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US 6,660,759 B1Granted
4.5-diaryloxazole compounds with prostaglandin I2 (PGI2) agonistic activity
AssigneeFujisawa Pharmaceutical Co., Ltd.
InventorsKouji Hattori, Akira Tanaka
Life of this patent
Estimating the term…
Abstract
Heterocyclic compounds of formula (I), wherein R1 is carboxy or protected carboxy, R2 is aryl which may have suitable sustituent(s), R3 is aryl which may have suitable substituent(s), R4 is hydrogen, lower alkyl, hydroxy or aryl, A1 is lower alkylene, (a) is (b), etc., —A3— is (c), etc. and n is 0 or 1, and pharmaceutically acceptable salts thereof which are useful as a medicament.
Claims6
A compound of the formula:
- wherein
- R1 is carboxy or lower alkoxycarbonyl,
- R2 is phenyl or lower alkylphenyl,
- R3 is phenyl or lower alkylphenyl, and
- R5 is hydroxy or lower alkoxy, and
- A1 and A2 are each independently methylene.
3 more elements
A process for preparing a compound of the formula:
- wherein
- R1 is carboxy or protected carboxy,
- R2 is phenyl or lower alkylphenyl,
- R3 is phenyl or lower alkylphenyl,
- R5 is hydroxy or lower alkoxy, and
- A1 and A2 are each independently methylene and a prodrug thereof, and its salt,
- which comprises
- (1) reacting a compound of the formula:
- or its salt with a compound of the formula:
- or its salt to give a compound of the formula:
- or its salt,
- in the above formulas,
- R1, R2, R3, X, A1 and A2 are each as defined above,
- Y is leaving group, or
- (2) subjecting a compound of the formula:
- or its salt to elimination reaction to give a compound of the formula:
- or its salt,
- in the above formulas,
- R, R3, X, A1 and A2 are each as defined above,
- R1a is lower alkoxycarbonyl, and
- R1b is carboxy.
18 more elements
A method, comprising:
- treating a subject with a therapeutically effective amount of a compound of the formula:
- wherein
- R1 is carboxy or lower alkoxycarbonyl,
- R2 is phenyl or lower alkylphenyl,
- R3 is phenyl or lower alkylphenyl, and
- R5 is hydroxy or lower alkoxy, and
- A1 and A2 are each independently methylene, thereby treating the conditions of thrombosis, arterial obstruction, cerebrovascular disease, gastric ulcer, hepatitis, hepatic insufficiency, hepatic cirrhosis, arteriosclerosis, ischemic heart disease, restenosis or ischemic complications after coronary angioplasty, hypertension, inflammation, autoimmune disease, heart failure, renal disease, diabetic complications, peripheral circulatory disturbance, dermatitis, chilblain, baldness, bedsores, inflammatory bowel disease, ischemic colitis or idiopathic inflammatory bowel disease.
4 more elements
Dependencies are inferred from the claim text.