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Title:
USE OF SEX HORMONES TO OBTAIN A NASAL PHARMACEUTICAL COMPOSITION THAT IS USEFUL IN THE TREATMENT OF UNDESIRABLE UTERINE BLEEDING
Document Type and Number:
WIPO Patent Application WO/2000/059447
Kind Code:
A2
Abstract:
The invention relates to the use of a sex hormone (in particular estradiol on its own or with noresthisterone combined with methyl cyclodextrine) to obtain a pharmaceutical composition that is suitable for nasal administration in order to treat undesirable uterine bleeding phenomena in women.

Inventors:
TSOUDEROS YANNIS (FR)
Application Number:
PCT/FR2000/000790
Publication Date:
October 12, 2000
Filing Date:
March 30, 2000
Export Citation:
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Assignee:
ADIR (FR)
TSOUDEROS YANNIS (FR)
International Classes:
A61K9/00; A61K9/08; A61K31/565; A61K31/567; A61K45/06; A61K47/02; A61K47/40; A61P15/00; C07J1/00; (IPC1-7): A61K/
Domestic Patent References:
WO1998003207A11998-01-29
WO1997046574A11997-12-11
Foreign References:
US4383993A1983-05-17
EP0349091B11992-05-06
Other References:
KARTHAUS M. ET AL: "Acute abdomen due to endometriosis as a diagnostic and therapeutic challenge in the treatment of acute myelocytic leukemia." ANNALS OF HEMATOLOGY, (1997) 74/1 (29-31)., XP000856615
BAYER S.R. ET AL: "Clinical manifestations and treatment of dysfunctional uterine bleeding." JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, (1993) 269/14 (1823-1828)., XP000856624
BRUN J.L.: "ÄManagement of uterine bleeding in 1994Ü. LE POINT SUR LE TRAITEMENT DES MENOMETRORRAGIES EN 1994." CONTRACEPTION FERTILITE SEXUALITE, (1994) 22/3 (147-151)., XP000856625
NILLIUS S.J.: "LH-RH nasal spray in contraception Future Aspects in Contraception. International Symposium. Heidelberg 5-8 September 1984." CONTRACEPT. DELIV. SYST., (1984) 5/3 (36)., XP000856854
COLL CAPDEVILA C: "Dysfunctional uterine bleeding and dysmenorrhea." EUROPEAN JOURNAL OF CONTRACEPTION AND REPRODUCTIVE HEALTH CARE, (1997 DEC) 2 (4) 229-37. REF: 28, XP000856691
BRENNER, PAUL F. ET AL: "Ovulation inhibition with nafarelin acetate nasal administration for six months" CONTRACEPTION (1985), 32(6), 531-51, XP000856801
Attorney, Agent or Firm:
Adir, Compagnie ET. (Courbevoie Cedex, Courbevoie Cedex, FR)
Adir, Compagnie ET. (Courbevoie Cedex, Courbevoie Cedex, FR)
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Claims:
Revendications
1. 1/Utilisation de 1'estradiol pour l'obtention d'une composition pharmaceutique convenant pour l'administration par voie nasale pour traiter les phénomènes de saignements utérins indésirables chez la femme. 2/Utilisation selon la revendication 1 caractérisée en ce que 1'estradiol est utilisé en mélange avec un progestatif.
2. 3/Utilisation selon la revendication.
3. caractérisée en ce que le progestatif est un dérivé de la 19nortestostérone. 4/Utilisation selon la revendication 3 caractérisée en ce que le progestatif est la noréthistérone. 5/Utilisation selon l'une quelconque des revendications 1 ou 2 caractérisée en ce que la composition convenant pour l'administration nasale contient de 1'estradiol ou un mélange estradiol/progestatif et une cyclodextrine. 6/Utilisation selon la revendication 5 caractérisée en ce que la cyclodextrine contenue dans la composition nasale est une cyclodextrine méthylée partiellement. 7/Utilisation selon la revendication 6 caractérisée en ce que la cyclodextrine méthylée partiellement contenue dans la composition nasale est méthylée de manière randomisée. 8/Composition pharmaceutique convenant pour l'administration par voie nasale selon l'une quelconque des revendications 1 ou 2, caractérisée en ce qu'elle se présente sous la forme d'une solution aqueuse contenant de 1'estradiol ou un mélange estradiol/progestatif et une cyclodextrine méthylée partiellement et randomisée. 9/Composition pharmaceutique selon la revendication 8 caractérisée en ce qu'elle contient 0,21 g d'hémihydrate d'estradiol, 2,10 g de cyclodextrine méthylée partiellement et randomisée, 0,9 g de chlorure de sodium pour une quantité d'eau purifiée suffisante pour obtenir un volume total de solution de 100 ml, le pH de ladite solution ayant été ajusté à 6.
