Oxazolidinone derivatives and pharmaceutical compositions containing them
First Claim
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1. An oxazolidinone derivative represented by the general formula:
- ##STR61## wherein R is(a) hydrogen atom,(b) C1 -C8 alkyl,(c) C3 -C6 cycloalkyl,(d) amino,(e) C1 -C8 alkylamino,(f) C1 -C8 dialkylamino,(g) C1 -C8 alkoxy, or(h) C1 -C8 halogenoalkyl;
R1 and R3 are each and independently(a) hydrogen atom,(b) halogen atom,(c) C1 -C8 alkyl,(d) C3 -C6 cycloalkyl,(e) --(CH2)m --OR11, or(f) --C(═
O)--R41 ;
X and Y are each and independently(a) hydrogen atom, or(b) halogen atom;
R4 and R5 are each and independently(a) hydrogen atom,(b) C1 -C8 alkyl,(c) C1 -C8 alkoxy,(d) C1 -C8 alkylthio,(e) --(CH2)m --OR51,(f) --O--(CH2)m --OR51,(g) --NR42 R52,(h) --N═
CH--NR44 R55,(i) --C(═
O)--NR42 R52, or(j) --(CH2)m --C(═
A)--R41, or they may combine together to form(k) ═
O,(l) ═
NR43,(m) ═
S,(n) ═
CR44 R54, or(o) an optionally substituted, unsaturated or saturated 5- or 6-membered hetero ring having 1-3 hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom;
R11 and R12 are each and independently(a) hydrogen atom,(b) C1 -C8 alkyl, or(c) methoxymethyl;
R41 is(a) hydrogen atom,(b) --(CH2)m --OH,(c) C1 -C8 alkyl,(d) C1 -C8 alkoxy,(e) --O--CH2 --O--C(═
O)--R11, or(f) --(CH2)m --C(═
O)--OR11 ;
R42 and R52 are each and independently(a) hydrogen atom,(b) --(CH2)m --OR11,(c) C1 -C8 alkyl,(d) --C(═
O)--R41,(e) --C(═
O)--NR11 R12,(f) --(CH2)p -phenyl,(g) thiazol-2-yl, or they may combine together to form a pyrrolidino group, a piperidino group, a piperazino group, a morpholino group, or a thiomorpholino group, each of which may be substituted by C1 -C8 alkyl or --(CH2)m --OH;
R43 is(a) hydrogen atom,(b) --OR51,(c) C1 -C8 alkyl,(d) C1 -C8 alkoxy,(e) --(CH2)p -phenyl,(f) --NR42 R52,(g) --NH--C(═
NH)--NH2,(h) [1,2,4]triazol-4-yl, or(i) cyano;
R44 and R54 are each and independently(a) hydrogen atom,(b) C1 -C8 alkyl,(c) --C(═
O)--R41, or(d) --(CH2)p -phenyl;
R51 is(a) hydrogen atom,(b) C1 -C8 alkyl,(c) C1 -C8 alkyl substituted by one or more hydroxy,(d) C2 -C8 alkenyl,(e) C1 -C8 halogenoalkyl,(f) --(CH2)m --OR11,(g) --(CH2)m --C(═
O)--R41,(h) --C(═
O)--(CH2)m --OR44, or(i) tosyl;
A is(a) oxygen atom, or(b) ethyleneketal;
.sup.... is a double bond or a single bond;
m'"'"'s are each and independently 0, 1 or 2;
n is 0 or 1;
p'"'"'s are each and independently 1, 2, 3 or 4;
and C1 -C8 alkyl, in each of the above definitions, may be each and independently substituted by one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, C1 -C8 alkoxy group, C1 -C8 acyloxy group, an amino group, C1 -C8 alkylamino group, C1 -C8 dialkylamino group, --CN group and a carboxyl group,or a pharmaceutically acceptable salt thereof.
