US4089959A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Long-acting xanthine bronchodilators and antiallergy agents
Assignee: Cooper Laboratories Inc
•
Filing: 1976-03-31
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Granted: 1978-05-16
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Expires: 1996-03-31
Abstract
Abstract Prolonged bronchodilation and prolonged inhibition of allergic mediator release in mammals are produced by administering an effective amount of a substituted xanthine compound having the formula: ##STR1## wherein: R 1 = methyl R 3 = c 4 -c 7 alkyl, C 4 -C 7 cycloalkylalkyl C 4 -C 7 alkenyl, C 4 -C 7 alkynyl, or C 4 -C 7 cycloalkyl R 8 = c 1 -c 2 alkyl These compounds are useful in the treatment of bronchial asthma and other bronchospastic and allergic diseases. The compounds are also novel. The bronchodilator and antiallergy agents may be administered in the form of tablets, capsules, aerosols, solutions, suspensions or suppositories.
Inventors
- 👤 Julius Diamond
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 12:53
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; C07D239/545; C07D473/00; C07D473/02; C07D473/04; C07D473/06
Claims Analysis
Total Claims: 45
Claim 1
Independent Claim
74 words
A method for producing prolonged bronchodilation and prolonged inhibition of allergic mediator release in mammals by administering to a mammal in need thereof an effective amount of a compound having the formula: ##STR22## wherein: R 1 = methyl R 3 = c 4 -c 7 alkyl, C 4 -C 7 alkenyl, C 4 -C 7 alkynyl, C 4 -C 7 cycloalkyl, C 4 -C 7 cycloalkylalkyl R 8 = c 1 -c 2 alkyl.
Claim 2
Independent Claim
74 words
A method for producing prolonged bronchodilation and prolonged inhibition of allergic mediator release in mammals by administering to a mammal in need thereof an effective amount of a compound having the formula: ##STR22## wherein: R 1 = methyl R 3 = c 4 -c 7 alkyl, C 4 -C 7 alkenyl, C 4 -C 7 alkynyl, C 4 -C 7 cycloalkyl, C 4 -C 7 cycloalkylalkyl R 8 = c 1 -c 2 alkyl.
Claim 3
Dependent Claim
17 words
A method according to claim 1 wherein R 3 is --CH 2 (C 3 -C 6 alkyl).
Claim 4
Dependent Claim
17 words
A method according to claim 1 wherein R 3 is --CH 2 --(C 3 -C 6 cycloalkyl).
Claim 5
Dependent Claim
27 words
A method according to claim 1 wherein R 3 is selected from the group consisting of methallyl, n-butyl, isobutyl, n-pentyl, 2-methyl-1-butyl, 3-methyl-1-butyl, 2,2-dimethylpropyl, 2-methyl-1-pentyl, cyclopropylmethyl, and cyclobutylmethyl.
Claim 6
Dependent Claim
11 words
A method according to claim 1 wherein R 3 is 2-methyl-1-butyl.
Claim 7
Dependent Claim
11 words
A method according to claim 1 wherein R 3 is isobutyl.
Claim 8
Dependent Claim
11 words
A method according to claim 1 wherein R 8 is ethyl.
Claim 9
Dependent Claim
11 words
A method according to claim 1 wherein R 8 is methyl.
Claim 10
Dependent Claim
12 words
A method according to claim 1 wherein said substituted xanthine is 1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 11
Dependent Claim
12 words
A method according to claim 1 wherein said substitued xanthine is 1,8-dimethyl-3-isobutylxanthine.
Claim 12
Dependent Claim
23 words
A method according to claim 1 wherein said substituted xanthine is administered to humans in a dose of between 0.2 and 200 mg.
Claim 13
Dependent Claim
21 words
A method according to claim 1 wherein said substituted xanthine is incorporated with inert excipients into a capsule and administered orally.
Claim 14
Dependent Claim
21 words
A method according to claim 1 wherein said substituted xanthine is incorporated with inert excipients into a tablet and administered orally.
