公开(公告)号：US06310099B1

公开(公告)日：2001-10-30

申请号：US09722767

申请日：2000-11-27

申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer ,  Daqiang Xu

发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer ,  Daqiang Xu

IPC分类号： C07C22942

CPC分类号： C07C229/42

摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

摘要翻译： 公开了式I的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; R5是氯，氟，三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。

公开(公告)号：US06451858B2

公开(公告)日：2002-09-17

申请号：US09950957

申请日：2001-09-13

申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

IPC分类号： C07C22942

CPC分类号： C07C229/42

摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

摘要翻译： 公开了式I的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; R5是氯，氟，三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。

公开(公告)号：US06727281B2

公开(公告)日：2004-04-27

申请号：US10201336

申请日：2002-07-23

申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

IPC分类号： C07C22942

CPC分类号： C07C229/42

摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

摘要翻译： 公开了式I的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; R5是氯，氟，三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。

公开(公告)号：US06291523B1

公开(公告)日：2001-09-18

申请号：US09139254

申请日：1998-08-25

申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer ,  Daqiang Xu

发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer ,  Daqiang Xu

IPC分类号： A61K31216

CPC分类号： C07C229/42

摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

公开(公告)号：US07202364B2

公开(公告)日：2007-04-10

申请号：US10724457

申请日：2003-11-25

申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Lauren G. Monovich ,  Benjamin B. Mugrage ,  David T. Parker ,  John H. VanDuzer ,  Sompong Wattanasin

发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Lauren G. Monovich ,  Benjamin B. Mugrage ,  David T. Parker ,  John H. VanDuzer ,  Sompong Wattanasin

IPC分类号： C07D215/38 ,  C07D215/44 ,  C07C229/00

CPC分类号： C07D215/38 ,  C07C229/42 ,  C07D215/40 ,  C07D215/44 ,  C07D317/58 ,  C07D333/20 ,  C07D333/28

摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3–C6)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3–C6)cycloalkyl-monocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

摘要翻译： 式（I）化合物

公开(公告)号：US4977144A

公开(公告)日：1990-12-11

申请号：US405926

申请日：1989-09-12

申请人： Roger A. Fujimoto ,  John E. Francis ,  Alan J. Hutchison

发明人： Roger A. Fujimoto ,  John E. Francis ,  Alan J. Hutchison

IPC分类号： C07H19/052

CPC分类号： C07H19/052

摘要： Disclosed are the compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, or optionally lower alkyl substituted (C.sub.3 -C.sub.7 -cycloalkyl, bicycloheptyl, bicycloheptenyl, adamantyl, tetrahydropyranyl or tetrahydrothiopyranyl)-lower alkyl, or diaryl-lower alkyl; R.sub.2 represents hydrogen or lower alkyl; R.sub.3 represents hydroxymethyl or --CONHR.sub.4 in which R.sub.4 represents hydrogen, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which one or more of the hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods of preparation; pharmaceutical compositions; and their use as adenosine-2 agonists in mammals.

摘要翻译： 公开了式（I）的化合物，其中R表示氢，低级烷基，芳基或芳基 - 低级烷基; 碳原子或杂环芳基 - 低级烷基，C 3 -C 7 - 环烷基或任选的低级烷基取代的（C 3 -C 7 - 环烷基，双环庚基，双环庚烯基，金刚烷基， 四氢吡喃基或四氢噻喃基） - 低级烷基或二芳基 - 低级烷基; R2代表氢或低级烷基; R3表示羟甲基或-CONHR4，其中R4表示氢，低级烷基，芳基 - 低级烷基，C3-C7-环烷基，C3-C7-环烷基 - 低级烷基或羟基 - 低级烷基; 其药学上可接受的酯衍生物，其中一个或多个羟基以药学上可接受的酯的形式酯化; 及其药学上可接受的盐; 准备方法; 药物组合物; 以及它们在哺乳动物中作为腺苷-2激动剂的用途。

公开(公告)号：US06380259B2

公开(公告)日：2002-04-30

申请号：US09732453

申请日：2000-12-07

申请人： Paul J. Marshall ,  Roger A. Fujimoto

发明人： Paul J. Marshall ,  Roger A. Fujimoto

IPC分类号： A61K31165

CPC分类号： A61K31/166

摘要： Use in medicaments for the treatment of chronic obstructive pulmonary disease of compounds of formula wherein the C(═NH)—NHR3 group may be in tautomeric or isomeric form, or a pharmaceutically acceptable salt thereof, in which: R1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy or is hydroxy which is etherified by an aliphatic, araliphatic or aromatic alcohol or by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy or which is esterified by an aliphatic or araliphatic carboxylic acid; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently or one another, are oxygen (—O—) or sulphur (—S—); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical; wherein the phenyl rings of formula I may be, independently or one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical.