2-Amino Quinazoline Derivative
The present invention provides a compound represented by Formula (I) (wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like, R 3 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group and the like, R 4 and R 5 are the same or different, and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl and the like, proviso that they are not simultaneously hydrogen atoms, and R 6 represents hydroxy or substituted or unsubstituted lower alkoxy), or a pharmaceutically acceptable salt thereof and the like.
1 . A 2-amino quinazoline derivative represented by formula (I)
(wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted alicyclic heterocyclic group, or R 1 and R 2 are combined together with the adjacent nitrogen atom to form a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted alicyclic heterocyclic group,
R 3 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or a substituted or unsubstituted alicyclic heterocyclic group,
R 4 and R 5 are the same or different, and each represents a hydrogen atom, halogen, hydroxy, carboxy, substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkoxy, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted alicyclic heterocyclic group, proviso that they are not simultaneously hydrogen atoms, and
R 6 represents hydroxy or substituted or unsubstituted lower alkoxy), or a pharmaceutically acceptable salt thereof.
2 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or substituted or unsubstituted cycloalkyl.
3 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, methyl, ethyl, or isopropyl.
4 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 represents a hydrogen atom, and R 2 represents substituted or unsubstituted lower alkyl, or substituted or unsubstituted cycloalkyl.
5 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 represents a hydrogen atom, and R 2 represents methyl, ethyl, or isopropyl.
6 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 represents a hydrogen atom, and R 2 represents cyclopropyl or cyclopropylmethyl.
7 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 represents a hydrogen atom, and R 2 represents aralkyl.
8 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 2 , wherein R 3 represents a substituted or unsubstituted aromatic heterocyclic group, or substituted or unsubstituted aryl.
9 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 2 , wherein R 3 represents substituted or unsubstituted pyridyl.
10 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 3 represents substituted or unsubstituted aryl.
11 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 2 , wherein R 3 represents substituted or unsubstituted phenyl.
12 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 2 , wherein R 3 represents substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, or a substituted or unsubstituted alicyclic heterocyclic group.
13 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 4 or R 5 represents formyl or carboxy.
14 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 4 represents substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower alkenyl.
15 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 4 represents lower alkyl which substituted with carboxy, or lower alkenyl which substituted with carboxy.
16 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 4 represents substituted or unsubstituted aryl.
17 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 8 , wherein R 4 represents aryl which substituted with carboxy.
18 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkenyl, or substituted or unsubstituted cycloalkenyl.
19 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group.
20 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents lower alkyl which substituted with carboxy, lower alkenyl which substituted with carboxy, aryl which substituted with carboxy, an aromatic heterocyclic group which substituted with carboxy, or an alicyclic heterocyclic group which substituted with carboxy.
21 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents lower alkyl which substituted with carboxy.
22 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents aryl which substituted with carboxy.
23 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents phenyl which substituted with carboxy.
24 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents an aromatic heterocyclic group which substituted with carboxy.
25 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents an alicyclic heterocyclic group which substituted with carboxy.
26 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents an alicyclic heterocyclic group which substituted with carboxymethyl.
27 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to any one of claims 14 to 17 , wherein R 5 represents halogen.
28 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 18 , wherein R 6 represents substituted or unsubstituted lower alkoxy.
29 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 18 , wherein R 6 represents methoxy.
30 . The 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 18 , wherein R 6 represents hydroxy.
31 . A pharmaceutical composition which comprises the 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient together with a pharmaceutically acceptable excipient.
32 - 33 . (canceled)
34 . A method for preventing and/or treating diseases related to the function of phosphodiesterase (PDE)-IV which comprises a step of administering an effective amount of the 2-amino quinazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 to a patient in need thereof.
35 - 36 . (canceled)