Plural Compounds Containing Cyclopentanohydrophenanthrene Ring Systems Patents (Class 514/170)
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Publication number: 20140072615Abstract: A transdermal hormone delivery system (THDS) is disclosed. The THDS is useful for control of fertility and as therapy for a variety of diseases and conditions treatable by robust delivery of progestin and estrogen hormones, particularly the progestin, levonorgestrel. The THDS comprises a backing layer, an adjoining adhesive polymer matrix comprising an effective amount of at least a progestin hormone, delivery of which is enhanced by one or more skin permeation enhancing agents present in pre-determined amounts. The THDS is capable of providing effective daily doses of progestin and estrogen hormones from a small surface area in contact with the skin, e.g., less than 20 square centimeters. Methods of fertility control and various types of hormone replacement therapy utilizing the THDS are also disclosed.Type: ApplicationFiled: November 15, 2013Publication date: March 13, 2014Applicant: Agile Therapeutics, Inc.Inventor: Te-Yen CHIEN
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Patent number: 8668901Abstract: Methods, devices and compositions for treatment of severe and uncontrolled asthma are provided by which high amounts of an inhaled corticosteroid are directed to the small airways of the lower lungs. The invention provides for a substantial decrease in the dose of concurrently administered oral corticosteroids. A particular advantage of the invention is the significant reduction in corticosteroid-related adverse effects.Type: GrantFiled: February 3, 2010Date of Patent: March 11, 2014Assignee: Activaero GmbH Research & DevelopmentInventors: Bernard Muellinger, Gerhard Scheuch, Thomas Hofmann, Philipp Kroneberg
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Publication number: 20140056916Abstract: Compositions and methods for inducing the deposition of elastin by administering compositions including a mineralocorticoid, such as, for example, aldosterone and, optionally, a secondary active agent for enhancing or modulating the effect of the mineralocorticoid are described herein.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicants: THE HOSPITAL FOR SICK CHILDREN, HUMAN MATRIX SCIENCES, LLCInventors: Aleksander HINEK, Thomas F. MITTS
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Publication number: 20140056848Abstract: A method for treating a subject with multiple sclerosis is disclosed herein. In one embodiment, a method is provided for treating a subject with multiple sclerosis that includes administering to the subject a therapeutically effective amount of 2ME2 or a derivative thereof.Type: ApplicationFiled: March 8, 2013Publication date: February 27, 2014Applicant: ENTREMED, INC.Inventors: Tak Wah Mak, Gordon Stuart Duncan
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Publication number: 20140056962Abstract: The subject invention provides a drug delivery system comprising at least one compartment comprising (i) a drug-loaded thermoplastic polymer core layer, (ii) a drug-loaded thermoplastic polymer intermediate layer and (iii) a non-medicated thermoplastic polymer skin covering the intermediate layer, wherein said core layer is loaded with crystals of a first (pharmaceutically) active compound and said intermediate layer is loaded with crystals of the second (pharmaceutically) active compound.Type: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Applicant: Merck Sharp & Dohme B.V.Inventors: Wouter de Graaff, Raymond Zeeman
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Patent number: 8658628Abstract: A hormone delivery system and method are provided for administering bio identical human hormones using a combination of modalities for the treatment of human physiological conditions.Type: GrantFiled: June 18, 2010Date of Patent: February 25, 2014Inventor: Karan Y. Baucom
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Patent number: 8658627Abstract: The present invention relates to pregnancy hormone combinations and methods of treatment for autoimmune diseases having at least two hormonal components, a pregnancy hormone (such as estriol), and a gestagen (such as levonorgestrel or norethindrone) thereby providing for the continuous, uninterrupted administration of pregnancy hormones for the treatment for autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: June 4, 2008Date of Patent: February 25, 2014Assignee: The Regents of the University of CaliforniaInventor: Rhonda Voskuhl
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Publication number: 20140050794Abstract: A pharmaceutical composition comprises, as a first active agent, 6?,7?;15?,16?-dimethene-3-oxo-17?-pregn-4-ene-21,17-carbolactone (drospirenone) in an amount corresponding to a daily dosage, on administration of the composition, of from about 2 mg to about 4 mg, and, as a second active agent, 17?-ethinylestradiol (ethinylestradiol) in an amount corresponding to a daily dosage of from about 0.01 mg to about 0.05 mg, together with one or more pharmaceutically acceptable carriers or excipients. In a specific embodiment, the composition consists of a number of separately packaged and individually removable daily dosage units placed in a packaging unit and intended for oral administration for a period of at least 21 consecutive days, wherein said daily dosage units comprises the combination of drospirenone and ethinylestradiol. The composition may further comprise 7 or less daily dosage units containing no active agent or containing ethinylestradiol alone.Type: ApplicationFiled: May 23, 2013Publication date: February 20, 2014Inventors: Juergen Hilman, Wolfgang Heil, Ralph Lipp, Renate Heithecker, Michael Huempel, Johannes W. Tack
