Title:
HETEROAROMATIC OXAZOLE COMPOUNDS AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/1996/019463
Kind Code:
A1
Abstract:
A heteroaromatic oxazole compound represented by general formula (I) of a pharmaceutically acceptable salt thereof: wherein Z represents oxygen; one of R and R1 represents a group represented by formula (a), (wherein R3 represents lower alkyl, amino or lower alkylamino; and R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogeno, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R4, R5, R6 and R7 is not hydrogen), while another of them represents optionally substituted cycloalkyl, an optionally substituted heretocyclic group or optionally substituted aryl; and R2 represents lower alkyl or halogenated lower alkyl. The compound or a pharmaceutically acceptable salt thereof has an antipyretic/analgesic effect and an anti-inflammatory effect and, in particular, selectively inhibits cyclooxygenase 2 (COX-2). Thus it is expected to be useful as an anti-inflammatory agent, etc., with little side effects such as gastrointestinal disorders.
Inventors:
HARUTA JUNICHI (JP)
HASHIMOTO HIROMASA (JP)
MATSUSHITA MUTSUYOSHI (JP)
HASHIMOTO HIROMASA (JP)
MATSUSHITA MUTSUYOSHI (JP)
Application Number:
PCT/JP1995/002600
Publication Date:
June 27, 1996
Filing Date:
December 18, 1995
Export Citation:
Assignee:
JAPAN TOBACCO INC (JP)
HARUTA JUNICHI (JP)
HASHIMOTO HIROMASA (JP)
MATSUSHITA MUTSUYOSHI (JP)
HARUTA JUNICHI (JP)
HASHIMOTO HIROMASA (JP)
MATSUSHITA MUTSUYOSHI (JP)
International Classes:
A61K31/42; A61K31/421; A61P25/04; A61P29/00; A61P43/00; C07C45/00; C07C49/563; C07C49/567; C07C49/792; C07C49/813; C07C69/007; C07C233/31; C07C233/47; C07C235/74; C07C251/40; C07C251/42; C07C251/48; C07C311/16; C12N9/99; C07C311/29; C07C311/32; C07C311/37; C07C317/22; C07C317/24; C07C317/32; C07D207/333; C07D263/30; C07D263/32; C07D265/30; C07D295/10; C07D307/46; C07D333/22; C07D413/02; C07D413/04; (IPC1-7): C07D263/32; C07D413/04; A61K31/42; C07D207/333; C07D265/30; C07D295/10; C07D307/46; C07D333/22; C07C251/48; C07C49/782; C07C49/792; C07C49/813; C07C317/14; C07C311/16; C07C311/29; C07C233/61; C07C233/76
Domestic Patent References:
| WO1994027980A1 | 1994-12-08 |
Foreign References:
| US4782058A | 1988-11-01 | |||
| JPS62138485A | 1987-06-22 | |||
| JPS59155365A | 1984-09-04 |
Other References:
J. ORG. CHEM., Vol. 43, No. 15, (1978), PAUL D. SEEMUCH et al., "Alpha-Hetero-Substituted Phosphonate Carbanions. 7. Synthesis of Deoxy Benzoins and Benzo(b)Furans", p. 3063-3065.
J. ORG. CHEM., Vol. 53, No. 24, (1988), SCOTT C. BERK et al., "General Approach to Highly Functionalized Benzylic Organonetallics of Zinc and Copper", p. 5789-5791.
J. AM. CHEM. SOC., Vol. 115, No. 8, (1993), TAEHEE NOH et al., "Photochemistry of Alpha-(-Tolyl) Acetone and Some Derivatives: Triplet Alpha-Cleavage and Singlet Delta-Hydrogen Abstraction", p. 3105-3110.
J. ORG. CHEM., Vol. 53, No. 24, (1988), SCOTT C. BERK et al., "General Approach to Highly Functionalized Benzylic Organonetallics of Zinc and Copper", p. 5789-5791.
J. AM. CHEM. SOC., Vol. 115, No. 8, (1993), TAEHEE NOH et al., "Photochemistry of Alpha-(-Tolyl) Acetone and Some Derivatives: Triplet Alpha-Cleavage and Singlet Delta-Hydrogen Abstraction", p. 3105-3110.
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