The Nitrogen Of The Z Radical Is Directly Bonded To A Benzene Ring Which Is Directly Bonded To The C(=o) Group Patents (Class 514/535)
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Patent number: 8754124Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: GrantFiled: November 21, 2012Date of Patent: June 17, 2014Assignee: Board of Regents, The University of Texas SystemInventors: Jung-Mo Ahn, Ganesh Raj
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Patent number: 8747885Abstract: The present invention provides to patches having excellent skin-permeability and therapeutic effect by the drug with lower irritation. In an external patch in which an adhesive layer containing an adhesive base and a drug are laminated with a backing, the external patch wherein the adhesive base contains 5-50% by weight of synthetic rubber polymer, 10-60% by weight of adhesive resin and 25-60% by weight of liquid paraffin, and the drug is etofenamate. According to the present invention, there is obtainable the patches having excellent skin-permeability and therapeutic effect by the drug with lower irritation.Type: GrantFiled: December 15, 2004Date of Patent: June 10, 2014Assignees: Teikoku Seiyaku Co., Ltd., Drossapharm AGInventors: Tomohiro Ishima, Hiroyuki Yamasaki, Masahiro Yamaji
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Patent number: 8748347Abstract: The present invention relates to methods, use and compositions for combating harmful fungi and bacteria in plants. More specifically, it relates to methods and compositions for controlling, preventing, or treating plant pathogens using UV filters for combating phytotoxin-producing fungi and/or bacteria, in particular, for combating harmful fungi and/or bacteria producing photodynamically active phytotoxins.Type: GrantFiled: March 25, 2010Date of Patent: June 10, 2014Assignee: BASF SEInventors: Richard Riggs, Dieter Strobel, Jochen Prochnow, Helmut Herrmann, Michael Ishaque, Christian Bittner
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Publication number: 20140142107Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.Type: ApplicationFiled: September 4, 2013Publication date: May 22, 2014Applicant: University of MassachusettsInventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
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Publication number: 20140127285Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.Type: ApplicationFiled: October 28, 2013Publication date: May 8, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
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Patent number: 8710098Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.Type: GrantFiled: September 28, 2009Date of Patent: April 29, 2014Assignee: Institute of Medicinal Biotechnology Chinese Academy of Medical ScienceInventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhuorong Li, Yanping Li, Jian Xu
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Patent number: 8697680Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.Type: GrantFiled: September 6, 2009Date of Patent: April 15, 2014Assignee: Ramot At Tel Aviv University Ltd.Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
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Publication number: 20140094457Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating a genetic disease caused by premature termination codons, or other conditions that render messenger ribonucleic acid (mRNA) susceptible to nonsense mediated RNA decay, in a subject. Also disclosed is a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy. The present invention also relates to a method of identifying inhibitors of nonsense mediated RNA decay and/or inducing autophagy. The present invention further relates to a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy in a subject.Type: ApplicationFiled: October 2, 2013Publication date: April 3, 2014Applicant: NEW YORK UNIVERSITYInventors: Lawrence B. Gardner, Timothy J. Cardozo, Leenus Martin
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Patent number: 8669290Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).Type: GrantFiled: November 28, 2012Date of Patent: March 11, 2014Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Shirou Sawa, Shuhei Fujita
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Publication number: 20140057979Abstract: The present invention provides substances that can be used in a broad range of applications and effectively regulate clock gene expression. Provided is a clock gene expression regulating agent comprising, as an active ingredient, one or more selected from the group consisting of caryophyllene oxide and compounds represented by the following structural formula: wherein X is CH3, NH2 or NHCH3.Type: ApplicationFiled: October 15, 2013Publication date: February 27, 2014Applicant: Shiseido Company, Ltd.Inventors: Yoko Gozu, Shinichiro Haze
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Publication number: 20140039009Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: October 15, 2013Publication date: February 6, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Zhiqiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
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Publication number: 20140031370Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Publication number: 20140018422Abstract: Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.Type: ApplicationFiled: December 14, 2012Publication date: January 16, 2014Inventors: Jeffrey Karpen, Sarah Kirk, Adriana Andrade, Michelle Schaffer, Kenneth Melich
