，其中Y 是氧或硫; 或R3是氢; A是氮或CR 2，其中R 2是氢或卤素，或R 2与R一起形成式-X-CH 2 -CH（R 6） - 或-X-CH 2 -CH = CH 2的基团，其中X是CH 2， O，S，NH或NCH 3，R 6是氢，烷基或C 1 -C 3卤代烷基; 或R是（1）C1-C4烷基，（2）低级环烷基，（3）烷基氨基，（4）卤代烷基，（5）芳族杂环或（6）取代苯基; Z是碳环基; 或其药学上可接受的盐。本发明的化合物可用作抗菌剂。 1

9. 发明授权

US07910595B2 Anti-viral compounds 有权
标题翻译：抗病毒化合物
公开(公告)号：US07910595B2
公开(公告)日：2011-03-22
申请号：US11613810
申请日：2006-12-20
申请人： David A. Betebenner , David A. DeGoey , Clarence J. Maring , Allan C. Krueger , Nobuhiko Iwasaki , Todd W. Rockway , Curt S. Cooper , David D. Anderson , Pamela L. Donner , Brian E. Green , Dale J. Kempf , Dachun Liu , Keith F. McDaniel , Darold L. Madigan , Christopher E. Motter , John K. Pratt , Jason P. Shanley , Michael D. Tufano , Rolf Wagner , Rong Zhang , Akhteruzzaman Molla , Hongmei Mo , Tami J. Pilot-Matias , Sherie V L. Masse , Robert J. Carrick , Wenping He , Liangjun Lu , David J. Grampovnik
发明人： David A. Betebenner , David A. DeGoey , Clarence J. Maring , Allan C. Krueger , Nobuhiko Iwasaki , Todd W. Rockway , Curt S. Cooper , David D. Anderson , Pamela L. Donner , Brian E. Green , Dale J. Kempf , Dachun Liu , Keith F. McDaniel , Darold L. Madigan , Christopher E. Motter , John K. Pratt , Jason P. Shanley , Michael D. Tufano , Rolf Wagner , Rong Zhang , Akhteruzzaman Molla , Hongmei Mo , Tami J. Pilot-Matias , Sherie V L. Masse , Robert J. Carrick , Wenping He , Liangjun Lu , David J. Grampovnik
IPC分类号： C07D471/04 , A01N31/519 , A61P31/12
CPC分类号： C07D471/04 , C07D495/04 , C07D513/04
摘要： Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
摘要翻译：公开了有效抑制丙型肝炎病毒（“HCV”）或其他病毒复制的化合物。本发明还涉及包含这些化合物的组合物，这些化合物与其它抗病毒剂或治疗剂的共同配制或共同给药，用于合成这些化合物的方法和中间体，以及使用这些化合物治疗 HCV或其他病毒感染。

10. 发明授权

US08497275B2 HCV protease inhibitors and uses thereof 有权
标题翻译： HCV蛋白酶抑制剂及其用途
公开(公告)号：US08497275B2
公开(公告)日：2013-07-30
申请号：US12492518
申请日：2009-06-26
申请人： Brian E. Green , David D. Anderson , Todd D. Bosse , Curt S. Cooper , Larry L. Klein , Allan C. Krueger , Daniel P. Larson , Dachun Liu , Keith F. McDaniel , Christopher E. Motter , John K. Pratt , Todd W. Rockway , Teresa A. Rosenberg , Ming C. Yeung , Hui-Ju Chen , Jason P. Shanley
发明人： Brian E. Green , David D. Anderson , Todd D. Bosse , Curt S. Cooper , Larry L. Klein , Allan C. Krueger , Daniel P. Larson , Dachun Liu , Keith F. McDaniel , Christopher E. Motter , John K. Pratt , Todd W. Rockway , Teresa A. Rosenberg , Ming C. Yeung , Hui-Ju Chen , Jason P. Shanley
IPC分类号： A61K31/4965 , A61K31/40 , A61K38/00 , A61K38/05
CPC分类号： C07D403/12 , C07D207/16 , C07D241/24 , C07D403/14 , C07D409/14 , C07K7/02
摘要： This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.
摘要翻译：本发明涉及：（a）式I化合物及其盐，其特别可用作丙型肝炎病毒（HCV）抑制剂; （b）可用于制备这些化合物和盐的中间体; （c）包含这些化合物和盐的药物组合物; 和（d）使用这些化合物，盐和组合物的方法。

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