30 results about "Male contraceptive" patented technology

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and / or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and / or other clinical therpauetic and / or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and / or prevention of acute and / or chronic muscular wasting conditions; e) preventing and / or treating dry eye conditions; f) oral androgen replacement therapy; and / or g) decreasing the incidence of, halting or causing a regression of prostate cancer.

The present invention provides prodrugs of selective androgen receptor modulators (SARMs), and their use in treating or reducing the incidence of osteoporosis, a variety of hormone-related conditions, conditions associated with Androgen Decline in Aging Male (ADAM); conditions associated with Androgen Decline in Female (ADIF), and muscular wasting conditions, obesity, dry eye conditions, and prostate cancer. The prodrugs are also useful in oral androgen replacement therapy and male contraception.

The present invention relates to non-hormonal compositions and methods for inducing a condition of aspermia, azoospermia, or severe oligozoospermia in the male subject such that these compositions and methods for administering the same may be used as male contraception. Embodiments of the present invention may comprise a composition comprising an alpha-1-adrenoreceptor antagonist, such as (R)-silodosin, for daily administration to a male subject. The compositions and related methods may further include pharmaceutically acceptable carriers. The present invention further includes formulations which allow for a delay such that delayed or missed dose(s) do not nullify the contraceptive effect of the treatment regimen. Such compositions and methods may also avoid the side effects associated with typical formulations of alpha-1-adrenoreceptor antagonists.

Methods for treating FSH related conditions, such as prostatic intraepithelial neoplasia, pedophilia, infertility, or vaginal bleeding, with GnRH antagonists are disclosed. The methods of the invention generally feature administering to a subject a GnRH antagonist suitable for in vivo administration and able to reduce both plasma FSH and LH levels in a subject, in an amount or in a formulation effective to reduce plasma FSH levels in the subject to a symptom alleviating level. In vitro fertilization and male contraceptive methods are also provided.

A gene sequence related to the rat spermatozoa pertains to the field of genetic engineering technology. The nucleotide sequence encoded by the gene related to the rat spermatogenesis, isolated or purified by the invention and its protein molecule sequence are provided, wherein, the nucleotide sequence is related to an DNA molecule of the isolated or purified nucleotide sequence having high homology with the rat gene, and the molecule has at least 70% homology with the nucleotide sequence from 459 to 1214 bit of the SEQ ID NO.3. The present invention relates to the gene that has important function for study of the molecular mechanism of spermatogenesis and simultaneously provides new information for understanding of male reproduction, the development of male contraceptives as well as how to improve male reproductive capacity in livestock breeding.

The invention relates to an application of a gene C9ORF135, specifically to the gene C9ORF135, its encoding protein, an application of an antibody against the protein and a kit thereof. The invention brings forward an application of the gene C9ORF135, its encoding protein and the antibody against the protein in diagnosis, detection or treatment of sperm abnormality, an application in a latent target site as a male contraceptive, an application in diagnosis, detection or treatment of sperm vitality reduction and sperm abnormality caused by aging, and an application in detection of differentiation of embryonic stem cells. The invention also brings forward a kit for detecting sperm abnormality, a kit for screening male contraceptives, a kit for detecting differentiation of embryonic stem cells and their usage method.

The invention provides a novel male contraception gel system. According to the novel male contraception gel system, calcium alginate hydrogel (SA), an EDTA (Ethylene Diamine Tetraacetic Acid) solutionand polyethylene glycol (PEG) / nano gold (AuNps) are combined for the first time and a contraception system can be noninvasively relieved at any time through infrared irradiation. The novel male contraception gel system is a simple, efficient and reversible male contraception method.

The invention relates to beta-defensin 15 of specific antibacterial peptides of rat epididymis and application thereof, in particular to Defb15 genes of rats or orthologous genes thereof or application of amino acid sequences of the Defb15 genes or the orthologous genes thereof in the preparation of medicines for regulating and controlling male fertility, the development of male contraceptive medicines and the preparation of medicines for diagnosing and treating male infertility and resisting genital tract infection. The invention also relates to a medicinal composition containing the genes or the amino acid sequences.