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Publication number: 20140017346Abstract: Disclosed is a gelatin-free soft caramel including a soft caramel base mass that contains at least one polysaccharide hydrocolloid as texturing agent, a crystalline sweetener phase formed by isomaltulose, and a noncrystalline sweetener phase, wherein the caramel is gelatin-free. It can be made by providing a noncrystalline sweetener phase by dissolving at least one soluble sweetener in water, adding polysaccharide hydrocolloid, fat component, emulsifier and a part of the total amount of the isomaltulose to the noncrystalline sweetener phase, steam heating the mixture to a temperature of at least 100° C., adding the remaining isomaltulose to the heated mixture while stirring, incorporating air into the mixture and cooling.Type: ApplicationFiled: September 16, 2013Publication date: January 16, 2014Applicant: Sudzucker Aktiengesellschaft Mannheim/OchsenfurtInventors: Jorg Bernard, Kowalczyk Jorg
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Patent number: 8623334Abstract: A topical anesthetic is provided containing about 3 wt % to 10 wt % tetracaine in a vehicle suitable for administration to the mucosa. The vehicle for transporting the tetracaine includes a water soluble mucoadhesive or a combination of mucoadhesives such as a high molecular weight poly(ethylene oxide) homopolymer and a cellulose polymer. The vehicle also includes propylene glycol. The tetracaine is ground into a powder and is suspended in a plasticized hydrocarbon gel which completes the vehicle.Type: GrantFiled: September 10, 2012Date of Patent: January 7, 2014Inventors: Alan J. Wickenhauser, Stephen E. Peipert
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Publication number: 20130344150Abstract: This invention is related to direct compression of otilonium or its pharmaceutically acceptable salt having perfect powder flowability, good tablet weight distribution and no sticking to the punches.Type: ApplicationFiled: June 12, 2013Publication date: December 26, 2013Inventors: Farhad FARSHI, Recep AVCI, Urun KANDEMIRER, Serdar SOYLEMEZ, Fikret KOC
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Publication number: 20130315842Abstract: The present invention provides methods of administering an active agent to a localized mucous membrane in the oral cavity of a mammal, as well as oral dissolving film formed therefore.Type: ApplicationFiled: January 1, 2013Publication date: November 28, 2013Inventor: Andrew L. SKIGEN
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Publication number: 20130310325Abstract: The inventors have unexpectedly discovered that shock and/or potential multi-organ failure due to shock can be effectively treated by administration of liquid high-dose protease inhibitor formulations to a location upstream of where pancreatic proteases are introduced into the gastrointestinal tract. Most preferably, administration is directly to the stomach, for example, via nasogastric tube under a protocol effective to treat shock by such administration without the need of providing significant quantities of the protease inhibitor to the jejunum and/or ileum.Type: ApplicationFiled: September 23, 2011Publication date: November 21, 2013Inventors: Geert W. Schmid-Schonbein, Yung-Tsai Lee, Jeng Wei, Marisol Chang, Pedro Cabrales
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Publication number: 20130304002Abstract: A dermal drug delivery system is provided which comprises at least two components, for example, a sheet of a solid and flexible material, and a vehicle liquid comprising a solvent and optionally other ingredients. A drug, which can be unstable in said solvent but needs the solvent for being delivered into the skin, can be impregnated in the sheet. Other ingredients, such as agents for fastening the drug on the sheet can also be impregnated in the sheet. These two components may be stored separately and joined either shortly before or at the time of application. To use the system, the vehicle liquid may be applied either on the target skin area or on the sheet, and the sheet may then be applied on the target skin area so that the vehicle liquid is positioned between the sheet and the skin and brought into contact with the ingredients impregnated in the sheet.Type: ApplicationFiled: November 8, 2011Publication date: November 14, 2013Inventor: Jie Zhang
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Publication number: 20130296323Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.Type: ApplicationFiled: February 27, 2013Publication date: November 7, 2013Applicant: COYOTE PHARMACEUTICALS, INC.Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
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Publication number: 20130237542Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.Type: ApplicationFiled: October 17, 2011Publication date: September 12, 2013Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
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Publication number: 20130231385Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: ApplicationFiled: May 27, 2011Publication date: September 5, 2013Applicant: The Board of Regents of the University of Texas SystemsInventors: Jung-Mo Ahn, Ganesh Raj
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Patent number: 8497304Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).Type: GrantFiled: January 19, 2012Date of Patent: July 30, 2013Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Shirou Sawa, Shuhei Fujita
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Publication number: 20130184343Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicants: Syngenta Crop Protection LLC, Syngenta Participations AGInventor: Syngenta Participations AG
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Publication number: 20130184345Abstract: The present invention provides bis- and tris-benzamide compounds in the treatment of breast, brain and ovarian cancers.Type: ApplicationFiled: November 21, 2012Publication date: July 18, 2013Applicant: The Board of Regents of the University of Texas SystemInventor: The Board of Regents of the University of Texas S
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Patent number: 8486998Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.Type: GrantFiled: April 3, 2009Date of Patent: July 16, 2013Assignee: The University of MississippiInventors: Mahmoud A. Elsohly, Waseem Gul, Mohammad Khalid Ashfaq, Susan P. Manly
