WO2009095445A1 - New second medical use of 3-(2,2,2-trimethylhydrazine)propionate dihydrate - Google Patents
New second medical use of 3-(2,2,2-trimethylhydrazine)propionate dihydrate Download PDFInfo
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- WO2009095445A1 WO2009095445A1 PCT/EP2009/051016 EP2009051016W WO2009095445A1 WO 2009095445 A1 WO2009095445 A1 WO 2009095445A1 EP 2009051016 W EP2009051016 W EP 2009051016W WO 2009095445 A1 WO2009095445 A1 WO 2009095445A1
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- Prior art keywords
- propionate
- impotence
- impotentia
- trimethylhydrazine
- new
- Prior art date
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- 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
- A61K31/13—Amines
- A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
-
- 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
Definitions
- the present invention relates to the new medical use of 3-(2,2,2- trimethylhydrazine)propionate dihydrate and is generally related to the treatment of impotentia generandi. Background Art
- Reproduction in humans and other mammals is the process by which sperm and egg cells are produced, brought together, join and develop into a new individual. Inability to take part and complete the sexual activity and / or inability to reproduce is the Impotence.
- Impotentia coeundi there are two types of impotence: the so-called impotentia coeundi and impotentia generandi R. FARINA, et al. Surgical Treatment of Male Impotence. Aesthetic Plastic Surgery. 1982, vol.6, no.3, p.165.
- Impotentia coeundi better known as sexual erectile dysfunction is the inability to engage in intercourse due the old age, neurogenic, internal, urological or psychological factors after operations or due to the use of medicines, including medicines for high blood pressure.
- Impotentia coeundi is also known as erectile dysfunction.
- Impotentia generandi commonly known as infertility is reproductive incapacity whereby intercourse can take place but reproduction is not possible, for example due to a lack of viable sperm cells. This makes it more difficult to conceive.
- the word infertility refers to the inability to reproduce, while the term subfertility refers to reduced fertility. There are many reasons for male infertility. A few of them are: Sperm disorder, retrograde ejaculation, hormonal imbalance variococeles, surgical, medicinal, genetic, psychological etc.
- Erectile dysfunction is a condition where the penis does not harder and expands when a man is sexually excited, or when he cannot keep an erection this kind of impotence refers to lmpotentia coeundi.
- Patent EP 1429753 B (KALVINSH IVARS (LV); VEVERIS MARIS (LV); BIRMANS ANATOLIJS (LV)) 23.06.2004 disclosed gamma-butyrobetaine and/or 3-(2,2,2- trimethylhydrazinium)propionate dihydrate induce substantial and long-lasting increase of sexual activity in laboratory animals. Moreover, the combinations of both substances produce a more prolonged and higher increase of the intracavernous pressure than each of the constituent substances separately. Moreover, GBB or combination thereof with 3-(2,2,2- trimethylhydrazinium)propionate dihydrate, exert a positive influence on intracavernous pressure, induced by refectory stimulation.
- GBB or combination thereof with 3-(2,2,2-trimethylhydrazinium)propionate dihydrate are useful for stimulating of both the sexual activity and potency of mammals. Nevertheless this kind of impotence refers to lmpotentia coeundi.
- 3-(2,2,2-Trimethylhydrazinium) propionate dihydrate is known as compound with cardioprotective properties (this substance being known under its International Nonproprietary Name of Meldonium and its Trademark is Mildronate).
- 3-(2,2,2- Trimethylhydrazinium) propionate dihydrate is disclosed in US 4481218 (INST ORGANICHESKOGO SINTEZA) 06.11.1984.
- L-carnitine (carnitine)
- ACL acetyl-L-carnitine
- EP 1039894 B (SIGMA-TAU HEALTHSCIENCE S.P.A) 01.12.1997 discloses a pharmaceutical composition of L-carnitine and/or acetyl-L-carnitine for increasing the concentration and/or motility of spermatozoa in humans, including compositions for treating humans affected by idiopathic asthenozoospermia.
- Table 1 The activity of boars' sperm shows results of experimental and control group.
- the dose of Meldonium was 2 g daily.
- activity of sperm was 8.0 points of experimental group and 5.8 points in control group.
- p ⁇ 0.01 in experimental group comparing with control.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Reproductive Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to use of 3-(2,2,2-trimethylhydrazinium)propionate dihydrate for the treatment of impotentia generandi.
