WO2004032825A2 - Use of 2,3 alkylcarbonyloxybenzoic acids in the treatment of anthrax - Google Patents
Use of 2,3 alkylcarbonyloxybenzoic acids in the treatment of anthrax Download PDFInfo
- Publication number
- WO2004032825A2 WO2004032825A2 PCT/US2002/035056 US0235056W WO2004032825A2 WO 2004032825 A2 WO2004032825 A2 WO 2004032825A2 US 0235056 W US0235056 W US 0235056W WO 2004032825 A2 WO2004032825 A2 WO 2004032825A2
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- WO
- WIPO (PCT)
- Prior art keywords
- alkylcarbonyloxybenzoic
- acid
- subject
- amount
- administered
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/225—Polycarboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- A61K38/46—Hydrolases (3)
- A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
- A61K38/482—Serine endopeptidases (3.4.21)
- A61K38/4866—Protein C (3.4.21.69)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
Definitions
- This invention is directed to the field of treating anthrax. More particularly, this invention is directed to the field of repairing damage to tissue such as lung tissue caused by the Bacillus anthracis bacterium.
- Inhalation anthrax is a disease resulting from inhalation of spores of the bacterium Bacillus anthracis.
- the spores are the dormant form of the bacterium.
- the bacteria multiply and produce toxins. These toxins cause inflammation, fluid buildup and hemorrhaging in the lungs, followed in most cases by rapid death.
- the anthrax toxins were considered to be the cause of the vascular damage, resulting in the fluid buildup and hemorrhaging.
- the toxins were found to have three components: protective antigen, edema factor, and lethal factor.
- protective antigen edema factor
- lethal factor edema factor
- Certain antibiotics are known to prevent inhalation anthrax, but only if the antibiotics are administered prior to spore germination in the lungs. There presently are no known therapeutic agents for the treatment for inhalation anthrax once lung activity has begun. This is especially problematic in that early symptoms of inhalation anthrax resemble flu symptoms. When anthrax enters the secondary stage, death of the subjects is near certain, generally resulting from the vascular permeability and resulting pulmonary edemas caused by the toxins. Even if antibiotics are used effectively in treatment, there has been no method reported for reversing the above-described lung damage.
- the present invention is directed to such a therapeutic agent.
- the invention encompasses methods for treating inhalation anthrax by the use of 2,3- alkylcarbonyloxybenzoic acids in which the alkylcarbonyloxy group has 2-18 carbon atoms.
- One particularly preferred compound is 2,3-diacetoxybenzoic'acid.
- the preferred method of treatment involves administering 2,3-alkylcarbonyloxybenzoic acid to a subject known or suspected to have inhalation anthrax.
- the 2,3-alkylcarbonyloxybenzoic acid can be administered by any known therapeutic method, and in combination with other compounds known or believed to prevent or treat anthrax. More than one of the 2,3- alkylcarbonyloxybenzoic acid compounds can also be blended.
- a therapeutic ally effective amount of a compound selected from the group consisting of 2,3-alkylcarbonyloxybenzoic acids and salts thereof in which the alkylcarbonyloxy group has 2-18 carbon atoms is administered to subjects who have indications for inhalation anthrax.
- any reference to 2,3- alkylcarbonyloxybenzoic acids shall be construed to include the salts thereof.
- the 2,3- alkylcarbonyloxybenzoic acids have been shown to ameliorate the damage resulting from increased vascular permeability and the resulting pulmonary edema caused by increased microvascular permeability to protein and solutes resulting from Adult Respiratory Distress Syndrome and sepsis. This effect is detailed in U.S. Patent No. 5,504,111, issued April 2, 1996 to Flavin et al.
- a particularly prefe ⁇ -ed compound in the class of 2,3-alkylcarbonyloxybenzoic acid compounds is 2,3-diacetoxybenzoic acid.
- 2,3- diacetoxybenzoic acid is administered to a subject, either via intravenous or aerosol spray means in a therapeutically effective amount. This amount is preferably, but not exclusively, in the range of 1-100 mg/kg of body weight of the subject. More preferably, the range is 5-
- the range is 5-20 mg/kg of body weight.
- anthrax treatment product may also comprise 2,3-dihydroxybenzoic acid, whether administered directly or through chemical conversion in the subject.