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Patent number: 8653051Abstract: The invention relates to the field of male and/or female sexual dysfunction. The invention specifically relates to the use of 3-alpha-androstanediol, preferably in combination with a type 5 phosphodiesterase (PDE5) inhibitor.Type: GrantFiled: November 2, 2007Date of Patent: February 18, 2014Assignee: Emotional Brain B.V.Inventors: Jan Johan Adriaan Tuiten, Johannes Martinus Maria Bloemers, Robertus Petrus Johannes De Lange
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Patent number: 8653057Abstract: Testosterone levels in a patient predicts whether or not the patient is likely to recover sexual potency following radical prostatectomy. Lower levels of testosterone are associated with a lower rate of potency recovery and with more aggressive prostate cancers. Therapeutically increasing circulating testosterone leads to improved rates of return to potency.Type: GrantFiled: July 29, 2011Date of Patent: February 18, 2014Assignee: The Regents of the University of CaliforniaInventors: Thomas E. Ahlering, Douglas Skarecky
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Patent number: 8653052Abstract: The present invention is a product comprising a ?2 agonist and a progestin, as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of muscle loss. The present invention is also a ?2 agonist selected from R,R-formoterol, indacaterol or ritodrine, for use in the treatment or prevention of muscle loss.Type: GrantFiled: April 24, 2008Date of Patent: February 18, 2014Assignee: Acacia Pharma LimitedInventors: Julian Clive Gilbert, Robert William Gristwood
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Patent number: 8648060Abstract: The invention relates to the field of male and/or female sexual dysfunction. The invention specifically relates to the use of 3-alpha-androstanediol, preferably in combination with a 5-HT1A agonist. Optionally, said 3-alpha-androstanediol and said 5HT1a agonist are further combined with a type 5 phosphodiesterase (PDE5) inhibitor.Type: GrantFiled: November 2, 2007Date of Patent: February 11, 2014Assignee: Emotional Brain B.V.Inventors: Jan Johan Adriaan Tuiten, Johannes Martinus Maria Bloemers, Robertus Petrus Johannes De Lange
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Patent number: 8642568Abstract: Known or suspected traumatic brain injuries may be treated therapeutically by administering a therapeutically effective dose of resibufogenin. A preferred method for determining if a patient has a traumatic brain injury includes obtaining a body specimen from the patient, determining the concentration of marinobufagenin in the body specimen, comparing the concentration of marinobufagenin to the concentration in such body specimens in normal patients, and if the marinobufagenin concentration is substantially above the concentration of a normal patient, concluding traumatic brain injury exists. In a preferred embodiment, a substantial elevation is deemed to be an increase of about 30 percent above the marinobufagenin concentration of a normal patient. The body specimen may be blood, urine, or cerebrospinal fluid.Type: GrantFiled: June 15, 2011Date of Patent: February 4, 2014Inventors: Jules B. Puschett, Lee Shapiro
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Publication number: 20140031323Abstract: The various embodiments of the present invention relate to a human identical flowable hormone composition dispersed in a cream or gel contained in the novel “Smart” metered dose applicator, which facilitates numerous patient specific dosing options, dose titration, as well as continuous and variable dosing. The composition is designed for transdermal usage for consumers who follow a specified dosage protocol resulting in static and cyclic variations on serum hormone levels over a 28 day cycle stretched over the span of a month. The regimen is modeled after nature, in an attempt to replicate temporal variations in serum progesterone and estradiol hormone levels of premenopausal females with healthy hormone cycles. A dispenser is also disclosed for flowable cream-base medicaments, specifically; a unidirectional rotatable platform attached to a screw that is slipped into a barrel where it is secured in place and it joins the said components that house an elevator.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Inventor: Ramiro M. Perez
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Publication number: 20140024627Abstract: The current invention provides a new and original method for treatment of ocular inflammatory diseases. More particularly, the present invention relates a mineralocorticoid receptor agonist for use in the treatment of an ocular inflammatory disease.Type: ApplicationFiled: January 3, 2012Publication date: January 23, 2014Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PARIS DESCARTESInventors: Francine Behar-Cohen, Elodie Bousquet
