Therapeutic composition and methods

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

Reexamination Certificate

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C514S143000, C514S134000, C514S102000, C514S075000

Reexamination Certificate

active

06525035

ABSTRACT:

PRIORITY OF INVENTION
This application claims priority of invention under 35 U.S.C. §119 from Russian Patent Number 2129867 filed Jun. 10, 1998, and allowed May 10, 1999.
BACKGROUND OF THE INVENTION
Russian patent number 2005475 (1994) discloses compositions comprising polyprenil phosphate which are reported to possess antiviral activity.
L. L. Danilov, et al.,
Archivum Immunologiae and Thrapiae Experimentalis,
1996, 44, 395-400 disclose a polyprenyl phosphate composition (PHOSPRENYL) that has antiviral and immunomodulatory activity. A. N. Narovlyansky, et al., Abstracts of the Second Joint Meeting of the International Cytokine Society and International Society for Interferon and Cytokine research, Jerusalem, Israel, Oct. 25-30 1998, and A. V. Sanin, et al., Abstracts of VII International Conference on AIDS, Amsterdam, the Netherlands, Jul. 19-24, 1992, also describe similar biological activity for PHOSPRENYL.
A. V. Sanin, et al. Abstracts of the meeting “Dolichols and Related Lipids”, Aug. 11-13, 1993, Zakopane, Poland, disclose a phosphorylated polyisoprenoid composition P16 that is reported to be a novel immunomodulatory agent and antiviral drug that might be promising in immunotherapy of infectious diseases. The composition is reported to modulate NK activity, enhance X-ray resistance, modulate GM-CSF levels, stimulate hematopoietic stem cell migration, stimulate interferon activity, and to possess mild adjuvant activity. The composition is also disclosed to possess a strong dose-dependent inhibitory activity against HIV-1 infection in MT4 cells, and to inhibit hepatitis A virus, bovine leukemia virus, adenovirus, and tick encephalitis.
Additionally, European Patent Application 0 350 801 discloses polyprenols and polyprenyl phosphates that are useful for the inhibition of tumor metastasis.
Despite the above disclosures, there is currently a need for additional therapeutic agents with antiviral and immunomodulatory activity. In particular, there is a need for agents that have improved activity or improved physical characteristics compared to known agents. For example, the PHOSPRENYL composition identified above is limited for therapeutic purposes by a low solubility in water and other polar solvents.
SUMMARY OF THE INVENTION
Applicant has discovered certain compositions that are useful for the prevention, treatment, and liquidation of consequences of diseases, including viral, chlamidial, bacterial related diseases, oncology related diseases, diseases related to the liver, gastrointestinal, urologic and reproductive systems, and diseases related to the function of the immune system. The compositions are also useful in the treatment of wounds, bums, and stresses, and are useful for medical (human) and veterinary applications. The pyrophosphate containing compositions of the invention have improved solubility compared to related known compositions, and as a result, demonstrate improved levels of activity against certain diseases.
Accordingly, the invention provides a composition comprising, 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive, or a salt thereof.
The invention also provides a composition comprising polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive, or a salt thereof.
The invention also provides a pharmaceutical composition comprising 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof; and a pharmaceutically acceptable carrier.
The invention also provides a pharmaceutical composition comprising polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O) (OH)
2
wherein m is an integer from 6-19 inclusive, or a salt thereof; and a pharmaceutically acceptable carrier.
The invention also provides a method for producing an antiviral effect in an animal comprising administering to an animal in need of such treatment, an effective antiviral amount of a composition comprising 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof. As used herein “animal” includes for example mammals (e.g. a dog, cow, cat, or human), birds (e.g. poultry), and other animals that can effectively be treated with the compositions of the invention.
The invention also provides a method for producing an antiviral effect in an animal comprising administering to an animal in need of such treatment, an effective antiviral amount of a composition comprising polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof.
The invention also provides a method for modulating (e.g. normalizing or upregulating) the immune system of an animal comprising administering to an animal in need of such treatment, an effective immunomodulatory amount of a composition comprising 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof.
The invention also provides a method for modulating (e.g. normalizing or upregulating) the immune system of an animal comprising administering to an animal in need of such treatment, an effective immunomodulatory amount of a composition comprising polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof.
The invention also provides a method for the treatment of disease caused by distemper virus (DV), canine enteritis (parvo, rota, and corona viruses; CEV), canine infectious hepatitis (CIH), feline infectious gastroenteritis (panleukopenia, FIE), feline infectious rhinotracheitis (agent—herpes virus; FIR), feline infectious enteritis and peritonitis (agent—corona virus, FIP), swine transmissive gastroenteritis (agent—rotavirus; STG), murine ectromelia (ME), cattle leukemia (CL), calf mixed viral infection (agents—parvo, adeno, and corona viruses; CMVI), western equestrian encephalomyelitis (WEE), or rabies (RV), comprising administering to an animal in need of such treatment, an effective therapeutic amount of a composition comprising 1) polyprenol monophosphates of the formula H—[—CH2-C(CH3)═CH—CH2]n-O—P(═O)(OH)2 wherein n is an integer from 6-19 inclusive or a salt thereof, and 2) polyprenol pyrophosphates of the formula H—[—CH2-C(CH3)═CH—CH
2
]
m
—O—P(═O)(OH)—O—P(═O)(OH)
2
wherein m is an integer from 6-19 inclusive or a salt thereof.
The invention also provides a method for the treatment of distemper virus (DV), canine enteritis (parvo, rota, and corona viruses; CEV), canine infectious hepatitis (CIH), feline infectious gastroenteritis (panleukopenia, FIE), feline infectious rhinotracheitis (agent—herpes virus; FIR), feline infectious enteritis and peritonitis (agent—corona virus, FIP), swine transmissive gastroenteritis (agent—rotavirus; STG), murine ectromelia (ME

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