US 7,485,755 B2
Acid addition salt of carbasugar amine derivative
Kiyoshi Suzuki, Tokyo (Japan); Masami Iida, Kanagawa (Japan); Yuji Kaneda, Tokyo (Japan); Naoko Kajimoto, Tokyo (Japan); and Miwa Sawa, Saitama (Japan)
Assigned to Seikagaku Corporation, Tokyo (Japan)
Appl. No. 10/557,851
PCT Filed May 19, 2004, PCT No. PCT/JP2004/007138
§ 371(c)(1), (2), (4) Date Nov. 21, 2005,
PCT Pub. No. WO2004/101493, PCT Pub. Date Nov. 25, 2004.
Claims priority of application No. 2003-140868 (JP), filed on May 19, 2003.
Prior Publication US 2007/0010585 A1, Jan. 11, 2007
Int. Cl. C07C 211/40 (2006.01); A61K 31/13 (2006.01)
U.S. Cl. 564—462  [514/659] 27 Claims
 
1. An acid addition salt of a carba-sugar amine derivative of formula (1):

OG Complex Work Unit Drawing
wherein R1 and R2 each independently is a hydrogen atom, or an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group which may have one or two of the following substituents (I) or (II), or R1 and R2 are taken together to be a substituent (III):

OG Complex Work Unit Drawing
wherein R8 to R12 each independently is an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group;
with the proviso that both R1 and R2 are not a hydrogen atom at the same time;
R3, R4 and R7 each independently is a hydroxyl group or a hydroxyl group having a substituent; and
R5 and R6 each independently is a hydrogen atom, a hydroxyl group or a hydroxyl group having a substituent, with the proviso that when one of R5 and R6 is a hydrogen atom, the other is a hydroxyl group or a hydroxyl group having a substituent,
wherein the hydroxyl group having a substituent at positions R3-R7 is a hydroxyl group where the hydrogen of the hydroxyl group is replaced with a substituent selected from the group consisting of an aralkyl group, a silyl group, an alkanoyl group, an aroyl group, an alkoxyalkyl group, and a aralkyloxyalkyl group or wherein two hydroxyl groups at positions R3-R7 together form a substituent selected from the group consisting of an alkylidene group, an isopropylidene group, and an aralkylidene group,
wherein said salt of a carba-sugar amine derivative is a hydrochloride or sulfate salt.