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    • 4. 发明申请
    • NICOTINE ADDICTION REDUCING HETEROARYL FUSED AZAPOLYCYCLIC COMPOUNDS
    • 尼古丁加入减少异氟醚融合的化合物
    • WO2005007655A1
    • 2005-01-27
    • PCT/IB2004/002261
    • 2004-07-08
    • PFIZER PRODUCTS INC.ALLEN, Martin, PatrickCOE, Jotham, WadsworthLIRAS, SpirosO'DONNELL, Christopher, JohnO'NEILL, Brian, Thomas
    • ALLEN, Martin, PatrickCOE, Jotham, WadsworthLIRAS, SpirosO'DONNELL, Christopher, JohnO'NEILL, Brian, Thomas
    • C07D471/08
    • C07D471/08
    • The present invention provides a compound having the structure of formula (I): wherein R 1 is hydrogen, (C 1 -C 6 ) alkyl, unconjugated (C 3 -C 6 ) alkenyl, benzyl, YC(=O)(C 1 -C 6 ) alkyl or -CH 2 CH 2 -O-(C 1 -C 4 ) alkyl; X is CH 2 or CH 2 CH 2 ; Y is (C 2 -C 6 ) alkylene; Z is (CH 2 ) m , CF 2 , or C(=O), where m is 0, 1 or 2; R 2 and R 3 are selected independently from hydrogen, halogen, - (C 1 -C 6 ) alkyl optionally substituted with from 1 to 7 halogen atoms, and -O(C 1 -C 6 ) alkyl optionally substituted with from 1 to 7 halogen atoms, or R 2 and R 3 each together with the atom to which it is connected independently form C(=O), S→O , S(=O) 2 , or N→O; and Het is a 5- to 7- ­membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups. The compounds can be used to treat disease states mediated by neuronal nicotinic acetylcholine specific receptor sites.
    • 本发明提供具有式(I)结构的化合物:其中R 1是氢,(C 1 -C 6)烷基,未结合的(C 3 -C 6)烯基,苄基,YC(= O)(C 1 -C 6) 烷基或-CH 2 CH 2 -O-(C 1 -C 4)烷基; X是CH 2或CH 2 CH 2; Y是(C 2 -C 6)亚烷基; Z是(CH 2)m,CF 2或C(= O),其中m是0,1或2; R 2和R 3独立地选自氢,卤素,任选被1至7个卤素原子取代的 - (C 1 -C 6)烷基和任选被1至7个取代的-O(C 1 -C 6)烷基 卤素原子或R 2和R 3各自与其连接的原子一起独立地形成C(= O),S-> O,S(= O)2或N-> O; 吡啶基,咪唑基,嘧啶基,吡唑基,三唑基,吡嗪基,呋喃基,噻唑基,异恶唑基,噻唑基,恶唑基,异噻唑基,吡咯基,噌啉基,三嗪基 ,恶二唑基,噻二唑基和呋咱基。 该化合物可用于治疗由神经元烟碱乙酰胆碱特异性受体位点介导的疾病状态。