[发明专利]可用于治疗包括肥胖症和糖尿病的代谢疾患的大麻素受体拮抗剂/逆激动剂

权利要求书

1.一种式I的化合物或其立体异构体或药学上可接受的盐：

其中：

X、Y、X′、Y′、X″和Y″独立地选自：H、C_1-6烷基、卤素、CF₃、O-C_1-6烷基、NO₂、NR₂、O(CH₂)_nCO₂R、O(CH₂)_nCN、OCH₂CH＝CHCO₂R、CH₂O(CH₂)_nCO₂R、CH₂OCH₂CH＝CHCO₂R、O(CH₂)_nPO(OR)₂、CH₂O(CH₂)_nPO(OR)₂、NR^a(CH₂)_nCO₂R、NR^a(CH₂)_nPO(OR)₂、NR^aCH₂CH＝CHCO₂R、NR^aSO₂R、NR^aCO(CH₂)_nCO₂R、NR^aCO(CH₂)_nCONR^a₂、O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄(CH₂)_nCO₂R、CH₂O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄CONR^a₂、O(CH₂)_nC₆H₄(CH₂)_nCONR^a₂、O(CH₂)_nC₆H₄-四唑、CH₂O(CH₂)_nC₆H₄CONR^a₂、CH₂O(CH₂)_nC₆H₄-四唑、O(CH₂)_nC₆H₄(CH₂)_n-四唑、NR^a(CH₂)_nC₆H₄CO₂R、CH₂NR^a(CH₂)_nC₆H₄CO₂R、NR^a(CH₂)_nC₆H₄(CH₂)_nCO₂R、NR^a(CH₂)_nC₆H₄CONR^a₂、CH₂NR^a(CH₂)_nC₆H₄CONR^a₂、NR^a(CH₂)_nC₆H₄(CH₂)_nCONR^a₂、NR^a(CH₂)_nC₆H₄-四唑、CH₂NR^a(CH₂)_nC₆H₄-四唑、NR^a(CH₂)_nC₆H₄(CH₂)_n-四唑、CONHOH、C(NH)NR^a₂、(CH₂)_nC(NH)NR^a₂、O(CH₂)_nCONR^a₂、O(CH₂)_nC(NH)NR^a₂、O(CH₂)_nC(NOH)NR^a₂、CH₂O(CH₂)_nCONR^a₂、NR^a(CH₂)_nCONR^a₂、OCH₂CH＝CHCONR^a₂、CH₂OCH₂CH＝CHCONR^a₂、NR^aCH₂CH＝CHCONR^a₂、(CH₂)_m-四唑、O(CH₂)_n-四唑、O(CH₂CH₂O)PR、NR^a(CH₂CH₂O)_pR和SO₂NHCH₃；

Z选自：H、C_1-6烷基、OH、O-C_1-6烷基、O(CH₂CH₂O)_PR、OC(O)-C_1-6烷基、O(CH₂)_nCO₂R、OCH₂CH＝CHCO₂R、O(CH₂)_nPO(OR)₂、O(CH₂)_nCONR^a₂、O(CH₂)_nC(NH)NH₂、O(CH₂)_nC(NOH)NR^a₂、OCH₂CH＝CHCONR^a₂、O(CH₂)_n-苯基-(CH₂)_mCO₂R和O(CH₂)_n-苯基-(CH₂)_m-四唑；

Z′选自H、CO₂R和CONR^a₂；

Q选自：(CH₂)_nCHA(CH₂)_mC(O)NR₂、(CH₂)_mCAA″(CH₂)_mC(O)NR₂、(CH₂)_nCHA(CH₂)_mCO₂R、(CH₂)_mCAA″(CH₂)_mCO₂R、(CH₂)_mCHA(CH₂)_mSO₂NR₂、(CH₂)_mCHA(CH₂)_mSO₃R、(CH₂)_mCHA(CH₂)_mC(NH)NH₂、(CH₂)_mCHA(CH₂)_mC(NOH)NH₂、(CH₂)_mCHA(CH₂)_mCONHCHA(CH₂)_mCO₂R、(CH₂)_mCAA″(CH₂)_mCONHCHA(CH₂)_mCO₂R、(CH₂)_mCHA(CH₂)_mCONHCHA(CH₂)_mCONHCHA(CH₂)_mCO₂R、(CH₂)_mCHA(CH₂)_mCONHCHA(CH₂)_mCONR^a₂(CH₂)_mCAA″(CH₂)_mCONHCHA(CH₂)_mCONR^a₂、(CH₂)_mCHA(CH₂)_mCONHCHA(CH₂)_mCONHCHA(CH₂)_mCONR^a₂、C₃-C₆-环氨基-(CH₂)_mCO₂R、C₃-C₆-环氨基-(CH₂)_mCONR^a₂、C₃-C₆-环亚烷基-(CH₂)_mCO₂R和C₃-C₆-环亚烷基-(CH₂)_mCONR^a₂；

前提是当Q是(CH₂)_mCAA″(CH₂)_mC(O)NR₂或(CH₂)_mCAA″(CH₂)_mCO₂R时，则(a)m不是0，(b)A不是H，或(c)(a)和(b)两者；

A选自H、C_1-6烷基、(CH₂)_mC_3-6-环烷基、OH、CH₂OH、CH(CH₃)OH、C(CH₃)₂OH、(CH₂)_nCO₂R^b、(CH₂)_nC(O)NR^b₂和(CH₂)_m-苯基，其中所述苯基被选自H、C_1-4烷基、卤素、CF₃、O-C_1-4烷基和NO₂的0-3个基团取代；

可选地，Q是CHA(CH₂)_mC(O)NR₂或CHA(CH₂)_mCO₂R，且(a)A选自OH、(CH₂)_nCO₂R^b和(CH₂)_nC(O)NR^b₂；(b)R是(CH₂)_m(CHR^b)_n(CH₂)_mOH或CH(CH₂OH)₂；或(c)(a)和(b)两者；

A″是C_1-6烷基；

M是C＝O或SO₂；

R独立地选自H、(CH₂)_m(CHR^b)_n(CH₂)_mOH、CH(CH₂OH)₂、C_1-6烷基、C_2-6烯基和C_2-6炔基；

R^a独立地选自H、(CH₂)_m(CHR)_n(CH₂)_mOH、C_1-6烷基、C_2-6烯基和C_2-6炔基，

R^b独立地选自H、C_1-6烷基、C_2-6烯基和C_2-6炔基；

p选自2、3、4、5、6、7、8、9、10、11和12；

m选自0、1、2、3和4；且

n选自1、2、3和4。