1-Hydroxy-1,3-dihydro-benzo[c][1,2]oxaboroles and their derivatives

• Main Authors: SINGH, RAJESHWAR, PLATTNER, JACOB, J, ZHANG, YONG-KANG, SHARMA, RASHMI, HA, MINH, HERNANDEZ, VINCENT, S, LU, XIAOSONG, NIEMAN, JAMES, A, BAKER, STEPHEN, J, MOHAMMAD, RAHIM, PHILLIPS, JAMES G, ZHOU, HUCHEN, AKAMA, TSUTOMA, XIA, YI, ALLEY, MICHAEL, RICHARD, KEVIN, KERAMANE, EL MEHDI
• Format: Patent
• Language: English
• Published: 27.07.2012
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; CHEMISTRY; FISHING; FORESTRY; HUMAN NECESSITIES; HUNTING; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; TRAPPING

Disclosed are 1-hydroxy-1,3-dihydro-benzo[c][1,2]oxaboroles and their derivatives as represented by the general formula (I), wherein: R* is H; R3 is selected from H, cyano, substituted or unsubstituted nitroalkyl and substituted or unsubstituted aminoalkyl; Ra is YR5; wherein Y is O or S; R5 is selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl; and with the proviso that when R3 is H, Ra is not unsubstituted benzyloxy, Ra is not -OCH2COOH, Ra is not -OCH3 or Ra is not -OCH2CH3; or a salt, hydrate or solvate or anhydride thereof. Of particular importance is the compound (S)-1-hydroxy-3-aminomethyl-7-(3-hydroxypropyloxy)-3H-benzo[c][1,2]oxaborole. Further disclosed is a pharmaceutical formulation which comprises: a compound as defined above, or a pharmaceutically acceptable salt, hydrate, solvate or anhydride thereof, and a pharmaceutically acceptable excipient; for killing or preventing the growth of a microorganism, or for treating a bacterial infection in a mammal.