Description
Description
New second medical use of 3-(2,2,2-trimethylhydrazine)propionate dihydrate
Technical Field
The present invention relates to the new medical use of 3-(2,2,2- trimethylhydrazine)propionate dihydrate and is generally related to the treatment of impotentia generandi. Background Art
Reproduction in humans and other mammals is the process by which sperm and egg cells are produced, brought together, join and develop into a new individual. Inability to take part and complete the sexual activity and / or inability to reproduce is the Impotence.
There are two types of impotence: the so-called impotentia coeundi and impotentia generandi R. FARINA, et al. Surgical Treatment of Male Impotence. Aesthetic Plastic Surgery. 1982, vol.6, no.3, p.165. Impotentia coeundi , better known as sexual erectile dysfunction is the inability to engage in intercourse due the old age, neurogenic, internal, urological or psychological factors after operations or due to the use of medicines, including medicines for high blood pressure. Impotentia coeundi is also known as erectile dysfunction. Impotentia generandi, commonly known as infertility is reproductive incapacity whereby intercourse can take place but reproduction is not possible, for example due to a lack of viable sperm cells. This makes it more difficult to conceive. The word infertility refers to the inability to reproduce, while the term subfertility refers to reduced fertility. There are many reasons for male infertility. A few of them are: Sperm disorder, retrograde ejaculation, hormonal imbalance variococeles, surgical, medicinal, genetic, psychological etc.
Several medicaments are known, such as Viagra®, which is disclosed in EP 0702555 B (PFIZER LTD) 27.03.1996, Levitra®. which is disclosed in EP 1049695 B (BAYER AG) 08.11.2000 and Cialis® which is disclosed in EP 0740668 B (GLAXO LAB SA) 06.11.1996 all these medicaments are used to treat erectile dysfunction. Erectile dysfunction is a condition where the penis does not harder
and expands when a man is sexually excited, or when he cannot keep an erection this kind of impotence refers to lmpotentia coeundi.
Patent EP 1429753 B (KALVINSH IVARS (LV); VEVERIS MARIS (LV); BIRMANS ANATOLIJS (LV)) 23.06.2004 disclosed gamma-butyrobetaine and/or 3-(2,2,2- trimethylhydrazinium)propionate dihydrate induce substantial and long-lasting increase of sexual activity in laboratory animals. Moreover, the combinations of both substances produce a more prolonged and higher increase of the intracavernous pressure than each of the constituent substances separately. Moreover, GBB or combination thereof with 3-(2,2,2- trimethylhydrazinium)propionate dihydrate, exert a positive influence on intracavernous pressure, induced by refectory stimulation. GBB or combination thereof with 3-(2,2,2-trimethylhydrazinium)propionate dihydrate, are useful for stimulating of both the sexual activity and potency of mammals. Nevertheless this kind of impotence refers to lmpotentia coeundi. 3-(2,2,2-Trimethylhydrazinium) propionate dihydrate is known as compound with cardioprotective properties (this substance being known under its International Nonproprietary Name of Meldonium and its Trademark is Mildronate). 3-(2,2,2- Trimethylhydrazinium) propionate dihydrate is disclosed in US 4481218 (INST ORGANICHESKOGO SINTEZA) 06.11.1984. It is well known that 3-(2,2,2-Trimethylhydrazinium) propionate as dihydrate is widely used for controlling carnitine and gamma-butyrobetaine concentration ratio and consequently the speed of fatty acid beta-oxidation in the body DAMBROVA M., LIEPINSH E., KALVINSH I. Mildronate:cardioprotective action through carnitine-lowering effect.. Trends in Cardiovascular Medicine, . 2002, vol.12, no.6, p.275-279.
Due to these properties, Meldonium is extensively applied in medicine as an anti- ischemic, stress-protective and cardioprotective drug in treating various cardiovascular diseases and other pathologies involving tissue ischemia KARPOV R. S., KOSHELSKAYA O.A., VRUBLEVSKY A.V., SOKOLOV A.A, TEPLYAKOV AT., SKARDA I., DZERVE V., KLINTSARE D., VITOLS A., KALNINS U., KALVINSH I., MATVEYA L., URBANE D. Clinical Efficicay and Safety of Mildronate in Patients
With Ischemic Heart Disease and Chronic Heart Failure. Kardiologiya. 2000, no.6, p.69-74.
L-carnitine (LC) (carnitine) and acetyl-L-carnitine (ACL) play major roles in cell energy and lipid metabolism. Supplementation with these nutrients, which are highly popular in USA, has been associated with favourable effects, including anti-oxidant action, neuro- and cardioprotection, immunomodulation and cognitive enhancement.
