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    • 2. 发明授权
    • 퀴놀린 카르복실산 유도체와 그 제조방법
    • QUINO / ONE衍生物
    • KR1019940002954B1
    • 1994-04-09
    • KR1019910006362
    • 1991-04-20
    • 한국화학연구원
    • 김완주박명환이태석백경업하재두김봉진남근수
    • C07D487/04
    • The quinolone carboxylic acid derivs. are prepd. by heating and reacting the cpd. (II) with the amine cpd. of formula (III) or (IIIa) in presence of the base in the solvent at 20-200 deg.C. In the formulas, R1=C1-4 alkyl, haloalkyl, hydroxyalkyl, alkenyl, C3-6 cycloalkyl or halogen-substd. phenyl; R2 is H, protecting gp. of carboxyl of pharmacentically usable metallic or organic cation; R3 is H, C1-4 lower alkyl, hydroxyalkyl, cycloalkyl or N-protecting gp. decomposable in human body; n=1,2; m=1,2 or 3; Z is H, halogen, amino or methyl, and contains pharmaceutically usuable acid added salt or its hydrate if R2 is H. (I) has excellent antibiosis to the gram positive (or negative) bacillus.
    • 喹诺酮羧酸衍生物。 是prepd 通过加热和反应cpd。 (II)与胺cpd反应。 在式(III)或(IIIa)的存在下,在溶剂中在20-200℃下。 式中R1 = C1-4烷基,卤代烷基,羟基烷基,烯基,C3-6环烷基或卤素取代基。 苯基; R2是H,保护gp。 的药物可用的金属或有机阳离子的羧基; R3是H,C1-4低级烷基,羟烷基,环烷基或N-保护基。 在人体内可分解; N = 1,2; m = 1,2或3; Z是H,卤素,氨基或甲基,并且如果R2是H,则含有药学上可用的酸加成盐或其水合物。(I)对革兰氏阳性(或阴性)杆菌具有优异的抗生素。
    • 6. 发明授权
    • 신규한 퀴놀론 화합물
    • 新颖的喹啉酮化合物
    • KR1019930006162B1
    • 1993-07-08
    • KR1019910003932
    • 1991-03-12
    • 한국화학연구원
    • 김완주박명환김은희백경업
    • C07D401/10
    • Quinolone derivs. of formula (I) and their salts are new. In (I), X=N or C-Y; Y=H,F,Cl, methoxy or methyl; Z=H, halogen or amino; R1=C1-4 alkyl, haloalkyl, hydroxyalkyl or alkenyl, C3-6 cycloalkyl, fluoro-substd. phenyl, X-O (or S) CH2CH(CH3)-N, etc.; R2=H or a cation; R3=H or lower alkyl; R4 and R5 each = H, lower alkyl, cycloalkyl or OH; m = 1 or 2. Also claimed is the prepn. of (I) which comprises a condensation reaction of the cpd. of formula (II) and the cpd. of formula (III) at 20-180 deg.C for 1-12 hr(s). The cpds. (I) have a good antibacterial activity.
    • 喹诺酮衍生物。 的式(I)及其盐是新的。 在(I)中,X = N或C-Y; Y = H,F,Cl,甲氧基或甲基; Z = H,卤素或氨基; R 1 = C 1-4烷基,卤代烷基,羟基烷基或烯基,C 3-6环烷基,氟取代基。 苯基,X-O(或S)CH 2 CH(CH 3)-N等; R2 = H或阳离子; R3 = H或低级烷基; R4和R5各自为H,低级烷基,环烷基或OH; m = 1或2.还要求是prepn。 的(I),其包含cpd的缩合反应。 的式(II)和cpd。 的式(III)在20-180℃下反应1-12小时(s)。 cpds。 (I)具有良好的抗菌活性。