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1. 发明授权

US07361648B2 Heterocyclylakylamines as muscarinic receptor antagonists 失效
标题翻译：杂环辛胺作为毒蕈碱受体拮抗剂
公开(公告)号：US07361648B2
公开(公告)日：2008-04-22
申请号：US11508581
申请日：2006-08-22
申请人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号： A61K31/395 , A61K31/553 , A61K31/55
CPC分类号： C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
摘要翻译：本发明涉及通常为毒蕈碱性M2 / M3受体拮抗剂并由式I表示的化合物：其中X，Y和Z为O，S或NR 5，其它取代基为在规范中定义; 和前药，各异构体，异构体的外消旋或非外消旋混合物及其药学上可接受的盐或溶剂合物。本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法。

2. 发明授权

US06667301B2 Heterocyclylalkylamines as muscarinic receptor antagonists 有权
标题翻译：杂环烷基胺作为毒蕈碱受体拮抗剂
公开(公告)号：US06667301B2
公开(公告)日：2003-12-23
申请号：US09862286
申请日：2001-05-22
申请人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07D24108
CPC分类号： C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
摘要翻译：本发明涉及通常为毒蕈碱性M2 / M3受体拮抗剂并由式I表示的化合物：其中X，Y和Z为O，S或NR 5，其它取代基如说明书中所定义; 和前药，各异构体，异构体的外消旋或非外消旋混合物及其药学上可接受的盐或溶剂合物。本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法。

3. 发明授权

US07094778B2 Heterocyclylalkylamines as muscarinic receptor antagonists 有权
公开(公告)号：US07094778B2
公开(公告)日：2006-08-22
申请号：US10685124
申请日：2003-10-14
申请人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
发明人： Charles Alois Dvorak , Lawrence Emerson Fisher , Keena Lynn Green , Ralph New Harris, III , Hans Maag , Anthony Prince , David Bruce Repke , Russell Stephen Stabler
IPC分类号： A61K31/513 , C07D279/06 , C07D413/12 , C07D239/10 , C07D241/08
CPC分类号： C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

4. 发明申请

US20060287293A1 Heterocyclylalkylamines as muscarinic receptor antagonists 失效
标题翻译：杂环烷基胺作为毒蕈碱受体拮抗剂
公开(公告)号：US20060287293A1
公开(公告)日：2006-12-21
申请号：US11508581
申请日：2006-08-22
申请人： Charles Dvorak , Lawrence Fisher , Keena Green , Ralph Harris , Hans Maag , Anthony Prince , David Repke , Russell Stabler
发明人： Charles Dvorak , Lawrence Fisher , Keena Green , Ralph Harris , Hans Maag , Anthony Prince , David Repke , Russell Stabler
IPC分类号： A61K31/553 , A61K31/551 , A61K31/55
CPC分类号： C07D207/27 , A61K31/55 , A61K31/551 , A61K31/553 , C07D211/76 , C07D223/10 , C07D225/02 , C07D239/10 , C07D241/08 , C07D243/04 , C07D243/08 , C07D265/10 , C07D267/06 , C07D267/10 , C07D267/22 , C07D279/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
摘要翻译：本发明涉及通常为毒蕈碱性M2 / M3受体拮抗剂并由式I表示的化合物：其中X，Y和Z为O，S或NR 5，其它取代基为在规范中定义; 和前药，各异构体，异构体的外消旋或非外消旋混合物及其药学上可接受的盐或溶剂合物。本发明还涉及含有这些化合物的药物组合物及其用作治疗剂的方法。

5. 发明授权

US4051148A 6,11-Dihydrodibenzo-[b.e.]-thiepin-11-one-3-carboxaldehyde 失效
标题翻译： 6,11-二氢二苯并[b，b] {9-硫杂-11-酮-3-甲醛
公开(公告)号：US4051148A
公开(公告)日：1977-09-27
申请号：US697648
申请日：1976-06-18
申请人： Anthony Prince , Otto Halpern , Jack Ackrell
发明人： Anthony Prince , Otto Halpern , Jack Ackrell
IPC分类号： C07C205/57 , C07D337/12
CPC分类号： C07D337/12 , C07C205/57 , C07C323/00
摘要： This invention relates to a novel method for the preparation of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid and the novel intermediate 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-carboxaldehyde used in the preparation thereof.
摘要翻译：本发明涉及一种制备6,11-二氢二苯并[b]硫杂-11-酮-3-乙酸的新方法和新的中间体6,11-二氢二苯并[a]硫杂-11-酮 -3-甲醛用于制备它。

6. 发明申请

US20050130915A1 Polymorphic antiviral nucleoside compounds 失效
标题翻译：多态抗病毒核苷化合物
公开(公告)号：US20050130915A1
公开(公告)日：2005-06-16
申请号：US10939648
申请日：2004-09-13
申请人： Kondamraj Birudaraj , Anthony Prince , Keith McCarthy
发明人： Kondamraj Birudaraj , Anthony Prince , Keith McCarthy
IPC分类号： A61K31/7056 , A61K38/21 , C07H19/056
CPC分类号： C07H19/056 , Y10S514/885
摘要： The present invention relates to the polymorphic crystalline hydrochloride salts of a nucleoside valinate ester according to formula Ib, methods of treating diseases mediated by Hepatitis C Virus and pharmaceutical composition containing Ib.
摘要翻译：本发明涉及根据式Ib的核苷缬氨酸酯的多晶型结晶盐酸盐，治疗由丙型肝炎病毒介导的疾病的方法和含有Ib的药物组合物。