EP 1039894 B (SIGMA-TAU HEALTHSCIENCE S.P.A) 01.12.1997 discloses a pharmaceutical composition of L-carnitine and/or acetyl-L-carnitine for increasing the concentration and/or motility of spermatozoa in humans, including compositions for treating humans affected by idiopathic asthenozoospermia.
Disclosure of Invention
Accordingly, it is an object of the invention to provide pharmaceutical composition for the treatment impotentia generandi caused by male infertility. To our surprise, using Meldonium dihydrate we unexpectedly found that it increases the motility of spermatozoa.
Best Mode for Carrying Out the Invention
The following examples further illustrate the invention.
Improved spermatozoa motility Experimental period:
This period was started when boars were taught to give sperm on phantom and they have achieved breed, aged 8-9 months. Experiment lasted 3 months, and when experiment started, animals were weighted and dispanserized. In this period animals from the experimental group started to get Meldonium, 2 g daily with food. At the end of experiment, the activity of sperm was assessed by scale after 10 points; it corresponds - 100%, what means that all spermies are moving on a straight way.
When the ejaculate was collected, there were determined its activity of sperm.
The main changes in the experimental group, comparing with control group we detected in the activity of sperm. At the start of experiment, the activity of sperm in both groups was almost equal.
The activity of sperm in experimental group significantly increased and at the end of experiment there were surprised changes, see Table.1.
H Control group ■ Experimental group
Table 1 The activity of boars' sperm shows results of experimental and control group. In experimental group the dose of Meldonium was 2 g daily. At the end of experiment, i.e., after three months, activity of sperm was 8.0 points of experimental group and 5.8 points in control group. p<0.01 in experimental group, comparing with control.
Claims
1. Use of 3-(2,2,2-Trimethylhydraziniunn) propionate or its pharmaceutically acceptable salt in the manufacture of a medicament for use in treating of male sexual impotence.
2. Use according to claim 1 , wherein impotence is impotentia generendi.
3. Use according to claim 2, wherein impotentia generendi is caused by decreased sperm motility or/and at least can be treated by increasing sperm motility.
4. 3-(2,2,2-Trimethylhydrazinium) propionate or its pharmaceutically acceptable salt for use in treating of male impotence whereby such impotence is caused by decreased sperm motility or/and at least can be treated by increasing sperm motility.
5. Use of 3-(2,2,2-Trimethylhydrazinium) propionate or its pharmaceutically acceptable salt for manufacture medicament for use in veterinary therapy for increasing sperm motility.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08150764 | 2008-01-29 | ||
| EP08150764.2 | 2008-01-29 | ||
| EP08165359 | 2008-09-29 | ||
| EP08165359.4 | 2008-09-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2009095445A1 true WO2009095445A1 (en) | 2009-08-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2009/051016 WO2009095445A1 (en) | 2008-01-29 | 2009-01-29 | New second medical use of 3-(2,2,2-trimethylhydrazine)propionate dihydrate |
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| Country | Link |
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| WO (1) | WO2009095445A1 (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003022262A1 (en) * | 2001-09-07 | 2003-03-20 | Ivars Kalvinsh | Pharmaceutical composition comprising gamma-butyrobetaine |
| WO2005012233A1 (en) * | 2003-08-04 | 2005-02-10 | 'joint Stock Company Grindeks' | Meldonium salts, method of their preparation and pharmaceutical composition on their basis |
| WO2006099244A1 (en) * | 2005-03-11 | 2006-09-21 | Hong Kong Nitric Oxide Limited | Combination therapy for endothelial dysfunction, angina and diabetes |
-
2009
- 2009-01-29 WO PCT/EP2009/051016 patent/WO2009095445A1/en active Application Filing
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003022262A1 (en) * | 2001-09-07 | 2003-03-20 | Ivars Kalvinsh | Pharmaceutical composition comprising gamma-butyrobetaine |
| WO2005012233A1 (en) * | 2003-08-04 | 2005-02-10 | 'joint Stock Company Grindeks' | Meldonium salts, method of their preparation and pharmaceutical composition on their basis |
| WO2006099244A1 (en) * | 2005-03-11 | 2006-09-21 | Hong Kong Nitric Oxide Limited | Combination therapy for endothelial dysfunction, angina and diabetes |
Non-Patent Citations (1)
| Title |
|---|
| DAMBROVA MAIJA ET AL: "Effect of inhibiting carnitine biosynthesis on male rat sexual performance", PHYSIOLOGY & BEHAVIOR, vol. 95, no. 3, October 2008 (2008-10-01), pages 341 - 347, XP002518535, ISSN: 0031-9384 * |
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