Title:
ピリミジンA2b選択的アンタゴニスト化合物、それらの合成、及び使用
Document Type and Number:
Japanese Patent JP4440642
Kind Code:
B2
Abstract:
The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, -C(O)-alkyl, -C(O)-O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.
Inventors:
Castel Hano, Erlind El
Stanig, Arno
McKibben, Brian
Collington, Eric William
Stanig, Arno
McKibben, Brian
Collington, Eric William
Application Number:
JP2003554126A
Publication Date:
March 24, 2010
Filing Date:
December 20, 2002
Export Citation:
Assignee:
OSI Pharmaceuticals Incorporated
International Classes:
C07D239/48; C07D243/08; A61K31/506; A61K31/513; A61K31/519; A61K31/5377; A61K31/55; A61K31/551; A61P1/00; A61P1/12; A61P3/10; A61P9/00; A61P9/10; A61P9/12; A61P11/06; A61P17/00; A61P17/04; A61P19/02; A61P27/02; A61P35/00; A61P37/08; A61P43/00; C07D239/42; C07D401/12; C07D401/14; C07D403/12; C07D405/12; C07D405/14; C07D409/12; C07D409/14; C07D411/12; C07D413/12; C07D417/12; C07D471/10; C07D487/04
Domestic Patent References:
| JP11158073A |
Foreign References:
| WO1999064407A1 |
Other References:
Giuliana Biagi et al.,Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl-pyrimidines and their affinity towards A1 adenosine receptors,Farmaco,1997年,Vol.52, No.1,p.61-65
Attorney, Agent or Firm:
Takehiko Suzue
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto
Satoshi Kono
Makoto Nakamura
Kurata Masatoshi
Takashi Mine
Yoshihiro Fukuhara
Sadao Muramatsu
Ryo Hashimoto