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Abstract
The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel oxazolidinone derivatives represented by chemical formula (I), or pharmaceutically acceptable salts thereof, as well as antimicrobial compositions containing said derivatives or salts thereof as active ingredients. ##STR1##
48 Citations
5 Claims
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1. An oxazolidinone derivative represented by the general formula:
- ##STR61## wherein R is
(a) hydrogen atom, (b) C1 -C8 alkyl, (c) C3 -C6 cycloalkyl, (d) amino, (e) C1 -C8 alkylamino, (f) C1 -C8 dialkylamino, (g) C1 -C8 alkoxy, or (h) C1 -C8 halogenoalkyl; R1 and R3 are each and independently (a) hydrogen atom, (b) halogen atom, (c) C1 -C8 alkyl, (d) C3 -C6 cycloalkyl, (e) --(CH2)m --OR11, or (f) --C(═
O)--R41 ;X and Y are each and independently (a) hydrogen atom, or (b) halogen atom; R4 and R5 are each and independently (a) hydrogen atom, (b) C1 -C8 alkyl, (c) C1 -C8 alkoxy, (d) C1 -C8 alkylthio, (e) --(CH2)m --OR51, (f) --O--(CH2)m --OR51, (g) --NR42 R52, (h) --N═
CH--NR44 R55,(i) --C(═
O)--NR42 R52, or(j) --(CH2)m --C(═
A)--R41,or they may combine together to form (k) ═
O,(l) ═
NR43,(m) ═
S,(n) ═
CR44 R54, or(o) an optionally substituted, unsaturated or saturated 5- or 6-membered hetero ring having 1-3 hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom; R11 and R12 are each and independently (a) hydrogen atom, (b) C1 -C8 alkyl, or (c) methoxymethyl; R41 is (a) hydrogen atom, (b) --(CH2)m --OH, (c) C1 -C8 alkyl, (d) C1 -C8 alkoxy, (e) --O--CH2 --O--C(═
O)--R11, or(f) --(CH2)m --C(═
O)--OR11 ;R42 and R52 are each and independently (a) hydrogen atom, (b) --(CH2)m --OR11, (c) C1 -C8 alkyl, (d) --C(═
O)--R41,(e) --C(═
O)--NR11 R12,(f) --(CH2)p -phenyl, (g) thiazol-2-yl, or they may combine together to form a pyrrolidino group, a piperidino group, a piperazino group, a morpholino group, or a thiomorpholino group, each of which may be substituted by C1 -C8 alkyl or --(CH2)m --OH; R43 is (a) hydrogen atom, (b) --OR51, (c) C1 -C8 alkyl, (d) C1 -C8 alkoxy, (e) --(CH2)p -phenyl, (f) --NR42 R52, (g) --NH--C(═
NH)--NH2,(h) [1,2,4]triazol-4-yl, or (i) cyano; R44 and R54 are each and independently (a) hydrogen atom, (b) C1 -C8 alkyl, (c) --C(═
O)--R41, or(d) --(CH2)p -phenyl; R51 is (a) hydrogen atom, (b) C1 -C8 alkyl, (c) C1 -C8 alkyl substituted by one or more hydroxy, (d) C2 -C8 alkenyl, (e) C1 -C8 halogenoalkyl, (f) --(CH2)m --OR11, (g) --(CH2)m --C(═
O)--R41,(h) --C(═
O)--(CH2)m --OR44, or(i) tosyl; A is (a) oxygen atom, or (b) ethyleneketal; .sup.... is a double bond or a single bond; m'"'"'s are each and independently 0, 1 or 2; n is 0 or 1; p'"'"'s are each and independently 1, 2, 3 or 4; and C1 -C8 alkyl, in each of the above definitions, may be each and independently substituted by one or more substituents selected from the group consisting of a halogen atom, a hydroxy group, C1 -C8 alkoxy group, C1 -C8 acyloxy group, an amino group, C1 -C8 alkylamino group, C1 -C8 dialkylamino group, --CN group and a carboxyl group, or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5)
- ##STR61## wherein R is
Specification
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Current AssigneePharmacia & Upjohn Company (Pfizer Inc.)
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Original AssigneePharmacia & Upjohn Company (Pfizer Inc.)
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InventorsYamada, Hiroyoshi, Taniguchi, Mikio, Munesada, Kiyotaka
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Primary Examiner(s)Ivy, C. Warren
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Assistant Examiner(s)DAHLEN, GARTH
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Application NumberUS08/714,117Time in Patent Office372 DaysField of Search540/603, 544/129, 544/364, 546/19, 546/208, 546/209, 546/210US Class Current546/209CPC Class CodesC07D 263/38 attached in position 2C07D 413/10 linked by a carbon chain co...C07D 413/14 containing three or more he...C07D 417/14 containing three or more he...C07D 491/10 Spiro-condensed systems