- the 2,3-alkylcarbonyloxybenzoic acid can be used either on a' preventative basis, or after anthrax disease has been diagnosed, either in the initial or secondary stage of diagnosis.
- the 2,3-alkylcarbonyloxybenzoic acid can be administered to human or animal subjects.
- the 2,3-alkylcarbonyloxybenzoic acid is typically produced in solid form.
- it is preferably formulated into a liquid form by use of a sodium bicarbonate buffer present in an amount to effectively solubilize and stabilize the acid.
- the acid is also converted to a sodium salt.
- the buffered salt can then be constituted into aerosol form using conventional methods of forming aerosol products. Administration of the aerosol form can be accomplished via either nasally or orally, including forms such as metered inhaled forms.
- 2,3-alkylcarbonyloxybenzoic acid Treatment with 2,3-alkylcarbonyloxybenzoic acid can be used as a sole treatment mechanism, or in combination with other therapeutic agents.
- 2,3- alkylcarbonyloxybenzoic acid can be administered in conjunction with antibiotic therapy.
- Antiobiotics have been shown to treat the Bacillus anthracis bacterium, but not the damage caused by the toxins produced by the bacteria.
- a combination of 2,3- alkylcarbonyloxybenzoic acid and one or more antibiotics is expected to be an especially useful therapeutic combination.
- the antibiotics may be selected from the group comprising ciprofloxacin, doxycycline, rifampin, vancomycin, imipenem, chloramphenicol, penicillin, clindamycin, clarithromycin, and analogs, homologs, and derivatives thereof which have antibiotic functionality.
- 2,3-alkylcarbonyloxybenzoic acid can also be combined with other therapeutic agents which are used in the treatment of sepsis or other conditions in which bacteria and their toxins spread through lung tissues.
- An example of such a therapeutic agent is drotrecogin alfa (Xigris ® brand, Eli Lilly & Co.), but any similar therapeutic agents also can be used.
- a benefit of co-treatment with drotrecogin alfa is that the mechanism of drotrecogin alfa differs from that of 2,3-alkylcarbonyloxybenzoic acid.
- the present invention teaches a novel method for the treatment of inhalation anthrax, and the novel use of 2,3-alkylcarbonyloxybenzoic acids and salts thereof.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Otolaryngology (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pulmonology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2002368208A AU2002368208A1 (en) | 2001-11-02 | 2002-10-31 | Use of 2,3 alkylcarbonyloxybenzoic acids in the treatment of anthrax |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33600601P | 2001-11-02 | 2001-11-02 | |
| US60/336,006 | 2001-11-02 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2004032825A2 true WO2004032825A2 (en) | 2004-04-22 |
| WO2004032825A3 WO2004032825A3 (en) | 2004-12-02 |
Family
ID=32093654
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2002/035056 Ceased WO2004032825A2 (en) | 2001-11-02 | 2002-10-31 | Use of 2,3 alkylcarbonyloxybenzoic acids in the treatment of anthrax |
Country Status (3)
| Country | Link |
|---|---|
| US (1) | US20040029783A1 (en) |
| AU (1) | AU2002368208A1 (en) |
| WO (1) | WO2004032825A2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6063121B2 (en) * | 2011-12-26 | 2017-01-18 | 任天堂株式会社 | Communication system, communication terminal, communication method and program |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK483587D0 (en) * | 1987-09-15 | 1987-09-15 | Riemann & Co Aps Claus | ANTIPERSPIRANT PREPARATION |
| US5504111A (en) * | 1994-12-30 | 1996-04-02 | Medichem Research, Inc. | Use of 2,3 alkylcarbonyloxybenzoic acid in treating adult respiratory distress syndrome |
| US5744453A (en) * | 1996-01-05 | 1998-04-28 | Mintz; Clifford S. | Polyamine conjugates for treatment of infection |
-
2002
- 2002-10-31 WO PCT/US2002/035056 patent/WO2004032825A2/en not_active Ceased
- 2002-10-31 US US10/284,768 patent/US20040029783A1/en not_active Abandoned
- 2002-10-31 AU AU2002368208A patent/AU2002368208A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2002368208A1 (en) | 2004-05-04 |
| WO2004032825A3 (en) | 2004-12-02 |
| US20040029783A1 (en) | 2004-02-12 |
| AU2002368208A8 (en) | 2004-05-04 |
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