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1. 发明公开

EP0485171A3 Esters and amides of substituted phenyl and pyridyl amino carboxylates 失效
标题翻译：取代苯基和吡啶基氨基甲酸酯的酯和氨基
公开(公告)号：EP0485171A3
公开(公告)日：1993-01-27
申请号：EP91310224.0
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/08 , C08F8/00 , C08G73/04
CPC分类号： C08B37/003 , A61K47/58 , A61K47/61 , C08F8/30
摘要： Esters and amides of substituted phenyl and pyridyl amino carboxylates having the formula

where Y is CH or N ;
R 1 is one or more substituents independently chosen from lower alkyl, lower haloalkyl, halo, alkoxy or benzyloxy ; Q is the deprotonated residue of a polymeric or macromolecular structure having a molecular weight of at least 1000 containing at least primary and/or secondary amino groups and/or hydroxy groups ; and n is an integer of at least 2 are useful in the treatment of colonic polyps.

2. 发明公开

EP0485173A3 Esters and amides of substituted fused ring phenyl acetic acids 失效
标题翻译：替代熔融环苯乙酸的酯和氨基酸
公开(公告)号：EP0485173A3
公开(公告)日：1993-01-27
申请号：EP91310226.5
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/08 , C08F8/00 , C08G73/04
CPC分类号： C08G73/0206 , A61K47/58 , A61K47/59 , A61K47/61 , A61K47/645 , C08B37/003 , C08F8/14 , C08F8/30
摘要： Esters and amides of substituted fused ring phenyl acetic acids having the formula

wherein Y, together with the ring to which it is fused forms a multi-ring system selected from napthyl, [1]benzopyranol [2, 3-b], pyridine, phenothiazine, carbazole, and benzoxazole ;
R 1 is lower alkyl or hydrogen ; R 2 is one or more independently selected from cyano, nitro, amino, alkylamino, hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, phenyl or phenyl substituted with halogen, alkyl or alkoxy ; wherein Q is the deprotonated residue of a polymer or macromolecular structure having a molecular weight of at least 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups ; and n is an integer of at least 2 are useful in treating colonic polyps.

3. 发明公开

EP0485157A2 Esters and amides of substituted pyrrole acetic acids 失效
标题翻译： Pyrrol-Essigsäureesternund Amiden。
公开(公告)号：EP0485157A2
公开(公告)日：1992-05-13
申请号：EP91310204.2
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/08 , C08F8/00 , C07K13/00 , A61K37/02
CPC分类号： C08F8/30 , A61K47/58 , C08B11/14 , C08B37/003
摘要： Esters and amides of substituted pyrrole acetic acids of the formula :
wherein n is 0 or 1, and X represents a condensed phenyl ring ;

one of R 1 and R 2 is independently selected from hydrogen, halogen, lower alkyl ; and the other of R 1 and R 2 is independently selected from substituted or unsubstituted phenyl, benzyl, thienyl, napthyl, pyridyl, furyl, biphenyl, benzoyl, cinnamoyl, thienylcarbonyl, napthylcarbonyl, pyridylcarbonyl, furylcarbonyl or biphenylcarbonyl wherein said substituents are selected from amino, halogen, lower alkyl, lower alkylthio, lower alkoxy or lower haloalkyl ;
m is an integer from 1 to 3 ;
R 3 is selected from hydrogen and lower alkyl, or one or more of hydrogen and lower alkyl when m is greater than 1 ;
R 4 is one or more of hydrogen, lower alkyl, alkoxy, haloalkyl, alkylthio, and halogen ;
p is an integer of at least 2 ;
Q is the deprotonated residue of a polymer or macromolecular structure having at least two primary and/or secondary amines and/or hydroxy groups ; and
when n is 0, R 5 is selected from hydrogen, halogen, lower alkyl, alkoxy, alkylthio, and halogen are useful in the treatment of colonic polyps.
摘要翻译：下式的取代吡咯乙酸的酯和酰胺：其中n为0或1，X为稠合苯环; R 1和R 2之一独立地选自氢，卤素，低级烷基; R 1和R 2中的另一个独立地选自取代或未取代的苯基，苄基，噻吩基，萘基，吡啶基，呋喃基，联苯基，苯甲酰基，肉桂酰基，噻吩基羰基，萘基羰基，吡啶基羰基，呋喃基羰基或联苯基羰基，其中所述取代基选自氨基，，低级烷基，低级烷硫基，低级烷氧基或低级卤代烷基; m为1〜3的整数; 当m大于1时，R 3选自氢和低级烷基，或者一个或多个氢和低级烷基; R4是氢，低级烷基，烷氧基，卤代烷基，烷硫基和卤素中的一个或多个; p为至少2的整数; Q是具有至少两个伯和/或仲胺和/或羟基的聚合物或大分子结构的去质子化残基; 当n为0时，R5选自氢，卤素，低级烷基，烷氧基，烷硫基和卤素，可用于治疗结肠息肉。

4. 发明公开

EP0508586A1 Substituted indenyl compounds 失效
标题翻译：取代茚基。
公开(公告)号：EP0508586A1
公开(公告)日：1992-10-14
申请号：EP92301821.2
申请日：1992-03-03
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Brendel, Klaus
IPC分类号： A61K31/10 , A61K31/16 , A61K31/19
CPC分类号： A61K31/198 , A61K31/16 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , B07C1/00
摘要： Substituted indenyl sulfonyl acetic acids are seful in the treatment of precancerous lesions.