7. 发明申请

US20050080252A1 Process for preparing antiviral nucleoside derivatives 审中-公开
标题翻译：制备抗病毒核苷衍生物的方法
公开(公告)号：US20050080252A1
公开(公告)日：2005-04-14
申请号：US10939819
申请日：2004-09-13
申请人： Andrew Briggs , Charles Dvorak , Anthony Prince , Keith McCarthy
发明人： Andrew Briggs , Charles Dvorak , Anthony Prince , Keith McCarthy
IPC分类号： C07H19/056
CPC分类号： C07H19/056
摘要： Process and novel intermediates for preparing 2-aminocarboxylic acid esters of the 5-hydroxymethyl group of levovirin (1-(3S,4R-dihydroxy-5S-hydroxymethyl-tetrahydro-furan-2S-yl)-1H-[1,2,4]triazole-3-carboxylic acid amide; Id: R1═R2═R3═H) and acid addition salts thereof. The present process provides the monoesters selectively in high purity with increased efficiency with reduced number of production steps. The process involves condensation of a cyclopentylidene levovirin compound with a N-urethane-N-carboxylic anhydride and subsequent deprotection to directly provide the hydrochloride salt of the product. The mono esters are useful for treatment of viral diseases and are absorbed more efficiently than the parent compound.
摘要翻译：用于制备左旋病毒5-羟甲基的2-氨基羧酸酯的方法和新型中间体（1-（3S，4R-二羟基-5S-羟甲基 - 四氢 - 呋喃-2S-基）-1H- [1,2,4 ]三唑-3-羧酸酰胺; Id：R 1 = R 2 = R 3 = H）及其酸加成盐。本方法提供了选择性高纯度的单酯，其生产步骤减少，效率提高。该方法包括将亚环戊基纤溶蛋白化合物与N-氨基甲酸酯-N-羧酸酐缩合并随后脱保护直接提供产物的盐酸盐。单酯可用于治疗病毒性疾病，并且比母体化合物更有效地吸收。

8. 发明授权

US06864244B2 Anhydrous crystalline 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine hemisulfate as useful as an antiviral agent 失效
标题翻译：含水结晶4-氨基-1 - （（2r，3r，4s，5r）-5-叠氮基-3,4-二羟基-5-羟甲基 - 四氢 - 呋喃-2-基）-1H-嘧啶-2-酮
公开(公告)号：US06864244B2
公开(公告)日：2005-03-08
申请号：US10731582
申请日：2003-12-09
申请人： Terrence Joseph Connolly , Joseph Armstrong Martin , Anthony Prince , Keshab Sarma
发明人： Terrence Joseph Connolly , Joseph Armstrong Martin , Anthony Prince , Keshab Sarma
IPC分类号： A61K31/70 , A61K31/7052 , A61K31/7068 , A61K31/7072 , A61P31/12 , C07H19/06 , C07H19/067
CPC分类号： C07H19/06 , Y10S514/894 , Y10S514/934
摘要： The present invention relates to the hemisulfate salt of 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine (Ia) with improved stability and physical properties which facilitate manufacturing, handling and formulating I and polymorphic crystalline forms thereof.
摘要翻译：本发明涉及4-氨基-1 - （（2r，3r，4s，5r）-5-叠氮基-3,4-二羟基-5-羟甲基 - 四氢 - 呋喃-2-基）-1h的半硫酸盐盐 - 嘧啶-2-酮，其具有改进的稳定性和物理性质，其有利于制备，处理和配制I和多晶型晶型。

9. 发明授权

US5274108A Process for preparing 1,3-dioxolane derivatives 失效
公开(公告)号：US5274108A
公开(公告)日：1993-12-28
申请号：US993789
申请日：1992-12-21
申请人： Norman H. Dyson , John O. Gardner , Anthony Prince , Denis J. Kertesz
发明人： Norman H. Dyson , John O. Gardner , Anthony Prince , Denis J. Kertesz
IPC分类号： C07D521/00 , C07D405/00 , C07D405/14
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.

10. 发明授权

US5208331A Process for preparing 1,3-dioxolane derivatives 失效
标题翻译： 1,3-二氧戊环衍生物的制备方法
公开(公告)号：US5208331A
公开(公告)日：1993-05-04
申请号：US900568
申请日：1992-06-18
申请人： Norman H. Dyson , John O. Gardner , Anthony Prince , Denis J. Kertesz
发明人： Norman H. Dyson , John O. Gardner , Anthony Prince , Denis J. Kertesz
IPC分类号： C07D233/60 , C07D405/06 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.
摘要翻译：本发明提供了制备式（I）化合物的改进方法：其中：n为0,1或2; 每个R 1独立地为卤素或低级烷基; R2是硝基或-N（R3）R4，其中R3是氢或低级烷基; R4是氢，低级烷基，低级烷基磺酰基或-C（Y）R5，其中Y是氧或硫，R5是氢，低级烷基，低级烷氧基或-N（R6）R7，其中R6是氢或低级烷基，R7是氢，低级烷基或低级烷氧基羰基; 或R 3和R 4与N一起为吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代或哌嗪子基，其中哌嗪基在4-位被-C（O）R 8任选取代，其中R 8是氢，低级烷基，低级烷氧基或氨基; 或其药学上可接受的盐。这些化合物可用于治疗以高胆固醇血症为特征的疾病状态。

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