Title:
COMPOSITIONS COMPRISING PHOSPHODIESTERASE INHABITORS FOR THE TREATMENT OF SEXUAL DISFUNCTION
Document Type and Number:
WIPO Patent Application WO/2000/066099
Kind Code:
A2
Abstract:
The present invention relates to highly selective phosphodiesterase (PDE) enzyme inhibitors and to their use in pharmaceutical articles of manufacture. In particular, the present invention relates to potent inhibitors of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase type 5 (PDE5) that when incorporated into a pharmaceutical product at about 1 to about 20 mg unit dosage are useful for the treatment of sexual dysfunction.
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Inventors:
PULLMAN WILLIAM ERNEST (US)
WHITAKER JOHN STEVEN (US)
WHITAKER JOHN STEVEN (US)
Application Number:
PCT/US2000/011129
Publication Date:
November 09, 2000
Filing Date:
April 26, 2000
Export Citation:
Assignee:
LILLY ICOS LLC (US)
PULLMAN WILLIAM ERNEST (US)
WHITAKER JOHN STEVEN (US)
PULLMAN WILLIAM ERNEST (US)
WHITAKER JOHN STEVEN (US)
International Classes:
A61K9/00; C07D471/14; A61K9/08; A61K9/20; A61K9/48; A61K31/00; A61K31/4985; A61K45/00; A61P15/00; A61P15/10; A61P43/00; C07D487/14; (IPC1-7): A61K31/00
Domestic Patent References:
| WO1997003675A1 | 1997-02-06 | |||
| WO1999059584A1 | 1999-11-25 | |||
| WO1995019978A1 | 1995-07-27 |
Other References:
DATABASE WPI Section Ch, Week 200029 Derwent Publications Ltd., London, GB; Class B02, AN 2000-339026 XP002152606 & WO 00 20033 A (EISAI CO LTD), 13 April 2000 (2000-04-13)
ISRAEL M: "VIAGRA: THE FIRST ORAL TREATMENT FOR IMPOTENCE" PHARMACEUTICAL JOURNAL,PHARMACEUTICAL SOCIETY, LONDON,GB, vol. 261, 1 August 1998 (1998-08-01), pages 164-165, XP000919343 ISSN: 0031-6873
GOLDENBERG M M: "SAFETY AND EFFICACY OF SILDENAFIL CITRATE IN THE TREATMENT OF MALE ERECTILE DYSFUNCTION" CLINICAL THERAPEUTICS,US,EXCERPTA MEDICA, PRINCETON, NJ, vol. 20, no. 6, 1998, pages 1033-1048, XP000853855 ISSN: 0149-2918
See also references of EP 1173181A2
ISRAEL M: "VIAGRA: THE FIRST ORAL TREATMENT FOR IMPOTENCE" PHARMACEUTICAL JOURNAL,PHARMACEUTICAL SOCIETY, LONDON,GB, vol. 261, 1 August 1998 (1998-08-01), pages 164-165, XP000919343 ISSN: 0031-6873
GOLDENBERG M M: "SAFETY AND EFFICACY OF SILDENAFIL CITRATE IN THE TREATMENT OF MALE ERECTILE DYSFUNCTION" CLINICAL THERAPEUTICS,US,EXCERPTA MEDICA, PRINCETON, NJ, vol. 20, no. 6, 1998, pages 1033-1048, XP000853855 ISSN: 0149-2918
See also references of EP 1173181A2
Attorney, Agent or Firm:
Napoli, James J. (O'Toole Gerstein, Murray & Borun, 6300
Sears Tower, 233 South Wacker Driv, Chicago IL, US)
Download PDF:
Claims:
WHAT IS CLAIMED IS:
| 1. | A pharmaceutical unit dosage composi tion comprising about 1 to about 20 mg of a compound having the structural formula: said unit dosage form suitable for oral administra tion. |
| 2. | The dosage form of claim 1 comprising about 2 to about 20 mg of the compound in unit dosage form. |
| 3. | The dosage form of claim 1 comprising about 5 to about 20 mg of the compound in unit dosage form. |
| 4. | The dosage form of claim 2 comprising about 2.5 mg of the compound in unit dosage form. |
| 5. | The dosage form of claim 3 comprising about 5 mg of the compound in unit dosage form. |
| 6. | The dosage form of claim 3 comprising about 10 mg of the compound in unit dosage form. |
| 7. | The dosage form of claims 1 through 6 wherein the unit dose is in a form selected from the group consisting of a liquid, a tablet, a capsule, and a gelcap. |
| 8. | The dosage form of claims 1 through 6 wherein the unit dose is in the form of a tablet. |
| 9. | The dosage form of claims 1 through 6 for use in treating a condition where inhibition of PDE5 is desirable. |
| 10. | The dosage form of claim 9 wherein the condition is a sexual dysfunction. |
