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US4212866A
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Pharmaceutically active derivatives of 9-[3-(4-amino-piperidino)-propyl]-adenines
Assignee: Roche Diagnostics GmbH
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Filing: 1979-01-24
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Granted: 1980-07-15
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Expires: 1999-01-24
Abstract
Abstract Novel 9-[3-(4-amino-piperidino)-propyl]-adenine derivatives of the formula <IMAGE> wherein R1 is a hydrogen atom or a lower alkyl radical, R2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R1 and the nitrogen atom to which they are attached form a heterocyclic ring, and R3 is a hydrogen atom or an acyl radical, or salts thereof with pharmacologically acceptable acids, characterized by anti-allergic, anti-inflammatory and anti-oedematous activity.
Inventors
- 👤 Walter-Gunar Friebe
- 👤 Max Thiel
- 👤 Androniki Roesch
- 👤 Otto-Henning Wilhelms
- 👤 Wolfgang Schaumann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 10:33
CPC Classifications
C; C07; C07D; C07D473/00; C07D473/26; C07D473/32; C07D473/34; A; A61; A61P; A61P29/00; A61P37/00; A61P37/08; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/56; C07D211/58
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
77 words
A 9-[3-(4-amino-piperidino)-propyl]-adenine of the formula ##STR8## wherein R 1 is a hydrogen atom or a lower alkyl radical, R 2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R 1 and the nitrogen atom to which they are attached form a tetramethyleneimino, pentamethyleneimino or hexamethyleneimino ring, and R 3 is a hydrogen atom or an acyl radical, or a salt thereof with a pharmacologically acceptable acid.
Claim 2
Dependent Claim
77 words
A 9-[3-(4-amino-piperidino)-propyl]-adenine of the formula ##STR8## wherein R 1 is a hydrogen atom or a lower alkyl radical, R 2 is a hydrogen atom, an aryl radical, a lower alkyl radical, a hydroxy lower alkyl radical, or together with R 1 and the nitrogen atom to which they are attached form a tetramethyleneimino, pentamethyleneimino or hexamethyleneimino ring, and R 3 is a hydrogen atom or an acyl radical, or a salt thereof with a pharmacologically acceptable acid.
Claim 3
Dependent Claim
146 words
A compound or salt according to claim 1, wherein R 1 is a hydrogen atom or an alkyl radical with up to 4 carbon atoms, R 2 is a hydrogen atom, a phenyl radical, a naphthyl radical, an alkyl or hydroalkyl radical with up to 4 carbon atoms, or together with R 1 and the nitrogen atom to which they are attached form a tetramethyleneimino, pentamethyleneimino or hexamethyleneimino ring, and R 3 is a hydrogen atom; a lower alkanoyl radical optionally substituted by halogen atoms, a phenyl radical and/or a naphthyl radical; a lower alkenoyl radical substituted by a phenyl or naphthyl radical; a C 3-7 -cycloalkylcarbonyl, benzoyl, furanecarbonyl, thiophenecarbonyl or pyridinecarbonyl radical optionally substituted by halogen atoms, or a hydroxyl, lower alkyl, lower alkoxy, lower alkoxycarbonyl, lower acyloxy, carboxyl, nitro, amino, cyano, trifluoromethyl, carbamoyl or benzyl radical; or a benzene sulphonic or methylsulphonic acid radical.
Claim 4
Dependent Claim
17 words
A compound or salt according to claim 1, wherein such compound is 9-{3-[4-(4-fluorobenzamido)-piperidino]-propyl}-adenine of the formula ##STR9##
Claim 5
Dependent Claim
17 words
A compound or salt according to claim 1, wherein such compound is 9-{3-[4-(4-methylbenzamido)-piperidino]-propyl}-adenine of the formula ##STR10##
Claim 6
Dependent Claim
19 words
A compound or salt according to claim 1, wherein such compound is N 6 -(2-hydroxethyl)-9-[3-(4-benzamido-piperidino)-propyl]-adenine of the formula ##STR11##
Claim 7
Dependent Claim
19 words
A compound or salt according to claim 1, wherein such compound is N 6 -n-butyl-9-[3-(4-benazmido-piperidino)-propyl]-adenine of the formula ##STR12##
Claim 8
Dependent Claim
17 words
A compound or salt according to claim 1, wherein such compound is 9{-3-[4-(4-chlorobenzamido)-piperidino]-propyl}-adenine of the formula ##STR13##
Claim 9
Dependent Claim
24 words
A composition comprising an anti-allergic, anti-inflammatory and anti-oedematous effective amount of an adenine according to claim 1, in admixture with a pharmacologically compatible diluent.
Claim 10
Dependent Claim
27 words
A method of diminishing an allergic condition in a patient which comprises administering to such patient an anti-allergically effective amount of a compound according to claim 1.
Claim 11
Dependent Claim
19 words
The method of claim 9, wherein such compound is 9-{3-[4-(4-fluorobenzamido)-piperidino]-propyl}-adenine, 9-{3-[4-(4methylbenzamido)-piperidino]-propyl}-adenine, N 6 -(2-hydroxyethyl)-9-[3-(4-benzamido-piperidino)-propyl]-adenine, N 6 -n-butyl-9-[3-(4-benzamido-piperidino)-propyl]-adenine, or 9-{3-[4-(4-chlorobenzamido)-piperidino]propyl}-adenine.
Claim 12
Dependent Claim
27 words
A method of diminishing an inflammatory condition in a patient which comprises administering to such patient an anti-inflammatory effective amount of a compound according to claim 1.
Claim 13
Dependent Claim
27 words
A method of diminishing an oedematous condition in a patient which comprises administering to such patient an anti-oedematally effective amount of a compound according to claim 1.
Claim 14
Dependent Claim
15 words
A compound or salt according to claim 1, wherein R 3 is a hydrogen atom.
Claim 15
Dependent Claim
40 words
A compound or salt according to claim 1, wherein R 3 is a benzoyl radical optionally substituted by halogen atoms, or a hydroxyl, lower alkyl, lower alkoxy, lower alkoxycarbonyl, lower acyloxy, carboxyl, nitro, amino, cyano, trifluoromethyl, carbamoyl or benzyl radical.
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) | 1983-07-15 | 1984-01-14 | 1984-07-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-07-15 | 1988-01-14 | 1988-07-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-07-15 | 1992-01-14 | 1992-07-15 | $7700.00 | Window Closed / Lapsed |