KR920021559A - Novel cefem derivatives and preparation method - Google Patents

Abstract

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Novel cefem derivatives and preparation method

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Claims (21)

Cephalosporin derivatives of formula (I) and pharmaceutically acceptable nontoxic salts thereof and physiologically hydrolysable esters, hydrates or solvates thereof Wherein R ¹ is a lower alkyl group, or -C (R ^a ) (R ^b ) COOH, wherein R ^a , R ^b may be the same or different when R ¹ is represented by -C (R ^a ) (R ^b ) COOH Each represent hydrogen or a lower alkyl group, and R ² is an amino group or a lower alkyl group. The term "lower" here refers to C ₁ to C ₂ carbon atoms. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (methoxyimino) acetamido] -3- (4,6-diamino-1- Ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable esters, hydrates and solvates thereof. 7-[(Z) -2 (2-aminothiazol-4-yl) -2- (carboxymethoxyimino) acetamido] -3- (4,6-diamino-1- Ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable esters, hydrates and solvates thereof. The compound of claim 1, wherein 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (1-carboxyate-1-oxyimino) acetamido] -3 (4,6- Diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester thereof, Hydrates and solvates. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxyprop-2-oxyimino) acetamido] -3- (4,6 -Diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester thereof , Hydrates and solvates. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (methoxyimino) acetamido] -3- (4,6-diamino-1- Ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable esters, hydrates and solvates thereof. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (carboxymethoxyimino) acetamido] -3- (4,6-diamino-1 Ethyl-l, 3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester, hydrate and solvate thereof . 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (1-carboxy-1-oxyimino) acetamido] -3- (4,6) -Diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester thereof , Hydrates and solvates. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxylop-2-oxyimino) acetamido] -3- (4,6) -Diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or pharmacologically acceptable nontoxic salt thereof, physiologically hydrolysable ester thereof , Hydrates and solvates. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (methoxyimino) acetamido] -3-(-4,6-triamino-1 according to claim 1 , 3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable esters, hydrates and solvates thereof. 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (carboxymethoxyimino) acetamido] -3-(-4,6-triamino- according to claim 1 1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable nontoxic salt thereof, physiologically hydrolysable ester, hydrate and solvate thereof. 7-[(Z) -2-C-aminothiazol-4-yl) -2- (1-carboxy-1-oxyimino) acetamido] -3-(-4,6 -Triamino-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable nontoxic salt thereof, physiologically hydrolysable ester, hydrate and solvent thereof freight. The compound according to claim 1, wherein 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxylop-2-oxyimino) acetamido] -3-(-4, 6-triamino-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate or a pharmaceutically acceptable nontoxic salt thereof, physiologically hydrolysable ester thereof, hydrate and Solvates. By reacting a compound of formula (III) with a compound of formula (IV) in the presence of a solvent, the compound of formula (II) or a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester, hydrate and solvent How to manufacture a cargo. Wherein R ¹ is a lower alkyl group, or ^{-C (R a) (R b} ) COOH [ wherein R ¹ is ^{-C (R a) (R b} ) R a, R b be displayed in the COOH may be the same or different, Each represent hydrogen or a lower alkyl group, and R ² is an amino group or a lower alkyl group. The term "lower" here refers to C ₁ to C ₂ carbon atoms. The method according to claim 14, wherein the solvent used is water or a mixed aqueous solution of water and a water miscible solvent. 16. The method of claim 15, wherein the water-thermotable solvent is acetonitrile, acetone. The method according to claim 14, wherein the amount of the compound of formula (IV) is 1 to 1.5 equivalents based on the compound of formula (III). The method according to claim 14, wherein the pH of the reaction solvent is 7.0 to 7.5. The method of claim 14, wherein the reaction is carried out in the presence of a stabilizer. The method of claim 19, wherein the stabilizing agent is sodium iodide, potassium iodide, bromosodium. A method of selecting one of bromopotassium or potassium thiocyanate. A therapeutically effective amount and pharmaceutical composition of at least one compound as an active ingredient in a compound as defined in claims 1 to 3, a pharmaceutically acceptable nontoxic salt thereof, a physiologically hydrolysable ester, hydrate or solvate thereof Method comprising an acceptable carrier, excipient or other additives. ※ Note: The disclosure is based on the initial application.