5. 发明公开

EP0485172A2 Esters and amides of substituted indenyl acetic acids 失效
标题翻译：酯和酰胺取代基茚基 - Essigsäuren。
公开(公告)号：EP0485172A2
公开(公告)日：1992-05-13
申请号：EP91310225.7
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： C08B11/00 , C08F8/00 , C08B37/08 , C08G69/48 , A61K31/735 , A61K31/765
CPC分类号： C08B37/003 , C08B11/14 , C08F8/14 , C08F8/30 , C08F8/34 , C08G69/10
摘要： Esters and amides of substituted indenyl acetic acids of the formula :

n is an integer of at least 2 ;

Q is a deprotonated residue of polymer or macromolecular structure having a molecular weight of at least about 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups ;
R 1 is selected from hydrogen, lower alkyl, or haloalkyl ;
R 2 is selected from hydrogen or alkyl ;
R 3 and R 4 are one or more members each independently chosen from hydrogen, alkyl, acyloxy, alkoxy, nitro, amino, acylamino, alkylamino, diakylamino, dialkylaminoalkyl, sulfamyl, alkythio, mercapto, hydroxy, hydroxyalkyl, alkylsulfonyl, halogen, cyano, carboxyl, carbalkoxy, carbamido, haloalkyl or cycloalkoxy ; and
R 5 is selected from alkylsulfenyl, alkylsulfinyl or alkylsulfonyl. are useful in the treatment of colonic polyps.
摘要翻译：下式的取代茚基乙酸的酯和酰胺为： n为至少2的整数; Q是分子量至少约为1000的含有至少两个伯和/或仲氨基和/或羟基的聚合物或大分子结构的去质子化残基; R1选自氢，低级烷基或卤代烷基; R2选自氢或烷基; R3和R4是一个或多个各自独立地选自氢，烷基，酰氧基，烷氧基，硝基，氨基，酰氨基，烷基氨基，二烷基氨基，二烷基氨基烷基，氨基磺酰基，链炔基，巯基，羟基，羟基烷基，烷基磺酰基，卤素，氰基，羧基，烷氧基，氨基甲酰基，卤代烷基或环烷氧基; 并且R 5选自烷基亚磺酰基，烷基亚磺酰基或烷基磺酰基。可用于治疗结肠息肉。

6. 发明公开

EP0485158A3 Esters and amides of substituted phenyl acetic acids 失效
标题翻译：取代苯乙酸的酯和氨基酸
公开(公告)号：EP0485158A3
公开(公告)日：1993-01-27
申请号：EP91310205.9
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/00 , C08F8/00 , C08G73/04
CPC分类号： C08B37/003 , A61K47/58 , A61K47/59 , A61K47/61 , A61K47/645 , C08B11/14 , C08F8/14 , C08F8/30 , C08F8/34 , C08G73/0206
摘要： Esters and amides of substituted phenyl acetic acids having the formula

wherein Q is a deprotonated residue of a polymer or macromolecular structure having a molecular weight of at least 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups ;
n is an integer of at least 2 ; R 1 and R 2 are independently selected from hydrogen, halogen, alkyl, alkenyl, alkinyl or halo alkyl ; R 3 is one or more substituents selected from halogen, alkyl, alkenyl or alkinyl, cycloalkyl, oxo-substituted alkylcycloalkyl, haloalkyl, alkoxy, alkenyloxy, alkinyloxy, alkylamino, alkenylamino, alkinylamino, alkysulfonyl, alkenylsulfonyl, alkinylsulfonyl, alkylsulfinyl, alkenylsulfinyl, alkinylsulfinyl, alkylsulfenyl, alkenylsulfenyl, alkinylsulfenyl, pyrrolyl, piperidinyl, benzoyl, imidazolpyridinyl, isoindolyl, oxo-substituted isoindolyl, thionylcarbonyl, phenyl, phenoxy and halo-substituted phenoxy are useful in the treatment of colonic polyps.

