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filingDate 2003-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2005-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1f8dcc69f9f0d64ac8f13904efd434b8
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publicationDate 2005-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1485352-B1
titleOfInvention Azaspiro compounds for the treatment of pain
abstract New azaspiro compounds (I) useful as medicaments. Azaspiro compounds of formula (I) and their tautomers and salts useful as medicaments are new; [Image] X1, X2H; X1+X2S or NOH; R1H; R2H, OH, CHO, COOH, halo, SH, sulfonyl, amino, amido or R7Q1; R3H, OH, amino or R8Q2; Z : 4-to 10-membered C-bonded ring that contains 0-2 O or S atoms and is optionally substituted with OH, CHO, COOH, halo, SH, sulfonyl, amino, amido or R9Q3; R7-R9A, 3-6C cycloalkyl, 2-5C alkenyl, 2-5C alkynyl, OA, COA, COOA, SA, NHA, SOA, SO2A, A'NHA, A'SA or A'OA; A : 1-5C alkyl; A' : 1-5C alkylene; Q1-Q3H, OH, CHO, COOH, halo, SH, sulfonyl, amino or amido, but Q2 is not amino; R1+R2oxo or thioxo. Independent claims are also included for: (1) a pharmaceutical composition comprising (I) and an excipient; and (2) the use of an azaspiro compound of formula (II) for producing a medicament for treating pain. [Image] X3, X4H; X3+X4S or NOH; R4, R5H, OH, CHO, COOH, halo, SH, sulfonyl, amino, amido or R10Q4; R4+R5oxo or thioxo; R6H, OH, amino or R11Q5; Z24- to 10-membered C-bonded ring that contains 0-2 O or S atoms and is optionally substituted with OH, CHO, COOH, halo, SH, sulfonyl, amino, amido or R12Q6; R10-R12A, 3-6C cycloalkyl, 2-5C alkenyl, 2-5C alkynyl, OA, COA, COOA, SA, NHA, SOA, SO2A, A'NHA, A'SA or A'OA; Q4-Q6H, OH, CHO, COOH, halo, SH, sulfonyl, amino or amido. All other definitions are as above. ACTIVITY : Analgesic; Antiinflammatory. 2-Azaspiro[4,6]undecane-3-thione gave an 83% reduction in foot licking over controls in the Wheeler-Aceto formalin test after 20-25 minutes at an intraperitoneal dose of 32 mg/kg, compared with 64% for gabapentin lactam. MECHANISM OF ACTION : None given.
priorityDate 2002-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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