KR970061897A - New cephalosporin antibiotics - Google Patents

New cephalosporin antibiotics Download PDF

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Publication number
KR970061897A
KR970061897A KR1019960003219A KR19960003219A KR970061897A KR 970061897 A KR970061897 A KR 970061897A KR 1019960003219 A KR1019960003219 A KR 1019960003219A KR 19960003219 A KR19960003219 A KR 19960003219A KR 970061897 A KR970061897 A KR 970061897A
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KR
South Korea
Prior art keywords
cephem
carboxylate
protecting group
hydrogen
carboxy
Prior art date
Application number
KR1019960003219A
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Korean (ko)
Other versions
KR0177900B1 (en
Inventor
방찬식
이창석
오성호
오정인
김용주
Original Assignee
성재갑
주식회사 Lg 화학
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Priority to KR1019960003219A priority Critical patent/KR0177900B1/en
Publication of KR970061897A publication Critical patent/KR970061897A/en
Application granted granted Critical
Publication of KR0177900B1 publication Critical patent/KR0177900B1/en

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Abstract

The present invention relates to 7- (Z) -2- (aminothiazol-4-yl) -2- ( -Carboxy-3,4-substituted benzyloxyimino) acetamide group and at the same time introduced with an ethene group substituted by a heterocycle at the C-3 position, has strong microbial activity, broad spectrum antimicrobial spectrum and improved pharmacokinetic properties A physiologically hydrolyzable ester, a solvate thereof, an isomer thereof, and an antimicrobial agent composition containing the same as an active ingredient.

Represents the above formula, Q is CH or N, R 1 represents a hydrogen or an amino protecting group, R 2 and R 3 are the same or different, each independently represent hydrogen or a hydroxy protecting group, the R 2 and R 3 Together form a cyclic diol protecting group, R 4 and R 5 represent hydrogen or a carboxyl protecting group, R 6 represents a heterocyclic compound of the following formula,

Wherein R 7 and R 8 are each independently hydrogen, substituted or unsubstituted amino, hydroxy, alkoxy, C 1 -C 4 alkyl, carboxylalkoxycarbonyl or halogen, R 9 is C 1 -C 4 Alkyl, C 3 -C 4 alkenyl, carboxymethyl or amino.

Description

New cephalosporin antibiotics

Since this is a trivial issue, I did not include the contents of the text.

Claims (5)

A compound of the general formula (I), a pharmaceutically acceptable non-toxic salt thereof, a physiologically hydrolyzable ester, a solvate and an isomer thereof. Represents the above formula, Q is CH or N, R 1 represents a hydrogen or an amino protecting group, R 2 and R 3 are the same or different, each independently represent hydrogen or a hydroxy protecting group, the R 2 and R 3 Together form a cyclic diol protecting group, R 4 and R 5 represent hydrogen or a carboxyl protecting group, R 6 represents a heterocyclic compound of the following formula, Wherein R 7 and R 8 are each independently hydrogen, substituted or unsubstituted amino, hydroxy, alkoxy, C 1 -C 4 alkyl, carboxylalkoxycarbonyl or halogen, R 9 is C 1 -C 4 Alkyl, C 3 -C 4 alkenyl, carboxymethyl or amino. 3. A compound according to claim 1 , wherein R 1 , R 4 and R 5 are hydrogen, R 2 and R 3 are each independently hydrogen or acetyl, R 7 and R 8 are each independently hydrogen, halogen or C 1 -C 4 Alkyl, and R < 9 > is methyl. The method according to claim 1, wherein 7 - [(Z) -2- ( - (carboxy-3,4-dihydroxybenzyloxyimino) -2- (2-aminothiazol-4-yl) acetamido] -3- ] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( -3 - [(Z) -2- (2-thiophenyl) -ethynyl] -carbodiimide Yl] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( - (carboxy-3,4-dihydroxybenzyloxyimino) -2- (2-aminothiazol-4-yl) acetamido] -3- ] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( - (carboxy-3,4-dihydroxybenzyloxyimino) -2- (2-aminothiazol-4-yl) acetamido] -3- Yl) ethynyl] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( - (carboxy-3,4-dihydroxybenzyloxyimino) -2- (2-aminothiazol-4-yl) acetamido] -3- ] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( (Z) -2- (N-methylpyrrol-2-yl) -acetic acid ethyl ester Yl) ethenyl] -3-cephem-4-carboxylate (S and R); 7 - [(Z) -2- ( -3 - [(Z) -2- (2-imidazolyl) ethynyl] -3- (4-hydroxybenzyloxyimino) -2- Yl] -3-cephem-4-carboxylate (S and R); Or 7 - [(Z) -2- ( -3 - [(Z) -2- (N-methylimidazole-2-carboxy-3,4-dihydroxybenzyloxyimino) -2- Yl) ethenyl] -3-cephem-4-carboxylate (S and R). An antimicrobial composition comprising the compound of claim 1 as an active ingredient and combined with a pharmaceutically acceptable excipient, 5. The composition of claim 4 containing 50 to 1,500 mg of the compound of claim 1 in a unit dose. ※ Note: It is disclosed by the contents of the first application.
KR1019960003219A 1996-02-09 1996-02-09 Novel cephalosporin antibiotics KR0177900B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019960003219A KR0177900B1 (en) 1996-02-09 1996-02-09 Novel cephalosporin antibiotics

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019960003219A KR0177900B1 (en) 1996-02-09 1996-02-09 Novel cephalosporin antibiotics

Publications (2)

Publication Number Publication Date
KR970061897A true KR970061897A (en) 1997-09-12
KR0177900B1 KR0177900B1 (en) 1999-03-20

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KR1019960003219A KR0177900B1 (en) 1996-02-09 1996-02-09 Novel cephalosporin antibiotics

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20000002217A (en) * 1998-06-18 2000-01-15 김종인 Novel cephalosporin antibiotics and manufacturing method of it

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20000002217A (en) * 1998-06-18 2000-01-15 김종인 Novel cephalosporin antibiotics and manufacturing method of it

Also Published As

Publication number Publication date
KR0177900B1 (en) 1999-03-20

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