Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-03-26
1999-09-28
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544222, 544225, 544227, A61K 31545, C07D50159, C07D50122, C07D50156
Patent
active
059589140
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to new cephem compounds and pharmaceutically acceptable salts thereof.
More particularly, it relates to new cephem compounds and pharmaceutically acceptable salts thereof, which have antimicrobial activities, to processes for preparation thereof, to pharmaceutical composition comprising the same and to a method for treating infectious diseases in human being and animals.
Accordingly, one object of the present invention is to provide the cephem compounds and pharmaceutically acceptable salts thereof, which show highly activity against a number of pathogenic microorganisms.
Another object of the present invention is to provide processes for the preparation of the cephem compounds and salts thereof.
A further object of the present invention is to provide a pharmaceutical composition comprising, as an active ingredient, said cephem compounds or their pharmaceutically acceptable salts.
Still further object of the present invention is to provide a method for treating infectious diseases caused by pathogenic microorganisms, which comprises administering said cephem compounds to infected human being or animals.
DISCLOSURE OF INVENTION
The object cephem compounds of the present invention are novel and can be represented by the following general formula (I): ##STR2## wherein R.sup.1 is amino or protected amino, R.sup.2 is hydrogen or hydroxy protective group, substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio or optionally substituted heterocyclic-thio(lower)alkylthio, and
The object compound (I) of the present invention can be prepared by the following processes. ##STR3## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined above, imino protective group and
Regarding the compounds (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih) and (III), it is to be understood that said compounds include syn isomer(Z), anti isomer (E) and a mixture thereof.
For example, with regard to the object compound (I), syn isomer(Z) means one geometrical isomer having the partial structure represented by the following formula: ##STR4## (wherein R.sup.1, R.sup.2 and R.sup.5 are each as defined above), and anti isomer(E) means the other geometrical isomer having the partial structure represented by the following formula ##STR5## (wherein R.sup.1, R.sup.2 and R.sup.5 are each as defined above), and all of such geometrical isomers and mixture thereof are included within the scope of this invention. geometrical isomers and mixture thereof are represented for convenient sake by the following formula: ##STR6## (wherein R.sup.1, R.sup.2 and R.sup.5 are each as defined above).
It is to be noted that the compound (I) and the other compounds of this invention may include one or more stereoisomers due to asymmetric carbon atom(s), and all of such isomers and mixture thereof are included within the scope of this invention.
In the above and subsequent descriptions of the present specification, suitable examples and illustrations of the various definitions, which the present invention include within the scope thereof, are explained in detail as follows.
The term "lower" is intended to mean 1 to 6 carbon atom(s) unless otherwise indicated.
Suitable "lower alkyl" may include straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, t-butyl, pentyl, hexyl, and the like, in which more preferred one may be C.sub.1 -C.sub.4 alkyl and the most preferred one may be methyl, ethyl or propyl.
Suitable "lower alkenyl" may be straight or branched ones such as vinyl, allyl, 2-butenyl, 2-methyl-3-butenyl, 3-pentenyl, 1-hexenyl, or the like, in which the preferred one may be (C.sub.2 -C.sub.4)alkenyl.
Suitable "aryl" may include phenyl, naphthyl and the like.
Suitable "protected amino" may include an acylamino or an amino group substituted by a conventional protecting group such as ar (lower) alkyl which may have suitable substituent(s) (e.g. benzyl, trityl, etc.) or the like.
Suitable
REFERENCES:
patent: 4452851 (1984-06-01), Takaya
Mochida, Chem Abs 110, 114556, May 1986.
Eikyu Yoshiteru
Kawabata Kohji
Okuda Shinya
Takasugi Hisashi
Yamamoto Hirofumi
Berch Mark L.
Fujisawa Pharmaceutical Co. Ltd.
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