The present invention discloses a quinazol derivative of a structural formula I, comprising the 3-substituted-4(3H)-quinazol derivative (compound 1-8) and the 6- substituted-4(3H)-quinazol derivative (compound 9-27). By testing each of the target compounds of the present invention in vitro inhibition of human sperm acrosin activity, the result shows that, compared with the publically reported acrosin inhibitor TLCK (N-toluene sulfonyl-L-lysyl-chloromethyl ketone), all target compounds have inhibit activity to human sperm acrosin. The quinazol derivative can be applied for preparing anti-fertility drugs and providing a new male contraceptive medicine in clinical field, and has a great application value. The present invention further provides a preparation method of the derivative I.

The invention discloses a functional peptide piece of an epididymal protease inhibitor and a multiplex antigenic peptide constructed by the functional peptide piece. The functional peptide piece of the epididymal protease inhibitor is selected from the amino acid sequence shown by SEQ ID No.1 or SEQ ID No.2, which is characterized by single component, simple structure and pertinent triggered immune response and can be used for preparing immunogen. The complex antigenic peptide constructed by the functional peptide piece is obtained by the covalent connection of the functional peptide piece toa branch of the treelike core formed by one or a plurality of bifunctional units. The multiplex antigenic peptide can improve the immunogenicity of the functional peptide piece without affecting the antigenic specificity, stimulate the organism to generate an antibody which has high-titre and is specific with the functional peptide piece, reduce the level of the serum epididymal protease inhibitor and induce efficient, safe and reversible antifertility action, thus being applicable to preparing male contraceptive vaccine.

The invention discloses a seminiferous duct contraceptive suppository conveyor which comprises a sleeve pipe, wherein the front end of the sleeve pipe is provided with a positioning cavity; a cavity is arranged in the sleeve pipe; the front end of the sleeve pipe is provided with a suppository seat; the rear end of the suppository seat is provided with a positioning column; the positioning columnis inserted in and matched with the positioning cavity; suppository seat cavities are arranged from the positioning column to the front end of the suppository seat in the suppository seat; the front end of the suppository seat is bent to one side; the front end of the suppository seat is provided with a needle seat; a needle head is installed on the needle seat, and a guide rod is installed in the cavity; a guide rod inner cavity is arranged in the guide rod, and a guide thread is installed in the guide rod inner cavity. A memory alloy silica gel mesh duct-shaped seminiferous duct contraceptive suppository matched with the seminiferous duct contraceptive suppository conveyor comprises a suppository body, wherein an inner cavity is arranged in the suppository body, and one end of the suppository body is provided with a suppository body opening; two silica gel spacers are installed in the inner cavity in parallel; and the periphery of the suppository body is provided with a silica gel layer. The invention overcomes the defects that male contraceptive methods are few at present, and only one long-term measure of vasoligature is available, and provides technical support and a contraceptive device for improving males to participate in family planning.

The invention provides an immunogen for preparing mPRα monoclonal antibody, which belongs to the field of biotechnology. The immunogen is a polypeptide, and the amino acid sequence is YEARRPIYE PLHTHWPHN. The present invention also provides a method for preparing the mPRα monoclonal antibody prepared from the immunogen, by cross-linking the target polypeptide YEARRPIYE PLHTHWPHN with KLH, and then preparing the immunogen and immunizing mice, hybridoma cells, Fusion cell screening, cloning of hybridoma cells, preparation of monoclonal antibodies by ascites method, identification and purification of monoclonal antibodies, etc. The present invention also provides an application of the above-mentioned mPRα monoclonal antibody in the preparation of a drug with a sperm physiological regulation mechanism or a male contraceptive. The mPRα monoclonal antibody produced by the immunogen has high titer and specificity, can specifically recognize mPRα, and can be a new molecular target for regulating sperm function compounds and male contraceptives.