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Publication number: 20130150442Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: ApplicationFiled: November 21, 2012Publication date: June 13, 2013Applicant: The Board of Regents of the University of Texas SystemInventor: The Board of Regents of the University of Texas S
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Patent number: 8449863Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.Type: GrantFiled: March 25, 2010Date of Patent: May 28, 2013Assignee: Lyotropic Therapeutics, Inc.Inventor: David Anderson
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Publication number: 20130109639Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: November 1, 2012Publication date: May 2, 2013Inventors: Adam D. HUGHES, Erik FENSTER, Melissa FLEURY, Roland GENDRON
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Publication number: 20130109674Abstract: The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and/or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.Type: ApplicationFiled: December 17, 2010Publication date: May 2, 2013Applicant: Achelios Therapeutics LLCInventors: Harry J. Leighton, Matthew J. Buderer, Crist J. Frangakis
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Publication number: 20130101667Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: ApplicationFiled: October 24, 2012Publication date: April 25, 2013Applicant: ENDO PHARMACEUTICALS, INC.Inventor: Endo Pharmaceuticals, Inc.
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Publication number: 20130096191Abstract: Oral dosage forms of benzonatate useful for anti-tussive and anti-tussive/combination applications.Type: ApplicationFiled: December 13, 2012Publication date: April 18, 2013Inventors: William Wayne Howard, Russell Francis Somma
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Publication number: 20130079311Abstract: The invention provides compositions and methods for the convenient compounding of pharmaceuticals. Single and multiple unit of use kits are provided which contain all the necessary components required for preparing a compounded pharmaceutical. The kits of the invention include a first container having a first active agent and a second container having at least one second inactive agent. The kits of the invention are also useful for compounding veterinary pharmaceuticals.Type: ApplicationFiled: September 27, 2012Publication date: March 28, 2013Applicant: CutisPharma, Inc.Inventor: Indu Muni
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Publication number: 20130064784Abstract: A concentrated treatment composition includes a bird repelling composition, a glycol, and a fragrance-containing/odor control composition. The concentrated treatment composition provides a stable product that is miscible with water. Methods for applying to the treatment compositions are also provided.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: AVIAN ENTERPRISES, LLCInventor: Avian Enterprises, LLC
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Publication number: 20130064820Abstract: The present disclosure relates to, inter alia, compositions containing an inhibitor of human complement and/or an inhibitor of interferon alpha, and the use of the compositions in methods for treating or preventing Degos' disease in a subject. In some embodiments, the inhibitor is an antibody, or antigen-binding fragment thereof, that binds to a human complement component C5 protein or to a biologically-active fragment of C5 such as C5a or C5b. In some embodiments, the inhibitor is an antibody, or an antigen-binding fragment thereof, that binds to interferon alpha or to an interferon alpha receptor.Type: ApplicationFiled: March 1, 2011Publication date: March 14, 2013Applicant: ALEXION PHARMACEUTICALS, INCInventor: Cynthia Magro
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Publication number: 20130058880Abstract: Compositions, kits and methods of preparing a biocompatible film for cosmetic or medical uses are disclosed. The compositions or kits contain polyvinyl acetal (PVA), siloxane and a solvent. The siloxane can have a hydrophilic group. Once the solvent content is reduced, for instance, by evaporation, the mixture of PVA and siloxane is solidified, forming a film. The compositions and kits, optionally, further include one or more of an antimicrobial agent, a pigment, an anti-inflammatory agent, an anesthetic agent or a hemostatic agent. Such a film can be used, for example, in the form of an antimicrobial sealant, a liquid bandage, body paints, scar camouflage, water-proof sun block, makeup sealer, or antimicrobial wipe or spray.Type: ApplicationFiled: May 9, 2011Publication date: March 7, 2013Inventor: Shaosheng Dong
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Patent number: 8389500Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: October 28, 2009Date of Patent: March 5, 2013Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Publication number: 20130040919Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.Type: ApplicationFiled: August 20, 2012Publication date: February 14, 2013Inventor: S. Bruce King
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Patent number: 8367677Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1?H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: GrantFiled: March 18, 2005Date of Patent: February 5, 2013Assignee: Revotar Biopharmaceuticals AGInventors: Remo Kranich, Ewald Mirko Aydt
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Publication number: 20130018078Abstract: Transdermal drug delivery patches and methods of their production are described. The patches can be made such that the accommodate highly plasticizing drugs such as selegiline and/or the use of protonated forms of various drugs.Type: ApplicationFiled: September 20, 2012Publication date: January 17, 2013Applicant: MYLAN TECHNOLOGIES INC.Inventor: Mylan Technologies Inc.
