US4518588A
Expired / Lapsed
US
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Process for the preparation of an inclusion complex of N-(1--phenylethyl)-3,3-diphenylpropylamine and the hydrochloride thereof respectively with cyclodextrin
Assignee: Chinoin Private Co Ltd
•
Filing: 1982-05-12
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Granted: 1985-05-21
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Expires: 2002-05-12
Abstract
Abstract An inclusion complex is disclosed of N-(1-phenylethyl)-3, 3-diphenyl-propylamine or its hydrochloride complexed with a cyclodextrin as well as a process for the preparation thereof and pharmaceutical compositions containing same. The new inclusion complexes have coronary dilatory activity and have greater water soluble than simple N-(1-phenylethyl)-3, 3-diphenyl-propyl amine or the hydrochloride thereof.
Inventors
- 👤 Jozsef Szejtli
- 👤 Agnes Stadler nee Szoke
- 👤 Maria Vikmon nee Kiraly
- 👤 Dezso Korbonits
- 👤 Sandor Virag
- 👤 Istvan Turcsan
- 👤 Pal Kiss
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 14:46
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; A61K31/00; A61K31/13; A61K31/135; B; B82; B82Y; B82Y5/00; C; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0012; C08B37/0015
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
55 words
A process for the preparation of inclusion complexes of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride with cyclodextrin, which comprises reacting N-(1-phenylethyl)-3,3-diphenylpropylamine base or hydrochloride thereof with cyclodextrin in an amount of 1 to 3 mmoles of the cyclodextrin per mmole of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride, under stirring at 4° to 60° C. in aqueous or ethanolic medium.
Claim 2
Dependent Claim
55 words
A process for the preparation of inclusion complexes of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride with cyclodextrin, which comprises reacting N-(1-phenylethyl)-3,3-diphenylpropylamine base or hydrochloride thereof with cyclodextrin in an amount of 1 to 3 mmoles of the cyclodextrin per mmole of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride, under stirring at 4° to 60° C. in aqueous or ethanolic medium.
Claim 3
Dependent Claim
19 words
A process as claimed in claim 1 which comprises using N-(1-phenylethyl)-3,3-diphenylpropylamine and cyclodextrin at a molar ratio of 1:3.
Claim 4
Dependent Claim
19 words
A process as claimed in claim 1 which comprises using N-(1-phenylethyl)-3,3-diphenylpropylamine and cyclodextrin at a molar ratio of 1:1.
Claim 5
Dependent Claim
19 words
A process as claimed in claim 1 which comprises using N-(1-phenylethyl)-3,3-diphenylpropylamine-hydrochloride and cyclodextrin at a molar ratio of 1:1.
Claim 6
Dependent Claim
28 words
A process as defined in claim 1 which comprises performing the reaction in aqueous medium in the presence of 1-20 ml. of water to 1 mmole of cyclodextrin.
Claim 7
Dependent Claim
19 words
A process as defined in claim 1 which comprises conducting the reaction in 5-32% by volume of aqueous-ethanolic medium.
Claim 8
Dependent Claim
13 words
A process as claimed in claim 1, which comprises reacting N-(1-phenylethyl)-3,3-diphenylpropylamine with cyclodextrin.
Claim 9
Dependent Claim
14 words
A process as claimed in claim 1, which comprises reacting N-(1-phenylethyl)-3,3-diphenylpropylamine hydrochloride with cyclodextrin.
Claim 10
Dependent Claim
20 words
A process as claimed in claim 1, which comprises using hydrochloride of N-(1-phenylethyl)-3,3-diphenylpropylamine formed in situ in the complex formation.
Claim 11
Dependent Claim
13 words
A process as claimed in claim 1, which comprises using α-cyclodextrin as cyclodextrin.
Claim 12
Dependent Claim
13 words
A process as claimed in claim 1, which comprises using β-cyclodextrin as cyclodextrin.
Claim 13
Dependent Claim
13 words
A process as claimed in claim 1, which comprises using γ-cyclodextrin as cyclodextrin.
Claim 14
Dependent Claim
28 words
Coronary dilatator calcium antagonist pharmaceutical compositions containing as active ingredient a pharmaceutically effective amount of either N-(1-phenylethyl)-3,3-diphenylpropylamine-hydrochloride cyclodextrin complex or N-(1-phenylethyl)-3,3-diphenylpropylamine-cyclodextrin complex admixed with a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
28 words
Coronary dilatator calcium antagonist pharmaceutical compositions containing as active ingredient a pharmaceutically effective amount of either N-(1-phenylethyl)-3,3-diphenylpropylamine-hydrochloride cyclodextrin complex or N-(1-phenylethyl)-3,3-diphenylpropylamine-cyclodextrin complex admixed with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
7 words
N-(1-phenylethyl)-3,3-diphenylpropylamine-α-cyclodextrin complex as defined in claim 1.
Claim 17
Dependent Claim
7 words
N-(1-phenylethyl)-3,3-diphenylpropylamine-β-cyclodextrin complex as defined in claim 1.
Claim 18
Dependent Claim
7 words
N-(1-phenylethyl)-3,3-diphenylpropylamine-γ-cyclodextrin complex as defined in claim 1.
Claim 19
Dependent Claim
9 words
N-(1-phenylethyl)-3,3-diphenylpropylamine hydrochloride β-cyclodextrin complex as defined in claim 1.
Claim 20
Dependent Claim
24 words
An inclusion complex of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride complexed with a cyclodextrin selected from the group which consists of a α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin.
Claim 21
Dependent Claim
24 words
An inclusion complex of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride complexed with a cyclodextrin selected from the group which consists of a α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin.
Claim 22
Dependent Claim
45 words
A coronary dilatative calcium antagonist method of treatment which comprises administering to a susceptible subject an effective amount of a composition consisting essentially of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride complexed with at least one cyclodextrin selected from the group which consists of α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin.
Claim 23
Dependent Claim
45 words
A coronary dilatative calcium antagonist method of treatment which comprises administering to a susceptible subject an effective amount of a composition consisting essentially of N-(1-phenylethyl)-3,3-diphenylpropylamine or its hydrochloride complexed with at least one cyclodextrin selected from the group which consists of α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin.
References Cited (Backward Citations)
US3553191A
Cited
US4407795A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-05-20 | 1988-11-19 | 1989-05-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-05-20 | 1992-11-19 | 1993-05-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-05-20 | 1996-11-19 | 1997-05-21 | $7700.00 | Window Closed / Lapsed |