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JPH0524156B2 |
Disclosed are novel carbapenem derivatives characterized by a 2- substitutent of the formula wherein A represents C2-C6 straight or branched chain alkylene group and R<10> and R<11> each independently represents optionally substituted al...
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JPH0524155B2 |
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JPH0578360A |
PURPOSE: To provide the subject novel compound having high antibacterial activity against sensitive/resistant gram-positive and gram-negative bacteria and high stability to β-lactamase and DHP-I, thus useful as an antibacterial agent. C...
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JPH0578359A |
PURPOSE: To provide the subject new compound having high antibacterial activity against sensitive/resistant gram-positive and gram-negative bactera and high stability to β-lactamase and DHP-I, thus useful as an antibacterial agent. CONS...
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JPH059426B2 |
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JPH056550B2 |
Compounds of the formula:and the pharmaceutically acceptable salts thereof whereinwherein each R is hydrogen or alkyl of 1 to 6 carbon atoms are disclosed. The compounds are useful as antibiotics.
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JPH053471B2 |
Compounds represented by formula (I), (wherein X represents a lower alkenylene or lower alkylene group optionally containing a hydroxy group, Y represents (1) a lower alkyl group, (2) a C3-8 cycloalkyl group, (3) a lower alkenyl group, (...
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JPH05384B2 |
Disclosed is a process for preparing 7-(1-hydroxethyl)-3-(2-aminoethylthio)-1-carbadethiaceph-3-e
m-3-carbox ylic acid and its pharmaceutically acceptable salts and esters (I) by total synthesis starting with L-aspartic acid and proceedi...
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JPH04368386A |
PURPOSE: To readily produce the subject compound useful as an antibiotic by subjecting a compound which is produced from two kinds of specific compounds to a ring-closing reaction under heating in a solvent. CONSTITUTION: A compound of f...
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JPH0475238B2 |
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JPH04330075A |
PURPOSE: To obtain lactams each of which is useful as an intermediate for the production of an antibiotic in high quality and high yield by mixing a specified diazoester with rhodium carboxylate in an inert solvent in a specified temp. r...
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JPH04330054A |
PURPOSE: To profitably provide a carbapenem derivative through a novel intermediate. CONSTITUTION: A compound of formula I [R2 is hydroxy (lower)alkyl, protected hydroxy (lower)alkyl; R3 is H, lower alkyl; R6 is organic group; R is H, gr...
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JPH0471913B2 |
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JPH0466872B2 |
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JPH0463878B2 |
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JPH0463076B2 |
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JPH04282383A |
PURPOSE: To provide a new compd. having antimicrobial activity which is useful for the treatment for microbial infection. CONSTITUTION: This compd. is expressed by formula I (wherein, R1 is H, 1-6C alkyl; (n) is 0 to 2; R3 is H, 1-6C alk...
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JPH04279587A |
PURPOSE: To rapidly obtain the subject compd. at a high yield by bringing a specific compd. and a tervalent org. phosphorus compd. into reaction. CONSTITUTION: A compd. of formula I [X is O, S; R(1), R(2) are each H, a 1 to 4C alkyl, 1 t...
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JPH04243881A |
PURPOSE: To obtain a antibacterial which is quite stable against activity of dehydropeptitaze. CONSTITUTION: This is a compound of the formula I, e.g. potassium (5R, 6S)-2-(4-[4'-pyridiylcarbonyloxymethyl]phenyl)-6-(1R-hydroxy
-ethyl)car...
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JPH04234886A |
PURPOSE: To obtain the new title compound capable of exhibiting strong antimicrobial action to wide pathogenic microbe as an antimicrobial agent and being remarkably stable to dehydropeptidase and having high discharge property into urin...
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JPH04234884A |
PURPOSE: To provide the novel compd. useful as an antibacterial agent. CONSTITUTION: This compd. is expressed by formula I (R is H, carboxylic acid protective group; R1 is H lower alkyl, etc.; R2, R3 are each H, lower alkoxy, etc.; Y is ...
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JPH04234885A |
PURPOSE: To provide the novel compd. which is useful as antibiotics and β- lactamase inhibitors. CONSTITUTION: This compd. is expressed by formula I (R1 is H methyl, etc.; R2 is H, 1 to 6C alkyl, etc.; R3 is H, methoxymethyl, etc.; X is...
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JPH04230384A |
PURPOSE: To provide new 2-naphthyl carbapenems that are useful intermediate of antibacterial agent. CONSTITUTION: The compound of formula I, for example, (5R,6S)-2-(1- hydroxymethyl-3-naphtyl)-6-[1R-(allyloxycarbonyl oxy)ethyl]carbapen-2...
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JPH04211687A |
PURPOSE: To obtain a synthetic intermediate for antibiotic C-2 substd. carbapenems, by reacting a carbapenem compound with an organostannane in an aprotic polar coordination solvent in the presence of a palladium compound and a halogen c...
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JPH04211083A |
PURPOSE: To provide a novel carbapenem-3-carboxylic acid derivative having an excellent antibiotic activity and stable against dehydropeptidase. CONSTITUTION: A compound of the formula [R1 is H, methyl; A is alkylene, alkenylene, aralkyl...
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JPH04198164A |
NEW MATERIAL:The optically active compound of formula I [R1 is benzyl; R2 is 1-6C alkyl; R3 is 1-6C alkyl, benzyl or allyl; R4 is H, 1-6C alkyl (substituted with protected OH), vinyl, (substituted) phenyl, (substituted) benzyl or heteroc...
