Chalcogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/254.07)
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Publication number: 20140288032Abstract: Agents that inhibit or prevent restenosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on cell proliferation, thrombosis, tissue modeling, and inflammation. Treatment for restenosis is provided using compositions of the invention.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: DiscoveRx CorporationInventors: Eric J. Kunkel, Evangelos Hytopoulos, Ivan Plavec
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Publication number: 20140271923Abstract: Patients inflicted with various clustering chronic diseases require treatment with multiple drugs having distinct mechanisms of action. Accordingly, patients with multiple conditions suffer from cumulative side effects of multiple drugs as well as drug-drug interactions. Embodiments, agents, compounds or drugs of the present invention, such as sesquiterpenes, e.g., Zerumbone, replace an equal or larger number of approved drugs during patient treatment. Examples of disorders prevented or ameliorated by administration of the formulations of this invention include but are not limited to inflammatory diseases that may be, oncological, genetic, ischemic, infectious, neurological, hematological, ophthalmological, rheumatoid, orthopedic, neurological, hematological, kidney, vascular, dermatological, gynecological, or obstetric.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventor: Christopher Brian Reid
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Patent number: 8835436Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: GrantFiled: July 9, 2010Date of Patent: September 16, 2014Assignee: Green Cross CorporationInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong Yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho Kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
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Patent number: 8829004Abstract: The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. According to the present invention inhibitors of the nitric oxide dioxygenase or arginase can be used for the manufacture of a medicament for the treatment of cancer. The present invention further provides a method for identifying compounds which can be used for the treatment of cancer, wherein the method allows to specifically identify compounds which induce apoptosis through the ROS signaling pathway. The present invention also provides a kit for identifying compounds which induce tumor apoptosis by inactivating a catalase on the tumor cell surface.Type: GrantFiled: September 27, 2012Date of Patent: September 9, 2014Assignee: Universitaetsklinikum FreiburgInventor: Georg Bauer
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Publication number: 20140248376Abstract: The present invention relates to a composition for the treatment of skin and ear infections in humans and animals such as dogs, cats and horses. In particular, the present invention relates to a topical composition comprising acetic acid, an antibacterial and/or an anti-fungal, and preferably also an anti-inflammatory. More specifically, the composition of the present invention is a bandage, bedding, clothing, conditioner, cream, drape, dressing, film, foam, gauze, gel, lotion, mousse, otic solution, pad, patch, serum, shampoo, solution, spray, or wipe for treatment or prevention of skin infections, wherein the composition comprises about 0.1-10% acetic acid, about 0.1-10% boric acid, about 0.01-20% azole, and optionally about 0.01-20% corticosteroid.Type: ApplicationFiled: May 13, 2014Publication date: September 4, 2014Applicant: DECHRA VETERINARY PRODUCTS, LLCInventor: Steven A. MELMAN
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Publication number: 20140234225Abstract: The present invention is directed to nanoparticulate active agent compositions comprising lysozyme as a surface stabilizer. Also encompassed by the invention are pharmaceutical compositions comprising a nanoparticulate active agent composition of the invention and methods of making and using such nanoparticulate and pharmaceutical compositions.Type: ApplicationFiled: February 17, 2014Publication date: August 21, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Christian F. Wertz, Niels P. Ryde
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Publication number: 20140228334Abstract: Process for producing composite materials by reactive spray-drying, where a liquid phase A, which comprises inorganic cations, and a liquid phase B, which comprises anions which, with the inorganic cations, form a salt that is insoluble in the mixture of the liquid phases are sprayed together using at least one multi-substance nozzle, and where at least one hydrophobic active ingredient is present in dissolved form in at least one liquid spraying phase, and where the salt formed from the cations of phase A and the anions of phase B has a solubility of less than 0.02 mol/l in the neutral aqueous medium.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: BASF SEInventors: Andreas Kempter, Max Siebert, Heidrun Debus
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Publication number: 20140219929Abstract: The invention relates to stable oleaginous cosmetic or therapeutic foam compositions containing certain active agents, having unique therapeutic properties and methods of treatment using such compositions. The foamable composition includes at least one solvent selected from a hydrophobic solvent, a silicone oil, an emollient, a co-solvent, and mixtures thereof, wherein the solvent is present at a concentration of about 70% to about 96.5% by weight of the total composition, at least a non-ionic surface-active agent at a concentration of about 0.1% to less than about 10% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a therapeutically effective amount of at least one active agent; and at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: Foamix Ltd.Inventors: Dov Tamarkin, Doron Friedman, Meir Eini, Alex Besonov
