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| Number | Title | Issue Date |
| 4424230 | 6-(1'-Hydroxyethyl)-3-substituted amino-1-azabicyclo-[3.2.0]hept-2-en-7-one-2-carboxylic acid Disclosed are 6-(1'-hydroxyethyl)-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R' and R" are independently selected from H, substituted and unsubstituted alkyl and aralkyl groups, or together form a ... | 01/03/1984 |
| 4369187 | 3-Substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid Disclosed are 3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R is, inter alia, acyl, alkyl, and aralkyl. Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful... | 01/18/1983 |
| 4361512 | 2-Substituted thio-6-substituted-carbapen-2-em-3-carboxylic acids Disclosed are 2-substituted thio-6-substituted-carbapen-2-em-3-carboxylic acids (I) and their pharmaceutically acceptable salt, ester and amide derivatives which are useful as antibiotics: ##STR1## wherein: R5 is CN, ##STR2## (R... | 11/30/1982 |
| 4360684 | Process for the preparation of (2S)-tetrahydro-2-methyl-6-oxo-4ଲ-carboxylic acid Disclosed is a process for preparing (2S)-tetrahydro-2-methyl-6-oxo-4ଲ-amino-2H-pyran-3-carb oxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)... | 11/23/1982 |
| 4358447 | 7-N-Heterocyclyl cephalosporins Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia... | 11/09/1982 |
| 4349687 | Intermediate for synthesis of thienamycin via (3SR, 4RS)-3-[1 (SR)-hydroxyethyl]-2-oxo-4-azetidineacetic acid Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: ##STR1## wherein R is a readily removable carboxyl protecting group.... | 09/14/1982 |
| 4348320 | Substituted azetidiones Disclosed are substituted azetidinones (1) which are useful in the preparation of 1-carba-2-penem-3-carboxylic acids (I): ##STR1## wherein R is hydrogen or a blocking group and R1, R2 and R3 are, inter alia, independe... | 09/07/1982 |
| 4348325 | Methyl 3-azido-4-C-cyano-2,3,4,6-tetradeoxy--D-arabino-hexopyranoside Disclosed is methyl 3-azido-4-C-cyano-2,3,4,6-tetradeoxy--D-arabino-hexopyranoside and processes for its preparation from methyl 3-azido-2,3,6-trideoxy--D-arabino-hexopyranoside via the 4-bromo-4-deoxy intermediate; wherein the two inve... | 09/07/1982 |
| 4344885 | Intermediate for the preparation of thienamycin Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.... | 08/17/1982 |
| 4341791 | 6-, 2- and 1,1-Disubstituted-1-carbadethiapen-2-em-3-carboxylic acid S-oxides Disclosed are S-oxides of 6-, 2- and 1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: n is 1 or 2; and R1, R2, R6, R7 and R8 are, inter alia... | 07/27/1982 |
| 4341706 | Process for the preparation of carbapenem antibiotics Disclosed is a process for the synthesis of carbapenem antibiotics I and their pharmaceutically acceptable salts and esters from 1: ##STR1## wherein: R7, R6, R1, R2 and R8 are selected from hydro... | 07/27/1982 |
| 4335212 | Fermentation process for (5R,6S,8S)-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3. 2.0]hept-2-ene-2-carboxylic acid Disclosed is a fermentation process for preparing and isolating the antibiotic, (5R,6S,8S)-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2. 0]hept-2-ene-2-carboxylic acid in substantially pure form.... | 06/15/1982 |
| 4324900 | 3-Amino-4-C-carboxy-2,3,4,6-tetradeoxy-D-arabino-hexose trimethylene dithioacetal Disclosed is a chiral, total synthesis of thienamycin from D-glucose, which proceeds via intermediates I, II, and III and joins aldehyde IV or acid V, which are known to be useful in the total synthesis of thienamycin (VI): ##STR1## wherein R1 | 04/13/1982 |
| 4318912 | 6-(1-Hydroxyethyl)-3-substituted-1-azabicyclo(3.2.0)-hept-2-en-7-one-2-ca rboxylic acid Disclosed are 6-(1'-hydroxyethyl)-3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-car boxylic acids(I): ##STR1## wherein X is halo, oxygen (the 2-3 bond is saturated and the species I exists as the carboxylate salt or ester), or --OR wherein R... | 03/09/1982 |
| 4312871 | 6-, 1- And 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids Disclosed are 6-, 1- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein: R1, R2, R6, R7 and R8 are, inter alia, independently selected from the grou... | 01/26/1982 |
| 4311704 | Substituted N-methylene derivatives of thienamycin Disclosed are substituted N-methylene derivatives of thienamycin having the formula: ##STR1## wherein: (1.) X.dbd.--NR1 R2, and Y.dbd.--R'--N.dbd.CRNR1 R2, and (2.) X.dbd.R, and Y.dbd.--NR1 R'N.d... | 01/19/1982 |
| 4309438 | N-Alkyl-N-iminomethyl derivatives of thienamycin Disclosed are N-alkyl-N-iminomethyl derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein R5 is, inter alia, alkyl, alkenyl, aryl, or aralkyl, R6 is selected from R, OR, SR and... | 01/05/1982 |
| 4298741 | 6-Amido-3-substituted-1-azabicyclo[3.2.0]-hept-2-en-7-one-2-carboxylic acid Disclosed are 6-amido-3-substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I): ##STR1## wherein R1 is hydrogen or acyl; and X is halo, oxygen (the 2-3 bond is saturated and the species I exists as a carboxylate salt or... | 11/03/1981 |
| 4281002 | 3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyc lo(3.2.0)-hept-2-ene-2-carboxylic acid Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein R1 is hydrogen or acyl. Such compounds as well as their pharmaceutically acceptable salt, ester and a... | 07/28/1981 |
| 4271159 | 7-N-Heterocyclyl-2-substituted 1-oxadethia-cephalosporins Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia... | 06/02/1981 |