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Publication number: 20140017299Abstract: The present invention is directed to film dosage compositions for delivery of testosterone esters. In particular, a film dosage composition is provided that includes: a) a first region including: i) a first polymeric matrix and ii) a first plurality of particles including: 1) a first testosterone ester and 2) a first surfactant; and b) a second region including: i) a second polymeric matrix and ii) a second plurality of particles including: 1) a second testosterone ester and 2) a second surfactant.Type: ApplicationFiled: March 15, 2013Publication date: January 16, 2014Applicant: MONOSOL RX, LLCInventor: MONOSOL RX, LLC
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Publication number: 20140018751Abstract: The invention relates to pharmaceutical formulations, in particular to transdermal therapeutic systems, which are characterized in that little or no active ingredient crystallizes out at the interface between the removable protective film (release liner) and the active-ingredient-containing matrix.Type: ApplicationFiled: September 17, 2013Publication date: January 16, 2014Applicant: Bayer Intellectual Property GmbHInventors: Stefan BRACHT, lldiko TEREBESI, Thomas LANGGUTH
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Patent number: 8629129Abstract: Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and/or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.Type: GrantFiled: September 4, 2012Date of Patent: January 14, 2014Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Publication number: 20140011780Abstract: A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.Type: ApplicationFiled: July 5, 2013Publication date: January 9, 2014Inventor: Om Dhingra
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Publication number: 20140011781Abstract: Disclosed is a method for treating or preventing anemia. The method includes administering a testis extract serving as an active ingredient for treating or preventing anemia to a mammal. The testis extract is extracted by chloroform and methanol mixed solvent. The testis extract includes nandrolone, testosterone, androstenedione, estradiol, and estrone. The testis extract is prepared by using a method including: adding an extraction solvent to a testis to homogenize; filtering the homogenized mixing solution to remove residues; fractionating a filtrate without the residue to separate a supernatant and a under layer; removing water from the separated under layer; and concentrating an extract without water.Type: ApplicationFiled: September 17, 2013Publication date: January 9, 2014Applicant: Industry-Academic Cooperation Foundation, Yeungnam UniversityInventors: In-Ho Choi, Dong-Mok Lee, Eun-Ju Lee, Ki-Ho Lee, Yong-Pil Cheon, Tae-Hoon Chun
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Publication number: 20140010806Abstract: The invention relates to methods to use 17?-ethynylandrost-5-ene-3?,7?,17?-triol to treat ocular diseases or conditions such as dry eye, uveitis or retinitis. The compound can be administered topically to the eye, by intravitreal injection or systemically, e.g., orally.Type: ApplicationFiled: March 15, 2013Publication date: January 9, 2014Inventors: James M. Frincke, Christopher L. Reading, Clarence N. Ahlem
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Patent number: 8623850Abstract: The invention relates to 15,16-methylene-17-(1?-propenyl)-17-3?-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the Z, R4, R6a, R6b, R7 and R18 have the meanings stated in claim 1, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity.Type: GrantFiled: December 23, 2008Date of Patent: January 7, 2014Assignee: Bayer Intellectual Property GmbHInventors: Ulrich Klar, Joachim Kuhnke, Rolf Bohlmann, Jan Hübner, Sven Ring, Thomas Frenzel, Frederik Menges, Steffen Borden, Hans-Peter Muhn, Katja Prelle
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Patent number: 8618083Abstract: A combination hormone and melatonin therapy is provided to reduce the risk of developing, or to reduce the severity of, breast cancer by administering at least one estrogen hormone and optionally at least one progesterone-receptor-binding compound or composition and melatonin together, preferably at normal bed time.Type: GrantFiled: July 20, 2010Date of Patent: December 31, 2013Assignee: Duquesne University of the Holy SpiritInventors: Paula A Witt-Enderby, Vicki L Davis
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Publication number: 20130338122Abstract: Hormone replacement therapies are provided comprising solubilized progesterone alone and optionally with an estrogen, cyclic/sequential and continuous-combined dosing, and administered via transdermal HRT delivery systems.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Applicant: THERAPEUTICSMD, INC.Inventors: Brian A. Bernick, Julia M. Amadio, Peter H.R. Persicaner, Janice Louise Cacace, Neda Irani
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Publication number: 20130338123Abstract: Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Inventors: Brian A. Bernick, Janice Louise Cacace, Peter H.R. Persicaner, Neda Irani, Julia M. AMADIO
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Patent number: 8609043Abstract: The present invention relates to the use of a container, made of an inorganic additive containing plastic material, for reducing physical/chemical interaction between the container and an oil, fat and/or wax containing formulation contained therein.Type: GrantFiled: August 6, 2012Date of Patent: December 17, 2013Assignee: M & P Patent AktiengesellschaftInventor: Claudia Mattern
