Abstract: Described are 14,17-C.sub.2 -bridged steroids of the formula (I) defined in the specification. The compounds are available, even after peroral administration, with high gestagenic action and are suitable for the production of pharmaceutical agents.

Abstract: Disclosed are methods and compositions for oral contraception and for hormone replacement therapy. Certain compositions of the invention contain androgens, preferably methyltestosterone to be taken in conjunction with estrogens and progestins.

Abstract: A stable personal lubricant composition containing at least one water soluble polyhydric alcohol, a water soluble polymer derived from cellulose, tocopherol or a tocopherol derivative, an emulsifier and water.

Abstract: A method of contraception by delivering to the ovaries of a female mammal a pharmaceutically-effective dose of a PDE3-specific inhibitor at about the time of ovulation.

Abstract: A process for the preparation of spermicidal agents and other biologically active materials from neem oil or extractives by subjecting a neem feed obtained from neem oil to the step of enrichment. Such a step of enrichment is carried out in a chromatographic column containing a sorbant, and the feed is eluted with a non polar followed by a polar solvent or mixtures thereof. In accordance with one embodiment, the feed is formed by subjecting neem oil to the step of solvent partition, the precipitate being removed therefrom and the filterate forming the feed. In accordance with another embodiment, the feed is formed by adding a polar solvent to the filterate of the first embodiment, the lower layer formed therefrom being subjected to the step of distillation for removal of the solvent to obtain a feed.

Abstract: The invention relates to a steroid compound having the formula (I) ##STR1## comprising a ring E, said ring sharing carbon atoms at position 16 and 17 with the five-membered ring D and being .alpha. with respect to said D-ring. In addition, the carbon atom at position 17 is substituted with an oxygen atom-comprising group through a CO bond. The invention also relates to a pharmaceutical composition comprising said steroid compound. The steroid compounds of the present invention are very suitable for use in the prevention or treatment of peri-menopausal or menopausal complaints, more preferably the prevention or treatment of osteoporosis. Furthermore, the steroid compounds of the present invention can be used for contraceptive purposes.

Abstract: In order to prevent conception and/or the spread of sexually transmitted diseases (STD's) one or more lectins capable of binding sperm and/or the pathogenic microorganisms responsible for STD's are administered to the vagina prior to sexual intercourse. The lectins immobilize the sperm to render them incapable of fertilization and also bind to the microorganisms to render them non-pathogenic or to the cells to prevent infection by the microorganisms. Lectins can also be administered to treat sexually transmitted vaginal infections.The invention also encompasses a device for to be placed in the vault of the vagina which comprises a ring which surrounds the cervix and a membrane spanning the central aperture of the ring to prevent the direct contact of ejaculate with the cervical tissues. The device is impregnated or coated with lectins and releases them into the vaginal environment over a period of time.

Abstract: A method of therapy wherein there is administered to a person in need of such therapy a pharmacologically effective amount of a rupununine having the formula: ##STR1##

Abstract: Certain antibody molecules are so stable and so potent at immobilizing sperm as well as the pathogens for sexually transmitted diseases (STDs) that they make possible new prophylactic contraceptive methods: (a) for men, a skin lotion containing antibodies against sperm and against STD pathogens to be applied to the penis and external genitals during sexual activity, thereby delivering prophylactically effective doses of antibodies to virtually all areas of skin and epithelia across which most STDs, including AIDS, are usually transmitted, and, during vaginal intercourse, the penis will deliver a contraceptively reliable dose of the antibodies to the cervical region of the vagina; and (b) for women, intrauterine devices (IUDs) and intravaginal devices (IVDs) that release antibodies into the uterus or into the vagina to provide continuous protection against pregnancy and STDs for periods of months to years.

Abstract: In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers.The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions.In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid.

Abstract: The invention is directed to 20-keto-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.9, R.sup.12 and X are as defined by the specification. The compounds exhibit progestational and antiprogestational activities.

Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.

Abstract: Disclosed are methods and compositions for oral contraception and hormonal therapy. Certain compositions and methods of the invention contain androgens, and preferably methyltestosterone to be combined with estrogen and progestin compositions in a hormonal component of a pharmaceutical composition.

