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US 4,375,542 AGranted
Kijanimicin antibiotics and derivatives thereof
AssigneeSchering Corporation
InventorsJay A. Waitz, Mahesh G. Patel, Ann C. Horan
Life of this patent
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Abstract
Actinomadura Kijaniata nov. sp produces a novel antibiotic which we have designated kijanimicin. The antibiotic or cationic salts thereof exhibit anti-acne, antitumor, antimalarial, antibacterial and anti-inflammatory activity.
Claims7
Kijanimicin, having the following physicochemical characteristics:
- (a) A melting point with decomposition of 174.5.degree. C.;
- (b) A specific optical rotation as measured at the D line of sodium of 25.degree. C. of -116.4.degree..+-. at 0.3% in methanol;
- (c) Ultra-violet absorption maxima in 2,2,2-trifluoroethanol at 99 nm (E.sub.1 cm.sup.1% 328.4), 242 nm (E.sub.1 cm.sup.1% 56.2), 264 nm (E.sub.1 cm.sup.1% 63.1) and 274 nm (E.sub.1 cm.sup.1% 60.7);
- (d) Infrared Spectrum, lambda max (CHCL.sub.3) 3690, 3620, 3540, 3480, 3440, 2970, 2940, 1755, 1733, 1623, 1545, 1515, 1318, 1232, 1130, 1060 cm.sup.-1 ;
- (e) .sup.13 C-NMR Nuclear Magnetic Resonance .delta.C (CDCL.sub.3) 206.2, 201.5, 167.1, 157.4, 141.5, 137.1, 135.7, 126.7, 125.8, 123.6, 121.5, 119.3, 101.9, 99.8, 98.2, 97.1, 92.2, 91.0, 90.8, 84.5, 83.3, 82.6, 79.6, 78.4, 72.4, 71.8, 69.1, 68.1, 67.5, 67.1, 66.8, 65.1, 64.9, 64.4, 63.8, 62.6, 57.3, 53.8, 53.2, 52.7, 51.0, 43.1, 41.6, 40.2, 38.5, 36.8, 35.7, 35.5, 34.8, 34.4, 31.3, 31.1, 29.9, 29.7, 27.9, 25.3, 22.2, 18.4, 17.9,
- (f) .sup.1 H Nuclear Magnetic Resonance .delta.H (CDCl.sub.3)0.65 (2H,m), 1.06 (3H,d,J=7 H.sub.z), 1.18 (3H,d,J-6H.sub.z), 1.20-1.40 (envelop of signals), 1.60 (3H,S), 1.64 (3H,S), 3.45 (3H,S), 3.76 ppm (3H,S);
- (g) and having a planar structural formula substantially as follows:
- ##STR2## and the non-toxic pharmaceutically acceptable cationic salts thereof.
5 more elements
A salt of kijanimicin as defined in claim 5 selected from the group consisting of sodium, potassium, rubidium, N-methylglucamine and diethylamine.
Dependencies are inferred from the claim text.