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Title:
QUATERNARY AMMONIUM SALT COMPOUNDS OF SPIROCYCLOPIPERAZINES, PREPARATION METHODS AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2007/147346
Kind Code:
A1
Abstract:
Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically accepted salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A selected from bond, or substituted or unsubstituted hydrocarbon radical;R2, R3 each other independently is selected from hydrogen or methyl, which linked with the any position of spiro structure; n and m are integer of 0~2, and do not represent 0 at same time; B, D each other independently is lineared or branched alkylene; Y is selected from –CHR4-, O, S, -S(O)-, -SO2-, -NR4 or substituted or unsubstituted phenylene, in which R4 selected from H, saturated or unsaturated C1-C6-alkyl, substituted or unsubstituted aryl, or heteroaryl substituted methyl or ethyl; X- is pharmaceutically accepted inorganic or organic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.

Inventors:
LI RUNTAO (CN)
SUN QI (CN)
YE JIA (CN)
YUE CAIQIN (CN)
WANG XIN (CN)
GE ZEMEI (CN)
LI CHANGLING (CN)
CHENG TIEMING (CN)
Application Number:
PCT/CN2007/001887
Publication Date:
December 27, 2007
Filing Date:
June 15, 2007
Export Citation:
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Assignee:
UNIV BEIJING (CN)
LI RUNTAO (CN)
SUN QI (CN)
YE JIA (CN)
YUE CAIQIN (CN)
WANG XIN (CN)
GE ZEMEI (CN)
LI CHANGLING (CN)
CHENG TIEMING (CN)
International Classes:
C07D487/10; A61K31/495; A61K31/499; A61P25/04; C07D295/06; C07D471/10; C07D498/10; C07D513/10; C07D519/00
Foreign References:
CN1344717A2002-04-17
CN1734385A2006-02-15
CN1344717A2002-04-17
Other References:
GAO F.-L. ET AL.: "Unique spirocyclopiperazinium salt. I: synthesis and structure-Activity relationship of spirocyclopiperazinium salts as analgesics", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 13, no. 9, 2003, pages 1535 - 1537, XP002420363
CHEMICAL ABSTRACTS, vol. 142, 2005, Columbus, Ohio, US; abstract no. (142:482060), XP008101272
CHEMICAL ABSTRACTS, vol. 131, 1999, Columbus, Ohio, US; abstract no. (131:228607), XP008101274
CHEMICAL ABSTRACTS, vol. 115, 1991, Columbus, Ohio, US; abstract no. 115:193160, XP008101659
WANG X. ET AL.: "Unique spirocyclopiperazinium salts. Part 2. Synthesis and structure-activity relationship of bisspirocyclopiperazinium salts as analgesics", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 13, no. 10, 2003, pages 1729 - 1732, XP008100983
See also references of EP 2036909A4
Attorney, Agent or Firm:
BEIJING SUNHOPE INTELLECTUAL PROPERTY LTD. (Kunxun Plaza Zhichun Road 9, HaidianDistrict, Beijing 3, CN)
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