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    5,6,7-trisubstituted-4-amino-pyrido[2,3-d]pyrimidine compounds useful for inhibiting adenosine kinase
    2.
    发明专利
    5,6,7-trisubstituted-4-amino-pyrido[2,3-d]pyrimidine compounds useful for inhibiting adenosine kinase 未知

    公开(公告)号：NZ337125A

    公开(公告)日：2001-06-29

    申请号：NZ33712598

    申请日：1998-04-13

    Applicant: ABBOTT LAB

    Inventor： BHAGWAT SHRIPAD S ,  PERNER RICHARD J ,  GU YU GUI

    IPC: A61P25/04 ,  A61K31/519 ,  A61P1/00 ,  A61P3/10 ,  A61P9/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P29/00 ,  A61P31/00 ,  A61P37/06 ,  A61P43/00 ,  C07D471/04

    Abstract: A 5,6,7-trisubstituted-4-aminopyrido[2,3-d]pyrimidine derivative or a pharmaceutically acceptable salt or amide thereof has the formula (I) wherein: A) R1 and R2 are independently H, alkyl, arylalkyl or acyl or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-3 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or a heterocyclic group R5 is aryl, aralkyl, heteroaryl or a heterocyclic group and the dashed lines indicate a double bond is optionally present or B) R1 and R2 are independently H, alkyl, arylalkyl -C(O)-alkyl, -C(O)-aryl, -C(O)-heterocyclic or together with the nitrogen atom to which they are attached may form a 5 to 7 membered ring optionally containing 1-2 additional heteroatoms selected from N, O or S; R3 and R4 are independently alkyl, alkenyl, alkynyl, cycloalkyl, or optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl and R5 is optionally substituted heteroarylalkyl, aryl, arylalkyl, heteroarylalkenyl, arylalkenyl, arylalkynyl or heteroarylalkynyl; with the proviso that the compound may not be: i) 4-amino-5-(4-chlorophenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; ii) 4-amino-5-(4-methoxyphenyl)-7-(4-nitrophenyl)pyrido[2,3-d]pyrimidine; iii) 4-amino-5-(4-fluorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; iv) 4-amino-5-(4-chlorophenyl)-7-(4-fluorophenyl)pyrido[2,3-d]pyrimidine; v) 4-amino-5-phenyl-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; vi) 4-amino-5-phenyl-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine; vii) 4-amino-5-(4-methoxyphenyl)-7-(4-aminophenyl)pyrido[2,3-d]pyrimidine; viii) 4-amino-5-(4-methoxyphenyl)-7-(4-bromophenyl)pyrido[2,3-d]pyrimidine and ix) 4-amino-5,7-diphenylpyrido[2,3-d]pyrimidine. A pharmaceutical composition thereof is useful for inhibiting adenosine kinase, ischemia, neurological disorders, nociperception, inflammation, immunosuppression, gastrointestinal disjunctions, diabetes or sepsis.

    8.
    发明专利
    未知

    公开(公告)号：NO995036D0

    公开(公告)日：1999-10-15

    申请号：NO995036

    申请日：1999-10-15

    Applicant: ABBOTT LAB

    Inventor： BHAGWAT SHRIPAD S ,  LEE CHIH-HUNG ,  COWART MARLON D ,  MCKIE JEFFREY ,  GRILLOT ANNE LAURE

    IPC: A61K31/519 ,  A61P9/00 ,  A61P25/00 ,  A61P43/00 ,  C07D471/04 ,  C07D

    Abstract: A method for inhibiting adenosine kinase by administering a compound having formula (I) wherein R and R are independently selected from H, loweralkyl, C1-C6alkoxyC1-C6alkyl, arylC1-C6alkyl, -C(O)C1-C6alkyl, -C(O)aryl, -C(O)heterocyclic or may join together with the nitrogen to which they are attached to form a 5-7 membered ring optionally containing 1-2 additional heteroatoms selected from O, N or S; R is selected from the group consisting of loweralkyl, loweralkenyl, loweralkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocyclic group, heteroarylalkyl or heterocycloalkyl wherein the heteroaryl and heterocyclic groups are linked directly or indirectly by a ring carbon; R is selected from the group consisting of loweralkyl, loweralkenyl, loweralkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocyclic group heteroarylalkyl or heterocycloalkyl; and a dashed line --- indicates that a double bond is optionally present provided that proper valencies are maintained, a pharmaceutical composition comprising a therapeutically effective amount of a compound thereof above in combination with a pharmaceutically acceptable carrier, and a method of treating cerebral ischemia, epilepsy, nociperception, inflammation and sepsis in a mammal in need of such treatment, comprising administering to the mammal a therapeutically effective amount of a compound thereof, a process for preparing said compounds, and compounds having the above formula wherein R , R , R and R are separately defined.

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