Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K38/00—Medicinal preparations containing peptides
  • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
  • A61K38/08—Peptides having 5 to 11 amino acids
  • A61K38/095—Oxytocins; Vasopressins; Related peptides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence

Definitions

• the invention relates to medicine, namely to a new use of a pharmaceutical agent as a stimulator of sexual, sexual and reproductive function and can be used to treat:
• oxytocin - a nonapeptide containing a disulfide cycle
• Sus-Tur-Ilé-Glp-Asp-Sus-Progo-Leu-Glü-NNg is one of the most important regulators of the reproductive sphere of mammals.
• Oxytocin and its structural analogues, obtained by chemical synthesis methods, are widely used in medicine and veterinary medicine as medicines ( ⁇ aptor J.M., ⁇ ik
• Phsushorcharmacologo (Veri). - 1999. - Ju. - 144 (4). - P.355-362; Arletti R., Salza L., Giardiano L. Cehal imroteps is associated with a recessed prophylactic apd with ipreased sed apriouspurisulés Lettt. - 1997. - Ser 19. - 233 (2-3). - P.65-68).
• the objective of the present invention is to use for a new purpose as a stimulant of sexual, sexual and reproductive function in mammals, the heptapeptide of the formula: Thr-Lus-Progo-Agg-Progo-Glu-Progo.
• the technical result of the invention is achieved by the fact that the heptapeptide of the general formula: Thr-Lus-Pro-Agg-Pro-Glou-Pro, is used as a stimulator of sexual, sexual and reproductive function. It was found that the heptapeptide Thr -Lus-Rro-Arg-
• Rro-Glu-Rgo has a wider spectrum of action.
• the heptapeptide has an optimizing and activating effect on the mnemonic and cognitive functions of the brain, and also stimulates sexual, sexual and reproductive functions, which is an important positive part of its specific pharmacological activity.
• the possibility of an objective manifestation of a technical result when using the invention is confirmed by reliable data given in the examples containing experimental information obtained by the methods adopted in this field.
• the quantification scale is a sexological questionnaire, including questions on the state of the mental, secretory, orgasmic and risidual stages of the female copulative cycle (libido, mood, orgasm, physical condition and mood after sexual intercourse), indicating points for each answer option.
• Sexological studies have their own specifics, imposing special requirements for confidentiality of information received. Failure to do so may even invert the results of the study. To maintain confidentiality of information and ensure patient confidence (exclusion of a negative psychological factor), a special procedure for recording data was developed.
• Group I consisted of 8 healthy women
• Group II consisted of 10 women with sexual dysfunction not caused by other diseases
• Group III consisted of 31 women with orgasmic dysfunction
• Group IV consisted of women with a pronounced decrease (6 people) and with a lack of libido (2 people); Group V comprised 2 women with diagnosed infertility.
• Example 1 Data on the analyzed patient groups are presented in Examples 1-5.
• Example 1 Data on the analyzed patient groups are presented in Examples 1-5.
• a slight extinction of sexuality in healthy women is associated with social conditions: life, working conditions, stress, etc.
• the drug can increase the severity of the mental and orgasmic phases of the copulative cycle, revive the feeling of love and desire for sexual intercourse.
• vaginal mucus begins to stand out more quickly, an orgasm occurs with almost every sexual contact, even repeated orgasmic discharges appear, followed by a feeling of satisfaction and pleasant fatigue.
• the dependence of pleasure on the phase of the menstrual cycle has disappeared.
• Sexual intercourse has ceased to be a duty of conjugal duty, gratitude appears to the man for the pleasure experienced, and the level of sexual activity has increased.
• Libido was completely absent in two patients of group IV (25.0%). The age of these patients was 25-26 years. Both women noted the disappearance of libido and orgasm after childbirth. There were no pathologies in the prenatal period, in childbirth and in the postpartum period. Lactorrhea at the time of taking the heptapeptide was not observed. In women, the duration of labor was 1-2 years. Their curator noted a very pronounced violation of sexual function (complete lack of attraction, a rare appearance of lubrication, complete disappearance of orgasm, complete physical indifference at the end of sexual intercourse, aversion to sex).
• Gynecological status the external genitalia are developed correctly, in the mirrors: the cervix is conical, not eroded, the discharge is light.
• Uterine body increased to 5-6 weeks. Pregnancy round shape with uneven contours. Appendages are not clearly defined, painless. Vaults and parametries are free.
• Diagnosis premenopause. Uterine fibroids in combination with adenomyosis. Infertility 2 (secondary), endometriosis.