Abstract: The invention is directed to the control of cellular autophagy, cellular agglutination and the immobilization of motile cells. Such control is useful in, for example, the treatment of cancer, contraception, termination of pregnancy, removal of pathogenic organisms and removal of any abnormal cellular growth (malignant or otherwise); as a diagnostic and analytical tool whereby cell structure can be studied and testing could be undertaken for the presence (and subsequent analysis) of pathogenic and non-pathogenic organisms; and in the manufacture of biochemicals whereby certain cells must be destroyed or otherwise contained. From surface analysis of normal and abnormal cells, specific receptors on abnormal cells which are either not present on normal cells or are only present in significantly reduced numbers can be identified. Alkaloids and other pharmaceutically acceptable compounds are preferentially recognized by the abnormal cells, and which bind thereto and subsequently destroy.

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can prevent pregnancy in an individual.

Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or-oxytocin analogue antagonist or a prostaglandin.

Abstract: The invention relates to a process of making pharmaceutical dosage units comprising at least desogestrel or Org 30659 (17.alpha.-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one), present in an amount of about 0.005 to 1.0 percent by weight of each pharmaceutical dosage unit, characterized in that the steroidal agent, and when required pharmaceutically acceptable excipients, are mixed with water and granulated.

Abstract: This invention provides a method of contraception which comprises administering to a female of child bearing age for 23-25 consecutive days, a first phase combination of a progestin at a daily dosage of 40-500 .mu.g trimegestone, 250 .mu.g-4 mg dienogest, or 250 .mu.g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.g ethinyl estradiol for 9-13 days beginning on day 1 of the menstrual cycle, wherein the same dosage of the progestin and estrogen combination is administered in each of the 9-13 days, and a second phase combination of a progestin at a daily dosage of 40-500 .mu.g trimegestone, 250 .mu.g-4 mg dienogest, or 250 .mu.g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.

Abstract: This invention relates to personal lubricant compositions that are at least between three and eighteen times more lubricious than the compositions known previously. The compositions of this invention contain one or more polyhydric alcohols, one or more water-soluble polymers derived from cellulose, water and, optionally, preservatives and alkali metal or alkaline earth metal bases. The compositions of this invention can provide a vehicle for delivering medicaments for contraception and for the treatment and prevention of disease. This invention also relates to methods of using the personal lubricant compositions of this invention.

Abstract: The invention relates to an intravaginally-dissolvable contraceptive suppository, a method of using said suppository, and an improved method of manufacturing said birth control device. The suppositories of the invention, which comprise a lyophilized foam and a contraceptive, have a dissolution time of at least about 2 hours, and up to about 24 hours, and provide superior protection against pregnancy.

Abstract: This invention provides a bridged triphasic combination progestin/estrogen oral contraceptive regimen comprising the administration of a contraceptive progestin/estrogen combination for 23-25 days consecutive days beginning on the first day of menses, followed by the administration of an estrogen for 3-5 days following the administration of the estrogen/progestin combination, so that the total period of administration is 28 days per 28 day cycle. Particularly preferred progestins of this invention are trimegestone, dienogest, and drospirenone.

Abstract: A method for contraception which features administering to a patient a contraceptive agent having activin-antagonist activity. The contraceptive agent results in inhibition of the activin-stimulated release of FSH, thereby resulting in a decrease in fertility and facilitating contraception in the patient.

Abstract: Disclosed are methods and compositions for oral contraception. Certain compositions of the invention contain androgens, preferably methyltestosterone to be taken by younger users of the contraceptives to inhibit adverse effects of oral contraceptive use on bone mineral density.

Abstract: In order to prevent conception and/or the spread of sexually transmitted diseases (STD's) one or more lectins capable of binding sperm and/or the pathogenic microorganisms responsible for STD's are administered to the vagina prior to sexual intercourse. The lectins immobilize the sperm to render them incapable of fertilization and also bind to the microorganisms to render them non-pathogenic or to the cells to prevent infection by the microorganisms. Lectins can also be administered to treat sexually transmitted vaginal infections. The invention also encompasses a device for to be placed in the vault of the vagina which comprises a ring which surrounds the cervix and a membrane spanning the central aperture of the ring to prevent the direct contact of ejaculate with the cervical tissues. The device is impregnated or coated with lectins and releases them into the vaginal environment over a period of time.

