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    • 5. 发明申请
    • SUBSTITUTED PIPERODINES AND PYRROLIDINES AS CALCIUM SENSING RECEPTOR MODULATORS AND METHOD
    • 作为钙感测受体调节剂和方法的取代的哌嗪和吡咯烷
    • WO2004106295A3
    • 2005-12-29
    • PCT/US2004016712
    • 2004-05-27
    • SQUIBB BRISTOL MYERS CODICKSON JOHN KLAWRENCE R MICHAELROBERGE JACQUES YROTELLA DAVID PYANG WU
    • DICKSON JOHN KLAWRENCE R MICHAELROBERGE JACQUES YROTELLA DAVID PYANG WU
    • A61K31/40A61K31/401A61K31/4025A61K31/454A61K31/55C07D20060101C07D207/04C07D409/06
    • C07D207/06C07D207/08C07D207/10C07D211/18C07D211/22C07D333/28
    • Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula (I) wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R O, R R N, R OCO, R CO, R R NCO, R R NCONR , R OCONR , R CONR , R S, R SO, R SO2, R R NSO2, R R NSO2NR , and R SO2NR ; R is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R and R are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R ; R is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; Q is hydrogen, F, or hydroxyl. In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.
    • 提供化合物,其是钙感应受体的拮抗剂,并具有通式(I),其中m为0,1,2,3或4; 每个X独立地选自氢,卤素,氰基,硝基,OCF 3,羟基,氨基,羧基,烷基,烯基,炔基,环烷基,环杂烷基,卤代烷基,烷氧基,烷氧基羰基烷基,羟基羰基烷基,芳基,芳基烷基,杂芳基, 杂芳基烷基,环烷基烷基,R 1 O,R 1 R 2 N,R 1 OCO,R 1 CO,R 1 R 2 NCO,R 1 R 2, NCONR 2a,R 1 OCONR 2a,R 1 CONR 2a,R 1 S,R 1 SO,R 1 SO 2,R 1 R 2 NSO 2 R 1 R 2 NSO 2 NR 2a和R 1 SO 2 NR 2a; R 1是烷基,烯基,炔基,环烷基,环杂烷基,芳基,杂芳基,芳基烷基或杂芳基烷基; R 2和R 2a相同或不同并且独立地选自氢,烷基,烯基,炔基,环烷基,环杂烷基,芳基,杂芳基,芳基烷基或杂芳基烷基; n为1,2或3; W是O或H,R 3; R 3是氢或羟基; Ar是取代或未取代的芳基或取代或未取代的杂芳基; Q是氢,F或羟基。 此外,还提供了使用这些化合物治疗与异常或矿物质内稳态相关疾病的方法。