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Publication number: 20120329861Abstract: The present invention provides a method of treating cancer using benzoic acid derivatives, alone or in combination with standard treatments such as chemotherapy and radiotherapy. Also provided are methods of screening for benzoic derivatives based on their ability to inhibit the enzyme tyrosinase or to bind to and activate PXR/SXR xenobiotic receptors.Type: ApplicationFiled: May 14, 2012Publication date: December 27, 2012Applicant: NEW YORK UNIVERSITYInventors: Peter C. Brooks, Danielle Morais, Leonard Liebes, Dorothy Rodriguez
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Publication number: 20120288544Abstract: The present invention relates to an oral dosage form comprising N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine) or a pharmaceutically acceptable salt or solvate thereof, to a process for preparing such a dosage form and to the use of such a dosage form in medicine.Type: ApplicationFiled: January 18, 2011Publication date: November 15, 2012Applicant: GLAXO GROUP LIMITEDInventors: Matthew Burke, Charles Harding Rhodes
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Publication number: 20120289595Abstract: The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.Type: ApplicationFiled: July 25, 2012Publication date: November 15, 2012Applicant: Catholic University Industry Academy Cooperation FoundationInventor: Dong Heon Shin
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Publication number: 20120283326Abstract: Compounds of formula (I) are provided, wherein X is CH?CH, CH2O wherein the oxygen atom is bound to ring B, or OCH2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF3 and OCF3. The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions containing the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.Type: ApplicationFiled: July 17, 2012Publication date: November 8, 2012Inventors: Helén Tuvesson Andersson, Ulf Vellmar, Ingrid Hallin, Leif Svenson, Ingela Fritzson
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Publication number: 20120252720Abstract: The present invention relates to compositions and methods useful for the treatment of ear disorders, administered to a treated ear in the form of a foam or a mousse. Administering a medicament in such forms will increase the residence time of the medicament in the ear canal, provide relatively uniform distribution of the composition, and can increase the penetration of the active pharmaceutical ingredient in the affected area, may release active substances slowly, enhance treatment effectiveness, increase compliance and is more convenient to use than currently available ear medications. The administration in the form of a foam or a mousse may preferably be provided as a metered dose, of a volume suitable to fill the ear canal.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: Otic Pharma Ltd.Inventor: Eran Eilat
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Publication number: 20120248142Abstract: A pharmaceutical composition comprises an active ingredient dissolved in an essentially non-aqueous carrier system comprising volatile and non-volatile components, in which the volatile component comprises a volatile non-solvent for the active ingredient and a volatile solvation additive for the non-solvent and the non-volatile component comprises a non-volatile non-solvent and optionally a non-volatile solvent for the active ingredient, the volatile and non-volatile non-solvents comprising silicone fluids of respectively different viscosity.Type: ApplicationFiled: November 10, 2010Publication date: October 4, 2012Applicant: FUTURA MEDICAL DEVELOPMENTS LIMITEDInventor: Adrian Francis Davis
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Publication number: 20120234721Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.Type: ApplicationFiled: September 9, 2011Publication date: September 20, 2012Applicant: Neurotherapeutics Pharma, Inc.Inventors: Daryl W. HOCHMAN, John J. Partridge
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Publication number: 20120232104Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Patent number: 8263047Abstract: A topical anesthetic for dental procedures is provided containing about 3 wt % to 10 wt % tetracaine in a vehicle suitable for administration to the oral mucosa. The vehicle for transporting the tetracaine includes a water soluble mucoadhesive or a combination of mucoadhesives such as a high molecular weight poly(ethylene oxide) homopolymer and a cellulose polymer. The vehicle may additionally include a penetration enhancer such as propylene glycol. The tetracaine is ground into a powder and is suspended in a plasticized hydrocarbon gel which completes the vehicle.Type: GrantFiled: September 29, 2005Date of Patent: September 11, 2012Inventors: Alan J. Wickenhauser, Stephen E. Peipert