Patent US3315836A successfully refreshed from Google Patents.
US4144340A
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Basic substituted xanthine derivatives
Assignee: Evonik Operations GmbH
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Filing: 1977-04-12
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Granted: 1979-03-13
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Expires: 1997-04-12
Abstract
Abstract There are prepared compounds corresponding to the general formula T - Alk - NH - CH2 - CH(OH) - CH2 - O - Ar I in which T represents a theophyllinyl-(7) or theobrominyl-(1) radical, Alk is a linear or branched alkylene group with 2 to 5 carbon atoms which may also be substituted by a hydroxy group and Ar represents an aromatic monocyclic or condensed bicyclic, carbocyclic or heterocyclic radical optionally substituted by one or more alkyl groups with 1 to 6 carbon atoms, alkenyl groups with 2 to 6 carbon atoms, alkinyl groups with 2 to 6 carbon atoms, hydroxy groups, acyloxy groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 6 carbon atoms, alkenoxy groups with 2 to 6 carbon atoms, phenyl radicals, halogen atoms, amino groups, acyl groups with 2 to 6 carbon atoms, aminocarbonyl groups, ureido groups, acyl amino groups with 1 to 6 carbon atoms, cycloalkyl groups with 3 to 8 carbon atoms or by one or more cycloalkenyl groups with 4 to 8 carbon atoms, the heterocyclic radical consisting of individual rings with 5 to 6 members and containing from 1 to 4 heteroatoms, and their pharmaceutically acceptable salts. The compounds have beta-adrenolytic activity.
Inventors
- 👤 Heribert Offermanns
- 👤 Karl H. Klingler
- 👤 Klaus Thiemer
- 👤 Fritz Stroman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 11:12
CPC Classifications
C; C07; C07D; C07D473/00; C07D473/02; C07D473/04; C07D473/06; C07D473/08; A; A61; A61P; A61P25/00; A61P25/02; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
149 words
A compound of the formula T--Alk--NH--CH.sub.2 --CH(OH)--CH.sub.2 O--Ar (I) in which T represents theophyllinyl-(7) or theobrominyl-(1), Alk is alkylene group with 2 to 5 carbon atoms or alkylene group with 2 to 5 carbon atoms substituted by hydroxy group and Ar represents an unsubstituted aromatic benzene or naphthalene or heterocyclic ring or such aromatic ring substituted by alkyl with 1 to 6 carbon atoms, alkenyl with 2 to 6 carbon atoms, alkinyl with 2 to 6 carbon atoms, hydroxy, alkanoyloxy with 2 to 6 carbon atoms, alkoxy with 1 to 6 carbon atoms, alkenoxy with 2 to 6 carbon atoms, phenyl, halogen, amino, alkanoyl with 2 to 6 carbon atoms, aminocarbonyl, ureido, alkanoylamino with 1 to 6 carbon atoms, cycloalkyl with 3 to 8 carbon atoms or a cycloalkenyl with 4 to 8 carbon atoms, the heterocyclic ring being indole ring or insoindole ring, or pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
149 words
A compound of the formula T--Alk--NH--CH.sub.2 --CH(OH)--CH.sub.2 O--Ar (I) in which T represents theophyllinyl-(7) or theobrominyl-(1), Alk is alkylene group with 2 to 5 carbon atoms or alkylene group with 2 to 5 carbon atoms substituted by hydroxy group and Ar represents an unsubstituted aromatic benzene or naphthalene or heterocyclic ring or such aromatic ring substituted by alkyl with 1 to 6 carbon atoms, alkenyl with 2 to 6 carbon atoms, alkinyl with 2 to 6 carbon atoms, hydroxy, alkanoyloxy with 2 to 6 carbon atoms, alkoxy with 1 to 6 carbon atoms, alkenoxy with 2 to 6 carbon atoms, phenyl, halogen, amino, alkanoyl with 2 to 6 carbon atoms, aminocarbonyl, ureido, alkanoylamino with 1 to 6 carbon atoms, cycloalkyl with 3 to 8 carbon atoms or a cycloalkenyl with 4 to 8 carbon atoms, the heterocyclic ring being indole ring or insoindole ring, or pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
94 words
A compound according to claim 1 wherein the substituent on the aromatic ring is alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, alkinyl of 3 carbon atoms, cycloalkyl with 5 to 7 carbon atoms, cycloalkenyl with 5 to 7 carbon atoms, hydroxy, alkanoyloxy with 2 to 6 carbon atoms, alkoxy with 1 to 4 carbon atoms, alkenoxy with 3 to 4 carbon atoms, phenyl, halogen of atomic weight 9 to 80, amino, alkanoyl with 2 to 6 carbon atoms, aminocarbonyl, ureido, alkanoylamino with 1 to 5 carbon atoms.
