| 摘要 |
The invention provides compounds of the formula:;
in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma. |
| 主权项 |
1. A compound having the formula IIf:where:
X− is an anion of a pharmaceutically acceptable acid; R3 is selected from H and —C0-1alkylene-OH; Z is selected from a bond, —O—, —S—, —S(O)—, —SO2—, —SO2—NRZ1—, —NRZ1—SO2—, —C(O)—, —OC(O)—, —C(O)O—, —NRZ1C(O)—, —C(O)NRZ1, —NRZ2—C(O)—CRZ3—, —NRZ2—C(S)—NRZ3—, —CH(OH)—, and —C(═N—O—RZ4)—; where RZ1 is selected from H and —C1-4alkyl; RZ2 and RZ3 are independently selected from H, —C1-4alkyl, and —C3-6cycloalkyl, or RZ2 and RZ3 are taken together to form —C2-4alkylene- or —C2-3alkenylene-; and RZ4 is selected from —C1-4alkyl and benzyl; Q is an aryl or heteroaryl group; wherein the aryl in Q is optionally substituted with 1 to 5 RQ groups independently selected from halo, —C1-4alkyl, —C0-4alkylene-OH, cyano, —C0-2alkylene-COOH, —C(O)O—C1-4alkyl, —O—C1-4alkyl, —S—C1-4alkyl, —NH—C(O)—C1-4alkyl, —N-di-C1-4alkyl, and —N+(O)O; wherein each alkyl, alkylene, alkenyl, alkenylene, alkynyl, and cycloalkyl group in R3, Z, Q, and RQ, is optionally substituted with 1 to 5 fluoro atoms; and each —CH2— group in —(CH2)1-4— is optionally substituted with 1 or 2 substituents independently selected from —C1-2alkyl, —OH, fluoro, and phenyl; or a pharmaceutically acceptable salt thereof. |
