Novel cephalosporin compounds and process for preparing same

• Main Authors: YOON, HA SIK, JANG, YONG JIN, LEE, SEONG BAEK, LEE, CHANG SEOK, LEE, HYANG SUK, OH, SEONG HO, KIM, GEUN TAE, RYU, EUN JEONG
• Format: Patent
• Language: English; Korean
• Published: 17.01.2002
• Edition: 7
• Subjects: 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

PURPOSE: Provided are novel cephalosporin compounds of the formula(1), its pharmaceutically acceptable nontoxic salt, physiologically hydrolyzable ester, solvate, hydrate and enantiomers. And their preparing process is also provided. CONSTITUTION: The novel cephalosporin compound is represented by the formula(1), wherein R1 and R2 individually represent C5-6 heteroaryl including 1-2 heteroatom selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkylthio, aryl, arylthio or nitrogen atom and oxygen atom; R3 is hydrogen or carboxyl protection group; Q is sulfur, oxygen or CH2; Z is CH or N; n is an integer of 1 or 2; Ar is heteroaryl represented by the structural formulae (wherein, X, Y, W, A, B, D, E, G and I are individually represent N or C(or CH)); R4 hydrogen or C1-C4-alkyl, or substituted or unsubstituted amino group by a substituent selected from C1-C6-alkyl and C1-C6-hydroxyalkyl; R5 an R6 are individually hydrogen, hydroxy or C1-C4-alkyl or C1-C6-alkylthio, or substituted or unsubstituted amino by a substituent selected from the group consisting of C1-C6-alkyl, C1-C6-hydroxyalkyl and C1-C6-aminoalkyl; and R7, R8, R9, R10 and R11 are individually hydrogen or C1-C6-alkyl, or substituted or unsubstituted amino by a substituent selected from the group consisting of C1-C6-alkyl, C1-C6-hydroxyalkyl and C1-C6-aminoalkyl. 본 발명은 하기 화학식 (1)의 신규 세팔로스포린 화합물, 그의 약제학적으로 허용되는 무독성염, 생리학적으로 가수분해 가능한 에스테르, 수화물, 용매화물 및 이들의 이성체, 이들을 함유하는 약제학적 조성물 및 그의 제조방법에 관한 것이다: 상기 식에서, R, R, R, Z, Q, n 및 Ar 은 각각 명세서에 정의된 의미를 갖는다.