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US20060128807: Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof


Filing Information

Inventor(s) Junichi Kobayashi · Tetsuya Nakamura · Ritsu Suzuki · Hideyuki Muranaka · Tomonaga Ozawa · Yuichiro Kai · Takehiro Ishikawa · Tatsuhiro Kondo · Tetsuro Tamai · Satoshi Akahane ·
Correspondent SUGHRUE MION, PLLC ·
Application Number US10545380
Filing date 01/30/2004
PCT 371 date 08/12/2005
Publication date 06/15/2006
Predicted expiration date 01/30/2024
U.S. Classifications 514/567  · 562/442  ·
International Classifications A61K31195  · C07C22922  ·
Kind CodeA1
PCT Application Number WO20PCTJP0400893 - 01/30/2004
Foreign Priority JP03584772003 - 02/14/2003 · JP0419312003 - 02/20/2003 ·
18 Claims, No Drawings


The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Independent Claims | See all claims (18)

  1. 1. A compound represented by general formula (I): a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein each of R1 and R2 is independently a hydrogen atom or a lower alkyl group; each of R3, R4, R5 and R6 is independently a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; each of R7 and R8 is independently a hydrogen atom, a halogen atom, a lower alkyl group, a halo-lower alkyl group, a hydroxy-lower alkyl group, a cycloalkyl group, a heterocycloalkyl group, a lower alkoxy group, a di(lower alkyl)amino group, a cyclic amino group, a di(lower alkyl)amino-lower alkyl group, an aryl group, an aryloxy group, an aralkyloxy group, a heteroaryl group, a cyano group, a hydroxyl group, a lower acyl group, a lower alkylsulfanyl group, a lower alkylsulfonyl group, a carboxy group, a lower alkoxycarbonyl group or an aralkyloxycarbonyl group, or when R7 and R8 are adjacent each other, R7 and R8 are bonded together to form —O—(CH2)m—O—, —O—(CH2)n— or —(CH2)p—, wherein m is an integer of 1 to 3, n is an integer of 2 to 4, p is an integer of 3 to 5; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, wherein R10 is a hydroxyl group, a lower alkoxy group, an aralkyloxy group or —NR11R12, each of R11 and R12 is independently a hydrogen atom, a lower alkyl group, a carboxy-lower alkyl group or a lower alkoxycarbonyl-lower alkyl group, or R11 and R12, together with the nitrogen atom to which they are bonded, form a cyclic amine, A1 is a lower alkylene group or a lower alkenylene group, and A2 is a lower alkylene group.

References Cited

The current document has no citations.

Referenced By

Document NumberAssigneeInventorsIssue/Pub Date
US7579507 Kissei Pharmaceutical Co., Ltd. Kiyoshi Kasai et al. Aug 2009