• Past diseases childhood infections, hypertension - stage 1, gallstone disease - in remission.
• Gynecological history Chronic adnexitis in remission.
• Gynecological status external genitalia are developed correctly, in the mirrors: the cervix is cylindrical, not eroded, the discharge is light.
• the body of the uterus is normal in size, not enlarged, painless on palpation, appendages are not clearly defined, painless, arches and parametries are free.
• Diagnosis Late reproductive period, infertility 2 (secondary), endocrine form.
• the treatment was carried out: 0.1% heptopeptide solution of the formula: Thr-Lus-Pro-Arg-Pro-Glou-Progo intranasally for 30 days. After the treatment, 4 months later, pregnancy occurred, pregnancy was diagnosed on the basis of data obtained from:
• ZI has a diagnosis.
• heptopeptide of the formula: Thr-Lus-Progo-Arg-Pro-Glou-Pro The influence of the heptopeptide of the formula: Thr-Lus-Progo-Arg-Pro-Glou-Pro on the reproductive behavior of rats was studied using various methods of its administration (intramuscularly, intraperitoneally and intranasally) with different dosages (25-100 ⁇ g / animal). It was found that intranasal administration of a heptopeptide of the formula: Thr-Lus-Pro-Agg-Pro-Glou-Pro in 10-15 minutes caused pronounced behavioral changes in all the studied groups of animals, which consist in increasing interest and "other" behavior in relation to other individuals , elements of "healing" appeared with attempts at mating. Rats groomed themselves (autogrooming) and other individuals (allogrooming).
• rats In rats, a distinct anogenital study of another individual was observed. The latter consists of a cluster of behavioral reactions, including climbing under an individual of the opposite sex, sniffing at its anogenital region and its grooming. Not only in the evening, but also in the daytime, elements characteristic of mating were observed.
• old animals and operated animals detruction of the hippocampus, occlusion of achotis
• a heptopeptide of the formula: Thg-Lus-Pro-Arg-Pro-Glou-Pro freezing reactions (fading), which are a behavioral marker of stress, disappeared.
• Thr-Lus-Pro-Agg-Pro-Glou-Pro should include the strengthening of maternal instincts and the removal of aggression inherent in lactating females with respect to the experimenter.
• lactating females received cubs from other individuals (a phenomenon not characteristic of intact rats that ate “black” cubs).
• the enhancing effects on the reproductive behavior of rats are prolonged (up to 1.5-2 months). The latter is that in the 2nd group of animals (8 rats of 4 pairs - 1 male and 1 female), the secondary mating process took place early, against the background of feeding unripened cubs.
• heptopeptide of the formula: Thr-Lus-Pro-Arg-Pro-Glou-Pro helps to remove the neurotic disturbances and inhibition in laboratory rats, enhances the healing and grooming processes characteristic of this type of animal , promotes mating, not only at night, but also in the daytime, increases reproductive function. The latter is reflected in larger and better offspring. More pronounced effects on the reproductive function of rats occur upon intranasal twofold administration of a heptopeptide of the formula: Thr-Lus-Pro-Arg-Pro-Glou-Pro, in small (25 ⁇ g / animal) doses in groups consisting of pairs (1 bag + 1 male).
• the invention expands the arsenal of agents that stimulate the reproductive activity of mammals and humans.
• the technical result achieved by the implementation of the invention is the detection of a wide range of therapeutic effects of the known memory stimulant, which determines the possibility of its use in low doses as a stimulant sexual, sexual and reproductive function without undesirable side effects, with good tolerance.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Reproductive Health (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Endocrinology (AREA)
• Immunology (AREA)
• Gastroenterology & Hepatology (AREA)
• Epidemiology (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Gynecology & Obstetrics (AREA)
• Pregnancy & Childbirth (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Peptides Or Proteins (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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• 2009
  • 2009-06-04 RU RU2009121281/15A patent/RU2404793C1/ru active IP Right Revival
• 2010
  • 2010-06-01 CN CN201080033918.6A patent/CN102481335B/zh active Active
  • 2010-06-01 CA CA2764351A patent/CA2764351C/en active Active
  • 2010-06-01 EP EP10783644.7A patent/EP2465521B1/en active Active
  • 2010-06-01 BR BRPI1011071A patent/BRPI1011071B8/pt active IP Right Grant
  • 2010-06-01 ES ES10783644T patent/ES2831673T3/es active Active
  • 2010-06-01 JP JP2012513900A patent/JP5643816B2/ja active Active
  • 2010-06-01 WO PCT/RU2010/000285 patent/WO2010140926A1/ru not_active Ceased
  • 2010-06-01 US US13/376,023 patent/US8883741B2/en active Active

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