Claims
- 1. A polyazaheterocycle compound of the formula: ##STR1906## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen, C.sub.1-4 alkyl, C.sub.3-6 cycloakyl, furyl, thienyl, pyridyl or phenyl which may be optionally substituted by one or two substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, C.sub.1-4 alkoxy, phenyl-C.sub.1-3 alkyloxy, C.sub.1-4 alkylthio, phenyl-C.sub.1-3 alkylthio, acyl, hydroxy, amino, nitro and cyano;
- R.sup.1 is hydrogen, cyano, carbamoyl, carboxyl, C.sub.1-4 alkoxycarbonyl which may be optionally substituted in the alkoxy moiety by one or two substituents selected from the group consisting of C.sub.1-4 alkoxy, cyano, a group represented by the formula: --N (Ra.sup.1) (Rb.sup.1) (wherein each of Ra.sup.1 and Rb.sup.1 is C.sub.1-4 alkyl or phenyl-C.sub.1-3 alkyl, or Ra.sup.1 and Rb.sup.1 together with the adjacent nitrogen atom form a 5- to 7-membered heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine, piperazine, N-methylpiperzine, N-(2-hydroxymethyl)-piperazine, azepine and diazepine), nitro, phenyl, thienyl, furyl and pyridyl, or alkanoyl;
- R.sup.2 is C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, acetoxy-C.sub.1-4 alkyl, halo-C.sub.1-4 alkyl, dihalo-C.sub.1-4 alkyl, trifluoromethyl, C-.sub.1-4 alkoxy-C.sub.1-4 alkyl, di-C.sub.1-4 alkoxy-methyl, C.sub.1-4 alkylcarbamoyloxy-C.sub.1-4 alkyl, C.sub.1-4 alkyl-thiocarbamoyloxy-C.sub.1-4 alkyl, formyl, hydroxyiminomethyl or cyano.
- 2. The compound of claim 1:
- 7-(2-fluorophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 3. The compound of claim 1:
- 7-(2,5-difluorophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 4. The compound of claim 1:
- 6-ethoxycarbonyl-5-methyl-7-(2-trifluoromethylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 5. The compound of claim 1:
- 6-isopropoxycarbonyl-5-methyl-7-(2-trifluoromethylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 6. The compound of claim 1:
- 6-tert-butoxycarbonyl-5-methyl-7-(2-trifluoromethylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 7. The compound of claim 1:
- 7-(2-chlorophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 8. The compound of claim 1:
- 7-(2-bromophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 9. The compound of claim 1:
- 7-(2-chloro-3-fluorophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 10. The compound of claim 1:
- 6-isobutoxycarbonyl-5-methyl-7-(2-trifluoromethylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 11. The compound of claim 1:
- 1-phenyl-2-piperidinoethyl 5-methyl-7-(3-nitrophenyl)-4,7-dihydropyrozolo[1,5-a]pyrimidine-6-carboxylate.
- 12. The compound of claim 1:
- 7-(2-benzylthiophenyl)-6-ethoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 13. The compound of claim 1:
- 6-isopropoxycarbonyl-5-methyl-7-(2-methylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 14. The compound of claim 1:
- 7-(2,6-difluorophenyl)-6-isopropoxycarbonyl-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 15. The compound of claim 1:
- 6-ethoxycarbonyl-5-methyl-7-(2-trifluoromethylphenyl)-4,7-dihydropyrazolo[1,5-a]pyrimidine.
- 16. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier thereof.
Priority Claims (4)
Number |
Date |
Country |
Kind |
59-47357 |
Mar 1984 |
JPX |
|
59-104257 |
May 1984 |
JPX |
|
60-218306 |
Sep 1985 |
JPX |
|
61-98499 |
Apr 1986 |
JPX |
|
Parent Case Info
This is a continuation-in-part of application Ser. No. 137,088, filed Dec. 23, 1987, now abandoned; which is a divisional of application Ser. No. 911,803, filed Sept. 25, 1986, now abandoned; which is a continuation-in-part of both application Ser. No. 736,725, filed May 22, 1985, now abandoned and Ser. No. 888,497, filed Jul. 23, 1986, now abandoned; the latter of which is a continuation-in-part of application Ser. No. 796,479, filed Oct. 16, 1985, now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
3244717 |
Wagner |
Apr 1966 |
|
Foreign Referenced Citations (6)
Number |
Date |
Country |
0103796 |
Sep 1983 |
EPX |
0107619 |
May 1984 |
EPX |
0114273 |
Aug 1984 |
EPX |
0163240 |
Dec 1985 |
EPX |
0183848 |
Jun 1986 |
EPX |
0076677 |
Oct 1970 |
DDX |
Non-Patent Literature Citations (2)
Entry |
G. Auzzi et al., "I1 Farmaco, Ed. Sc.", vol. 34, 751-758 (1979). |
"Basic Abstracts Journal", Derwent Publications 84-173756/28 (Japanese Patent Appln. (Kokai) 59-95289). |
Divisions (1)
|
Number |
Date |
Country |
Parent |
911803 |
Sep 1986 |
|
Continuation in Parts (3)
|
Number |
Date |
Country |
Parent |
137088 |
Dec 1987 |
|
Parent |
736725 |
May 1985 |
|
Parent |
796479 |
Oct 1985 |
|