WO2010140926A1 - Стимулятор половой, сексуальной и репродуктивной функции - Google Patents
Стимулятор половой, сексуальной и репродуктивной функции Download PDFInfo
- Publication number
- WO2010140926A1 WO2010140926A1 PCT/RU2010/000285 RU2010000285W WO2010140926A1 WO 2010140926 A1 WO2010140926 A1 WO 2010140926A1 RU 2010000285 W RU2010000285 W RU 2010000285W WO 2010140926 A1 WO2010140926 A1 WO 2010140926A1
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- WO
- WIPO (PCT)
- Prior art keywords
- sexual
- pro
- patients
- lus
- effect
- Prior art date
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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)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (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)
Abstract
Description
Claims
Priority Applications (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2012513900A JP5643816B2 (ja) | 2009-06-04 | 2010-06-01 | 生殖、性的、および繁殖機能の刺激剤 |
CN201080033918.6A CN102481335B (zh) | 2009-06-04 | 2010-06-01 | 生殖器功能、性功能和生殖功能的刺激物 |
CA2764351A CA2764351C (en) | 2009-06-04 | 2010-06-01 | Stimulator of genital, sexual and reproductive function |
EP10783644.7A EP2465521B1 (en) | 2009-06-04 | 2010-06-01 | Stimulator of genital, sexual and reproductive function |
US13/376,023 US8883741B2 (en) | 2009-06-04 | 2010-06-01 | Stimulator of genital, sexual and reproductive function |
BRPI1011071A BRPI1011071B8 (pt) | 2009-06-04 | 2010-06-01 | uso de um heptapeptídeo para estimular a função genital, sexual ou reprodutiva em um mamífero |
ES10783644T ES2831673T3 (es) | 2009-06-04 | 2010-06-01 | Estimulador de la función genital, sexual y reproductiva |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
RU2009121281 | 2009-06-04 | ||
RU2009121281/15A RU2404793C1 (ru) | 2009-06-04 | 2009-06-04 | Стимулятор половой, сексуальной и репродуктивной функции |
Publications (1)
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WO2010140926A1 true WO2010140926A1 (ru) | 2010-12-09 |
Family
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PCT/RU2010/000285 WO2010140926A1 (ru) | 2009-06-04 | 2010-06-01 | Стимулятор половой, сексуальной и репродуктивной функции |
Country Status (9)
Country | Link |
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US (1) | US8883741B2 (ru) |
EP (1) | EP2465521B1 (ru) |
JP (1) | JP5643816B2 (ru) |
CN (1) | CN102481335B (ru) |
BR (1) | BRPI1011071B8 (ru) |
CA (1) | CA2764351C (ru) |
ES (1) | ES2831673T3 (ru) |
RU (1) | RU2404793C1 (ru) |
WO (1) | WO2010140926A1 (ru) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2015515855A (ja) * | 2013-05-28 | 2015-06-04 | アイビックス・リミテッドIvixltd. | 組換えペプチドを生産するための方法および得られるペプチド |
JP2018118973A (ja) * | 2018-02-23 | 2018-08-02 | アイビックス・リミテッドIvix Ltd. | 組換えペプチドを生産するための方法および得られるペプチド |
US10836794B2 (en) | 2016-10-24 | 2020-11-17 | “Ivix” Ltd. | Group of peptides for treating female sexual dysfunction |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2404793C1 (ru) | 2009-06-04 | 2010-11-27 | Общество с ограниченной ответственностью Био Пептид | Стимулятор половой, сексуальной и репродуктивной функции |
RU2507212C3 (ru) * | 2012-03-28 | 2022-05-04 | Общество С Ограниченной Ответственностью "Айвикс" | Способ получения рекомбинантного пептида и полученный пептид |
US9717903B1 (en) | 2015-03-17 | 2017-08-01 | Gary Barrett | Electronic process to restore, improve and/or strengthen the libido; method to mend the sex drive in males and females |
RU2655763C2 (ru) * | 2016-10-24 | 2018-05-29 | Общество С Ограниченной Ответственностью "Айвикс" | Фармацевтическая композиция и способ лечения женских сексуальных дисфункций |
JP6858227B2 (ja) * | 2019-07-11 | 2021-04-14 | アイビックス・リミテッドIvix Ltd. | 組換えペプチドを生産するための方法および得られるペプチド |
Citations (8)
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WO1994022460A1 (en) | 1993-04-05 | 1994-10-13 | University Patents, Inc. | Diagnosis and treatment of erectile dysfunction |
RU1124544C (ru) * | 1983-06-30 | 1995-01-09 | Институт молекулярной генетики РАН | Гептапептид, обладающий свойствами психостимулятора пролонгированного действия с иммунотропной активность |
RU2058791C1 (ru) | 1989-01-11 | 1996-04-27 | Государственное предприятие "Элер-микро" | Стимулятор репродуктивной способности у теплокровных животных |
