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US5382600A
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3,3-diphenylpropylamines and pharmaceutical compositions thereof
Assignee: Pfizer Health AB
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Filing: 1991-12-19
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Granted: 1995-01-17
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Expires: 2011-12-19
Abstract
Abstract ##STR1## Novel 3,3-diphenylpropylamines of formula (I) wherein R 1 signifies hydrogen or methyl, R 2 , R 3 and R 4 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphanoyl or halogen, and X represents a tertiary amino group -NR 5 , R 6 , wherein R 5 and R 6 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and which may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers, their use as drugs, especially as anticholinergic agents, their use for preparing an anticholinergic drug, pharmaceutical compositions containing the novel amines, and methods for preparing the same.
Inventors
- 👤 Nils A. Jonsson
- 👤 Bengt A. Sparf
- 👤 Lembit Mikiver
- 👤 Pinchas Moses
- 👤 Lisbet Nilvebrant
- 👤 Gunilla Glas
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 04:06
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/08; C07C; C07C215/00; C07C215/46; C07C215/48; C07C215/54; C07C217/00; C07C217/54; C07C217/56; C07C217/62; C07C309/00; C07C309/63; C07C309/72; C07C309/73; C07C43/00; C07C43/02; C07C43/20; C07C43/23; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/10; C07D211/14; C07D211/36; C07D211/40; C07D211/44; C07D211/46; C07C2603/00; C07C2603/56; C07C2603/58; C07C2603/70; C07C2603/74
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
122 words
3,3-Diphenylpropylamines of formula I ##STR31## wherein R 1 signifies hydrogen or methyl, R 2 , R 3 and R 4 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR32## wherein each of R 5 and R 6 independently signifies C 1-6 alkyl, which may be joined to form a non-aromatic ring having no hetero atom other than the amine nitrogen and each of which may carry a hydroxy substituent, or adamantyl, and wherein R 5 and R 6 together contain at least four carbon atoms, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.
Claim 2
Dependent Claim
122 words
3,3-Diphenylpropylamines of formula I ##STR31## wherein R 1 signifies hydrogen or methyl, R 2 , R 3 and R 4 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR32## wherein each of R 5 and R 6 independently signifies C 1-6 alkyl, which may be joined to form a non-aromatic ring having no hetero atom other than the amine nitrogen and each of which may carry a hydroxy substituent, or adamantyl, and wherein R 5 and R 6 together contain at least four carbon atoms, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.
Claim 3
Dependent Claim
24 words
3,3-Diphenylpropylamines according to claim 1, wherein at least one of R 5 and R 6 is C 1-6 alkyl comprising a branched carbon chain.
Claim 4
Dependent Claim
23 words
3,3-Diphenylpropylamines according to claim 1, wherein X signifies any of the following groups a)-f), each of which may carry a hydroxy substituent: ##STR33##
Claim 5
Dependent Claim
37 words
3,3-Diphenylpropylamines according to claim 1, selected from the group consisting of the following compounds, their salts with physiologically acceptable acids and, where possible, their racemates and individual enantiomers: N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine,N-methyl-N-tert.butyl-3-(2-hydroxyphenyl)-3-phenylpropylamine, N-methyl-N-tert.butyl-3-(2,4-dihydroxyphenyl)-3-phenylpropylamine, N-methyl-N-tert.butyl-3,3-bis-(2-hydroxyphenyl)propylamine, N,N-diisopropyl-3,3-bis-(2-hydroxyphenyl)propylamine, N,N-diisopropyl-3-(2,5-dihydroxyphenyl)-3-phenylpropylamine, N-methyl-N-tert.butyl-3-(2,5-dihydroxyphenyl)-3-phenylpropylamine,N-N-diisopropyl-3-(2-methoxyphenyl)-3-phenylpropylamine, N-2,2,6,6-tetramethylpiperdine,(+)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine, and N,N-diisopropyl-3-(5-chloro-2-hydroxyphenyl)-3-phenylpropylamine.
Claim 6
Dependent Claim
15 words
A pharmaceutical composition comprising a 3,3-diphenylpropylamine according to claim 1 and a compatible pharmaceutical carrier.
Claim 7
Dependent Claim
7 words
The 3,3-diphenylpropylamines of claim 1 being (+)-isomers.
Claim 8
Dependent Claim
15 words
The pharmaceutical composition of claim 5 wherein the 3,3-diphenylpropylamine is present in effective anticholinergic amount.
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) | 1998-01-16 | 1998-07-18 | 1999-01-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2002-01-16 | 2002-07-18 | 2003-01-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2006-01-16 | 2006-07-18 | 2007-01-17 | $7700.00 | Window Closed / Lapsed |