Title:
USE OF ANTIPROGESTAGENS IN COMBINED THERAPY
Document Type and Number:
WIPO Patent Application WO/2000/066129
Kind Code:
A2
Abstract:
It has been found that the compound satisfying the structural formula (I) given below has a surprisingly good suitability for being administered intermittently. This particular compound therewith has the highly advantageous property that it can be used in the specific medical application of combined therapy with progestagen-only preparations.
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Inventors:
COELINGH BENNINK HERMAN JAN TI (NL)
DECKERS GODEFRIDUS HERMANUS JO (NL)
DOLS PAUL PETER MARIE ANTONIUS (NL)
ORLEMANS EVERARDUS OTTO MARIA (NL)
SCHOONEN WILHELMUS GERARDUS ED (NL)
DECKERS GODEFRIDUS HERMANUS JO (NL)
DOLS PAUL PETER MARIE ANTONIUS (NL)
ORLEMANS EVERARDUS OTTO MARIA (NL)
SCHOONEN WILHELMUS GERARDUS ED (NL)
Application Number:
PCT/EP2000/003747
Publication Date:
November 09, 2000
Filing Date:
April 25, 2000
Export Citation:
Assignee:
AKZO NOBEL NV (NL)
COELINGH BENNINK HERMAN JAN TI (NL)
DECKERS GODEFRIDUS HERMANUS JO (NL)
DOLS PAUL PETER MARIE ANTONIUS (NL)
ORLEMANS EVERARDUS OTTO MARIA (NL)
SCHOONEN WILHELMUS GERARDUS ED (NL)
COELINGH BENNINK HERMAN JAN TI (NL)
DECKERS GODEFRIDUS HERMANUS JO (NL)
DOLS PAUL PETER MARIE ANTONIUS (NL)
ORLEMANS EVERARDUS OTTO MARIA (NL)
SCHOONEN WILHELMUS GERARDUS ED (NL)
International Classes:
A61K31/567; A61K31/58; A61P15/00; A61P15/18; (IPC1-7): A61K31/58
Domestic Patent References:
| WO1994004156A1 | 1994-03-03 | |||
| WO1993021927A1 | 1993-11-11 | |||
| WO1997049407A1 | 1997-12-31 | |||
| WO1993017686A1 | 1993-09-16 |
Foreign References:
| EP0549041A1 | 1993-06-30 |
Other References:
SCHOONEN W.G.E. ET AL: "Human progesterone receptor A and B isoforms in CHO cells. II. Comparison of binding, transactivation and EDD50 values of several synthetic (anti)progestagens in vitro in CHO and MCF-7 cells and in vivo in rabbits and rats" JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 64, no. 3, 1998, pages 157-170, XP002124156 United Kingdom
Attorney, Agent or Firm:
Kraak, Hajo (P.O. Box 20 BH Oss, NL)
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Claims:
Claims:
| 1. | The use of Org 33245 as defined in the description for the manufacture of a contraceptive or HRT agent wherein Org 33245 is to be administered intermittently, the intermission between each pair of sequentially administered dosage units of antiprogestagen being more than one day. |
| 2. | A use according to claim 1, characterised in that the intermittent administration of Org 33245 takes place as an addition to progestagenonly therapy. |
| 3. | The use of Org 33245 for the manufacture of a medicament for minimizing uterine bleeding in a female using a progestinonly pharmaceutical preparation, characterized in that the antiprogestagen is Org 33245 as defined in the description. |
| 4. | A use according to any of the preceding claims, characterised in that a dosage of Org 33245 is to be administered 17 days during a cycle of 2832 days, wherein one dosage marks the end of a cycle and the optional other dosages are to be administered regularly divided over the remaining days of the cycle. |
| 5. | A contraceptive kit providing means (a) for the daily administration of a progestagen and means (b) for the intermittent administration of an anti progestagen, wherein the latter means (b) comprises as the antiprogestagen the compound Org 33245 as defined in the description. |
| 6. | A combined means for the dosage of a progestagen and an antiprogestagen, characterised in that the antiprogestagen is Org 33245 as defined in the description. |
| 7. | A method of contraception comprising daily administering to a female of child bearing age a contraceptively effective amount of a progestagen and intermittently administering an antiprogestagen, wherein the antiprogestagen is Org 33245 as defined in the description. |