US5932548A (en) | 1998-06-03 | 1999-08-03 | Deghenghi; Romano | Lysine containing peptides for treatment of heart disease |
US5955421A (en) | 1990-05-11 | 1999-09-21 | Deghenghi; Romano | Peptides containing D-2-alkyl-Tryptophan |
RU2155065C1 (ru) | 1999-04-23 | 2000-08-27 | Институт молекулярной генетики РАН | Анксиолитическое средство и фармацевтическая композиция анксиолитического действия |
RU2264823C2 (ru) | 1999-11-10 | 2005-11-27 | Центарис Гмбх | Способ и пептиды для лечения эректильной дисфункции, способ и фармацевтическая композиция с использованием указанных пептидов |
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RU2252779C1 (ru) | 2003-09-23 | 2005-05-27 | Институт Молекулярной Генетики Российской Академии Наук (Имг Ран) | Способ профилактики и лечения язв желудочно-кишечного тракта |
CN101302246B (zh) * | 2007-05-09 | 2011-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | 黑色素皮质激素受体七肽类激动剂及其制备方法和用途 |
RU2404793C1 (ru) | 2009-06-04 | 2010-11-27 | Общество с ограниченной ответственностью Био Пептид | Стимулятор половой, сексуальной и репродуктивной функции |
EA200900804A1 (ru) | 2009-06-08 | 2010-08-30 | Общество С Ограниченной Ответственностью "Витанта" | Средство, активирующее половую функцию |
-
2009
- 2009-06-04 RU RU2009121281/15A patent/RU2404793C1/ru active IP Right Revival
-
2010
- 2010-06-01 WO PCT/RU2010/000285 patent/WO2010140926A1/ru active Application Filing
- 2010-06-01 ES ES10783644T patent/ES2831673T3/es active Active
- 2010-06-01 CA CA2764351A patent/CA2764351C/en active Active
- 2010-06-01 US US13/376,023 patent/US8883741B2/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 JP JP2012513900A patent/JP5643816B2/ja active Active
- 2010-06-01 CN CN201080033918.6A patent/CN102481335B/zh active Active
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RU1124544C (ru) * | 1983-06-30 | 1995-01-09 | Институт молекулярной генетики РАН | Гептапептид, обладающий свойствами психостимулятора пролонгированного действия с иммунотропной активность |
RU2058791C1 (ru) | 1989-01-11 | 1996-04-27 | Государственное предприятие "Элер-микро" | Стимулятор репродуктивной способности у теплокровных животных |
US5955421A (en) | 1990-05-11 | 1999-09-21 | Deghenghi; Romano | Peptides containing D-2-alkyl-Tryptophan |
WO1994022460A1 (en) | 1993-04-05 | 1994-10-13 | University Patents, Inc. | Diagnosis and treatment of erectile dysfunction |
US5932548A (en) | 1998-06-03 | 1999-08-03 | Deghenghi; Romano | Lysine containing peptides for treatment of heart disease |
RU2155065C1 (ru) | 1999-04-23 | 2000-08-27 | Институт молекулярной генетики РАН | Анксиолитическое средство и фармацевтическая композиция анксиолитического действия |
RU2264823C2 (ru) | 1999-11-10 | 2005-11-27 | Центарис Гмбх | Способ и пептиды для лечения эректильной дисфункции, способ и фармацевтическая композиция с использованием указанных пептидов |
RU2290195C1 (ru) * | 2005-04-21 | 2006-12-27 | Институт Молекулярной Генетики Российской Академии Наук (Имг Ран) | Средство с антикоагулянтной, антитромбоцитарной, антитромботической, фибриндеполимеризационной и фибринолитической активностями |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2015515855A (ja) * | 2013-05-28 | 2015-06-04 | アイビックス・リミテッドIvixltd. | 組換えペプチドを生産するための方法および得られるペプチド |
KR20160001591A (ko) * | 2013-05-28 | 2016-01-06 | “이빅스” 리미티드 | 재조합 펩타이드의 제조 방법 및 생성된 펩타이드 |
KR102093096B1 (ko) * | 2013-05-28 | 2020-03-25 | “이빅스” 리미티드 | 재조합 펩타이드의 제조 방법 및 생성된 펩타이드 |
US10836794B2 (en) | 2016-10-24 | 2020-11-17 | “Ivix” Ltd. | Group of peptides for treating female sexual dysfunction |
JP2018118973A (ja) * | 2018-02-23 | 2018-08-02 | アイビックス・リミテッドIvix Ltd. | 組換えペプチドを生産するための方法および得られるペプチド |
Also Published As
Publication number | Publication date |
---|---|
BRPI1011071A2 (pt) | 2016-09-27 |
CN102481335B (zh) | 2014-02-26 |
ES2831673T3 (es) | 2021-06-09 |
BRPI1011071B8 (pt) | 2021-05-25 |
CA2764351A1 (en) | 2010-12-09 |
EP2465521A4 (en) | 2012-12-19 |
RU2404793C1 (ru) | 2010-11-27 |
BRPI1011071B1 (pt) | 2020-10-20 |
EP2465521B1 (en) | 2020-10-14 |
JP2012528856A (ja) | 2012-11-15 |
CN102481335A (zh) | 2012-05-30 |
CA2764351C (en) | 2016-08-16 |
US8883741B2 (en) | 2014-11-11 |
EP2465521A1 (en) | 2012-06-20 |
US20120129791A1 (en) | 2012-05-24 |
JP5643816B2 (ja) | 2014-12-17 |
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