Title:
ANTIBIRAL COMPOSITIONS CONTAINING PHORBOL DERIVATIVES AS THE MAIN ACTIVE INGREDIENT
Document Type and Number:
WIPO Patent Application WO/2001/082927
Kind Code:
A1
Abstract:
Antiviral compositions containing as the active ingredients: (i) phorbol derivatives which are represented by the general formula (I), have a ratio r=CC¿0?/IC¿100? of 2 or more (wherein IC¿100? represents the concentration at which the cell pathogenic effect (CPE) of HIV-1 in MT-4 cells is inhibited at a ratio of 100%; and CC¿0? represents the concentration at which the survival of MT-4 cells is reduced in a cell proliferation test), and show activation of protein kinase C (PKC) at a concentration of 10 ng/mL of 30% or less; and (ii) a chemical capable of suppressing or inhibiting the replication process or the maturation process of viruses. In said formula (I), wherein R¿1?, R¿2?, R¿3?, R¿4? and R¿5? independently represent each hydrogen, an aliphatic carboxylate or an aromatic carboxylate. These compositions are efficacious particularly against human immunodeficiency virus (HIV).
Inventors:
HATTORI MASAO (JP)
YAMAMOTO NAOKI (JP)
MORI MASAO (JP)
YAMAMOTO NAOKI (JP)
MORI MASAO (JP)
Application Number:
PCT/JP2000/002913
Publication Date:
November 08, 2001
Filing Date:
May 02, 2000
Export Citation:
Assignee:
LEAD CHEM CO LTD (JP)
HATTORI MASAO (JP)
YAMAMOTO NAOKI (JP)
MORI MASAO (JP)
HATTORI MASAO (JP)
YAMAMOTO NAOKI (JP)
MORI MASAO (JP)
International Classes:
A61K31/22; A61K31/23; A61K31/231; A61P31/18; C07C69/00; (IPC1-7): A61K31/22; A61K31/122; A61K31/216; A61K31/23; A61K31/231; A61K45/00; A61P31/18
Domestic Patent References:
| WO1998004290A2 | 1998-02-05 |
Foreign References:
| JPH10287617A | 1998-10-27 |
Other References:
SAHAR EL-MEKKAWY ET AL.: "Anti-HIV-1 phorbol esters from the seeds of Croton tiglium", PHYTOCHEMISTRY,, vol. 53, no. 4, 9 February 2000 (2000-02-09), pages 457 - 464, XP002929556
SAHAR EL-MEKKAWY ET AL.: "12-O-acetylphorbol-13-decanoate potently inhibits cytopathic effects of human immuno-deficiency virus type 1 (HIV-1), without activation of protein kinase C", CHEM. PHARM. BULL.,, vol. 47, no. 9, 1999, pages 1346 - 1347, XP002929557
BEERS M.H., BERKOW R. (EDS.): "The Merck Manual of Diagnosis and Therapy", 1 January 1999, MERCK RESEARCH LABORATORIES, Whitehouse Station, N.J., ISBN: 978-0-911910-10-0, article BEERS M H, BERKOW R: "HUMAN IMMUNODEFICIENCY VIRUS INFECTION", pages: 1321 - 1324, XP002929558, 023624
SAHAR EL-MEKKAWY ET AL.: "12-O-acetylphorbol-13-decanoate potently inhibits cytopathic effects of human immuno-deficiency virus type 1 (HIV-1), without activation of protein kinase C", CHEM. PHARM. BULL.,, vol. 47, no. 9, 1999, pages 1346 - 1347, XP002929557
BEERS M.H., BERKOW R. (EDS.): "The Merck Manual of Diagnosis and Therapy", 1 January 1999, MERCK RESEARCH LABORATORIES, Whitehouse Station, N.J., ISBN: 978-0-911910-10-0, article BEERS M H, BERKOW R: "HUMAN IMMUNODEFICIENCY VIRUS INFECTION", pages: 1321 - 1324, XP002929558, 023624
Attorney, Agent or Firm:
Hanabusa, Tsuneo (Ochanomizu Square B 6 Kandasurugadai 1-chome Chiyoda-ku, Tokyo, JP)
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