Abstract: Sulfamate esters of the formula(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is aryloxyalkyl, p is the number of unreacted hydroxy groups present on the alkyl moiety and may be zero, z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups attached to carbons of the alkyl moiety and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy, and the like are useful in treating glaucoma.
Type:
Grant
Filed:
June 10, 1991
Date of Patent:
March 9, 1993
Assignee:
A. H. Robins Company, Incorporated
Inventors:
Young S. Lo, Joseph C. Nolan, Dwight A. Shamblee
Abstract: Novel 1-azabicyclo[3.2.1]octan-5-ylmethyl and 1-azabicyclo[3.3.1]nonan-5-ylmethyl amines and alcohols are coupled with aryl carboxylic acids to obtain compounds having the formula: ##STR1## wherein X is --O-- or --NH-- and n is 1 or 2 which are useful in increasing gastric motility, in preventing emesis and emesis caused by anticancer treatments, anxiety, certain arrhythmias, and disorders caused by serotonin imbalances.
Type:
Grant
Filed:
March 26, 1992
Date of Patent:
March 2, 1993
Assignee:
A. H. Robins Company, Incorporated
Inventors:
Harry R. Munson, Jr., Gunnar E. Jagdmann
Abstract: The compounds of this invention having Angiotensin II receptor binding properties and thus useful in the treatment of hypertension are of the formula: ##STR1## wherein: X.sup.1 =H, lower alkyl, phenyl or naphthyl;X.sup.2 is X.sup.1, perfluoroalkyl or halogen;X.sup.1 and X.sup.2 together are --(CH.sub.2).sub.n --where n is 3-6;X.sup.3 =H, lower alkyl, perfluoroalkyl, perchloroalkyl or halogen;X.sup.4 =5-tetrazolyl, carboxy or cyano;X.sup.5 =H, lower alkoxy or halogen;and the pharmaceutically acceptable salts thereof.
Abstract: This invention relates to an improved process for the preparation of 3-phenoxy-1-azetidinecarboxamides of Formula I which are useful ##STR1## in the treatment of epileptic seizures. Under Formula I, n is 1 to 3, X is H, halogen, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, acetyl, or aminocarbonyl, and R is H or methyl. This process involves heating a 3-phenoxyazetidine with urea to obtain the Formula I compound. Urea is inexpensive and easily removed by washing the solid Formula I product with water.