ANTIBIOTIC CARBAPENEM DERIVATIVES

• Main Authors: BETTS, MICHAEL JOHN, SWAIN, MICHAEL LINGARD
• Format: Patent
• Language: English; Korean
• Published: 15.06.1999
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

본 발명은 하기 일반식(Ⅰ)의 카르바페넴 화합물, 또는 그것의 약학적 허용염 또는 그것의 생체내 가수분해성 에스테르에 관한 것이다 : 상기 식에서, R은 1-히드록시에틸, 1-플루오로에틸 또는 히드록심메틸이고: R는 수소 또는 C알킬이고: R는 수소 또는 C알킬이고: R는 히드록시 또는 카르복시이며: 페닐 고리는 할로, 시아노, C알킬, 니트로, 히드록시, 카르복시, C알콜시, 트리플루오로메틸, C알콜시카르보닐, 카르바모일, C알킬카르바모일, 디-C알킬카르바모일, 아미노, C알킬아미노, 디-C알킬아미노, 설폰산, C알킬 S(0)n-(이때, n은 0 내지 2임), N-C알칸설폰아민도, C알카노일아미노 및 C알카노일(N-C알킬)아미노로부터 선택되는 하나 또는 두개의 치환체에 의해 더 치환되거나 또는 치환되지 않으며 ; 단, 페닐 고리가 하나 이상의 카르복시에 의해 치환되어 있을 것을 조건으로 한다. A carbapenem compound of the formula (I) wherein: R is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R is hydrogen or C1-4alkyl; R is hydrogen or C1-4alkyl; R is hydroxy or carboxy; and the phenyl ring is optionally further substituted by one or two substitutents selected from halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, trifluoromethyl, C1-4alkoxycarbonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl, amino, C1-4alkylamino, di-C1-4alkylamino, sulphonic acid, C1-4alkylS(O)n- (wherein n is 0-2), N-C1-4alkanesulphonamido, C1-4alkanoylamino and C1-4alkanoyl(N-C1-4alkyl)amino: provided that the phenyl ring is substituted by at least one carboxy; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.