[发明专利]用于治疗肥胖症的大麻素受体拮抗剂/反向激动剂

权利要求书

1.一种下式I的化合物或其立体异构体或药学上可接受的盐：

其中：

X和Y独立选自H、卤素、C_1-6烷基、NO₂、CF₃、NR₂、OR、CO₂R、(CH₂)_nCO₂R、O(CH₂)_nCO₂R、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^aSO₂CH₃、NR^aCO(CH₂)_nCO₂R、O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄(CH₂)_nCO₂R、CH₂O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄CONH₂、O(CH₂)_nC₆H₄(CH₂)_nCONH₂、CH₂O(CH₂)_nC₆H₄CONH₂、O(CH₂)_nC₆H₄-四唑、CH₂O(CH₂)_nC₆H₄-四唑、O(CH₂)_nC₆H₄(CH₂)_n-四唑、NR^a(CH₂)_nC₆H₄CO₂R、CH₂NR^a(CH₂)_nC₆H₄CO₂R、NR^a(CH₂)_nC₆H₄CONH₂、CH₂NR^a(CH₂)_nC₆H₄CONH₂、NR^a(CH₂)_nC₆H₄-四唑、CH₂NR^a(CH₂)_nC₆H₄-四唑、-CN、(CH₂)_mC(NH)NH₂、CONR₂、(CH₂)_nCONR₂、O(CH₂)_nCONR₂、CH₂O(CH₂)_nCONH₂、NR^a(CH₂)_nCONR₂、OCH₂CH＝CHCONR₂、CH₂OCH₂CH＝CHCONR₂、NR^aCH₂CH＝CHCONR₂、-四唑、O(CH₂CH₂O)_PR、NR^a(CH₂CH₂O)_pR和SO₂NR^aCH₃；

X＇和Y＇独立选自H、卤素、C_1-6烷基、NO₂、CF₃、NR₂、OR、CO₂R、(CH₂)_nCO₂R、O(CH₂)_nCO₂R、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^aSO₂CH₃、NR^aCO(CH₂)_nCO₂R、O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄(CH₂)_nCO₂R、CH₂O(CH₂)_nC₆H₄CO₂R、O(CH₂)_nC₆H₄CONH₂、O(CH₂)_nC₆H₄(CH₂)_nCONH₂、CH₂O(CH₂)_nC₆H₄CONH₂、O(CH₂)_nC₆H₄-四唑、CH₂O(CH₂)_nC₆H₄-四唑、O(CH₂)_nC₆H₄(CH₂)_n-四唑、NR^a(CH₂)_nC₆H₄CO₂R、CH₂NR^a(CH₂)_nC₆H₄CO₂R、NR^a(CH₂)_nC₆H₄CONH₂、CH₂NR^a(CH₂)_nC₆H₄CONH₂、NR^a(CH₂)_nC₆H₄-四唑、CH₂NR^a(CH₂)_nC₆H₄-四唑、-CN、(CH₂)_mC(NH)NH₂、CONR₂、(CH₂)_nCONR₂、O(CH₂)_nCONR₂、CH₂O(CH₂)_nCONH₂、NR^a(CH₂)_nCONR₂、OCH₂CH＝CHCONR₂、CH₂OCH₂CH＝CHCONR₂、NR^aCH₂CH＝CHCONR₂、-四唑、O(CH₂CH₂O)_PR、NR^a(CH₂CH₂O)_pR和SO₂NR^aCH₃；

A选自H、C_1-6烷基、(CH₂)_m-C_3-6-环烷基、(CH₂)_m-杂芳基和(CH₂)_m-芳基，

其中每个芳基和杂芳基被0-1个选自CF₃、卤素、C_1-4烷基、-CN、CONR₂、NO₂、NR₂和OR的基团取代；

R＇选自H、C_1-6烷基、CH(A)-(CH₂)_mCO₂R、CH(A)-(CH₂)_mCONH₂、CH(A)-(CH₂)_mC(NH)NH₂、(CH₂)_m-苯基-(CH₂)_mCO₂R、(CH₂)_m-吡啶基-(CH₂)_mCO₂R、(CH₂)_m-苯基-(CH₂)_mCONH₂、(CH₂)_m-吡啶基-(CH₂)_mCONH₂、(CH₂)_m-苯基-(CH₂)_mC(NH)NH₂、(CH₂)_m-吡啶基-(CH₂)_m(CN)NH₂、(CH₂)_m-苯基-(CH₂)_m-四唑和(CH₂)_m-吡啶基-(CH₂)_m-四唑；