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Patent number: 8604010Abstract: A method for producing a high sapogenin content composition, including: allowing a strong acid aqueous solution having a concentration of 0.01 mol/L to 4 mol/L to act on a saponin-containing plant, so as to perform hydrolysis treatment; neutralizing a liquid obtained by the hydrolysis treatment; filtering the liquid so as to obtain a residue; and drying the residue.Type: GrantFiled: March 8, 2011Date of Patent: December 10, 2013Assignee: Lion CorporationInventors: Naho Suzuki, Hidehiko Ishimaru
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Publication number: 20130303495Abstract: A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.Type: ApplicationFiled: March 15, 2013Publication date: November 14, 2013Inventors: Om Dhingra, James S. Bernstein
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Publication number: 20130295022Abstract: The present invention provides a highly tolerable, hydrating lanolin containing foamable composition for administration to the skin, body surface, body cavity or mucosal surface, e.g., the mucosa of the nose, mouth, eye, ear, respiratory system, vagina or rectum. The foamable composition includes lanolin, a surface-active agent, about 0.01% to about 5% by weight of at least one polymeric additive selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent, water, and a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition.Type: ApplicationFiled: June 6, 2013Publication date: November 7, 2013Inventors: Doron Friedman, Alex Besonov, Dov Tamarkin, Meir Eini
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Publication number: 20130295117Abstract: Compositions and methods for inducing the deposition of elastin in skin by administering compositions including a mineralocorticoid, such as, for example, aldosterone and, optionally, a secondary active agent for enhancing or modulating the effect of the mineralocorticoid are described herein.Type: ApplicationFiled: June 21, 2013Publication date: November 7, 2013Inventors: Aleksander HINEK, Thomas MITTS
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Patent number: 8575142Abstract: To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance or ameliorate the pathosis, the present invention provides an agent or a food or drink which contains a compound having a lophenol skeleton, or an organic solvent extract or a hot water extract of a Liliaceae plant or, a fraction thereof containing the compound as an active ingredient.Type: GrantFiled: September 22, 2006Date of Patent: November 5, 2013Assignee: Morinaga Milk Industry Co., Ltd.Inventors: Miyuki Tanaka, Eriko Misawa
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Publication number: 20130289008Abstract: The present invention relates to methods of administering compositions comprising a progesterone receptor antagonist for use in treating estrogen-dependent conditions. The invention is also directed to methods for treating pain associated with endometriosis. The compositions may be administered to females with endometriosis as well as to females undergoing estrogen and/or selective estrogen receptor modulator (SERM) therapy. In certain embodiments, the invention provides a method for suppressing endometrial proliferation.Type: ApplicationFiled: April 2, 2013Publication date: October 31, 2013Applicant: REPROS THERAPEUTICS INC.Inventor: Joseph S. Podolski
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Publication number: 20130280213Abstract: The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, more particularly, Th1-mediated (cell-mediated) autoimmune diseases including: multiple sclerosis (MS), rheumatoid arthritis (RA), autoimmune thyroiditis and uveitis. Most preferably the invention is used to treat a patient with a therapeutically effective amount of estriol of 8 milligrams once daily via oral administration to treat the symptoms or prevent the onset of multiple sclerosis.Type: ApplicationFiled: February 11, 2013Publication date: October 24, 2013Inventor: Rhonda R. VOSKUHL
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Publication number: 20130266632Abstract: A drug delivery system consisting of one or more compartments and comprising a progestogenic compound dissolved in a thermoplastic polyethylene vinylacetate copolymer whereby, if the delivery system consists of one compartment, the compartment comprises (i) a core of a thermoplastic polyethylene vinylacetate copolymer comprising the progestogenic compound, such progestogenic compound being dissolved in the polyethylene vinylacetate copolymer up to a concentration below the saturation level at 25° C., and an estrogenic compound; and (ii) a skin of a thermoplastic polyethylene vinylacetate copolymer covering the core, said skin being permeable for both compounds; if the delivery system consists of more than one compartment, only one compartment comprises (iii) the progestogenic compound, such progestogenic compound being dissolved in a core of a thermoplastic polyethylene vinylacetate copolymer up to a concentration below the saturation level at 25° C.Type: ApplicationFiled: June 5, 2013Publication date: October 10, 2013Inventors: Wouter de Graaff, Janneke Sophie Groen, Marcus Antonius Bemardus Kruft, Johannes Antonius Hendrikus Van Laarhoven, Herman Vromans, Raymond Zeeman
