Female (mammal) Patents (Class 514/843)
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Patent number: 6506742Abstract: This invention provides a convenient process for preparing an oral contraceptive liquid formulation having improved solubility, bioavailability and stability useful as a reference standard.Type: GrantFiled: December 1, 2000Date of Patent: January 14, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: George Wong, Shifeng Wei, Herling Uang
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Patent number: 6500814Abstract: The present invention relates to a hormonal contraceptive product having two hormonal components, an estrogen and a gestagen, and a process for the combined, continuous administration of the product of the invention.Type: GrantFiled: June 5, 2000Date of Patent: December 31, 2002Assignee: Wyeth PharmaceuticalsInventor: Rolf-Dieter Hesch
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Patent number: 6479475Abstract: 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 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol for 3-8 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 3-8 days, a second phase combination of a progeslin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol, for 4-15 days beginning on the day immediately following the last day of administration of the first phase combination, wherein the same dosage of the progestin and estrogen combination is administered in each ofType: GrantFiled: July 2, 1997Date of Patent: November 12, 2002Assignee: WyethInventor: Michael J. Gast
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Patent number: 6476079Abstract: A device for the controlled release over a prolonged period of time of a drug having antiprogestinic properties, the device including a core containing the drug, optionally a membrane encasing the core, where at least one of the core and membrane, when present, is made of a siloxane-based elastomer composition including at least one elastomer and optionally a non-crosslinked polymer. The device is characterized in that the elastomer composition includes poly(alkylene oxide) groups and that the poly(alkylene oxide) groups are present in the elastomer or polymer as alkoxy-terminated grafts of polysiloxane units, or as blocks, the grafts or blocks being linked to the polysiloxane units by silicon-carbon bonds, or as a mixture of these forms.Type: GrantFiled: December 23, 1999Date of Patent: November 5, 2002Assignee: Leiras OyInventors: Harri Jukarainen, Tommi Markkula, Juha Ala-sorvari, Matti Lehtinen, Jarkko Ruohonen
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Patent number: 6451778Abstract: This invention provides a method of contraception which comprises administering to a female of child beating age for a combination of a progestin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol for 23-25 days beginning on day 1 of the menstrual cycle, and wherein the same dosage of the progestin and estrogen combination is administered in each of the 23-25 days.Type: GrantFiled: July 2, 1997Date of Patent: September 17, 2002Assignee: WyethInventor: Michael J. Gast
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Patent number: 6444668Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 allyl C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alknyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 andType: GrantFiled: April 19, 2000Date of Patent: September 3, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6362237Abstract: This invention describes the use of at least one compound with a progesterone-antagonistic (PA) action and at least one compound with an antiestrogenic (AE) action, each in a non-ovulation-inhibiting dosage in a single dosage unit, for the production of pharmaceutical agents for female contraception.Type: GrantFiled: December 26, 1995Date of Patent: March 26, 2002Assignee: Schering AktiengesellschaftInventors: Kristof Chwalisz, Klaus Stöckemann
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Patent number: 6355235Abstract: 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.Type: GrantFiled: November 23, 1999Date of Patent: March 12, 2002Assignee: Johns Hopkins UniversityInventors: Richard A. Cone, Kevin J. Whaley
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Patent number: 6340688Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11&bgr;,19-[4-(cyanophenyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11&bgr;,19-[4-(3-pyridinyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.Type: GrantFiled: September 17, 1998Date of Patent: January 22, 2002Assignee: Schering AktiengesellschaftInventors: Krzystof Chwalisz, Walter Elger, Karin Schmidt-Gollwitzer, Eckhard Ottow
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Patent number: 6333058Abstract: A process for preparing a spermicidal agent from neem oil includes (a) mixing neem oil with an aliphatic hydrocarbon solvent so that a precipitate forms, and filtering the mixture to separate the filtrate solution from the precipitate; (b) contacting the filtrate solution of step (a) with a polar extractant solvent whereby a spermicidal agent is extracted from the filtrate solution into the polar extractant solvent; and (c) removing solvent from the polar extractant solvent to produce a concentrated solution containing extract a spermicidal agent.Type: GrantFiled: January 15, 1998Date of Patent: December 25, 2001Assignee: National Research Development CorporationInventors: Govindaswamy Ilavazhagan, Chakra Devakumar
