- Preventives and remedies for ischemic intestinal lesion and ileus
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The present invention relates to a prophylactic and/or therapeutic composition for ischemic intestinal lesions and/or ileus which comprises as an active ingredient a pyrazolopyridine compound of the following formula: [wherein R1is lower alkyl group, etc; R2is a group of the formula: (wherein R4is protected amino group, etc; R5is hydrogen, etc); etc, and R3is hydrogen, etc] or a salt thereof.
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- Process development of a novel non-xanthine adenosine A1 receptor antagonist
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(+)-(R)-1-[(E)-3-(2-phenylpyrazolo[l,5-a]pyridin-3-yl)acryloyl]-2- piperidine ethanol (FK453) is a novel, potent adenosine AI receptor antagonist for the regulation of renal function. The development of a reliable process suitable for large scale manufacture is described. A Horner-Emmons reaction and a 1,3-dipolar cycloaddition were successfully scaled up to afford ethyl (E)-3-(2-phenylpyrazolo[l,5-a]pyridin-3-yl)acryloylate, with excellent regioselectivity and stereoselectivity. Process improvements and optimization of each step permitted elimination of column chromatography, resulting in a straightforward, practical synthesis of FK453.
- Zanka, Atsuhiko,Uematsu, Ryoichi,Morinaga, Yasuhiro,Yasuda, Hironobu,Yamazaki, Hiroshi
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p. 389 - 393
(2013/09/08)
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- Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist
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Novel 2-phenylpyrazolo[1,5-a]pyridine-3-acryloylamides were synthesized and evaluated for diuretic activities. FK453 (1d), the most potent compound in this series, was found to be a potent and selective adenosine A1 receptor antagonist, whereas 1e, the (S)-enantiomer of FK453, was a weak and non-selective adenosine antagonist.
- Akahane, Atsushi,Katayama, Hirohito,Mitsunaga, Takafumi,Kita, Yasuhiro,Kusunoki, Takahiro,Terai, Takao,Yoshida, Keizo,Shiokawa, Youichi
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p. 2059 - 2062
(2007/10/03)
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- Method of treating kidney disease using pyrazolopyridine compound
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The invention relates to a method for the treatment of renal toxicity, nephrosis or nephritis which comprises administering an effective amount of the pyrazolopyridine compounds of the invention.
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- Pharmaceutical method of treatment using pyrazolopyridine compound
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The invention relates to a method for the treatment of ailments which comprises administering an effective amount of the pyrazolopyridine compounds of the invention.
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- Pyrazolopyridine compound and processes for preparation thereof
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The disclosure deals with pyrazolopyridine compounds of the formula STR1 wherein the variables are defined in the specification. The compounds are useful in the treatment of bronchial asthma, immunosuppression, diabetes, etc.
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- Pharmaceutically useful pyrazolopyridines
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The disclosure deals with a pyrazolopyridine compound of the formula STR1 wherein the variables are defined in the specification. The compounds are useful as a diuretic, antihypertensive agent, etc.
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