KR890002180A - Cephalosporin derivatives - Google Patents

Cephalosporin derivatives Download PDF

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KR890002180A
KR890002180A KR1019870006965A KR870006965A KR890002180A KR 890002180 A KR890002180 A KR 890002180A KR 1019870006965 A KR1019870006965 A KR 1019870006965A KR 870006965 A KR870006965 A KR 870006965A KR 890002180 A KR890002180 A KR 890002180A
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compound
lower alkyl
group
amino
salt
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KR1019870006965A
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Korean (ko)
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미쓰요시 와가쓰마
도요나리 오오이네
도오따로오 야마구찌
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아다찌 게이지로오
다나베 세이야꾸 가부시기 가이샤
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Priority to KR1019870006965A priority Critical patent/KR890002180A/en
Publication of KR890002180A publication Critical patent/KR890002180A/en

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Abstract

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Description

세팔로스포린 유도체Cephalosporin derivatives

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (13)

일반식(Ⅰ)의 세팔로스포린 유도체 또는 그 염.Cephalosporin derivatives of general formula (I) or salts thereof. 위의 일반식에서 R1은 보호될 수 있는 아미노이고, R2는 질소 및 유황으로 이루어진 그룹으로 부터 선택한 1 내지 3의 헤테로 원자를 갖는 치환 또는 비치환된 복소환기이고, R3은 보호될 수 있는 카르복실기이거나 -COO-이다.In the above general formula, R 1 is amino which can be protected, R 2 is a substituted or unsubstituted heterocyclic group having 1 to 3 hetero atoms selected from the group consisting of nitrogen and sulfur, and R 3 can be protected carboxyl or -COO - is. 제1항에 있어서, R2가 다음 일반식의 기인 화합물 또는 그 염.The compound or a salt thereof according to claim 1, wherein R 2 is a group of the following general formula. 위의 기에서, R4는 저급알케닐, 치환 또는 비치환된 5 또는 6원의 질소함유 복소환, 아실아미노이거나 치환 또는 비치환된 저급알킬이고, R5및 R6은 동일 또는 상이하며 각각 수소, 저급알킬, 아미노, 아실아미노, 카르복실, 카르바모일, 티오 카르바모일 또는 저급알콕시 카르보닐이고, R7, R8및 R9는 각각 저급알킬이고, V 및 W는 동일 또는 상이하며, -CH= 또는 -N=이고, Q1및 Q2는 인접한 두개의 탄소원자와 함께 5 내지 6원의 환기를 형성할 수 있는데, 환중에는 질소원자가 함유될 수 있고, R3은 -COO-이다.In the above groups, R 4 is lower alkenyl, substituted or unsubstituted 5 or 6 membered nitrogen-containing heterocycle, acylamino or substituted or unsubstituted lower alkyl, and R 5 and R 6 are the same or different and each Hydrogen, lower alkyl, amino, acylamino, carboxyl, carbamoyl, thio carbamoyl or lower alkoxy carbonyl, R 7 , R 8 and R 9 are each lower alkyl, V and W are the same or different and , -CH = or -N = a, Q 1 and Q 2 is can form the ventilation of 5 to 6 with the two adjacent carbon atoms, may be included during the ring nitrogen atom, R 3 is -COO - to be. 제2항에 있어서, R2가 일반식(a)의 기인 화합물 또는 그 염.The compound according to claim 2 or a salt thereof, wherein R 2 is a group of formula (a). 