Claim 15
Dependent Claim
23 words
A method according to claim 1 wherein said substituted xanthine is incorporated with inert excipients into a rapidly disintegrating tablet and administered sublingually.
Claim 16
Dependent Claim
26 words
A method according to claim 1 wherein said substituted xanthine is incorporated with propellant and solvent into an aerosol and administered by inhalation of the mist.
Claim 17
Dependent Claim
21 words
A method according to claim 1 wherein said substituted xanthine is incorporated with fatty vehicles into a suppository and administered rectally.
Claim 18
Dependent Claim
19 words
A method according to claim 1 wherein said substituted xanthine is incorporated with a sterilized vehicle and administered parenterally.
Claim 19
Dependent Claim
36 words
A compound having the formula: ##STR23## wherein: R 1 = methyl R 3 = ch 2 --(c 3 -c 4 alkyl), --CH 2 --(C 3 -C 4 cycloalkyl), R 8 = c 1 -c 2 alkyl.
Claim 20
Dependent Claim
36 words
A compound having the formula: ##STR23## wherein: R 1 = methyl R 3 = ch 2 --(c 3 -c 4 alkyl), --CH 2 --(C 3 -C 4 cycloalkyl), R 8 = c 1 -c 2 alkyl.
Claim 21
Dependent Claim
19 words
A compound according to claim 18 wherein R 3 is selected from the group consisting of isobutyl and 2-methyl-1-butyl.
Claim 22
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is n-butyl.
Claim 23
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is isobutyl.
Claim 24
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is n-pentyl.
Claim 25
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is isopentyl.
Claim 26
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is 2-methyl-1-butyl.
Claim 27
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is cyclopropylmethyl
Claim 28
Dependent Claim
11 words
A compound according to claim 18 wherein R 3 is cyclobutylmethyl.
Claim 29
Dependent Claim
11 words
A compound according to claim 18 wherein R 8 is ethyl.
Claim 30
Dependent Claim
11 words
A compound according to claim 18 wherein R 8 is methyl.
Claim 31
Dependent Claim
1 words
1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 32
Dependent Claim
1 words
1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 33
Dependent Claim
1 words
dextro-1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 34
Dependent Claim
1 words
dextro-1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 35
Dependent Claim
1 words
levo-1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 36
Dependent Claim
1 words
levo-1,8-dimethyl-3-(2-methyl-1-butyl)xanthine.
Claim 37
Dependent Claim
1 words
1,8-dimethyl-3-isobutylxanthine.
Claim 38
Dependent Claim
1 words
1,8-dimethyl-3-isobutylxanthine.
Claim 39
Dependent Claim
25 words
A pharmaceutical composition comprising an amount of a compound according to claim 18 effective for bronchodilation in combination with a non-toxic inert pharmaceutically acceptable diluent.
Claim 40
Dependent Claim
12 words
A composition according to claim 33 in the form of a tablet.
Claim 41
Dependent Claim
12 words
A composition according to claim 33 in the form of a capsule.
Claim 42
Dependent Claim
13 words
A composition according to claim 33 in the form of a sublingual tablet.
Claim 43
Dependent Claim
13 words
A composition according to claim 33 wherein said diluent is an aerosol propellent.
Claim 44
Dependent Claim
15 words
A composition according to claim 33 comprising 1,8-dimethyl-3-(2-methyl-1-butyl)xanthine dissolved in a pharmaceutically acceptable aerosol propellant.
Claim 45
Dependent Claim
30 words
A pharmaceutical composition in the form of a tablet comprising between 1 mg and 100 mg of a compound according to claim 18 in combination with non-toxic pharmaceutically acceptable excipients.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-05-15 | 1981-11-14 | 1982-05-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-15 | 1985-11-14 | 1986-05-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-15 | 1989-11-14 | 1990-05-16 | $7700.00 | Window Closed / Lapsed |