Claim 4
Dependent Claim
11 words
A compound according to claim 2 wherein T is theophyllinyl-(7) radical.
Claim 5
Dependent Claim
17 words
A compound according to claim 3 wherein the aromatic ring of Ar is benzene, naphthalene or indole.
Claim 6
Dependent Claim
22 words
A compound to claim 4 wherein Ar is α-naphthyl, phenyl, methylphenyl, methoxyphenyl, allylphenyl, chlorophenyl, acetylaminophenyl, allyloxyphenyl, indolyl, methyl indolyl or dimethyl indolyl.
Claim 7
Dependent Claim
18 words
A compound according to claim 5 wherein Alk is alkyl of 2 to 4 carbon atoms of 2-hydroxypropylene.
Claim 8
Dependent Claim
20 words
A compound according to claim 3 wherein Alk is trimethylene or branched alkylene group of 3 to 5 carbon atoms.
Claim 9
Dependent Claim
17 words
A compound according to claim 7 wherein Ar is α-naphthyl, phenyl, o-allyloxyphenyl, p-allyloxyphenyl, indolyl-(4), 2-methylindolyl-(4) or 2,3-dimethylindolyl-(4).
Claim 10
Dependent Claim
19 words
A medicament containing as an active ingredient a compound of claim 1 together with a pharmacological excipient or diluent.
Claim 11
Dependent Claim
31 words
A method of blocking β-receptors of the adrenergic nervous system of a mammal comprising administering to the mammal an effective amount to block said β-receptor of a compound of claim 1.
Claim 12
Dependent Claim
19 words
A method according to claim 10 wherein there is administered at least 0.2 mg/kg body weight of the mammal.
Claim 13
Dependent Claim
19 words
A compound according to claim 1 wherein Ar is the heterocyclic ring and is indole ring or isoindole ring.
Claim 14
Dependent Claim
13 words
A compound according to claim 12 wherein the heterocyclic ring is indole ring.
Claim 15
Dependent Claim
22 words
A compound according to claim 13 wherein Ar is unsubstituted indolyl or indolyl substituted with alkyl of 1 to 4 carbon atoms.
Claim 16
Dependent Claim
15 words
A compound according to claim 14 wherein Ar is indolyl, methyl indolyl or dimethyl indolyl.
Claim 17
Dependent Claim
10 words
A compound according to claim 15 wherein T is theophyllinyl-(7).
Claim 18
Dependent Claim
13 words
A compound according to claim 15 wherein Ar is indolyl-(4), 2-methylindolyl-(4) or 2,3-dimethylindolyl-(4).
Claim 19
Dependent Claim
18 words
A compound according to claim 16 wherein Alk is alkyl of 2 to 4 carbon atoms or 2-hydroxypropylene.
Claim 20
Dependent Claim
20 words
A compound according to claim 16 wherein Alk is trimethylene or branched alkylene group of 3 to 5 carbon atoms.
Claim 21
Dependent Claim
20 words
A compound according to claim 16 wherein Alk is --CH 2 CH 2 CH(CH 3 )-- and Ar-O is 2-methylindolyl-(4)-oxy.
Claim 22
Dependent Claim
20 words
A compound according to claim 16 wherein Alk is --CH 2 CH 2 CH(CH 3 )-- and Ar-O is indolyl-(4)-oxy.
Claim 23
Dependent Claim
18 words
A compound according to claim 16 wherein Alk is --(CH 2 ) 3 -- and Ar-O is 2-methylindolyl-(4)-oxy.
Claim 24
Dependent Claim
20 words
A compound according to claim 16 wherein Alk is --CH 2 CH 2 CH(CH 3 )-- and Ar-O is 2,3-dimethylindolyl-(4)-oxy.
Claim 25
Dependent Claim
19 words
A medicament having as an active ingredient a compound of claim 14 together with a pharmacological excipient or diluent.
Claim 26
Dependent Claim
34 words
A method of blocking β-receptors of the adrenergic nervous system of a mammal comprising the step of administering to the mammal an effective amount to block said β-receptor of a compound of claim 14.
Claim 27
Dependent Claim
19 words
A method according to claim 25 wherein there is administered at least 0.2 mg/kg body weight of the mammal.
Claim 28
Dependent Claim
25 words
A medicament in unit dosage form having between 1 and 300 mg of a compound of claim 1 together with a pharmacological excipient or diluent.
References Cited (Backward Citations)
US3855221A
Cited
US3984413A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-12 | 1982-09-11 | 1983-03-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-12 | 1986-09-11 | 1987-03-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-12 | 1990-09-11 | 1991-03-13 | $7700.00 | Window Closed / Lapsed |