Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Abstract:||Novel .beta.-lactam compounds belonging to carbapenem or penem derivatives useful as antimicrobial agents or intermediates therefor and a process for producing these compounds are disclosed.|
|Inventor(s):||Sunagawa; Makoto (Osaka, JP), Matsumura; Haruki (Nara, JP), Inoue; Takaaki (Hyogo, JP), Fukasawa; Masatomo (Hyogo, JP), Kato; Masuhiro (Osaka, JP)|
|Assignee:||Sumitomo Pharmaceuticals Co., Ltd. (Osaka, JP)|
|Filing Date:||Oct 08, 1987|
|Claims:||1. A .beta.-lactam compound represented by the formula: ##STR386## wherein R.sub.1 represents a hydrogen atom, a 1-hydroxyethyl group or a 1-hydroxyethyl group in which the hydroxy group is protected with a protecting group for a hydroxy group; R.sub.2 represents a hydrogen atom or a protecting group for an amino group; R.sub.3 represents a hydrogen atom or a protecting group for a carboxyl group; X represents a sulfur atom; and Y represents a group of the formula (2): ##STR387## wherein R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group having 1 to 2 carbon atoms in the alkyl moiety thereof, a substituted alkyl group having 1 to 4 carbon atoms wherein said substituent is selected from the group consisting of hydroxyl, di-(C.sub.1 -C.sub.3)-alkylamino, carbamoyl, or R.sub.5 and R.sub.6 are taken together to represent an alkylene chain to form, together with the adjacent nitrogen atom, a 4- to 7-membered cyclic amino group. |
2. A (5R)-compound of the compound as claimed in any one of claims 1, which is represented by the formula: ##STR388##
4. (5R)-3-[2-((1-Pyrrolidino)carbonyl)pyrr olidin-4-ylthio-6-(1-hydroxyethyl)-1-azabicyclo[3,2,0]hept-2-ene-7-one-4-th ia-2-carboxylic acid, or a non-toxic pharmaceutically acceptable salt thereof.
5. (5R)-3 -[2-Carbamoylpyrrolidin-4-ylthio]-6-(1-hydroxyethyl)-1-azabicyclo[3,2,0]hep t-2-ene-7-one-4-thia-2-carboxylic acid, or a non-toxic pharmaceutically acceptable salt thereof.
6. A (5R,6S,8R)-compound of the compound as claimed in claim 2.
7. A (5R,6S,8R)-compound of the compound as claimed in any one of claims 3 to 5.
8. A (5R,6S,8R,2'S,4'S)-compound of the compound as claimed in claim 2.
9. A (5R,6S,8R,2'S,4'S)-compound of the compound as claimed in any one of claims 3 to 5.
10. A compound as claimed in claim 1, wherein R.sub.1 represents a hydrogen atom or a 1-hydroxyethyl group, R.sub.2 and R.sub.3 each represents a hydrogen atom.
11. A compound as claimed in claim 1, wherein R.sub.1 represents a 1-hydroxyethyl group, R.sub.2 and R.sub.3 each represents a hydrogen atom.
12. A compound as claimed in claim 11, wherein Y is represented by the formula: ##STR389##
13. A pharmaceutical composition for antimicrobial use which comprises as an active ingredient a pharmaceutically effective amount of at least one of the compounds as claimed in claim 1 and at least one pharmaceutically acceptable inert carrier or diluent.
14. A method of treating a bacterial infection comprising administering an effective amount of a compound according to claim 1 as an antimicrobial agent.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.