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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
•
Expires: 2002-05-12
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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 15:32
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

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