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Publication number: 20140221922Abstract: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: POLY-MED, INC.Inventors: Shalaby W. Shalaby, David Ingram, Georgios Hilas, Sheila Nagatomi
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Publication number: 20140221393Abstract: Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.Type: ApplicationFiled: September 7, 2012Publication date: August 7, 2014Inventors: Jun O. Liu, Wei Shi, Kalyan Kumar Pasunooti
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Publication number: 20140213532Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidine or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.Type: ApplicationFiled: December 24, 2013Publication date: July 31, 2014Applicant: KAI PHARMACEUTICALS, INC.Inventors: Jonathan B. Rothbard, Paul A. Wender, Leo P. McGrane, Lalitha V.S. Sista, Thorsten A. Kirschberg
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Patent number: 8790703Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.Type: GrantFiled: March 30, 2010Date of Patent: July 29, 2014Assignee: BASF SEInventors: Kathrin Meyer-Böhm, Rainer Dobrawa, Stefan Fischer, Karl Kolter
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Patent number: 8778938Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20140187531Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: March 3, 2014Publication date: July 3, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Xilu Wang, Noah P. Tu, Michael D. Wendt, Alexander R. Shoemaker, Michael J. Mitten
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Patent number: 8759400Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, this invention relates to compositions and methods for selectively enhancing fungal sensitivity to antifungal compounds.Type: GrantFiled: December 19, 2006Date of Patent: June 24, 2014Assignee: MethylGene Inc.Inventors: Nafsika Georgopapadakou, Wenqi Hu, Nadia Campeol, Jean Bedard, Robert Deziel, Alain Ajamian
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Publication number: 20140161892Abstract: The present invention relates to nanoparticles for encapsulating compounds, the preparation and uses thereof, said nanoparticles being based on half (C1-C4) alkyl esters of poly (methyl vinyl ether-co-maleic anhydride) (PVM/MA) copolymers. Said nanoparticles can encapsulate or incorporate a product of interest for use in the agricultural, cosmetic, food or pharmaceutical fields.Type: ApplicationFiled: April 16, 2012Publication date: June 12, 2014Applicant: BIONANOPLUS, S.L.Inventors: Hesham H.A. Salman, Izaskun Goni Azcarate
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Publication number: 20140134244Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: ApplicationFiled: November 1, 2013Publication date: May 15, 2014Applicant: Janssen Pharmaceutica N.V.Inventors: Lieven E.C. Baert, Geert Verreck, Dany Thone
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Patent number: 8722683Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 10, 2012Date of Patent: May 13, 2014Assignee: Hoffmann LA-Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20140107111Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.Type: ApplicationFiled: May 18, 2012Publication date: April 17, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
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Patent number: 8691235Abstract: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: GrantFiled: April 5, 2010Date of Patent: April 8, 2014Assignee: Poly-Med, Inc.Inventors: Shalaby W Shalaby, David Ingram, Georgios T Hilas, Sheila Nagatomi
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Publication number: 20140079636Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: March 15, 2013Publication date: March 20, 2014Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140066425Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.Type: ApplicationFiled: March 8, 2012Publication date: March 6, 2014Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.Inventor: Youzhi Tong
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Patent number: 8664224Abstract: External preparations for athlete's foot treatment capable of enhancing patient's compliance and capable of reducing the symptom of rubefaction, comprising an anti-trichophyton drug mixed with at least one compound selected from among 1-menthol, menthol analogue compounds and bactericidal compounds.Type: GrantFiled: July 15, 2011Date of Patent: March 4, 2014Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Toshihiro Shirouzu, Youichi Kawamura, Hiroki Kawatsura, Mitsuhiko Tokunaga
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Patent number: 8663695Abstract: The invention involves methods and formulations for treating or preventing rhinosinusitis, including fungus-induced rhinosinusitis in mammals. In one embodiment, the formulation of the present invention comprises a steroidal anti-inflammatory agent having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.Type: GrantFiled: October 31, 2007Date of Patent: March 4, 2014Assignee: Mylan Specialty L.P.Inventor: Imtiaz Chaudry
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Publication number: 20140050772Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: Hallux. Inc.Inventors: Frank Kochinke, Corrine Bright
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Patent number: 8653083Abstract: Compounds, compositions, kits and methods for modulating hedgehog pathway activity, and treating conditions related to abnormal or aberrant hedgehog pathway activity, are disclosed.Type: GrantFiled: August 22, 2006Date of Patent: February 18, 2014Assignee: The Johns Hopkins UniversityInventors: Philip A. Beachy, Jun O. Liu
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Patent number: 8648082Abstract: The invention provides a biological dressing for treatment of a dermatological disease comprised of a gum resin, a topically acceptable volatile solvent, and a pharmacologically active agent. The gum resin is present in a suitable amount that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin or mucosal membrane to which the composition is applied and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition. Biological dressings including tincture of benzoin and clotrimazole are shown to be efficacious for the long-term amelioration of symptoms of athlete's foot.Type: GrantFiled: October 23, 2002Date of Patent: February 11, 2014Assignee: Jaleva, LLCInventors: Alex Battaglia, Eva Beim