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Publication number: 20130267485Abstract: The present invention relates to a combination of resveratrol with progestogen, and medicaments and pharmaceutical compositions containing the same, which are useful in the treatment and/or prevention of myoma and/or endometriosis, providing their size reduction and the control of related symptoms. Said association may additionally comprise an estrogen component. A treatment method and a kit are also objects of this invention.Type: ApplicationFiled: September 15, 2011Publication date: October 10, 2013Applicant: LIBBS FARMACEUTICA LTDA.Inventor: Hugo Da Silva Maia Filho
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Patent number: 8551516Abstract: The present invention provides compositions, methods, and kits for improving health in a woman having elevated SHBG levels, or who is receiving oral estrogen supplementation, by non-orally administering an effective amount of an androgenic steroid. Further, the present invention provides compositions, methods, and kits for coadministering an effective amount of an orally administered estrogen and an effective amount of a non-orally administered androgenic steroid for women in need of estrogen supplementation.Type: GrantFiled: February 15, 2007Date of Patent: October 8, 2013Assignee: Actavis, Inc.Inventors: Theresa Rosario-Jansen, Norman A. Mazer
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Patent number: 8536156Abstract: A method for hormonal contraception comprising administering at least one contraceptive hormone in a plurality of linked taking periods optionally having a sequence lasting several years. Each taking period comprises at least one taking cycle. Each taking cycle comprises a duration-constant taking phase lasting several days and a taking pause lasting several days. In each taking phase the hormonal component is administrated in a daily unit. In each taking pause either a placebo or no unit is administered. The duration of the taking phase or phases of at least the final taking period is at least 22 days. The duration of each taking phase in any taking period preceding a following taking period is shorter than that in each of the taking phases in each following taking period.Type: GrantFiled: December 12, 2011Date of Patent: September 17, 2013Assignee: Bayer Intellectual Property GmbHInventor: Hermann Kulmann
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Publication number: 20130237506Abstract: A stanol composition containing in addition to sitostanol as the main component, also a substantial amount of at least 10% campestanol has been found to effectively lower serum cholesterol levels when incorporated in edible commodities. Upon esterification the composition is especially useful in edible fats and oils and in fat-containing foods.Type: ApplicationFiled: December 18, 2012Publication date: September 12, 2013Applicant: RAISIO NUTRITION LTD.Inventors: Ingmar WESTER, Tapio Palmu, Tatu Miettinen, Helena Gylling
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Publication number: 20130224268Abstract: The present invention relates to methods for treating, preventing, minimizing, and/or diminishing signs of aging in the skin comprising topically administering to the subject in need thereof a hormonal nano formulation.Type: ApplicationFiled: February 27, 2013Publication date: August 29, 2013Applicant: NEWGEN BIOPHARMA CORP.Inventor: NEWGEN BIOPHARMA CORP.
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Publication number: 20130225542Abstract: This invention describes the use of a therapeutic gestagen (e.g., drospirenone, cyproterone acetate, dienogest) for the production of a pharmaceutical agent for the treatment of premenstrual dysphoric disorder (PMDD), optionally in combination with a natural or synthetic estrogen (e.g., estradiol or ethinylestradiol).Type: ApplicationFiled: February 1, 2013Publication date: August 29, 2013Applicant: SCHERING AKITIENGESELLSCHAFTInventor: Schering Akitiengesellschaft
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Patent number: 8513226Abstract: The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene (4) and 3-acetoxy2?-chloro-5-androsteno[17,16-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole, a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1 g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.Type: GrantFiled: March 26, 2009Date of Patent: August 20, 2013Assignee: Council of Scientific and Industrial ResearchInventors: Romesh Chandra Boruah, Moyurima Borthakur, Madan Gopal Barthakur, Paruchuri Gangadhar Rao, Sudip Kumar Kar, Annalakshmi Chinniah, Suchandra Goswami, Pratap Kumar Das
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Patent number: 8513240Abstract: The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, and magnesium stearate; or can contain microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, povidone, and magnesium stearate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.Type: GrantFiled: December 22, 2010Date of Patent: August 20, 2013Assignee: Wyeth LLCInventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
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Publication number: 20130209539Abstract: It relates to a device comprising (a) a core comprising polyurethane; (b) a sheath comprising ethylene vinyl acetate copolymer, said sheath substantially or completely surrounding said core; and (c) one or more active pharmaceutical ingredients dissolved or dispersed in said core and/or said sheath; and to a process for its preparation.Type: ApplicationFiled: February 13, 2013Publication date: August 15, 2013Applicant: CHEMO RESEARCH, S.L.Inventor: CHEMO RESEARCH, S.L.
