Patent US2525445A successfully refreshed from Google Patents.
Patent US5605700A successfully refreshed from Google Patents.
US5605700A
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US
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Topical administration of toremifene and its metabolites
Assignee: Orion Oyj
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Filing: 1993-03-25
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Granted: 1997-02-25
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Expires: 2013-03-25
Abstract
Abstract PCT No. PCT/FI93/00119 Sec. 371 Date Oct. 31, 1994 Sec. 102(e) Date Oct. 31, 1994 PCT Filed Mar. 25, 1993 PCT Pub. No. WO93/19746 PCT Pub. Date Oct. 14, 1993Transdermal preparations containing as active ingredient toremifene or one of its metabolites N-demethyltoremifene or 4-hydroxy-toremifene or their pharmaceutically acceptable non-toxic salts are useful for the treatment of cancers localized in the skin or on a short distance form the skin such as metastatic lesions of breast cancer. They may also be used in adjuvant therapy of breast cancer and in the reversal of multidrug resistance of cancer cells to cytotoxic drugs. Such transdernal preparations are of particular interest in the treatment of melanoma, lymphoma, Kaposi's sarcoma and fungoides mycosis.
Inventors
- 👤 Michael W. DeGregorio
- 👤 Kauko O. A. Kurkela
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 05:41
CPC Classifications
B; B82; B82Y; B82Y5/00; A; A61; A61K; A61K31/00; A61K31/13; A61K31/135; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; A61P; A61P17/00; A61P35/00; A61P35/04
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
32 words
A transdermal preparation comprising as active ingredient toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N, N-dimethylamino)ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 2
Dependent Claim
32 words
A transdermal preparation comprising as active ingredient toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N, N-dimethylamino)ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 3
Dependent Claim
20 words
A preparation according to claim 1 which is in the form of an ointment, emulsion, lotion, solution, gel or cream.
Claim 4
Dependent Claim
15 words
A preparation according to claim 1 where the preparation is a transdermal delivery patch system.
Claim 5
Dependent Claim
20 words
A preparation according to claim 2 where the active ingredient is in the form of a complex of a cyclodextrin.
Claim 6
Dependent Claim
18 words
A preparation according to claim 1 where the active ingredient is toremifene or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
15 words
A transdermal preparation according to claiam 1 for use in the treatment of breast cancer.
Claim 8
Dependent Claim
15 words
A transdermal preparation according to claiam 1 for use in the treatment of breast cancer.
Claim 9
Dependent Claim
16 words
A transdermal preparation according to claim 1 for use in the adjuvant therapy of breast cancer.
Claim 10
Dependent Claim
21 words
A transdermal preparation according to claim 1 for use in the reversal of multidrug resistance of cancer cells to cytotoxic drugs.
Claim 11
Dependent Claim
20 words
A transdermal preparation according to claim 1 for use in the treatment of melanoma, lymphoma, Kaposi's sarcoma or fungoides mycosis.
Claim 12
Independent Claim
53 words
A method of treatment of breast cancer comprising administering transdermally to a subject in need of such treatment an effective amount of a transdermal preparation comprising as active incredient toremifene or one of its metabolites N-demethyl-toremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]-phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 13
Independent Claim
53 words
A method of treatment of breast cancer comprising administering transdermally to a subject in need of such treatment an effective amount of a transdermal preparation comprising as active incredient toremifene or one of its metabolites N-demethyl-toremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]-phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 14
Independent Claim
56 words
A method for reversing the multidrug resistance of cancer cells to a cytotoxic drug comprising administering transdermally a multidrug resistance reversal effective amount of toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethylamino)-ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients, to a subject in need of such treatment.
Claim 15
Independent Claim
56 words
A method for reversing the multidrug resistance of cancer cells to a cytotoxic drug comprising administering transdermally a multidrug resistance reversal effective amount of toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethylamino)-ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients, to a subject in need of such treatment.
Claim 16
Independent Claim
58 words
A method of treatment of melanoma, lymphoma, Kaposi's sarcoma or fungoides mycosis comprising administering transdermally to a subject in need of such treatment an effective amount of a transdermal preparation comprising as active incredient toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethyl-amino)ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 17
Independent Claim
58 words
A method of treatment of melanoma, lymphoma, Kaposi's sarcoma or fungoides mycosis comprising administering transdermally to a subject in need of such treatment an effective amount of a transdermal preparation comprising as active incredient toremifene or one of its metabolites N-demethyltoremifene(4-chloro-1,2-diphenyl-[4-[2-(N-methylamino)ethoxy]-phenyl]-1-butene) or 4-hydroxytoremifene(4-chloro-1-(4-hydroxyphenyl)-2-phenyl-1-[4-[2-(N,N-dimethyl-amino)ethoxy]phenyl]-1-butene) or a pharmaceutically acceptable non-toxic salt thereof, together with one or more pharmaceutically acceptable excipients.
Claim 18
Dependent Claim
20 words
A preparation according to claim 3 where the active ingredient is in the form of a complex of a cyclodextrin.
Claim 19
Dependent Claim
18 words
A preparation according to claim 2 where the active ingredient is toremifene or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
18 words
A preparation according to claim 3 where the active ingredient is toremifene or a pharmaceutically acceptable salt thereof.
Claim 21
Dependent Claim
18 words
A preparation according to claim 4 where the active ingredient is toremifene or a pharmaceutically acceptable salt thereof.
Claim 22
Dependent Claim
15 words
A transdermal preparation according to claim 2 for use in the treatment of breast cancer.
Claim 23
Dependent Claim
15 words
A transdermal preparation according to claim 3 for use in the treatment of breast cancer.
Claim 24
Dependent Claim
15 words
A transdermal preparation according to claim 4 for use in the treatment of breast cancer.
Claim 25
Dependent Claim
15 words
A transdermal preparation according to claim 5 for use in the treatment of breast cancer.
Claim 26
Dependent Claim
21 words
A transdermal preparation according to claim 2 for use in the reversal of multidrug resistance of cancer cells to cytotoxic drugs.
References Cited (Backward Citations)
EP0095875A2
Cited
US4996225A
Cited
US4919937A
Cited
EP0240131A2
Cited
US5132115A
Cited
US4990538A
Cited
US5189212A
Cited
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