Description:
INTERNATIONAL SEARCH REPORT nt ional Applicatlon wo PCT/FR00/00790 C. (Continuation) DOCUMENTS CONSIDERED TO BE RELEVANT Category Citation of document, with indication. where appropnate, of the relevant passages Relevant to daim No. X WO 98 03207 A (PHERIN CORP) 1 29 January 1998 (1998-01-29) abstract page 3, line 31-page 4, line 8 page 5, line 14-27 page 141, line 6-11 X WO 97 46574 A (PHERIN CORP) 1 11 December 1997 (1997-12-11) abstract page 4, paragraph 2 page 26, line 12-page 27, line 17 A KARTHAUS M. ET AL:"Acute abdomen due to 1-9 endometriosis as a diagnostic and therapeutic challenge in the treatment of acute myelocytic leukemia." ANNALS OF HEMATOLOGY, (1997) 74/1 (29-31)., XP000856615 abstract A BAYER S. R. ET AL:"Clinical 1-9 manifestations and treatment of dysfunctional uterine bleeding." JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION, (1993) 269/14 (1823-1828)., XP000856624 abstract page 1826, column 1, paragraph 3-page 1827, column 1, paragraph 4 A BRUN J. L. :"'Management of uterine 1-9 bleeding in 1994!. LE POINT SUR LE TRAITEMENT DES MENOMETRORRAGIES EN 1994." CONTRACEPTION FERTILITE SEXUALITE, (1994) 22/3 (147-151)., XP000856625 page 148, column 2, paragraph 2-page 149, column 1, paragraph 2 A NILLIUS S. J.:"LH-RH nasal spray in 1-9 contraception Future Aspects in Contraception. International Symposium. Heidelberg 5-8 September 1984." CONTRACEPT. DELIV. SYST., (1984) 5/3 (36)., XP000856854 abstract ___ 1 INTERNATIONAL SEARCH REPORT nt, cional Applicatlon o PCT/FR 00/00790 C. (Continuatlon) DOCUMENTS CONSIDERED TO BE RELEVANT Category ° Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No. A COLL CAPDEVILA C:"Dysfunctional uterine 1-9 bleeding and dysmenorrhea." EUROPEAN JOURNAL OF CONTRACEPTION AND REPRODUCTIVE HEALTH CARE, (1997 DEC) 2 (4) 229-37. REF: 28, XP000856691 abstract page 235, column 2, paragraph 3-page 236, column 2, paragraph 1 A BRENNER, PAUL F. ET AL:"Ovulation 1-9 inhibition with nafarelin acetate nasal administration for six months" CONTRACEPTION (1985), 32 (6), 531-51, XP000856801 the whole document 1 INTERNATIONAL SEARCH u alicauon No. PCT/FR00/00790 Continuation of box 1. 2 Claim 2 refers to a large number of possible compounds, i. e. « derivatives of 19- nortestosterone ». Said Claims lack clarity in such a way that it is practically impossible to carry out a full search owing to the fact that it is impossible to list in a comprehensive manner the compounds which can be designated by the term « derivatives of 19-nortestosterone ». Claims 2,3,5-8 refer to a compound/therapeutical application defined by the following pharmacological parameter: PI : a progestative. The use of said parameter in the present context is considered as leading to a lack of clarity as indicated in article 6 PCT. It is impossible to compare the parameter which the applicant chose to use with what is disclosed in prior art. In view of the lack of clarity arising therefrom it is practically impossible to carry out a full and meaningful search. For this reason, the search was restricted to compounds for which the relevant pharmacological data was provided and/or compounds mentioned in the claims and in the description of the present application, excluding « derivatives » of compounds specifically listed. The applicant is reminded that claims or parts of claims relating to inventions in respect of which no search report has been established need not be the subject of an international preliminary examination (PCT Rule 66.1 (e)). The EPO, in its capacity as the authority entrusted with the internal preliminary examination, does not as a general rule conduct a preliminary examination of subject matter for which no search report is available. This also applies to the case where the patent claims were amended after receipt of the international search report or to the case where the applicant provides new patent claims pursuant to the procedure mentioned in PCT Chapter II. INTERNATIONAL SEARCH REPORT Inte lonal AppilcatEn No Informationon patent famlly members PCT/FR 00/00790 PCT/FR 00/00790 Patent document Publication Patent family Publication cited in search report date member (s) date US 4383993 A 17-05-1983 US 4315925 A 16-02-1982 EP 0349091 A 03-01-1990 NL 8801670 A 01-02-1990 DE 68901417 D 11-06-1992 US 5089482 A 18-02-1992 WO 9803207 A 29-01-1998 US 6057439 A 02-05-2000 AU 3963797 A 10-02-1998 BG 103115 A 30-09-1999 BR 9711812 A 24-08-1999 CA 2260253 A 29-01-1998 CN 1226837 A 25-08-1999 EP 0914165 A 12-05-1999 NO 990305 A 22-03-1999 PL 331357 A 05-07-1999 US 6117860 A 12-09-2000 AU 4810397 A 24-04-1998 WO 9814194 A 09-04-1998 WO 9746574 A 11-12-1997 US 5922699 A 13-07-1999 AU 3307397 A 05-01-1998 BG 103060 A 29-10-1999 CA 2258177 A 11-12-1997 EP 0948521 A 13-10-1999 HU 9903432 A 28-03-2000 NO 990498 A 03-02-1999 PL 331522 A 19-07-1999