公开(公告)号：US20070142635A1

公开(公告)日：2007-06-21

申请号：US10582414

申请日：2004-12-08

申请人： David Askin ,  David Conlon ,  Yoshinori Kohmura ,  Jaemoon Lee ,  Brenda Pipik ,  Yong-Li Zhong

发明人： David Askin ,  David Conlon ,  Yoshinori Kohmura ,  Jaemoon Lee ,  Brenda Pipik ,  Yong-Li Zhong

IPC分类号： C07F9/6512 ,  C07D487/04

CPC分类号： C07F9/6561 ,  C07C251/60 ,  C07C255/26 ,  C07C259/14 ,  C07D239/557 ,  C07D487/04

摘要： Processes for preparing 10-amino-3-hydroxy-4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepine-2-carboxylates and related compounds are disclosed. The preparation of carboxamide derivatives from these carboxylates is also disclosed. The carboxamides are HIV integrase inhibitors and are useful for treating HIV infection and AIDS.

摘要翻译： 公开了制备10-氨基-3-羟基-4-氧代-4,6,7,8,9,10-六氢嘧啶并[1,2-a]吖庚因-2-羧酸酯和相关化合物的方法。 还公开了从这些羧酸盐制备羧酰胺衍生物。 甲酰胺是HIV整合酶抑制剂，可用于治疗艾滋病毒感染和艾滋病。

公开(公告)号：US20050192346A1

公开(公告)日：2005-09-01

申请号：US11066676

申请日：2005-02-25

申请人： Yao-Jun Shi ,  F. Conrad Engelhardt ,  Cameron John Cowden ,  David Conlon ,  Brenda Pipik

发明人： Yao-Jun Shi ,  F. Conrad Engelhardt ,  Cameron John Cowden ,  David Conlon ,  Brenda Pipik

IPC分类号： C07C315/02 ,  C07C315/04 ,  C07C317/46 ,  C07C319/20 ,  C07C323/62 ,  C07C317/24 ,  A61K31/21

CPC分类号： C07C315/04 ,  C07C315/02 ,  C07C319/20 ,  C07C323/62 ,  C07C317/46

摘要： The invention encompasses a novel process for making compounds of Formula I which are prodrugs of cyclooxygenase-2 selective inhibitors that convert in vivo to diaryl-2-(5H)-furanones and also liberate nitric oxide in vivo. As such, the compounds made by the present invention may be co-dosed with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions, effectively reduce the risk of thrombotic cardiovascular events and potentially renal side effects and at the same time reduce the risk of GI ulceration or bleeding. The present invention describes an efficient and economical process for the preparation of 2,3-disubstituted (2Z)-4-acetoxybut-2-enoate derivatives that is useful for the production of kilogram quantities of material for preclinical and clinical use.

摘要翻译： 本发明包括制备式I化合物的新方法，其为在体内将其转化为二芳基-2-（5H） - 呋喃酮并在体内释放一氧化氮的环氧合酶-2选择性抑制剂的前药。 因此，本发明制备的化合物可以与低剂量阿司匹林共同治疗以治疗慢性环氧合酶-2介导的疾病或病症，有效降低血栓性心血管事件和潜在的肾脏副作用的风险，同时减少 GI溃疡或出血的风险。 本发明描述了用于制备2,3-二取代（2Z）-4-乙酰氧基丁-2-烯酸酯衍生物的有效和经济的方法，其用于生产用于临床和临床应用的千克量的材料。

公开(公告)号：US20070054941A1

公开(公告)日：2007-03-08

申请号：US10526782

申请日：2003-09-12

申请人： Mirlinda Biba ,  Paul Collins ,  Christopher Welch ,  David Conlon ,  Antoinette Drahus

发明人： Mirlinda Biba ,  Paul Collins ,  Christopher Welch ,  David Conlon ,  Antoinette Drahus

IPC分类号： A61K31/4439

CPC分类号： C07D413/10

摘要： A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity.

摘要翻译： 制备取代的8-芳基喹啉的纯化方法，其中8位的芳基含有取代的取代的 - 烯基，采用聚苯乙烯基磺酰肼反应性树脂除去醛杂质。

公开(公告)号：US06740666B2

公开(公告)日：2004-05-25

申请号：US10040993

申请日：2001-11-09

申请人： Dwight Macdonald ,  Helene Perrier ,  Roch Thibert ,  Guo-Jie Ho ,  Anant Vailaya ,  David Conlon ,  Elizabeth Kwong ,  Sophie-Dorothee Clas

发明人： Dwight Macdonald ,  Helene Perrier ,  Roch Thibert ,  Guo-Jie Ho ,  Anant Vailaya ,  David Conlon ,  Elizabeth Kwong ,  Sophie-Dorothee Clas

IPC分类号： A61K3147

CPC分类号： C07D401/10 ,  C07D215/12 ,  C07D215/14 ,  C07D413/10 ,  C07D417/10

摘要： Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

摘要翻译： 其中8位的芳基含有取代的取代的链烯基的取代的8-芳基喹啉的新型硫酸，甲磺酸，对甲苯磺酸，2-萘磺酸，盐酸或苯磺酸盐是PDE4抑制剂 。

公开(公告)号：US5116204A

公开(公告)日：1992-05-26

申请号：US577364

申请日：1990-09-04

申请人： Peter A. Power ,  Adrian P. Power ,  Julian M. Power ,  David Conlon

发明人： Peter A. Power ,  Adrian P. Power ,  Julian M. Power ,  David Conlon

IPC分类号： G09F11/02 ,  G09F13/04

CPC分类号： G09F15/0037 ,  G09F11/02 ,  G09F13/04 ,  G09F2013/045

摘要： A display device comprises an elongate member which is formed of two identical moldings and rotatably mounted on two nylon bearings, each of which is secured to a post. One molding is oriented in a first direction and a second molding is oriented in a second opposite direction and the two moldings are engageable in the longitudinal direction. A male rim section of one molding engages in a female rim section of the second molding. Each side of the female rim section has a plurality of supporting lugs which support the male rim section of the other molding when engaged.