Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...
Patent
1977-10-31
1979-04-24
Curtis, Allen B.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Recombinant or stably-transformed bacterium encoding one or...
26050117, 260558R, 260559A, 562595, 424324, 424272, C07B103737, C07D26306, A61K 31165, A61K 3142
Patent
active
041512979
ABSTRACT:
1-Alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.0]-hex-6-yl)ethylaminocarbonyl]-1-phenoxy)-2-propano l and substituted derivatives thereof and methods for preparing such compounds are disclosed. 5-(3- Or 4-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]-phenoxy)methyl 3-alkyl-2-optionally substituted oxazolidine and derivatives thereof, and methods for preparing such compounds are also disclosed. These compounds exhibit cardiovascular acitivity and are useful in the treatment of abnormal heart condition as well as hypertension in mammals. The former compounds are prepared by treatment of the corresponding 1,2-epoxy-3-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl]phenoxy)propane with the desired alkylamine or by base or acid hydrolysis of the corresponding 5-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)-ethylaminocarbonyl)-3-alkyl oxazolidine. The latter compounds are prepared from the corresponding 1-alkylamino-3-(3- or 4-[2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl]-1-phenoxy)-2-propanol by treatment with an aldehyde having the desired optional substituent or by treating a 3- or 4-(2-(endobicyclo[3.1.0]hex-6-yl)ethylaminocarbonyl)-optionally substituted phenol with a 5-tosyloxy or mesyloxymethyl 3-alkyl)-methyloxazolidine-2-optionally substituted oxazolidine.
REFERENCES:
patent: 400193 (1976-12-01), Lunts et al.
patent: 3676493 (1972-07-01), Smith
patent: 3723524 (1973-03-01), Augstein et al.
patent: 4000192 (1976-12-01), Lunts et al.
patent: 4059621 (1977-11-01), Vincent et al.
Lewis Brian
Unger Stefan H.
Untch Karl G.
Blaufarb Gerard A.
Curtis Allen B.
Hammond Richard J.
Syntex (U.S.A.) Inc.
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