| 4269873 | 2-, 5-, and 6-Substituted-1-carbadethiapen-2-em-3-carboxylic acids Disclosed are 2-, 5- and 6-substituted-1-carbadethiapen-2-em-3-carboxylic acids having the structure: ##STR1## wherein R6, R7, R8 and R9 are, inter alia, independently selected from the group consisting of ... | 05/26/1981 |
| 4267188 | 5-Substituted-1-carba-pen-2-em-3-carboxylic acid Disclosed are 1-carba-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R1, R2, R3 and R4 are, inter alia, independently selected from the group consisting of hydrogen (R4 ... | 05/12/1981 |
| 4264621 | 5-Substituted-3 -(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-en e-2-carboxylic acid Antibiotic 5-substituted-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3 .2.0]hept-2-ene-2-carboxylic acids (I) are disclosed: ##STR1## wherein R is alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or heteroaryl.... | 04/28/1981 |
| 4263306 | 3-N-Pyridinium nocardicin and antibiotic composition thereof This invention relates to a new class of antibiotics (I): ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 3-amino nitrogen of nocardicin represents a mono- or polycyclic N-containing heterocyclic gro... | 04/21/1981 |
| 4260543 | Crystalline N-formimidoyl thienamycin Disclosed is crystalline N-formimidoyl thienamycin and a process for its preparation.... | 04/07/1981 |
| 4255424 | 7-N-Heterocyclyl 1-oxa, 1-aza, and 1-carbadethiacephalosporins Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia... | 03/10/1981 |
| 4241062 | Antibacterial penicillins This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## represents a mono... | 12/23/1980 |
| 4235920 | N-Alkylated derivatives of thienamycin Disclosed are N-alkylated derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such compounds and their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are proc... | 11/25/1980 |
| 4235917 | N-Alkyl-N-acyl derivatives of thienamycin Disclosed are N-alkyl- N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R1 is, inter alia, alkyl, alkenyl, aryl or aralkyl; and R2 is acyl. Such compounds, including thei... | 11/25/1980 |
| 4232030 | Substituted N-methylene derivatives of thienamycin sulfoxide and sulfone Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (I, n=1) and sulfone (I, n=2) which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR,... | 11/04/1980 |
| 4226870 | O-, N- and carboxyl derivatives of thienamycin Disclosed are O-, N- and substituted carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pha... | 10/07/1980 |
| 4224336 | 3-(2-Aminoethylthio)-6-amido-7-oxo-1-azabicyclo[3.2.0]- hept-2-ene-2-carboxylic acid Disclosed are 3-(2-aminoethylthio)-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxy lic acids having the structure: ##STR1## wherein R1 is hydrogen or acyl. Such compounds as well as their pharmaceutically acceptable salt, ester a... | 09/23/1980 |
| 4218459 | 6-Amido-1-carba-2-penem-3-carboxylic acid Disclosed are 6-amido-1-carba-2-penem-3-carboxylic acids of the following structure: ##STR1## wherein R1 is hydrogen or acyl and R3 is, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, ... | 08/19/1980 |
| 4218478 | Trichostatin as an antiprotozoal agent Trichostatin (I) is disclosed to be useful as an antiprotozoal agent for the treatment of diseases in man and animals. Also disclosed are pharmaceutical compositions comprising trichostatin for treating protozoal infections. Trichostatin has the structure... | 08/19/1980 |
| 4218463 | 3-Substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid Disclosed are 3-substituted thio-6-amido-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acids having the structure: ##STR1## wherein: R1 is hydrogen or acyl and R8 is, inter alia, independently selected from the group con... | 08/19/1980 |
| 4217453 | 6-Amido-3-substitu ted-amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid Disclosed are 6-amido-3-substituted-amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxyli c acids (I): ##STR1## wherein R1 is hydrogen or acyl; and R' and R" are independently selected from the group consisting of: hydrogen, substituted... | 08/12/1980 |
| 4212807 | Process for deacylating N-acyl-6-substituted-2-[2-aminoethylthio]-1-carbadethiapen-2-em-3-carbox ylic acids Disclosed is a process for chemically cleaving the acyl group from N-acyl-6-substituted-2-[2-aminoethylthio]-1-carbadethiapen-2-em-3-carboxyl ic acids which proceeds via an imino chloride intermediate. The acylated substrate and the deacylated product are ... | 07/15/1980 |
| 4211707 | Process for hydrolytically cleaving O-sulfo thienamycins Disclosed is a process for the hydrolytically cleaving O-sulfo thienamycins: ##STR1## wherein R is H or acetyl and M is H, an alkali or alkaline earth metal cation or an organo cationic species such as pyridinium; and wherein the dotted line ind... | 07/08/1980 |
| 4208330 | O-Derivatives of thienamycin Disclosed are O- derivatives (esters and ethers of the secondary alcohol group) of the antibiotic thienamycin which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of ... | 06/17/1980 |
| 4207395 | Process for deacylating N-acyl-6-substituted-2-[2-aminoethylthio]-1-carbadethiapen-2-em-3-carbox ylic acids Disclosed is a process for enzymatically cleaving the acyl group from N-acyl-6-substituted-2-substituted-1-carbadethiapen-2-em-3-carboxylic acids. The acylated substrate and the deacylated product are antibiotics.... | 06/10/1980 |
