C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 403/10 (2006.01) C07D 209/08 (2006.01) C07D 233/08 (2006.01) C07D 233/24 (2006.01) C07D 233/50 (2006.01) C07D 233/64 (2006.01) C07D 263/28 (2006.01) C07D 263/64 (2006.01) C07D 277/10 (2006.01) C07D 277/18 (2006.01) C07D 403/12 (2006.01)
Patent
CA 2418778
The present invention concerns novel compounds represented by the Formula: Image wherein: A is R1q(R3R60N)m,(Z)(NR2)n; m and q are each 0 or 1; with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C=O or SO 2; n is 1 with the proviso that, when Z is C=O, m is 1; X is -NH-, -CH2-, or -OCH2-; Y is 2-imidazoline, 2- oxazoline, 2-thiazoline, or 4-imidazole; R1 is H, lower alkyl, or phenyl ; R2, R3, R60 are each independently H, lower alkyl, or phenyl; R4, R5, R6, and R7 are each independently hydrogen, lower alkyl, -CF 3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R2 and R7 optionally may be taken together to form alkylene or alkenylene of 2 to 3 atoms in an unsubstituted or optionally substituted 5- or 6- membered ring, wherein the optional substituents on the ring are halo, lower alkyl, or -CN, with the proviso that, when R7 is hydroxyl or lower alkylsulfonarnido, then X is not -NH- when Y is 2-imidazoline. The compounds include pharmaceutically acceptable salts of the above. In the above formula A may be, for example, (R1S02NR2-),(R3R60NSO2NR2-), or (R3R60NCONR2-). The invention also includes the use of the above compounds, and compositions containing them, as alpha 1A/1L agonists in the treatment of various disease states such as urinary incontinence, nasal congestion, priapism, depression, anxiety, dementia, senility, Alzheimer's, deficiencies in attentiveness and cognition, and eating disorders such as obesity, bulimia, and anorexia.
Cournoyer Richard Leo
Keitz Paul Francis
O'yang Counde
Yasuda Dennis Mitsugu
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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