可选地，R＇是

R＂选自H、C_1-6烷基、(CH₂)_0-6芳基和(CH₂)_0-6杂芳基；

Z选自H、C_1-6烷基、芳基、NR₂、OR、-CN、(CH₂)_mC(NH)NH₂、CO₂R、(CH₂)_nCO₂R、O(CH₂)_nCO₂R、CH₂O(CH₂)_nCO₂R、NR^aCH(A)CO₂R、CH₂NR^aCH(A)CO₂R、NR^a(CH₂)_nCO₂R CH₂NR^a(CH₂)_nCO₂ROCH₂CH＝CHCO₂R、CH₂OCH₂CH＝CHCO₂R、O(CH₂)_nPO(OR)₂、CH₂O(CH₂)_nPO(OR)₂、O(CH₂)_nC₆H₄CO₂R、CH₂O(CH₂)_nC₆H₄CO₂R、CONR₂、(CH₂)_nCONR₂、O(CH₂)_nCONR₂、CH₂O(CH₂)_nCONR₂、OCH₂CH＝CHCONR₂、CH₂OCH₂CH＝CHCONR₂、CH₂NR^a(CH₂)_n四唑、CH₂O(CH₂)_n四唑和(CH₂)_m四唑；

Q选自N、CH和CQ＇；

Q＇选自H、CO₂R、(CH₂)_nCO₂R、CH₂O(CH₂)_nCO₂R、CH₂OCH₂CH＝CHCO₂R、CH₂O(CH₂)_nPO(OR)₂、CONR₂、(CH₂)_nCONR₂、CH₂O(CH₂)_nCONR₂、CH₂OCH₂CH＝CHCONR₂和(CH₂)_m四唑；

V选自H、C_1-6烷基、C_2-6烯基、CF₃、芳基、-CN、(CH₂)_mC(NH)NH₂、(CH₂)_mCO₂R、(CH₂)_mCONR₂、(CH₂)_m-四唑、(CH₂)_mCONR^aCH(A)-(CH₂)_mCO₂R、(CH₂)_mCONR^a(CH₂)_m-苯基-(CH₂)_mCO₂R、(CH₂)_mCONR^a(CH₂)_m-苯基-(CH₂)_m-四唑、CH₂O(CH₂)_nCO₂R、CH₂NR^a(CH₂)_nCO₂R、CH₂O(CH₂)_nCONH₂、CH₂NR^a(CH₂)_nCONH₂和CH₂O(CH₂)_n四唑；

R独立选自H、C_1-6烷基；

R^a独立选自H、C_1-6烷基、C_2-6烯基和C_2-6炔基；

m选自0、1、2、3和4；

n选自1、2、3和4；且

p选自1、2、3、4、5、6、7、8、9、10、11和12；

只要符合至少一个下述条件：

(a)至少一个X、Y、X＇和Y＇不是H、卤素、C_1-6烷基、NO₂、-CN、CF₃、OR和苯基；

(b)R＇选自CH(A)-(CH₂)_mCO₂R、CH(A)-(CH₂)_mCONH₂、CH(A)-(CH₂)_mC(NH)NH₂、(CH₂)_m-苯基-(CH₂)_mCO₂R、(CH₂)_m-吡啶基-(CH₂)_mCO₂R、(CH₂)_m-苯基-(CH₂)_mCONH₂、(CH₂)_m-吡啶基-(CH₂)_mCONH₂、(CH₂)_m-苯基-(CH₂)_mC(NH)NH₂、(CH₂)_m-吡啶基-(CH₂)_m(CN)NH₂、(CH₂)_m-苯基-(CH₂)_m-四唑和(CH₂)_m-吡啶基-(CH₂)_m-四唑；

(c)Z存在，且不是H、C_1-6烷基、芳基、NR₂和OR；

(d)Q存在，且为CQ＇，其中Q＇不是H；和/或

(e)V不是H、-CN、CF₃、C_2-6烯基、芳基和C_1-6烷基。