| 11. | The dosage form of claim 10 wherein the sexual dysfunction is male erectile dysfunction. |
| 12. | The dosage form of claim 10 wherein the sexual dysfunction is female arousal disorder. |
| 13. | A method of treating sexual dysfunc tion in a patient in need thereof comprising ad ministering one or more unit dose containing about 1 to about 20 mg, up to a maximum total dose of 20 mg per day, of a compound having the structure. |
| 14. | The method of claim 13 wherein the unit dose contains about 2 to about 20 mg of the compound. |
| 15. | The method of claim 13 wherein the unit dose contains about 5 mg of the compound. |
| 16. | The method of claim 13 wherein the unit dose contains about 10 mg of the compound and is administered once per day. |
| 17. | The method of claim 13 wherein the unit dose is in a form selected from the group con sisting of a liquid, a tablet, a capsule, and a gelcap. |
| 18. | The invention as hereinbefore de scribed. |
| 19. | Use of a unit dose containing about 1 to about 20 mg of a compound having the structure for the manufacture of a medicament for the treat ment of sexual dysfunction in a patient in need thereof. |
Description:
INTERNATIONALSEARCHREPORT r---------------. Tinter.nalApplicationNo PCT/US00/11129 C.(Continuation)DOCUMENTSCONSIDEREDTOBERELEVANT Category ° Citathn ofdocument,withindication,whereappropriate,oftherelevantpass
agesRelevanttoclaimNo. XWO9519978A(GLAXOLABSA;DAUGANALAIN1-12 CLAUDEMARIE(FR)) 27July1995(1995-07-27) cited intheapplication page8,line5-15;example78 page80,line21,22 page80,lastparagraph claims10,12,14 P,XDATABASEWPI1-12 SectionCh,Week200029 DerwentPublicationsLtd.,London,GB; ClassB02,AN2000-339026 XP002152606 &WO0020033A(EISAICOLTD), 13April2000(2000-04-13) abstract AISRAELM:"VIAGRA:THEFIRSTORAL1-19 TREATMENTFORIMPOTENCE" PHARMACEUTICALJOURNAL,PHARMACEUTICAL SOCIETY,LONDON,GB, vol.261,1August1998(1998-08-01), pages164-165,XP000919343 ISSN:0031-6873 page164,column1-2 AGOLDENBERGMM:"SAFETYANDEFFICACYOF1-19 SILDENAFILCITRATEINTHETREATMENTOF MALEERECTILEDYSFUNCTION" CLINICALTHERAPEUTICS,US,EXCERPTAMEDICA, PRINCETON,NJ, vol.20,no.6,1998,pages1033-1048, XP000853855 ISSN:0149-2918 page1041,column1-page1042,column1 2 INTERNATIONALSEARCHREPORT Inten nal ApplicationNo informationon patent tamily memiws PCT/US 00/11129 PatentdocumentPublication Patent family Publication citedinsearchreportdate member(s)date WO9703675A06-02-1997AU 704955 B 13-05-1999 AU 6419196 A 18-02-1997 BR 9609758 A 26-01-1999 CA 2226784 A 06-02-1997 CN 1195290 A 07-10-1998 CZ 9800033 A 13-05-1998 EP 0839040 A 06-05-1998 HU 9900065 A 28-05-1999 JP 11509221 T 17-08-1999 NO 980153 A 10-03-1998 PL 324495 A 25-05-1998 SK 3998 A 08-07-1998 US 6140329 A 31-10-2000 WO9959584A25-11-1999AU 4068599 A 06-12-1999 WO9519978A27-07-1995AP 556 A 07-11-1996 AT 169018 T 15-08-1998 AU 689205 B 26-03-1998 AU 1574895 A 08-08-1995 AU 707055 B 01-07-1999 AU 7391298 A 20-08-1998 BG 62733 B 30-06-2000 BG 100727 A 28-02-1997 BR 9506559 A 28-10-1997 CA 2181377 A 27-07-1995 CN 1143963A,B26-02-1997 CZ 9602116 A 11-06-1997 DE 69503753 D 03-09-1998 DE 69503753 T 21-01-1999 DK 740668 T 03-05-1999 EP 0740668 A 06-11-1996 ES 2122543 T 16-12-1998 FI 962927 A 19-07-1996 HR 950023 A 30-04-1998 HU 74943 A 28-03-1997 IL 112384 A 16-08-1998 JP 9508113 T 19-08-1997 LV 11690 A 20-02-1997 LV 11690 B 20-06-1997 NO 963015 A 09-09-1996 NZ 279199 A 26-01-1998 PL 315559 A 12-11-1996 RU 2142463 C 10-12-1999 SG 49184 A 18-05-1998 SI 740668 T 28-02-1999 SK 94096 A 09-04-1997 US 6025494 A 15-02-2000 US 6127542 A 03-10-2000 US 5859006 A 12-01-1999 ZA 9500424 A 27-09-1995 WO0020033A13-04-2000JP 2000178204 A 27-06-2000 JP 2000191518 A 11-07-2000
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