위의 일반식에서, R4는 저급알케닐, 피리딜, 옥소피롤리디닐, 아실아미노이거나 치환 또는 비치환 저급알킬인데, 치환기는 시아노, 하이드록실, 저급알콜깃, N-(저급알킬)카르바모일옥시, 카르복실, 아미노, N,N-디(저급알킬)아미노, 아실아미노, (N-(저급알킬)카르바모일)아미노, (N-(저급알킬)티오카르바모일)아미노, 저급알콕시 카르보닐아미노, 저급알킬티오, 페닐, 카르바모일페닐, 2-(저급알킬)-1,3,4-티아디아졸-5-일 및 식로 이루어진 그룹에서 선택한 것인데, 위 식에서 Ra및 Rb는 동일 또는 상이하며, 수소, 저급알킬, 하이드록실, 아미노 또는 저급알케닐이거나, Ra및 Rb는 인접한 질소원자와 함께 모프롤리노기를 형성하고, Z는 산소 또는 유황이며, R5, R6, V 및 W는 제2항에서 정의한 바와 같다.In the formula above, R 4 is lower alkenyl, pyridyl, oxopyrrolidinyl, acylamino or substituted or unsubstituted lower alkyl, wherein the substituents are cyano, hydroxyl, lower alcohol, N- (lower alkyl) Barmoyloxy, carboxyl, amino, N, N-di (lower alkyl) amino, acylamino, (N- (lower alkyl) carbamoyl) amino, (N- (lower alkyl) thiocarbamoyl) amino, Lower alkoxy carbonylamino, lower alkylthio, phenyl, carbamoylphenyl, 2- (lower alkyl) -1,3,4-thiadiazol-5-yl and formula In which R a and R b are the same or different and are hydrogen, lower alkyl, hydroxyl, amino or lower alkenyl, or R a and R b together with adjacent nitrogen atoms And Z is oxygen or sulfur and R 5 , R 6 , V and W are as defined in claim 2. 제3항에 있어서, R2가 아래 일반식의 기인 화합물 또는 그 염.The compound according to claim 3, or a salt thereof, wherein R 2 is a group of the general formula: 위 일반식에서, R4, R5및 R6은 제3항에서 정의한 바와같고, V 및 W는 -CH=이다.In the above general formula, R 4 , R 5 and R 6 are as defined in claim 3, and V and W are -CH =. 제 4항에 있어서, R5및 R6이 수소인 화합물 또는 그 염.The compound or a salt thereof according to claim 4, wherein R 5 and R 6 are hydrogen. 제 4항에 있어서, R2가 일반식(a')의 기인 화합물 또는 그 염.The compound according to claim 4 or a salt thereof, wherein R 2 is a group of formula (a '). 위의 일반식에서, R4는 저급알케닐, 피리딜, 저급알킬, N-(저급알킬)카르바모일-치환된 저급알킬 또는 페닐치환된 저급알킬이고, R5및 R6은 제4항에서 정의한 바와 같다.In the above formula, R 4 is lower alkenyl, pyridyl, lower alkyl, N- (lower alkyl) carbamoyl-substituted lower alkyl or phenylsubstituted lower alkyl, and R 5 and R 6 are As defined. 제6항에 있어서, R5및 R6가 수소인 화합물 또는 그 염.The compound or a salt thereof according to claim 6, wherein R 5 and R 6 are hydrogen. 제6항에 있어서, R4가 저급알케닐 또는 저급알킬이고, R5및 R6은 수소인 화합물 또는 그 염.The compound or a salt thereof according to claim 6, wherein R 4 is lower alkenyl or lower alkyl, and R 5 and R 6 are hydrogen. 제2항 내지 제8항의 어느 한항에 있어서, R1이 아미노인 화합물.The compound of any one of claims 2-8, wherein R 1 is amino. 제1항에 있어서, 화합물이 7β-{(Z)-2-(2-아미노티아졸-4-일)-2-[((3S)-2-옥소피롤리딘-3-일)옥시이미노]아세트 아미도}-3-(1-메틸-40-피리디니오)티오메틸-3-세펨-4-카르복실레이트인 화합물.The compound of claim 1, wherein the compound is 7β-{(Z) -2- (2-aminothiazol-4-yl) -2-[((3S) -2-oxopyrrolidin-3-yl) oxyimino ] Acet amido} -3- (1-methyl-40-pyridinio) thiomethyl-3-cepem-4-carboxylate. 제1항에 있어서, 화합물 7β-{(Z)-2-(2-아미노티아졸-4-일)-2-[((3S)-2-옥소피롤리딘-3-일)옥시이미노]아세트 아미도}-3-(1-메틸-2-피리디니오)티오메틸-3-세펨-4-카르복실레이트인 화합물.The compound of claim 1, wherein the compound 7β-{(Z) -2- (2-aminothiazol-4-yl) -2-[((3S) -2-oxopyrrolidin-3-yl) oxyimino] Acet amido} -3- (1-methyl-2-pyridinio) thiomethyl-3-cepem-4-carboxylate. 제1항에 있어서, 화합물이 7-{(Z)-2-(2-아미노티아졸-4-일)-2-[((3S)-2-옥소피롤리딘-3-일)옥시이미노]아세트 아미도}-3-(1-알릴-2-피리디니오)티오메틸-3-세펨-4-카르복실레이트인 화합물.The compound of claim 1, wherein the compound is 7-{(Z) -2- (2-aminothiazol-4-yl) -2-[((3S) -2-oxopyrrolidin-3-yl) oxyimino ] Acet amido} -3- (1-allyl-2-pyridinio) thiomethyl-3-cepem-4-carboxylate. 제1항에 있어서, R2가 아래 일반식의 기인 화합물 또는 그 염.The compound or salt thereof according to claim 1, wherein R 2 is a group of the formula 위의 일반식의 기에서 R5, R6, R7, R8, R9, V, W, Q1및 Q2는 제2항에서 정의한 바와 같고, R3은 보호될 수 있는 카르복실기이다.In the group of the general formula above, R 5 , R 6 , R 7 , R 8 , R 9 , V, W, Q 1 and Q 2 are as defined in claim 2 and R 3 is a carboxyl group which can be protected. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019870006965A 1987-07-01 1987-07-01 Cephalosporin derivatives KR890002180A (en)

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