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Patent number: 6328991Abstract: A chemical composition, method and product for administration into the vaginal canal. The composition, method and product are effective in preventing the spread of sexually transmitted diseases, including the spread of AIDS.Type: GrantFiled: November 30, 1999Date of Patent: December 11, 2001Inventor: John Myhling
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Patent number: 6312722Abstract: The present invention describes a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days.Type: GrantFiled: January 3, 2000Date of Patent: November 6, 2001Assignee: Schering AktiengesellschaftInventors: Karin Schmidt-Gollwitzer, Walter Klemann
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Patent number: 6281251Abstract: Mono- and di-iodinated nonoxynol-9-derivatives and methods for their use are disclosed.Type: GrantFiled: March 22, 1999Date of Patent: August 28, 2001Assignees: University of Kentucky Research Foundation, The Medical College of Hampton Roads, Eastern Virginia Medical SchoolInventors: George Digenis, Philip Fowler, Kazuya Matsumoto, Gustavo Doncel
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Patent number: 6251956Abstract: An oral contraception regimen which comprises sequentially administering two or more progestational agents exhibiting different effects on the human endometrium in combination with an estrogen. The invention is also directed to an extended use oral contraception regimen comprising the sequential administration of two or more progestational agents in combination with an estrogen.Type: GrantFiled: August 20, 1998Date of Patent: June 26, 2001Assignee: Ortho Pharmaceutical CorporationInventors: Michael Kafrissen, Haya Taitel
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Patent number: 6225298Abstract: Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.Type: GrantFiled: June 18, 1997Date of Patent: May 1, 2001Assignee: Balance Pharmaceuticals, Inc.Inventors: Darcy V. Spicer, Malcolm Cecil Pike, John R. Daniels
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Patent number: 6225297Abstract: This invention relates to a combination product that consists of individual dosage units of a competitive progesterone antagonist and, in addition, sequentially provided individual dosage units of a compound with gestagenic action, as well as its use for the production of contraceptives based on the inhibition of implantation (receptivity inhibition).Type: GrantFiled: November 1, 1996Date of Patent: May 1, 2001Assignee: Schering AkitiengesellschaftInventors: Klaus Stockemann, Kristof Chwalisz
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Patent number: 6156742Abstract: A kit which is adapted and designed to provide both data on the current reproductive status of a patient, and contraception for those who are not pregnant, but recently engaged in unprotected sex.Type: GrantFiled: August 1, 1997Date of Patent: December 5, 2000Assignee: Gynetics Inc.Inventor: Roderick L. Mackenzie
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Patent number: 6147065Abstract: 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.Type: GrantFiled: July 28, 1999Date of Patent: November 14, 2000Assignee: Schering AktiengesellschaftInventors: Klaus Schollkopf, Wolfgang Halfbrodt, Joachim Kuhnke, Wolfgang Schwede, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6143754Abstract: This invention describes the novel use of dissociated competitive progesterone antagonists for the production of a pharmaceutical agent for demand-oriented female birth control (pill on demand), which can be used regardless of the point in the menstrual cycle, in a dosage unit that is to be administered on a one-time basis, whose dosage is below the ovulation-inhibiting dosage.Type: GrantFiled: March 22, 1999Date of Patent: November 7, 2000Assignee: Schering AktiengesellschaftInventors: Kristof Chwalisz, Klaus Stockemann, Karin Schmidt-Gollwitzer, Walter Klemann
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Patent number: 6139873Abstract: 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.Type: GrantFiled: October 23, 1998Date of Patent: October 31, 2000Assignees: Cedars-Sinai Medical Center, Wake Forest UniversityInventors: Claude L. Hughes, Jr., Manuel J. Jayo
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Patent number: 6133251Abstract: The combination preparation for contraception includes a first stage of 2 to 4 first stage daily dosage portions, a second stage of two groups of second stage daily dosage portions, a third stage of 2 to 4 third stage daily dosage portions and an additional stage of 2 to 4 additional stage daily dosage portions. The first stage daily dosage portion is an effective amount of natural estrogen, the second stage daily dosage portion is an effective amount of a combination of natural estrogen and natural or synthetic gestogen, the third stage daily dosage portion is another effective amount of natural estrogen and an additional stage daily dosage portion consists of a placebo. The first group of the second stage consists of 3 to 5 daily dosage portions and the second group, 13 to 17 daily dosage portions. More of the gestogen is included in the effective amount in the second group of the second stage than in the first group.Type: GrantFiled: October 25, 1996Date of Patent: October 17, 2000Assignee: Jenapharm GmbH & Co. KGInventors: Michael Dittgen, Sabine Fricke, Herbert Hoffmann, Claudia Moore, Michael Oettel, Monika Ostertag
