Carbapenem derivatives and a preparation method thereof

Details Carbapenem derivatives and a preparation method thereof Carbapenem derivatives and a preparation method thereof

2000-05-18

2002-08-20

Berch, Mark L. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S350000, C548S536000, C548S537000

Reexamination Certificate

active

06436921

ABSTRACT:

TECHNICAL FIELD
The present invention relates to carbapenem derivatives of the following formula (I) and a preparation method thereof. The carbapenem derivatives can be used as antibiotics since they have excellent antibacterial activities.
wherein X is carbonyl or sulfonyl group, R
1
and R
2
are hydrogen, low alkyl or aliphatic cyclic alkyl groups and when R
1
is hydrogen, R
2
is hydrogen, methyl, hydroxyethyl or allyl group and when R
1
is methyl R
2
is methyl, hydroxyethyl or allyl group; or R
1
and R
2
taken together with a nitrogen atom to which they are attached, is a heterocyclic group such as pyrrolidinyl, morpholinyl and piperidinyl group.
BACKGROUND OF THE INVENTION
The commercially available carbapenem antibiotics so far include thienamycin and imipenem as described in the literature (
J. Antibiot.,
1979, 32, 1). However, these compounds can be degraded by human renal enzyme (renal dehydropeptidase I, DHP-I) and lose their activity.


REFERENCES:
patent: 4933333 (1990-06-01), Sunagawa
patent: 0 443 883 (1991-08-01), None

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