7. 发明公开

EP0485157A3 Esters and amides of substituted pyrrole acetic acids 失效
标题翻译：取代的吡咯烷酸的酯和氨基酸
公开(公告)号：EP0485157A3
公开(公告)日：1993-01-27
申请号：EP91310204.2
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/08 , C08F8/00 , C07K13/00 , A61K37/02
CPC分类号： C08F8/30 , A61K47/58 , C08B11/14 , C08B37/003
摘要： Esters and amides of substituted pyrrole acetic acids of the formula :
wherein n is 0 or 1, and X represents a condensed phenyl ring ;
one of R 1 and R 2 is independently selected from hydrogen, halogen, lower alkyl ; and the other of R 1 and R 2 is independently selected from substituted or unsubstituted phenyl, benzyl, thienyl, napthyl, pyridyl, furyl, biphenyl, benzoyl, cinnamoyl, thienylcarbonyl, napthylcarbonyl, pyridylcarbonyl, furylcarbonyl or biphenylcarbonyl wherein said substituents are selected from amino, halogen, lower alkyl, lower alkylthio, lower alkoxy or lower haloalkyl ; m is an integer from 1 to 3 ; R 3 is selected from hydrogen and lower alkyl, or one or more of hydrogen and lower alkyl when m is greater than 1 ; R 4 is one or more of hydrogen, lower alkyl, alkoxy, haloalkyl, alkylthio, and halogen ; p is an integer of at least 2 ; Q is the deprotonated residue of a polymer or macromolecular structure having at least two primary and/or secondary amines and/or hydroxy groups ; and when n is 0, R 5 is selected from hydrogen, halogen, lower alkyl, alkoxy, alkylthio, and halogen are useful in the treatment of colonic polyps.

8. 发明公开

EP0485173A2 Esters and amides of substituted fused ring phenyl acetic acids 失效
标题翻译： Ester and Amide von substituteierter kondensierterPhenylessigsäure。
公开(公告)号：EP0485173A2
公开(公告)日：1992-05-13
申请号：EP91310226.5
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： A61K47/48 , C08B37/08 , C08F8/00 , C08G73/04
CPC分类号： C08G73/0206 , A61K47/58 , A61K47/59 , A61K47/61 , A61K47/645 , C08B37/003 , C08F8/14 , C08F8/30
摘要： Esters and amides of substituted fused ring phenyl acetic acids having the formula

wherein Y, together with the ring to which it is fused forms a multi-ring system selected from napthyl, [1]benzopyranol [2, 3-b], pyridine, phenothiazine, carbazole, and benzoxazole ;

R 1 is lower alkyl or hydrogen ;
R 2 is one or more independently selected from cyano, nitro, amino, alkylamino, hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, phenyl or phenyl substituted with halogen, alkyl or alkoxy ;
wherein Q is the deprotonated residue of a polymer or macromolecular structure having a molecular weight of at least 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups ; and
n is an integer of at least 2 are useful in treating colonic polyps.
摘要翻译：具有式CHEM的取代的稠环苯乙酸的酯和酰胺，其中Y与稠合的环一起形成选自萘基，[1]苯并吡喃醇[2,3-b]的多环体系，吡啶，吩噻嗪，咔唑和苯并恶唑; R1是低级烷基或氢; R 2是独立地选自氰基，硝基，氨基，烷基氨基，氢，卤素，低级烷基，低级烷氧基，羟基，苯基或被卤素，烷基或烷氧基取代的苯基中的一个或多个; 其中Q是分子量至少为1000的含有至少两个伯和/或仲氨基和/或羟基的聚合物或大分子结构的去质子化残基; n为至少2的整数，可用于治疗结肠息肉。

9. 发明授权

EP0508586B1 Substituted indenyl compounds 失效
标题翻译：取代基茚并呋喃
公开(公告)号：EP0508586B1
公开(公告)日：1995-05-31
申请号：EP92301821.2
申请日：1992-03-03
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Brendel, Klaus
IPC分类号： A61K31/10 , A61K31/16 , A61K31/19
CPC分类号： A61K31/198 , A61K31/16 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , B07C1/00

10. 发明公开

EP0485172A3 Esters and amides of substituted indenyl acetic acids 失效
标题翻译：取代的丁酸的酯和氨基酸
公开(公告)号：EP0485172A3
公开(公告)日：1993-01-27
申请号：EP91310225.7
申请日：1991-11-05
申请人： FGN, INC. , THE UNIVERSITY OF ARIZONA
发明人： Pamukcu, Rifat , Gross, Paul , Brendel, Klaus
IPC分类号： C08B11/00 , C08F8/00 , C08B37/08 , C08G69/48 , A61K31/735 , A61K31/765
CPC分类号： C08B37/003 , C08B11/14 , C08F8/14 , C08F8/30 , C08F8/34 , C08G69/10
摘要： Esters and amides of substituted indenyl acetic acids of the formula :

n is an integer of at least 2 ;
Q is a deprotonated residue of polymer or macromolecular structure having a molecular weight of at least about 1000 containing at least two primary and/or secondary amino groups and/or hydroxy groups ; R 1 is selected from hydrogen, lower alkyl, or haloalkyl ; R 2 is selected from hydrogen or alkyl ; R 3 and R 4 are one or more members each independently chosen from hydrogen, alkyl, acyloxy, alkoxy, nitro, amino, acylamino, alkylamino, diakylamino, dialkylaminoalkyl, sulfamyl, alkythio, mercapto, hydroxy, hydroxyalkyl, alkylsulfonyl, halogen, cyano, carboxyl, carbalkoxy, carbamido, haloalkyl or cycloalkoxy ; and R 5 is selected from alkylsulfenyl, alkylsulfinyl or alkylsulfonyl. are useful in the treatment of colonic polyps.

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