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1. 发明授权

US07223870B2 Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction 失效
标题翻译：通过铜催化交叉偶联反应制备N-芳基化恶唑烷酮的方法
公开(公告)号：US07223870B2
公开(公告)日：2007-05-29
申请号：US10645779
申请日：2003-08-21
申请人： Arun Ghosh , Stephane Caron , Janice E. Sieser
发明人： Arun Ghosh , Stephane Caron , Janice E. Sieser
IPC分类号： C07D263/04
CPC分类号： C07D291/04 , C07D207/12 , C07D263/22
摘要： Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.
摘要翻译：公开了通过铜催化的交叉偶联反应制备N-芳基化恶唑烷酮化合物的方法。

2. 发明授权

US07045652B2 Processes for preparing substituted aryl boronic acids 失效
标题翻译：制备取代芳基硼酸的方法
公开(公告)号：US07045652B2
公开(公告)日：2006-05-16
申请号：US10453433
申请日：2003-06-03
申请人： Stephane Caron , Jolanta Nowakowski
发明人： Stephane Caron , Jolanta Nowakowski
IPC分类号： C07F5/02
CPC分类号： C07C213/08 , C07C217/20 , C07F5/025
摘要： The invention relates to processes for preparing a compound of the formula (V) and alkyl boronic esters thereof wherein R1 is attached at the 2 or 3 position of the benzene ring, R2 is attached at the 5 or 6 position, and R1, R2 and G are as defined herein. Said compound is a key synthetic intermediate in the preparation of 2-amino-6-(substituted-4-phenoxy)-substituted-pyridines useful as nitric oxide synthase (NOS) inhibitors in a mammal.
摘要翻译：本发明涉及制备式（Ⅴ）化合物及其烷基硼酸酯的方法，其中R 1连接在苯环的2或3位，R 2， SUP>连接在5或6位，R 1，R 2和G如本文所定义。所述化合物是制备用作哺乳动物中一氧化氮合酶（NOS）抑制剂的2-氨基-6-（取代-4-苯氧基） - 取代 - 吡啶的关键合成中间体。

3. 发明授权

US6096906A Processes for preparing substituted chromanol derivatives 失效
标题翻译：取代的色原烷醇衍生物的制备方法
公开(公告)号：US6096906A
公开(公告)日：2000-08-01
申请号：US367235
申请日：1999-03-05
申请人： Anthony Piscopio , Joel M. Hawkins , Stephane Caron , Sarah E. Kelly , Jeffrey W. Raggon , Michael J. Castaldi , Robert W. Dugger , Sally G. Ruggeri
发明人： Anthony Piscopio , Joel M. Hawkins , Stephane Caron , Sarah E. Kelly , Jeffrey W. Raggon , Michael J. Castaldi , Robert W. Dugger , Sally G. Ruggeri
IPC分类号： B01J23/44 , B01J31/24 , C07C33/50 , C07D311/22 , C07F5/02 , C07F5/04 , C07D311/24
CPC分类号： C07C33/50 , C07D311/22 , C07F5/025
摘要： The invention relates to processes for preparing a compound of the formula (X) and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R.sup.1, R.sup.2 and R.sup.3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula (X). ##STR1##
摘要翻译： PCT No.PCT / IB97 / 01024 Sec。 371日期1999年3月5日 102（e）1999年3月5日PCT 1997年8月25日PCT公布。公开号WO98 / 11085 日期：1998年3月19日本发明涉及制备式（X）化合物和所述化合物的对映异构体的方法，其中苯甲酸部分连接于苯并二氢吡喃环的6或7位，R1，R2和R3 如本文所定义。本发明还涉及可用于制备式（X）化合物的中间体。

4. 发明授权

US07479559B2 Benzyl(idene)-lactam derivatives 失效
标题翻译：苄基（idene） - 内酰胺衍生物
公开(公告)号：US07479559B2
公开(公告)日：2009-01-20
申请号：US11083188
申请日：2005-03-17
申请人： Michael Aaron Brodney , Stephane Caron , Christopher John Helal , Jeffrey W. Raggon , Yong Tao , Nga M. Do
发明人： Michael Aaron Brodney , Stephane Caron , Christopher John Helal , Jeffrey W. Raggon , Yong Tao , Nga M. Do
IPC分类号： C07D295/155 , C07D401/04 , C07D403/04 , C07D405/10 , C07D413/10 , C07D403/10
CPC分类号： C07D207/26 , C07D211/76 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
摘要翻译：本发明涉及新颖的苄基（内标）内酰胺衍生物，式Ⅰ化合物，其中R1是下述式G1或G2的基团，其中R1，R3，R6，R13X，a，n和m分别为其药学上可接受的盐和药物组合物，其包括5-羟色胺1（5-HT1）受体的选择性拮抗剂，反向激动剂和部分激动剂，特别是5-HT1A和5-HT1B受体中的一种或两种。本发明的化合物可用于治疗或预防抑郁，焦虑，强迫症（OCD）以及其中指示5-HT1激动剂或拮抗剂并且降低心脏副作用的潜在性，特别是QTc延长的其它病症。

5. 发明授权

US06444826B1 Processes and intermediates for preparing substituted chromanol derivatives 失效
标题翻译：制备取代苯并二氢吡喃衍生物的方法和中间体
公开(公告)号：US06444826B1
公开(公告)日：2002-09-03
申请号：US09999240
申请日：2001-10-31
申请人： Anthony Piscopio , Joel M. Hawkins , Stephane Caron , Sarah E. Kelly , Jeffrey W. Raggon , Michael J. Castaldi , Robert W. Dugger , Sally G. Ruggeri
发明人： Anthony Piscopio , Joel M. Hawkins , Stephane Caron , Sarah E. Kelly , Jeffrey W. Raggon , Michael J. Castaldi , Robert W. Dugger , Sally G. Ruggeri
IPC分类号： C07D26326
CPC分类号： C07C33/50 , C07D311/22 , C07F5/025
摘要： The invention relates to processes for preparing a compound of the formula and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.
摘要翻译：本发明涉及制备式的化合物和所述化合物的对映异构体的方法，其中苯甲酸部分连接于苯并二氢吡喃环的6或7位，R 1，R 2和R 3如本文所定义。本发明还涉及可用于制备上述式X化合物的中间体。