| 8. | A method of treatment of irregular or breakthrough uterine bleeding in a female using a progestagenonly preparation, comprising intermittenty administering an antiprogestagen, wherein the antiprogestagen is Org 33245 as defined in the description. |
| 9. | A method according to claim 7 or 8, wherein the antiprogestagen is administered on 14 days in a cycle of 2832 days. |
Description:
INTERNATIONAL SEARCH REPORT Intem al Applteation No PCT/EP 00/03747 C. (Continuation) DOCUMENTS CONSIDERED TO BE RELEVANT Category ° Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No. Y WO 97 49407 A (AKZO NOBEL N. V.) 1,2,4-7, 31 December 1997 (1997-12-31) 9 cited in the application page 2, line 18-28; claims 1-4,9,10 page 4, line 5-9 Y SCHOONEN W. G. E. ET AL:"Human 1,3,5-8 progesterone receptor A and B isoforms in CHO cells. II. Comparison of binding, transactivation and EDD50 values of several synthetic (anti) progestagens in vitro in CHO and MCF-7 cells and in vivo in rabbits and rats" JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULARBIOLOGY, vol. 64, no. 3,1998, pages 157-170, XP002124156 United Kingdom page 164, right-hand column-page 165 page 167, right-hand column, line 1-4 A WO 93 17686 A (SCHERING AG) 1,2,4-9 16 September 1993 (1993-09-16) page 4, line 14-16 page 5, line 28-36 page 7, line 3-7 page 10, line 19-23 page 9, line 31-page 10, line 9 A EP 0 549 041 A (AKZO N. V.) 1,3,5-8 30 June 1993 (1993-06-30) cited in the application claim 6 ; example 1 INTERNATIONAL SEARCH REPORT InterI Application No In-formation an patent family members PCT/EP 00/03747 PCT/EP00/03747 PatentPublication Patent family Publication cited in search report datemember (s) date WO 9404156 A 03-03-1994 AU 4708993 A 15-03-1994 MX 9304931 A 31-08-1994 ZA 9305617 A 07-03-1994 ZA 9305617 A 07-03-1994 WO 9321927 A 11-11-1993 WO 9321926 A 11-11-1993 AT 187644 T 15-01-2000 AU 1918092 A 29-11-1993 AU 4368593 A 29-11-1993 CA 2131911 A 11-11-1993 CN 1079651 A 22-12-1993 DE 69327319 D 20-01-2000 DE 69327319 T 13-07-2000 DK 646008 T 15-05-2000 EP 0646008 A 05-04-1995 ES 2142345 T 16-04-2000 FI 945207 A 04-11-1994 GR 3032797 T 30-06-2000 JP 8509456 T 08-10-1996 NO 944210 A 04-11-1994 NZ 253405 A 24-06-1997 PT 646008 T 28-04-2000 US 5622943 A 22-04-1997 ZA 9303153 A 06-12-1993 ZA 9303153 A 06-12-1993 WO 9749407 A 31-12-1997 AU 725670 B 19-10-2000 AU 3436097 A 14-01-1998 BR 9709934 A 10-08-1999 CZ 9804289 A 11-08-1999 EP 0912186 A 06-05-1999 NO 986104 A 23-12-1998 NZ 332894 A 28-05-1999 PL 330916 A 07-06-1999 PL 330916 A Q7-06-1999 WO 9317686 A 16-09-1993 CN 1079386 A 15-12-1993 AU 678150 B 22-05-1997 BR 9306005 A 23-06-1998 CA 2134961 A 03-09-1993 CZ 9402111 A 13-12-1995 EP 0630246 A 28-12-1994 FI 944022 A 01-09-1994 IL 104915 A 15-07-1998 JP 7509218 T 12-10-1995 MX 9301121 A 01-09-1993 NO 943234 A 01-11-1994 NZ 268304 A 24-02-1997 PL 174785 B 30-09-1998 PL 172790 B 28-11-1997 SK 104694 A 10-01-1996 ZA 9301492 A 23-12-1993 AU 3787993 A 05-10-1993 RU 2127112 C 10-03-1999 RU 2127112 C 10-03-1999 EP 549041 A 30-06-1993 AT 128983 T 15-10-1995 AU 655858 B 12-01-1995 AU 3009392 A 24-06-1993 CA 2084431 A 21-06-1993 DE 69205405 D 16-11-1995 DE 69205405 T 09-05-1996 INTERNATIONAL SEARCH REPORT Inte Xpplication No wormatlon on patenttarnily members PCT/EP 00/03747 l.. _. Patent document Publication Patent family Publication cited in search report date member (s) date EP 549041 A DK 549041 T 29-01-1996 ES 2081040 T 16-02-1996 FI 925790 A 21-06-1993 GR 3018630 T 30-04-1996 HK 1002033 A 24-07-1998 JP 5255380 A 05-10-1993 MX 9207394 A 30-07-1993 NO 302525 B 16-03-1998 NZ 245520 A 24-02-1995 US 5292878 A 08-03-1994 ZA 9209315 A 24-05-1993 ZA 9209315 A 24-05-1993