Abstract: This invention relates to immunogenic luteinizing hormone releasing hormone (LHRH) peptides that lead to suppression of LHRH activity in males or females. When male rats are immunized with these peptides, serum testosterone drops and androgen-dependent organs atrophy significantly. These peptides are useful for inducing infertility and for treating prostatic hyperplasia, androgen-dependent carcinoma, prostatic carcinoma and testicular carcinoma in males. In females, the peptides are useful for treating endometriosis, benign uterine tumors, recurrent functional ovarian cysts and (severe) premenstrual syndrome as well as prevention or treatment of estrogen-dependent breast cancer. The subject peptides contain a helper T cell epitope and have LHRH at the C terminus. The helper T cell epitope aids in stimulating the immune response against LHRH. The peptides, optionally contain an invasin domain which acts as a general immune stimulator.

Abstract: A method for preventing pregnancy in a mammal such as a human, by introducing into the reproductive tract of the mammal an effective contraceptive amount of beta-lactoglobulin, either alone or in combination with a pharmaceutically acceptable excipient, carrier or diluent.

Abstract: The present invention embraces essentially pure human FSH receptor, or a fragment or mutant thereof which binds FSH, DNA encoding said receptor, fragment or mutant, expression vectors comprising said DNA, cells transfected with said expression vectors, and methods of producing said receptor, fragment or mutant by culturing said transfected cells. The present invention also includes pharmaceutical compositions comprising said receptor, fragment or mutant, as well as methods of treating patients with such compositions to reduce endogenous FSH bioactivity. An improved assay for human FSH using the receptor, fragment or mutant of the present invention is also disclosed.

Abstract: Inhibition of ovulation in a female may be achieved by administering a nitric oxide synthase inhibitor, alone or in combination with one or more of a progestin, an estrogen, and an LH-RH antagonist, thereby preventing conception. The stimulation of ovulation in a female may be achieved by administering a nitric oxide source, optionally in further combination with one or more of clomiphene, a gonadotropin, and an LH-RH agonist.

Abstract: A method for contraception which features administering to a patient a contraceptive agent having activin-antagonist activity. The contraceptive agent results in inhibition of the activin-stimulated release of FSH, thereby resulting in a decrease in fertility and facilitating contraception in the patient.

Abstract: The progesterone analog ST1435 has now been found to attain therapeutically effective levels upon topical application to the skin. ST1435 can be administered topically either in liquid or semisolid base such as a cream or gel or in a solid base such as a transdermal device such as a disk, band patch or bracelet. The invention further provides topical applications suitable for transdermal delivery of therapeutically effective amounts of ST1435.

Abstract: This invention relates to a compound preparation for contraception and hormone replacement that consists of three steps totalling 28 daily doses. The pharmaceutical is characterized in thatstep 1 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component,step 2 consists of 20 to 22 daily doses, each containing a preparation in which the active ingredients are at least one biogenous estrogen and one gestagen component from the group of C.sub.21 -gestagens including progesterone, as well as dienogest, desogestrel, 3-keto desogestrel, gestodene, levonorgestrel, norgestimate, norethisterone, norethisterone acetate and dydrogesterone, andstep 3 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component.

Abstract: A rupununine, either in purified form or a derivative in which one or both of the hydroxyl groups is substituted, the rupununine having the formula: ##STR1## where R.dbd.--H or --CH.sub.3.

Abstract: Based on the discovery that normal pregnant mice have a striking reduction in committed precursors of B lymphocytes, which could be documented in mice as early as day 6 of gestation, when IL-7 responding colony forming cells were reduced as much as two-thirds of normal levels, it has been determined that estrogen and other hormones elevated in pregnancy induce a specific modulation of lymphocyte formation during pregnancy and lactation. It is therefore possible to immunomodulate in a specific manner an animal by administration of hormones elevated during pregnancy, such as estrogen and estrogen-like compounds, or antagonists of estrogen. This has potential in the treatment of a number of disorders, especially those found in very high percentages of women as compared with men, such as many of the autoimmune disorders, as well as in immune tolerance during pregnancy, cyclic neutropenia, and osteoporosis.

