摘要:
A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.
摘要:
A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.
摘要:
Carbapenem compounds of formula I and their pharmaceutically acceptable salts and esters are provided: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, p, q and r are as defined herein, which are useful as antibacterial agents.
摘要:
A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidino group, a piperazinyl group and a morpholino group, A is a carbonyl group or a single bond, and n is an integer of from 0 to 3; or a pharmaceutically acceptable salt or ester thereof.
摘要:
The present invention relates to stable crystalline (6R,7R)-7-(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxylimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.
摘要:
A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 is a hydrogen atom or a negative charge, R.sup.3 is a hydrogen atom or a lower alkyl group, Ar is a phenyl group, a naphthyl group or a group of: ##STR2## (wherein each of A.sub.4 and A.sub.5 is a single bond, --NHSO.sub.2 -- or the like, and Het is a pyrrolinyl group, a 1,4-diazabicyclo�2.2.2!octanyl group or the like which may be substituted with a hydroxyl group, a carbamoyl lower alkyl group or the like) which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfonyl group or the like; a hydroxyl group; a di-lower alkylsulfamoyl group or the like, each of A.sub.1, A.sub.2 and A.sub.3 is a single bond or a lower alkylene group which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfamoyl group or the like; a pyridyl group or a pyridino group; and W is a sulfur atom, a single bond; or a pharmaceutically acceptable salt or ester; a process for its production and an antibacterial agent containing it as an active ingredient.
摘要:
The present invention relates to stable cyrstalline (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxyl-1-methylethoxyimino)acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carboxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.
摘要:
A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4 is a hydrogen atom or a lower alkyl group, each of R.sup.5 and R.sup.6 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.5 and R.sup.6 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group and a piperidyl group), A is .dbd.NR.sup.7, .dbd.N.sup.+ (R.sup.7)R.sup.8, wherein each of R.sup.7 and R.sup.8 which may be the same or different, is a hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group, a formimidoyl group, an acetoimidoyl group, --COOR.sup.4, --CON(R.sup.5)R.sup.6, --N(R.sup.5)R.sup.6, --CH.sub.2 COOR.sup.4, --CH.sub.2 N(R.sup.5)R.sup.6 or --CH.sub.2 CON(R.sup.5)R.sup.6 (wherein R.sup.4, R.sup.5 and R.sup.6 are as defined above), p is an integer of from 0 to 3, and q is an integer of from 1 to 3; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译:下式的化合物:其中R是氢原子或甲基,R 1是氢原子或负电荷,R 2和R 3可以相同或不同,为氢原子 ,低级烷基,羟基低级烷基,亚氨基,亚氨酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5)R6或-CH2CON( R5)R6(其中R4是氢原子或低级烷基,R5和R6各自可以相同或不同,是氢原子或低级烷基,或R5和R6与相邻的氮原子一起形成) 选自氮丙啶基,氮杂环丁烷基,吡咯烷基和哌啶基的杂环基),A为= NR 7 = N +(R 7)R 8,其中R 7和R 8可以相同或不同, 不同的是氢原子,低级烷基,羟基低级烷基,亚氨基,亚氨代乙酰基,-COOR4,-CON(R5)R6,-N(R5)R6,-CH2COOR4,-CH2N(R5 )R6或-CH2CON(R5)R6(其中 在R4中,R5和R6如上所定义),p是0-3的整数,q是1至3的整数; 或其药学上可接受的盐或酯。
摘要:
A compound of the formula: ##STR1## wherein R is a hydrogen atom or a methyl group, R.sup.1 is a hydrogen atom or a negative charge, R.sup.2 is a lower alkyl group, a lower alkyl group substituted with a hydroxyl group or --COOR.sup.3 (wherein R.sup.3 is a hydrogen atom or a lower alkyl group), A is .dbd.NH, .dbd.NR.sup.4 or .dbd.N(R.sup.4)R.sup.5 (wherein each of R.sup.4 and R.sup.5 which may be the same or different, is a lower alkyl group or a lower alkyl group substituted with a hydroxyl group), p is an integer of from 0 to 3, and each of q and r which may be the same or different, is an integer of from 0 to 5, provided that q and r are not simultaneously 0 and q +r.ltoreq.6; or a pharmaceutically acceptable salt or ester thereof.
摘要:
The present invention relates to a compound having the formula: ##STR1## wherein R is a hydrogen atom, a carboxyl-protecting group or a negative charge and Q is a hydrogen atom, a halogen atom, a hydroxyl group, an acetoxy group, a carbamoyloxy group, an azide group, a substituted or unsubstituted quarternary ammonio group or a substituted or unsubstituted heterocyclic thio group having at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, or a non-toxic salt or physiologically hydrolyzable non-toxic ester thereof; a process for producing it; and an antibacterial agent comprising it as an active ingredient.Further, the present invention also relates to a compound having the formula: ##STR2## wherein R.sup.3 is a hydrogen atom or an amino-protecting group, and each of R.sup.4 and R.sup.5 which may be the same or different is a hydrogen atom or a carboxyl-protecting group, or a salt thereof; and a process for producing it.