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JPH04193879A |
NEW MATERIAL:A compound expressed by formula I [R1 us H or organic group removable in an acidic, an alkaline or a reductive manner; R2 is H or carboxyl-protecting group) in which the steric configuration at its 5-position is (R) configur...
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JPH0440338B2 |
Novel-Z-2-Acylamino-3-monosubstituted propenic acids and their esters and salts of the formula wherein R1 is, by preference, hydrogen, lower alkyl or a pharmaceutically acceptable cation, R2 is, by preference, methyl substituted cyclopro...
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JPH0440357B2 |
Disclosed are 1-, 6- and 2-substituted-1-carba-2-penem-3-carboxylic acids of the following structure: wherein R1, R2, R3 and R4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such...
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JPH0438756B2 |
Novel carbapenem compounds, (1R,5S,6S)-2-substituted thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylic
acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl gro...
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JPH0438754B2 |
Carbapenems having the formula:wherein:R1 is hydrogen or methyl;R4 and R5 are independently H, CH3-, CH3CH2-, (CH3)2CH-, HOCH2-, CH3CH(OH)-, (CH3)2C(OH)-, FCH2, F2CH-, F3C-, CH3CH(F)-, (CH3)2C(F)-, CH3CF2-;L is a bridging group comprisin...
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JPH0438753B2 |
Disclosed are 3-substituted-6-(1 min -hydroxyethyl)-7-oxo-1-azabicyclo [3.2.0] hept-2-ene -2-carboxylic acids having the structure: wherein R is, inter alia, selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralky...
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JPH0438755B2 |
Carbapenems and 1-methylcarbapenems having the formula:wherein - R1 and R2 are independently H. CH3. CH3CH2-, (CH3)2CH-, HOCH2, CH3CH(OH)-, (CH3)2C(OH)-, FCH2-, F2CH, F3C-, CH3CH(F)-, CH3CF2-, or (CH3)2C(F)-; R3 is H-or CH3; L is a bridg...
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JPH04178389A |
NEW MATERIAL:A compound shown by formula I [R1 is H or (substituted) hydrocarbon; COOR2 is (esterified) carboxyl; ring B is (substituted) cyclic group]. EXAMPLE: Sodium (5S,6S,7RS)-5-[(R)-hydroxyethyl]-4-oxo-3-aza-11 thiatricyclo[5,4,0,0...
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JPH0438390B2 |
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JPH04169584A |
NEW MATERIAL:(5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a] [1,2,4]triazolium-6-yl) thio]-6-[(R)-l-hydroxyethyl]-carbapen-2-em-3-carboxylate. USE: An antibacterial agent and β-lactamase inhibitor. PREPARATION: The objective compound can be ...
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JPH0435474B2 |
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JPH04164091A |
PURPOSE: To obtain the subject compound useful as a synthetic intermediate for antimicrobial agents by reacting a hydroxymethylcarbapenem compound with a phosphorylating agent and then reacting the resultant product with a halogenating a...
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JPH0432830B2 |
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JPH0429675B2 |
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JPH04134082A |
NEW MATERIAL:The compound of formula I (R1 is H or methyl; R2 and R3 are H, lower alkyl or together with adjacent N form aziridinyl, azetidinyl, pyrrolidinyl, piperidino, piperazinyl or morpholino; A is carbonyl or single bond; n is 0-3)...
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JPH04128286A |
NEW MATERIAL:The compound of formula I (R1 is H or methyl; R2 and R3 are H, lower alkyl or R2 and R3 together with adjacent N form a heterocyclic group such as aziridinyl, azetidinyl, pyrrolidinyl and morpholino; A is single bond, lower ...
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JPH0422908B2 |
In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: R = H, blocking group or salt cation there is disclosed a process for preparing III via wherein R is a protecting group.
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JPH04117382A |
NEW MATERIAL:A compound of formula I (R is lower alkyl; R1 is H, OH- protecting group; R2 is H, imino-protecting group; R" is H, carboxyl-protecting group). EXAMPLE: (1R, 5S, 6S)-2-[(2S, 4S)-2-(dimethylthiocarbamoyl)pyrrolidin-4- ylthio]...
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JPH04103584A |
NEW MATERIAL:2-(2-Oxopyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-1--
methylcarbapen-2-em-3-carboxylic acid pivaloyloxymethyl ester shown by formula I. USE: An antimicrobial agent having extremely excellent oral absorption, showing high stab...
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JPH0419230B2 |
Disclosed are 1-substituted-pen-2-em-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics; such compounds are prepared by total synthesis. wherein R1 is, inter alia, substituted an...
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JPH0474176A |
NEW MATERIAL:A compound of formula I (R1 is H, methyl; R2, R3 are H, lower alkyl; R4 is carboxyl, lower alkoxycarbonyl, carbamoyl, carbonyl, etc.,) or a salt or ester thereof. EXAMPLE: (5R, 6S)-2-[(3RS,5S)-5-carbamoyl-2-iminopyrrolidin-3...
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JPH047740B2 |
In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: R = H, blocking group or salt cation there is disclosed a process for preparing III via wherein R is a protecting group.
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JPH046704B2 |
Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: II wherein R is a readily removable carboxyl protecting group; and is a readily removable acyl group.
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JPH0426688A |
NEW MATERIAL:A compound expressed by formula I [R1 is H or methyl; R2 to R4 are H, lower alkyl, aminocarbonyl, lower alkoxy(carbonyl), cyano or nitro (except that all the R2 to R4 are H or lower alkyl)]. EXAMPLE: (5R,6S)-2-(trans-2-Carba...
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