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Publication number: 20130210783Abstract: Provided are methods for ameliorating a symptom of a neuropsychiatric disorder. Also provided are methods for ameliorating at least one symptom resulting from tobacco cessation; and for ameliorating a symptom of Alzheimer's disease or other cognitive disorder; of schizophrenia, schizoaffective disorder, or other psychotic disorder; of a depressive disorder; of bipolar disorder; of post-traumatic stress disorder or other anxiety disorder; of a pain disorder; or of traumatic brain injury. Also provided are methods for ameliorating a sleep disorder; for improving cognitive functioning; for predicting a predisposition to suicide, suicidal ideation, and/or suicidal behavior; and for ameliorating a neurodegenerative disorder. In some embodiments, the methods include administering to a subject in need thereof an effective amount of a neuroactive steroid composition, pharmaceutically acceptable salts thereof, derivatives thereof, or combinations thereof.Type: ApplicationFiled: August 31, 2012Publication date: August 15, 2013Applicant: Duke UniversityInventors: Christine E. Marx, Jed E. Rose
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Patent number: 8507559Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula, (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein T, W, X, Y, Z, R1, R2, R4 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula, (I) are disclosed.Type: GrantFiled: July 14, 2009Date of Patent: August 13, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Gregory D. Brown, George V. De Lucca, Douglas G. Batt, Rui-Qin Liu, Feng Qiu
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Patent number: 8507465Abstract: The present invention relates to a method of reducing the incidence of nausea and vomiting associated with the administration of oral contraceptive formulation and a method of preparation of oral contraceptive formulation comprising progestin and/or estrogen and an antiemetic. The preferred oral contraceptive formulation comprises of levonorgestrel and an antiemetic.Type: GrantFiled: October 24, 2008Date of Patent: August 13, 2013Assignee: Lupin LimitedInventors: Sheetal Kulkarni, Srirupa Das, Harshal Anil Jahagirdar, Satish Dalal, Shirish Kulkarni
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Patent number: 8501720Abstract: A method of treatment of dysmenorrhea in the context of oral contraception characterized by daily administration of ethinylestradiol and drospirenone in an extended regimen.Type: GrantFiled: August 1, 2005Date of Patent: August 6, 2013Assignee: Bayer Pharma AGInventors: Renate Heithecker, Bernd Duesterberg
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Publication number: 20130195956Abstract: Compositions and devices for transdermal hormone delivery are disclosed. The compositions and devices include desogestrel and enable delivery of effective amounts of progestin without the use of skin permeation enhancers.Type: ApplicationFiled: January 25, 2013Publication date: August 1, 2013Applicant: Agile Therapeutics, Inc.Inventors: Agis KYDONIEUS, Thomas M. ROSSI, Charles G. ARNOLD, Ajay K. BANGA, Vishal SACHDEVA
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Publication number: 20130196959Abstract: The present invention relates to formulations of poorly water soluble pharmaceutical agents of Formula I and II. The present invention also relates to compositions containing compounds of Formula I or II, and glucocorticoids, and methods for reducing side effects from glucocorticoid treatment by co-administration of compounds of Formula I and II. The compositions herein are useful for the treatment of diabetes and obesity related diseases including metabolic syndrome.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: Temple University - Of The Commonwealth System of Higher EducationInventor: Temple University - Of The Commonwealth System of Higher Education
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Publication number: 20130178452Abstract: The present invention relates to solid pharmaceutical compositions, in particular to oral contraceptives, comprising a progestogen, such as drospirenone; an estrogen, such as ethinylestradiol; a tetrahydrofolic acid or a pharmaceutically acceptable salt thereof, such as calcium 5-methyl-(6S)-tetrahydrofolate; and at least one pharmaceutical acceptable excipient or carrier. The compositions of the invention provide good stability of the tetrahydrofolic acid upon storage while still ensuring a fast and reliable release of the estrogen and the progestogen present in the composition.Type: ApplicationFiled: December 20, 2012Publication date: July 11, 2013Applicant: BAYER PHARMA AGInventor: Bayer Pharma AG