Title:
ANALGESICS
Document Type and Number:
WIPO Patent Application WO/1997/011946
Kind Code:
A1
Abstract:
Analgesics which contain as the active ingredient pyrazolo[1,5-a]pyrimidine derivatives represented by general formula (1), etc., have an analgetic action and thus are useful in relieving symptoms with pain such as postoperative pain, wherein R11 represents hydrogen, lower alkyl, pyridyl, furyl, thienyl, phenyl optionally having lower alkyl or phenylthio as substituent(s), N-(lower alkyl)pyrolyl, or pyrazinyl; R12 represents hydrogen, halogeno, phenyl, phenyl having substituent(s) selected from among halogeno, phenylthio and trifluoromethyl, phenyl having trifluoromethyl and nitro as substituents, or phenyl having lower alkoxy and phenylthio as substituents; R13 represents hydrogen, lower alkyl optionally having oxo, ethylenedioxy, lower alkanoyloxy, lower alkoxy, lower alkylthio, carboxy, halogeno or thienyl as substituent(s), lower alkenyl, cycloakyl, phenyl optionally having one to three substituents selected from among lower alkyl, halogeno and lower alkoxy, furyl, or thienyl; R14 represents hydrogen, carboxy, lower alkoxycarbonyl, nitro, halogeno, or lower alkyl having lower alkoxycarbonyl or an alkali metal carboxylate residue as substituent(s), or alternatively R13 and R14 may be bonded to each other to thereby form lower alkylene; R15 represents hydrogen, alkali metal, lower alkyl, phenyl optionally having one to three substituents selected from among lower alkyl and lower alkoxy, pyridyl optionally having lower alkyl or halogeno as substituent(s), quinolyl or isoquinolyl; and A represents a single bond or lower alkylene.
Inventors:
INOUE MAKOTO (JP)
OKAMURA TAKASHI (JP)
SHOJI YASUO (JP)
HASHIMOTO KINJI (JP)
OHARA MASAYUKI (JP)
YASUDA TSUNEO (JP)
OKAMURA TAKASHI (JP)
SHOJI YASUO (JP)
HASHIMOTO KINJI (JP)
OHARA MASAYUKI (JP)
YASUDA TSUNEO (JP)
Application Number:
PCT/JP1996/002759
Publication Date:
April 03, 1997
Filing Date:
September 24, 1996
Export Citation:
Assignee:
OTSUKA PHARMA CO LTD (JP)
INOUE MAKOTO (JP)
OKAMURA TAKASHI (JP)
SHOJI YASUO (JP)
HASHIMOTO KINJI (JP)
OHARA MASAYUKI (JP)
YASUDA TSUNEO (JP)
INOUE MAKOTO (JP)
OKAMURA TAKASHI (JP)
SHOJI YASUO (JP)
HASHIMOTO KINJI (JP)
OHARA MASAYUKI (JP)
YASUDA TSUNEO (JP)
International Classes:
C07D487/04; C07D487/14; (IPC1-7): C07D487/04; A61K31/505
Foreign References:
| JPH05125079A | 1993-05-21 |
Other References:
JOURNAL OF MEDICINAL CHEMISTRY, Vol. 26, No. 12, pp. 1706-1709, 1983 (USA), GABRIELLA AUZZI et al., "2-Phenylpyrazolo(1,5-a) Pyrimidin-7-Ones. A New Class of Nonsteroidal Anti-inflammatory Drugs Devoid of Ulcerogenic Activity".
JOURNAL OF PHARMACEUTICAL SCIENCES, Vol. 82, No. 5, pp. 580-586, 1993 (USA), FABRIZIO BRUNI et al., "Synthesis and Study of Anti-Inflammatory Properties of Some Pyrazolo(1,5-a)Pyrimidine Derivatives".
PHARMACOLOGICAL RESEARCH COMMUNICATIONS, Vol. 18, No. 3, pp. 241-256, 1986, PIRISINO-VETTORRI, L., "Pharmacological Activity of 2-Phenylpyrazolo-4-Ethyl-Anti-Inflammatory Agent".
See also references of EP 0795555A4
JOURNAL OF PHARMACEUTICAL SCIENCES, Vol. 82, No. 5, pp. 580-586, 1993 (USA), FABRIZIO BRUNI et al., "Synthesis and Study of Anti-Inflammatory Properties of Some Pyrazolo(1,5-a)Pyrimidine Derivatives".
PHARMACOLOGICAL RESEARCH COMMUNICATIONS, Vol. 18, No. 3, pp. 241-256, 1986, PIRISINO-VETTORRI, L., "Pharmacological Activity of 2-Phenylpyrazolo-4-Ethyl-Anti-Inflammatory Agent".
See also references of EP 0795555A4
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