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Patent number: 6110471Abstract: 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.Type: GrantFiled: September 12, 1997Date of Patent: August 29, 2000Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Marco Conti, Aaron J. W. Hsueh, Alexander Tsafriri
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Patent number: 6096732Abstract: Steroid esters of formula I ##STR1## are described, wherein m, n and x are as defined by the specification. The compounds are distinguished from the basic hydroxy compounds by considerably improved solubility as well by increased biological activity and selectivity.The compounds are suitable for the production of pharmaceutical agents.Type: GrantFiled: December 8, 1997Date of Patent: August 1, 2000Assignee: Schering AGInventors: Ulrich Klar, Arwed Cleve, Wolfgang Schwede, Gunter Neef, Eckhard Ottow, Kristof Chwalisz, Martin Schneider
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Patent number: 6066338Abstract: 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.Type: GrantFiled: June 15, 1998Date of Patent: May 23, 2000Assignee: Legere Pharmaceuticals, Ltd.Inventors: Michael J. Oldham, Bruce F. Rose, Howard C. Krivan
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Patent number: 6045786Abstract: 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.Type: GrantFiled: February 1, 1993Date of Patent: April 4, 2000Assignee: Johns Hopkins UniversityInventors: Richard A. Cone, Kevin J. Whaley
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Patent number: 6027749Abstract: The present invention describes a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days.Type: GrantFiled: June 3, 1998Date of Patent: February 22, 2000Assignee: Schering AGInventors: Karin Schmidt-Gollwitzer, Walter Klemann
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20-keto-11.beta.-arylsteroids and their derivatives having agonist or antagonist hormonal properties
Patent number: 6020328Abstract: 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.Type: GrantFiled: March 6, 1998Date of Patent: February 1, 2000Assignee: Research Triangle InstituteInventors: C. Edgar Cook, John A. Kepler, Ping-sheng Zhang, Yue-wei Lee, C. Ray Tallent -
Patent number: 6017882Abstract: The invention provides vitamin k-dependent polypeptides with enhanced membrane binding affinity. These polypeptides can be used to modulate clot formation in mammals. Methods of modulating clot formation in mammals are also described.Type: GrantFiled: October 23, 1997Date of Patent: January 25, 2000Assignee: Regents of the University of MinnesotaInventor: Gary L. Nelsestuen
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Patent number: 5989580Abstract: Disclosed are methods for sterilizing a female mammal wherein a composition comprising a biocompatible polymer and a biocompatible solvent is delivered to the fallopian tube of the female mammal.Type: GrantFiled: December 11, 1996Date of Patent: November 23, 1999Assignee: Micro Therapeutics, Inc.Inventors: George Wallace, Scott Evans, Richard J. Greff
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Patent number: 5980940Abstract: The invention provides a pharmaceutical combination preparation with two hormone components in a packaging unit and intended for time-sequential oral administration, comprising a number of daily dosage units physically separate and individually removable in the packaging unit, whereby as a hormonal active ingredient a first hormone component contains in combination an estrogen preparation and in at least a dosage that is sufficient to inhibit ovulation a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation, whereby the first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4, 3 or 2 daily units, and between these two hormone components, 2 or 1 active ingredient-free daily units are present or 2 or 1 blank pill days are indicated, and the total number of hormone daily units and the active ingredient-free daily units or the blank pill days is equal to the total number of days of the desired cycle,Type: GrantFiled: January 27, 1998Date of Patent: November 9, 1999Assignee: Schering AGInventors: Jurgen Spona, Bernd Dusterberg
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Patent number: 5965529Abstract: 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.Type: GrantFiled: June 6, 1995Date of Patent: October 12, 1999Assignees: The Board of Regents, University of Texas, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
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Patent number: 5962021Abstract: 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.Type: GrantFiled: June 22, 1998Date of Patent: October 5, 1999Assignee: Wake Forest UniverstiyInventors: Claude L. Hughes, Jr., Manuel J. Jayo
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Patent number: 5962413Abstract: 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.Type: GrantFiled: September 22, 1997Date of Patent: October 5, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5958399Abstract: 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.Type: GrantFiled: May 1, 1997Date of Patent: September 28, 1999Assignee: Procept, Inc.Inventors: Andrew J. Sonderfan, Albert T. Profy, Toni Chancellor, Margo McKinlay
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Patent number: 5958770Abstract: 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.Type: GrantFiled: November 6, 1996Date of Patent: September 28, 1999Inventors: Bill Elliot Cham, Brian Daunter
