Fungicidal composition comprising benzoylferrocene

 

(57) Abstract:

The invention relates to medicine. Described pharmaceutical or veterinary composition comprising a carrier and an active ingredient, representing a compound of formula I

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where R1and R2each independently of one another denotes hydrogen, halogen or methoxy group, and salts of compounds of formula I. the present invention also proposed the use of compounds of the indicated formula I for the preparation of pharmaceutical or veterinary compositions for the treatment of fungal infections. The composition is effective to kill fungal infections caused by dermatophytes. The composition is used for oral, parenteral or topical application, which also acts systemically. 7 C.p. f-crystals.

The technical field to which the invention relates

The present invention relates to a new use of derivatives benzoylferrocene. In particular, the present invention relates to the use of derivatives benzoylferrocene to combat fungal infections.

Background of the invention

Fungi are the causal factors of various superficial skin damage. Sibnarayan on different areas of the skin, including the legs, the area genitalia, nails, etc. also, sometimes, especially in patients with immune disorder, mushrooms can grow on various other tissues such as mucous membrane of the mouth. Moreover, sometimes fungal infections can be systemic.

The cells of fungi, usually have cell membranes, which contain complex polysaccharides, primary chitin, chitosan, glucans and mannans.

In the patent US 4798837 described N-benzoyl-N'-2,5-dichloro-4-hexadecyloxypropyl, which found that they are effective as pesticides, primarily for combating arthropod of the order Acarina. It is established that one of these compounds, known under the generic name of lufenuron (Lufenuron), can be used in veterinary medicine to combat fleas (sold under the trademark PROGRAMTM(Programs) by Novartis, Switzerland (this connection is trepiline the name N-[2,5-dichloro-4-(1,1,2,3,3,3-hexaphosphate)phenylenecarbonyl]-2, 6-differentated). Lufenuron in the form of pills or suspension is introduced to the animal orally to prevent infestation by fleas. Therapeutic effect of this medicinal product, as a rule, represent the and inventions detected, what treatment lufenuron effective to fight and destroy fungal infection, especially that which is caused by dermatophytes.

Thus, one of the objects of the present invention is a pharmaceutical or veterinary composition comprising a carrier and an active ingredient, which represents the following compound of formula I:

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where R1and R2each independently of one another denotes hydrogen, halogen or methoxy group, and salts of compounds of formula I.

The invention also relates to the use of compounds of the indicated formula I for the preparation of pharmaceutical or veterinary compositions intended for the treatment of fungal infections.

In addition, the invention relates to a method of treating a fungal infection involving the administration to a patient in need, an effective amount of a compound of a specified formula I.

Preferred compounds of formula I are compounds in which R1and R2each independently of the other denotes a fluorine, chlorine or methoxy group, primarily compounds in which both radicals R1and R2have the same value. Most predoctor> Salts of compounds of formula I may be a salt with the cation of an organic base. Examples of cations of organic bases are the following cations:

(CH3)4N+,

(C2H5)4N+,

(n-C3H7)4N+,

(ISO-C3H7)4N+,

(h-C4H9)4N,

(C4H9)3N+,

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and [CH3-(CH2)n]-N+-CH3,

where n denotes an integer from 8 to 12.

The media must represent a physiologically tolerable carrier that is compatible with the compound of the formula I or its salts. Examples of carriers are well known liquid or solid carriers, for example, described in patent US 4798837, the content of which is incorporated into this description by reference.

On the basis of the compounds of formula I can be prepared composition for oral, parenteral or topical application. Preferred are compositions of the compounds of formula I, intended for oral or parenteral administration, which also act systemically, especially predpochitayut number, effective to achieve therapeutic effects, which can manifest either as permanent or temporary improvement in the condition of the patient, or in reducing fungal infection. The effective amount may depend among other things on the treatment regimen, type of infection to be treated, namely, whether they are systemic, local, and so on, the type of patient to be treated, i.e., whether it is human or animal, and the type of animal, age of the patient, etc.

Pharmaceutical or veterinary composition according to the invention may, for example, be in the form of powder, freeze-dried, and so on, intended for dilution with saline solution, for example saline for parenteral administration. As another example, the pharmaceutical solution according to the invention can be prepared in the form of oral dosage forms, for example, in the form of pills or capsules. In addition, for some types of application of the pharmaceutical composition according to the invention can also be prepared in the form of a liquid solution, intended for oral administration. The composition according to the invention can also be prepared in a form suitable for local application.