Abstract: The present invention teaches that relatively low levels of serum progesterone, 1 to 6 ng/ml, may be used to prevent endometrial cancer. The vaginal delivery of progesterone using a cross-linked polycarboxylic polymer produces this low serum progesterone level while also providing the full secretory transformation of the endometrium, indicating the efficacy of the progesterone. Such low levels of serum progesterone will decrease the risk of breast cancer experienced by women undergoing hormone replacement therapy ("HRT") and minimize the potential of other undesirable progesterone associated side effects.

Abstract: A dissolvable element containing an agent material is used for local administration of the agent material in an internal body area. The dissolvable element is made of dissolvable polymer material and/or complex carbohydrate material which are food grade materials and have selected dissolving properties, such that it remains in substantially solid form before use, and dissolves due to human body temperatures and moisture during use to release the agent material in a desired timed release and dosage. As a contraceptive, the dissolvable element is preferably a film made of polyvinyl alcohol, polyethylene oxide, hydroxypropyl methyl cellulose and/or carboxymethyl cellulose. The dissolvable element may be formed as a laminate of different film layers for compound release properties, or it may be ground into particles and incorporated in a tampon or suppository. The dissolvable element may be foamed as a means for increasing its dissolution rate.

Abstract: A product for the administration of an active pharmaceutical agent via the vaginal canal comprising:(a) a sealed, air-tight package, enclosing therein;(b) a sponge impregnated with a liquid containing an effective amount of an active pharmaceutical agent, said liquid being present in an amount greater than that which is blocked within said sponge but less than the saturation value of said sponge such that when said sponge is inserted in the vaginal canal it will release liquid therefrom.

Abstract: A personal lubricant composition containing an antiviral, alkylphenoxypolyethoxyethanol spermicide, a water soluble polymer gel matrix and a solubilizer which permits the spermicide to be compatible with the gel matrix. Preferably, a polyethoxylated compound such as polyethoxylated castor oil may be used.

Abstract: An alternate approach to vasectomy for long term male contraception following a single intra-vas.application of a traditional plant (Azadirachta indica) product having immunomodulatory properties is described. The intra-vas administration of neem oil to male rats resulted in a block of spermatogenesis without affecting the testosterone production; the seminiferous tubules, although reduced in diameter, appeared normal and contained mostly early spermatogenic cells. No antisperm antibody could be detected in the serum. Unilateral administration of neem oil in the vas resulted in a significant reduction of testicular size and spermatogenic block only on the side of application; the draining lymph node cells of the treated side also showed enhanced proliferative response to in vitro mitogen challenge. These results indicate that intra-vas application of neem oil is effective in blocking fertility in male mammals after a single injection.

Abstract: It has been determined that estrogen and other hormones elevated in pregnancy induce a specific modulation of lymphocyte precursor cell production. The immune system of an animal or bone marrow cells in culture can therefore be modulated in a specific manner by administration of hormones elevated during pregnancy, such as estrogen and estrogen-like compounds or compounds that interfere with the synthesis or activity of these hormones, to increase or decrease production of B lymphocyte precursor cells.

Abstract: The present invention relates to a contraceptive for use by a male. The contraceptive consists of a copolymer of styrene maleic anhydride which is prepared by the step of irradiation at a dose of 0.2 to 0.24 megarad for every 40 gms. of the copolymer. The contraceptive consists of an injectable fluid of said copolymer and pure dimethyl sulphoxide.

Abstract: Inhibition of ovulation in a female may be achieved by administering an arginine derivative which acts as a nitric oxide sythase inhibitor, alone or in combination with one or more of a progestin, an estrogen, and an LH-RH antagonist, thereby preventing conception.

Abstract: A pharmaceutical composition for the prevention of sexually transmitted diseases, intended to be contacted with a mucosa. The composition contains, on the one hand, at least one constituent active against the viruses and bacteria responsible for the said sexually transmitted diseases and, on the other hand, a product inhibiting the penetration of the active constituent across a mucosa, in combination with a pharmaceutically acceptable vehicle adapted to the topical administration of this composition. Advantageously, the product inhibiting penetration is a film-former capable of forming a film with which the active constituent or constituents are associated.

