摘要:
There are disclosed a lactam derivative of the formula: wherein R 1 is a substituted or unsubstituted phenyl group; R 2 is a substituted or unsubstituted phenyl group, a cycloalkyl group or a nitrogen-containing 6-membered heterocyclic group; Z is oxygen atom or sulfur atom; and n is an integer of 2 or 3, and a salt thereof, and a preparation thereof. The above lactam derivative is novel and useful as a pharmaceutical compound. Accordingly, pharmaceutical preparations are also provided, together with the use of such derivatives for the manufacture of a medicament having valuable therapeutic properties.
摘要:
A process for preparing an S type 4-substituted hydroxypyrano-indolidine compound of the formula (VII): wherein R° is a residue of a nitrogen-containing fused heterocyclic carboxylic acid having an absolute configuration of "R" which is obtained by removing hydroxy group from the carboxyl group of said carboxylic acid (in which the nitrogen atom contained in the residue is protected), is described. The process involves reduction, alkanoylation, nitrosation, rearrangement and intramolecular cyclization reactions.
摘要:
An imidazopyridine derivative of the formula [I]:
wherein R¹ is hydrogen or lower alkyl, R² is hydrogen, lower alkylsulfonyl or a group of the formula:
(Z is oxygen atom or two hydrogen, R⁰ is substituted or unsubstituted lower alkyl, lower alkoxy, 5- or 6-membered heteromonocyclic, substituted or unsubstituted phenyl, hydrogen, substituted or unsubstitued amino or lower alkenyl), R³ is carboxyl or lower alkoxycarbonyl and Ring A is substituted or unsubstituted phenyl, and pharmaceutically acceptable salt thereof, and processes for preparation thereof, said imidazopyridine derivatives have excellent angiotensin II antagonistic activities and are useful in prophylaxis and treatment of hypertension.
摘要:
A chromene or thiochromene derivative of the formula: wherein A is oxygen or sulfur atom, R¹ is a halogenophenyl, R² and R³ are the same or different and are each a lower alkyl or R² and R³ are combined together to form -(CH₂) n - in which n is an integer of 4 to 6, or a pharmaceutically acceptable ester, amide, lactone or salt thereof, which has excellent HMG-CoA reductase inhibitory activity and is useful for prophylaxis and treatment of hyperlipidemic diseases, a process for preparing said compound and an intermediate compound used for preparing said compound. Further, a pharmaceutical composition containing the above mentioned chromene or thiochromene derivatives is disclosed.
摘要:
A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: wherein R° is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R 1 and R 2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.
摘要:
A novel phenylethylene derivative of the formula:
wherein R¹ is phenyl group, a fluorophenyl group, a methoxyphenyl group, thienyl group, furyl group, oxopyrrolidinyl group or pyridyl group, or a pharmaceutically acceptable ester, amide, lactone or salt, which has excellent HMG-CoA reductase inhibitory activity and is useful as an anti-hyperlipidemic agent, a pharmaceutical composition containing the same, and processes for preparing the same as well as an intermediate therefor.
摘要:
A novel phenylethylene derivative of the formula:
wherein R¹ is phenyl group, a fluorophenyl group, a methoxyphenyl group, thienyl group, furyl group, oxopyrrolidinyl group or pyridyl group, or a pharmaceutically acceptable ester, amide, lactone or salt, which has excellent HMG-CoA reductase inhibitory activity and is useful as an anti-hyperlipidemic agent, a pharmaceutical composition containing the same, and processes for preparing the same as well as an intermediate therefor.