Izobretenii, and local fungal infections. In particular, according to a preferred variant implementation of the present invention allows the treatment of skin fungal infections both in humans and in animals, fungal nail infections or genital organs in humans, fungal eye infections or fungal infections of the ear as humans and animals, and other infections. Specific examples of fungal infections that can be treated according to the invention, are infections that are caused by dermatophytes, such as the genus Microsporum (eg, Microsporum canis), which cause various fungal infections of the skin, nails or hair; representatives of the genus Aspergillus and yeast, for example Malassegia or Candida.

The invention may be used to treat animals, including dogs, cats, cows, sheep, pigs, poultry, but not limited to.

Hereinafter the invention will be illustrated by examples, not limiting its scope.

Example 1.

The presence of fungal infection were examined 4269 animals, including 2914 dogs and 1355 cats that are trapped in a veterinary clinic.

At the first visit in 62 dogs, which amounted to 2.13% of all examined dogs were found to have the go fungal infection of the skin.

429 dogs (14.7% of all surveyed dogs) and 102 females (7.5% of all surveyed cats) received lufenuron to prevent infestation of the skin by fleas.

All animals were tested for the presence of fungal infection on your next visit to the clinic. All cats or dogs, which was treated with lufenuron there were no signs of fungal infections. In all cases, when you have identified the initial signs of fungal infection (detected at the first visit), they disappeared.

Noted only one case, when the dog was subjected to monthly treatment lufenuron and contracted in the treatment of Aspergillus spp. After dose lufenuron was doubled, the dog recovered from the fungal infection within 14 days.

The animals were treated with lufenuron also examined in relation to the availability of yeast infection (Candida or Malassegia), but it was not detected in any of the treated animals.

Example 2.

Examined the dog, a female weighing 3.7 kg and found that her left paw has a round alopecia (baldness), which shone brightly under UV irradiation. Based on this characteristic, the infection was diagnosed as caused by Microsporum canis, which is in the tools and ProgramTMrepresenting small pills (each contains 67,8 mg lufenuron), one every two weeks. 14 days after the start of treatment, all the symptoms of fungal infection is gone.

Example 3.

The dog, a male weighing 4 kg was diagnosed with an infection caused by Microsporum canis, similar to that described in example 2. Dog first systemically treated with griseofulvin and local 1% ciclopiroxolamine without any signs of help.

Then the dog has appointed PROGRAMTM(1 small tablet) and 10 days were signs of healing and the growth of wool in the field of fungal infection.

Example 4.

In dogs weighing 5 kg on the right rear paw diagnosed with an infection caused by Trichophyton. Carried out the same treatment as that described in example 1. After 10 days from the start of treatment was detected wool growth at the site of infection.

Example 5.

The dog is a male weighing about 20 kg, had a symmetrical alopecia caused by infection, which shone brightly under UV irradiation, and on the basis of this characteristic, the infection was diagnosed as caused by Microsporum canis. This diagnosis was later confirmed by laboratory test is openarena) every two weeks. 10 days before taking the second pill on the infected skin signs of full recovery and the growth of wool.

Example 6.

The dog female weighing about 40 kg was detected infection caused by Microsporum canis, similar to that described in example 2. The dog in the quality of treatment appointed 1 large pill PROGRAM fundsTM(containing 409,8 mg lufenuron), and the second dose given 2 weeks later.

After 10 days the animal has detected signs of recovery, which was manifested by the growth of wool in place of the infection.

Example 7.

5 cats, living together in one house, different parts of the body were diagnosed with an infection caused by Trichophyton. Cats were treated with the suspension means PROGRAMTM(dose). In all cases, after 10 days was found complete recovery, reflected in the growth of hair on all infected places.

Example 8.

6 cats was diagnosed with an infection caused by Microsporum canis. This diagnosis was later confirmed by laboratory testing. Cats were treated with 1 injection injectable solution lufenuron at a dose of 20 mg/kg of body weight. After 8-11 days after the start of treatment the animals were discovered prize D. T. M.-plates.

1. Pharmaceutical or veterinary medicinal product for the treatment of local fungal infections caused by dermatophytes, comprising as active ingredient a compound of the formula I

where R1and R2each independently of one another denotes hydrogen, halogen or methoxy group,

and salts of compounds of formula I and at least one physiologically acceptable portable media.

2. Drug under item 1, where R1and R2each independently of the other denotes a fluorine, chlorine or methoxy group.

3. Drug under item 1, where R1and R2have the same values.

4. Drug under item 3, where R1and R2denote fluorine.

5. The drug according to any one of paragraphs.1-4 in the form intended for oral administration.

6. The drug according to any one of paragraphs.1-4 in the form intended for parenteral administration.

7. The drug according to any one of paragraphs.1-6, intended for the treatment of fungal infections caused by dermatophytes.

8. The drug according to any one of paragraphs.5-7, intended for the treatment of infections caused by Microsporum, T>6.04.1998 installed on the changes in PP.1-8.

 

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