Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-01-15
2000-02-15
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514409, 514183, 514212, A61K 3144, A61K 3140
Patent
active
060253649
DESCRIPTION:
BRIEF SUMMARY
This invention relates to a method of treating asthma, in mammals, including humans, which comprises administering to such human an effective amount of a substituted azaspirane.
Badger et al U.S. Pat. No. 4,963,557 (Badger I) discloses compounds of the Formula I ##STR1## wherein: n is 3-7; hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 5-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group having 3-7 carbon atoms:
R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen or straight chain alkyl having 1-3 carbon atoms; or R.sup.3 and R.sup.4 are joined together with the nitrogen atom to form a heterocyclic group having 5-8 atoms;
Badger I discloses compounds of Formula I as a class of novel compounds which induce an immunomodulatory effect which is characterised by the stimulation of suppressor cell activity. Particular disease states treatable with the compounds of Formula I, as disclosed in Badger I, are: rheumatoid arthritis, systemic lupus erythematosis, multiple sclerosis, acute transplantation/graft rejection, myasthenia gravis, progressive systemic sclerosis, multiple myeloma, atopic dermatitis, hyperimmunoglobin E, hepatitis B antigen negative chronic active hepatitis, Hasimoto's thyroiditis, Familial Mediterranean fever, Grave's disease, autoimmune hamolytic anaemia, primary biliary cirrhosis and inflammatory bowel disease.
International Application No. PCT/US91/06778, having the International Publication No. WO 92/04/899 and an International Publication Date of Apr. 2, 1992, discloses compounds of the above Formula I as being useful in treating a disease state which is exacerbated or caused by excessive glucose levels.
International Application No. PCT/US92/01283, having the International Publication No. WO 92/14462 and an International Publication Date of Sep. 3, 1992 (Badger II), discloses the compounds of the above Formula I as being useful in the inhibition of cytokines. Preferred disease states treatable with the compounds of Formula I, as disclosed in Badger II, are: increased bone resorption (including osteoporosis and Paget's disease), endotoxic shock, cachexia secondary to acquired immune deficiency syndrome (AIDS), AIDS and matrix.
U.S. Pat. No. 5,482,959 discloses compounds of the above Formula I as being useful in delaying AIDS in HIV infected individuals.
International Application No. PCT/US94/08275, having the International Publication No. WO 95/03041 and an International Publication Date of Feb. 2, 1995, International Application No. PCT/US94/08274, having the International Publication No. WO 95/03049 and an International Publication Date of Feb. 2, 1995, and International Application No. PCT/US94/08276, having the International Publication No. WO 95/03042 and an International Publication Date of Feb. 2, 1995, disclose the compounds of the above Formula I as being useful in various mechanisms of HIV inhibition.
None of the above references disclose the compounds of Formula I as being useful in treatment of asthma.
This invention relates to a method of treating asthma, in mammals, including humans, which comprises administering to a subject in need thereof an effective amount of a compound of the Formula I ##STR2## wherein: n is 3-7; hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 5-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group having 3-7 carbon atoms;
R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen or straight chain alkyl having 1-3 carbon atoms; or R.sup.3 and R.sup.4 are joined together with the nitrogen atom to form a heterocyclic group having 5-8 atoms;
In the alternative this invention relates to the use of a compound of Formula I ##STR3## wherein: n is 3-7; hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 5
REFERENCES:
patent: 4963557 (1990-10-01), Badger et al.
patent: 5482959 (1996-01-01), Badger
Anderson et al., "An in vivo model for measuring antigen-induced SRS-A-Mediated Bronchoconstriction and Plasma SRS-A-Levels in the Guinea-Pig", Br. J. Pharmac. (1983), 78, 67-74.
Badger Alison Mary
Gleason John Gerald
AnorMed Inc.
Spivack Phyllis G.
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