6. 发明授权

US06316632B1 Process for preparing 2-phenyl-3-aminopyridine, substituted phenyl derivatives, thereof, and salts thereof 失效
标题翻译：制备2-苯基-3-氨基吡啶，取代的苯基衍生物及其盐的方法
公开(公告)号：US06316632B1
公开(公告)日：2001-11-13
申请号：US09569010
申请日：2000-05-11
申请人： Tamim F. Braish , Stephane Caron , Michael James Castaldi
发明人： Tamim F. Braish , Stephane Caron , Michael James Castaldi
IPC分类号： C07D21172
CPC分类号： C07D213/73 , C07D213/75 , Y02P20/55
摘要： A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof.
摘要翻译：制备2-苯基-3-氨基吡啶的方法和取代的苯基衍生物及其盐。

7. 外观设计

USD500811S1 Signboard 失效
标题翻译：招牌
公开(公告)号：USD500811S1
公开(公告)日：2005-01-11
申请号：US29186689
申请日：2003-07-21
申请人： Stephan Ouelet , Stephane Caron
设计人： Stephan Ouelet , Stephane Caron

8. 发明申请

US20070049759A1 Methods for Preparing N-Arylated Oxazolidinones Via A Copper Catalyzed Cross Coupling 审中-公开
标题翻译：通过铜催化交联法制备N-甲酰化恶唑烷酮的方法
公开(公告)号：US20070049759A1
公开(公告)日：2007-03-01
申请号：US11461203
申请日：2006-07-31
申请人： Arun Ghosh , Stephane Caron , Janice Sieser
发明人： Arun Ghosh , Stephane Caron , Janice Sieser
IPC分类号： C07D263/00
CPC分类号： C07D291/04 , C07D207/12 , C07D263/22
摘要： Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.
摘要翻译：公开了通过铜催化的交叉偶联反应制备N-芳基化恶唑烷酮化合物的方法。

9. 发明申请

US20050245521A1 Novel benayl(idene)-lactam derivatives 失效
标题翻译：新颖贝那（idene） - 内酰胺衍生物
公开(公告)号：US20050245521A1
公开(公告)日：2005-11-03
申请号：US11083188
申请日：2005-03-17
申请人： Michael Brodney , Stephane Caron , Christopher Helal , Jeffrey Raggon , Yong Tao , Nga Do
发明人： Michael Brodney , Stephane Caron , Christopher Helal , Jeffrey Raggon , Yong Tao , Nga Do
IPC分类号： A61K31/496 , A61K31/5377 , C07D207/26 , C07D211/76 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D43/14
CPC分类号： C07D207/26 , C07D211/76 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
摘要翻译：本发明涉及新的苄基（idene） - 内酰胺衍生物，式I化合物，其中R 1是式G 1或G 2的基团其中R 1，R 3，R 6，R 13，X，A，，n和m如本文所定义，其药学上可接受的盐和药物组合物，其包括5-羟色胺1（5-HT 1 H 2）受体的选择性拮抗剂，反向激动剂和部分激动剂，特别是一种或多种 5-HT 1A 1A和5-HT 1B 1受体均为两者。本发明的化合物可用于治疗或预防抑郁，焦虑，强迫症（OCD）和其中指示5-HT 1激动剂或拮抗剂并且具有降低心脏侧潜力的其它病症效果，特别是QTc延长。

10. 发明授权

US06608070B1 2,3-substituted indole compounds as anti-inflammatory and analgesic agents 失效
标题翻译： 2,3-取代的吲哚化合物作为抗炎和止痛剂
公开(公告)号：US06608070B1
公开(公告)日：2003-08-19
申请号：US09355494
申请日：1999-07-28
申请人： Kazunari Nakao , Rodney William Stevens , Kiyoshi Kawamura , Chikara Uchida , Hiroki Koike , Stephane Caron
发明人： Kazunari Nakao , Rodney William Stevens , Kiyoshi Kawamura , Chikara Uchida , Hiroki Koike , Stephane Caron
IPC分类号： A01N4390
CPC分类号： C07D401/06 , C07D209/18 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D417/06 , C07D417/10
摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
摘要翻译：本发明提供下式的化合物或其药学上可接受的盐，其中Z是OH，C 1-6烷氧基，-NR 2 R 3或杂环; Q选自以下：（a）任选取代的苯基，（b）含有一个，两个，三个或四个氮原子的任选取代的6元单环芳族基团，（c）任选取代的5元含有一个选自O，S和N的杂原子，并且除了所述杂原子之外任选含有一个，两个或三个氮原子的单环芳基，（d）任选取代的C 3-7环烷基和（e）任选取代的苯并杂环杂环 R1是氢，C1-4烷基或卤素; R2和R3独立地是氢，OH，C1-4烷氧基，C1-4烷基或被卤素，OH，C1-4烷氧基或CN取代的C1-4烷基; X独立地选自H，卤素，C 1-4烷基，卤素取代的C 1-4烷基，OH，C 1-4烷氧基，卤素取代的C 1-4烷氧基，C 1-4烷硫基，NO 2，NH 2，二（C 1 -4烷基）氨基和CN; 并且n为0,1,2,3和4.本发明还提供了可用于治疗前列腺素作为病原体的医疗状况的药物组合物。

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