摘要:
A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1 and R2 are each H or lower alkyl, one of —COR32 and —COR42 is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof. Said compounds show excellent PAI-1 inhibitory activity and are useful in the prophylaxis or treatment of various thromboses such as myocardial infarction, intra-atrial thrombus in atrial fibrillation, cerebral infarction, angina pectoris, stroke, pulmonary infarction, deep venous thrombus (DVT), disseminated intravascular coagulation syndrome (DIC), diabetic complications, restenosis after percutaneous transluminal coronary angioplasty (PTCA), etc.
摘要:
A novel process for preparing a naphthalene derivative of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are a lower alkoxycarbonyl group or both may combine to form a group of the formula ##STR2## one of R.sup.3 and R.sup.4 is hydrogen atom or a lower alkoxy group and the other is a lower alkoxy group; ring A is a substituted or unsubstituted benzene ring, which is useful as a hypolipidemic agent, and a novel intermediate of the formula: ##STR3## wherein R1, R2, R3, R4 and ring A are the same as defined above.
摘要:
An improved process for preparing a 4-mercaptopyrrolidine compound [I]: ##STR1## wherein R is H, lower alkyl or lower alkanoyl, R.sup.1 is H or SH-protecting group, and X is O or S, which comprises reacting halogenobutyric acid compound [VI], or a salt thereof, with amine compound [VII], or a salt thereof, and if necessary, followed by thiocarbonylating the product and/or removing the protecting group, said 4-mercaptopyrrolidine compound [I] being useful as intermediate for carbapenem antibacterial agents.
摘要:
Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.
摘要:
An N-�2-(1-hydroxyethyl)-3-oxopropyl!amine compound of the formula �III!: ##STR1## wherein Ring B represents a benzene ring which may be substituted; W represents oxygen atom or sulfur atom; Y represents oxygen atom, sulfur atom or N R.sup.0, R.sup.0 represents hydrogen atom or a substituent; Z represents a substituted methylene group which contains at least one chiral center; R.sup.5 represents an aralkyloxycarbonyl group or an alkoxycarbonyl group; R.sup.6 represents hydrogen atom, an aralkyl group, an acyloxy group, a tri-substituted silyloxy group or an alkoxy group; or both of R.sup.5 and R.sup.6 bond at their termini and combine with the adjacent nitrogen atom to form phthalimido group, and a process thereof are disclosed. Said compound �III! is useful as a starting compound of .beta.-lactam antibacterial agents.
摘要:
Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom, or a pharmaceutically acceptable salt thereof, and a process for preparing the same.
摘要:
Novel process for preparing azetidinone compound of the formula �III!: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula �I!: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula �II!: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound �Ill! being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.