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US 4,070,464 AGranted
Method of treating autoimmune diseases
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., Clarence G. Van Arman
Life of this patent
Estimating the term…
Abstract
3,4-Dihydrospiro-2H-1,3-benzoxazines and pharmaceutical compositions thereof are useful in the treatment of autoimmune diseases.
Claims10
A method of treating an autoimmune disease selected from the group consisting of multiple sclerosis, and allergic encephalomyelitis which comprises oral or intravenous administration to a patient in need of such treatment from 1-50 mg/kg/day of a compound of formula:
- ##STR29## wherein R.sup.3 is
- 1. hydrogen,
- 2. methyl,
- 3. chloro, or
- 4. methoxy;
- R.sup.4 is
- 1. halo,
- 2. lower alkyl, or
- 3. adamantyl;
- R.sup.5 is
- 1. hydrogen,
- 2. lower alkyl,
- 3. lower alkoxy, or
- 4. halo;
- R.sup.6 is
- 1. halo,
- 2. lower alkyl,
- 3. lower alkylthio, or p2 4. trifluoromethyl;
- R.sup.5 and R.sup.6 taken together is -N.dbd.CH-CH.dbd.CH-, and
- R is
- 1. a spiro-carbocycle of 5,6, or 10-17 members, unsubstituted or substituted with
- a. lower alkyl,
- b. lower alkoxy,
- c. phenyl, or
- d. phenyl substituted with lower alkoxy, or
- e. lower alkanoyloxy;
- 2. a 6-membered spiroheterocycle containing 1 or 2 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen wherein the nitrogen heteroatom can be substituted with lower alkyl, phenyl-lower alkyl, or lower alkanoyl;
- 3. a spiro-polycycloalkyl of 6-15 members, or ##STR30##
25 more elements
Dependencies are inferred from the claim text.