Abstract: The invention provides methods of preparing a male antifertility agent composed of a diterpene lactone compound obtained from plants of the genus Tripterygium, the diterpene lactone compounds obtained from that method, and the use of the compounds as an antifertility agent.

Abstract: A dissolvable element containing an agent material is used for local administration of the agent material in an internal body area. The dissolvable element is made of dissolvable polymer material and/or complex carbohydrate material which are food grade materials and have selected dissolving properties, such that it remains in substantially solid form before use, and dissolves due to human body temperatures and moisture during use to release the agent material in a desired timed release and dosage. As a contraceptive, the dissolvable element is preferably a film made of polyvinyl alcohol, polyethylene oxide, hydroxypropyl methyl cellulose and/or carboxymethyl cellulose. The dissolvable element may be formed as a laminate of different film layers for compound release properties, or it may be ground into particles and incorporated in a tampon or suppository. The dissolvable element may be foamed as a means for increasing its dissolution rate.

Abstract: A method of entrapping a water-soluble substance in vesicles formed from a siloxane surfactant is carried out by dissolving the substance to be entrapped in water, adding a siloxane surfactant, mildly agitating the mixture, and removing excess of water and substance. Water-insoluble substances can be entrapped in the vesicles by dissolving the substance to be entrapped in the siloxane surfactant, and mildly agitating the substance and the siloxane surfactant. Suitable siloxane surfactants are R--[Si(Me).sub.2 O].sub.14 --Si(Me).sub.2 --R in which R is --(CH.sub.2).sub.3 (OCH.sub.2 CH.sub.2).sub.7 OH, R--[Si(Me).sub.2 O].sub.14 --Si(Me).sub.2 --R in which R is --(CH.sub.2).sub.3 (OCH.sub.2 CH.sub.2).sub.12 OH, Me.sub.3 SiO[Si(Me).sub.2 O].sub.22 --[SiMeRO].sub.2 --SiMe.sub.3 in which R is --(CH.sub.2).sub.3 (OCH.sub.2 CH.sub.2).sub.12 OH, and Me.sub.3 SiO[Si(Me).sub.2 O].sub.103 --[SiMeRO].sub.10 --SiMe.sub.3 in which R is --(CH.sub.2).sub.3 (OCH.sub.2 CH.sub.2).sub.12 OH.

Abstract: The invention relates to an intravaginally-dissolvable contraceptive suppository, a method of using said suppository, and an improved method of manufacturing said birth control device. The suppositories of the invention, which comprise a lyophilized foam and a contraceptive, have a dissolution time of at least about 2 hours, and up to about 24 hours, and provide superior protection against pregnancy.

Abstract: Compositions and methods which are effective to inhibit conception and to treat benign gynecological disorders for extended periods of time are described, wherein an effective amount of a gonadotropin hormone releasing hormone composition and an effective amount of an estrogenic composition are provided over a first period of time, in addition to a progestogen and optionally an androgenic composition. According to one protocol, the progestogen is provided for a second, shorter period of time; the progestogen is provided at a higher level for at least 5 to about 20 days, and then at a lower level for the remainder, if any, of the second period of time. In an alternative protocol, the progestogen is provided at a lower level substantially throughout the period of administration of gonadotropin hormone releasing hormone composition and estrogenic composition. An effective amount of the androgenic hormone is optionally provided over the first period of time.

Abstract: The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT.sub.2 receptors.

Abstract: Contraceptive devices which are effective for extended periods of time are described, in the form of means for releasing an effective amount of a gonadotropin hormone releasing hormone composition and means for releasing an effective amount of an estrogenic hormone over a first period of time, and means for releasing an effective amount of a progestogen for a second period of time, the second period of time being substantially shorter than and running simultaneously with a portion of the first period of time. The gonadotropin hormone releasing hormone composition is selected from gonadotropin hormone releasing hormone, gonadotropin hormone releasing hormone analogues, gonadotropin hormone releasing hormone agonists, gonadotropin hormone releasing hormone antagonists and mixtures thereof. Contraceptive methods employing the devices are also described.