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Patent number: 5955490Abstract: Methods of detecting and treating rapidly growing exogenous cells, such as Protista, or parasites, that preferentially accumulate a photoactivatable porphyrin in which 5-aminolevulinic acid or precursor thereof is administered to the patient, or contacted to the exogenous cells, in an amount sufficient to induce synthesis fluorescence and/or photosensitizing concentrations of a protoporphyrin IX in the exogenous cells, followed by exposure of the exogenous cells to light of photoactivating wavelengths.Type: GrantFiled: June 5, 1995Date of Patent: September 21, 1999Assignee: Queen's University at KingstonInventors: James C. Kennedy, Roy H. Pottier, Robert L. Reid, Arnold Sac-Morales, Lewis L. Tomalty
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Patent number: 5948762Abstract: 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.Type: GrantFiled: July 17, 1997Date of Patent: September 7, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5935578Abstract: The instant invention is drawn to a sperm surface protein in substantially pure form selected from a human PH30 beta chain protein and a mouse PH30 beta chain proteins. Such proteins are useful as contraceptive vaccines in humans and mice respectively, and for identifying small molecules that will disrupt sperm-egg interaction and fertilization.Type: GrantFiled: December 19, 1996Date of Patent: August 10, 1999Assignee: Merck & Co., Inc.Inventors: Kenneth Alves, Sunil K. Gupta, Gregory Franklin Hollis
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Patent number: 5916593Abstract: 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.Type: GrantFiled: September 16, 1997Date of Patent: June 29, 1999Assignee: Akzo Nobel, N.V.Inventors: Pieter de Haan, Jocominus Antonius Maria Zwinkels
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Patent number: 5898032Abstract: A method of female contraception involves administering a combination of estrogen and progestin for 60-110 consecutive days in which the daily amounts of estrogen and progestin are equivalent to about 5-35 mcg of ethinyl estradiol and about 0.025 to 10 mg of norethindrone acetate, respectively. The advantages include less menstrual bleeding, less patient anemia, less total exposure to medication, higher compliance rates and more lifestyle convenience for patients.Type: GrantFiled: June 23, 1997Date of Patent: April 27, 1999Assignee: Medical College of Hampton RoadsInventor: Gary D. Hodgen
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Patent number: 5888543Abstract: 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.Type: GrantFiled: July 2, 1997Date of Patent: March 30, 1999Assignee: American Home Products CorporationInventor: Michael J. Gast
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Patent number: 5863553Abstract: 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.Type: GrantFiled: March 7, 1997Date of Patent: January 26, 1999Assignee: McNeil-PPC, Inc.Inventors: Peter Britton, Patricia Flanagan, William P. Hart, Deborah Linkin
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Patent number: 5858405Abstract: 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.Type: GrantFiled: July 2, 1997Date of Patent: January 12, 1999Assignee: American Home Products CorporationInventor: Michael J. Gast
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Patent number: 5824637Abstract: 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.Type: GrantFiled: February 28, 1997Date of Patent: October 20, 1998Assignee: The General Hospital CorporationInventors: William F. Crowley, J. Larry Jameson, Alan L. Schneyer, Jeffrey Weiss
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Patent number: 5770226Abstract: 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.Type: GrantFiled: July 10, 1996Date of Patent: June 23, 1998Assignee: Wake Forest UniversityInventors: Claude L. Hughes, Jr., Manuel J. Jayo
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Patent number: 5766632Abstract: 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.Type: GrantFiled: February 29, 1996Date of Patent: June 16, 1998Assignee: Legere Pharmaceuticals, Ltd.Inventors: Michael J. Oldham, Bruce F. Rose
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Patent number: 5759576Abstract: A sugar coating composition for application to a compressed medicinal tablet comprising a sugar, a dose of a hormonal steroid and a steroid release rate controlling amount of microcrystalline cellulose.Type: GrantFiled: April 10, 1996Date of Patent: June 2, 1998Assignee: American Home Products CorporationInventor: Reginald J. Barcomb
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Patent number: 5759551Abstract: 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.Type: GrantFiled: December 26, 1995Date of Patent: June 2, 1998Assignee: United Biomedical, Inc.Inventors: Anna Efim Ladd, Chang Yi Wang, Timothy Joseph Zamb
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Patent number: 5759577Abstract: A compressed medicinal tablet comprising a tablet core and a sugar coating, said sugar coating containing a dose of a hormonal steroid and a steroid release rate controlling amount of microcrystalline cellulose.Type: GrantFiled: April 24, 1996Date of Patent: June 2, 1998Assignee: American Home Products CorporationInventor: Reginald J. Barcomb
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Patent number: 5756681Abstract: 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.Type: GrantFiled: April 2, 1997Date of Patent: May 26, 1998Assignees: New York Blood Center, Eastern Virginia Medical SchoolInventors: Alexander Robert Neurath, Mary C. Mahony