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Publication number: 20140031366Abstract: A parenteral azole composition comprises a first solvent, made of benzyl alcohol and/or an acidified alcohol such as ethanol, and a lipophilic component such as PEG400, and the azole, or triazole, such as itraconazole or posaconazole dissolved in this first composite solvent vehicle that is essentially free of surfactants, particularly non-ionic surfactants, and has low levels of water, preferably less than 5% water. The composition may be further diluted with an infusion fluid, such as normal saline or 5% or 10% dextrose in water, before infusion into an immunocompromized mammal, preferably a human. The composition is useful for the treatment and suppression of infections caused by microbes such as yeast and molds that are sensitive to azoles, but it may be extended to dissolve other pharmaceutically active agents that can be used to treat other types of infectious diseases or other ailments, such as malignant and autoimmune diseases.Type: ApplicationFiled: December 16, 2011Publication date: January 30, 2014Applicant: Board of Regents, The University of Texas SystemInventors: Borje S. Andersson, Jeffrey Tarrand, Benigno C. Valdez
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Publication number: 20140031334Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
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Publication number: 20140005205Abstract: The disclosure relates to, among other things, pharmaceutical compositions, such as solid oral dosage forms, comprising itraconazole, methods of making the compositions, and methods of using the same for treating disorders including, but not limited to, fungal infections.Type: ApplicationFiled: June 21, 2013Publication date: January 2, 2014Applicant: Mayne Pharma International Pty. Ltd.Inventors: Stuart James MUDGE, David Hayes, Stefan Lukas
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Publication number: 20140005204Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Ht, represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product shows an improved bioavailability.Type: ApplicationFiled: June 21, 2013Publication date: January 2, 2014Inventors: Gunther Berndl, Matthias Degenhardt, Markus Mägerlein, Gerrit Dispersyn
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Publication number: 20130338106Abstract: Disclosed are compounds of Formula I: and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRa-, and Ra, and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.Type: ApplicationFiled: February 23, 2012Publication date: December 19, 2013Inventors: John A. McCauley, Thomas J. Greshock, John Sanders, Heather H. Stevenson, Jonathan T. Kern, Ronald K. Chang
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Patent number: 8609645Abstract: Disclosed are novel formulations for the treatment of otic infections in an animal comprising a triazole anti-fungal compound, a quinolone antibiotic and a corticosteroid such as mometasone furoate monohydrate.Type: GrantFiled: November 10, 2011Date of Patent: December 17, 2013Assignee: Intervet Inc.Inventors: Abu S. Huq, Allan J. Weingarten, Robert D. Simmons
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Patent number: 8604022Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: January 26, 2012Date of Patent: December 10, 2013Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas, David Buttar
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Publication number: 20130324522Abstract: Insect repellent compositions are disclosed which are antagonists of insect odorant receptors. These compositions are useful as insect repellents and confusants. These insect repellent compositions may be suitable for topical application. Also disclosed are methods for interfering with the ability of an insect to detect odors. This is accomplished by exposing an insect to an olfactory-disrupting concentration of a compound. The abstract is shown below without the amendment markings: Insect repellent compositions are disclosed which are antagonists of insect odorant receptors. These compositions are useful as insect repellents and confusants. These insect repellent compositions may be suitable for topical application. Also disclosed are methods for interfering with the ability of an insect to detect odors. This is accomplished by exposing an insect to an olfactory-disrupting concentration of a compound.Type: ApplicationFiled: December 16, 2011Publication date: December 5, 2013Applicant: THE ROCKEFELLER UNIVERSITYInventors: Leslie Vosshall, Takao Nakagawa
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Publication number: 20130323179Abstract: Nanocrystals, compositions, and methods that aid particle transport in mucus are provided. In some embodiments, the compositions and methods involve making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The compositions and methods may include, in some embodiments, modifying the surface coatings of particles formed of pharmaceutical agents that have a low water solubility. Such methods and compositions can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for administration routes involving the particles passing through a mucosal barrier.Type: ApplicationFiled: May 3, 2013Publication date: December 5, 2013Applicant: Johns Hopkins University, TheInventors: Alexey Popov, Elizabeth M. Enlow, James Bourassa, Colin R. Gardner, Hongming Chen, Laura M. Ensign, Samuel K. Lai, Tao Yu, Justin Hanes, Ming Yang
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Patent number: 8598168Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: April 5, 2007Date of Patent: December 3, 2013Assignee: MethylGene Inc.Inventors: Oscar Moradei, Isabelle Paquin, Sylvie Frechette, Tammy Mallais, Simon Roy, Roger Machaalani, Arkadii Vaisburg, Jeffrey M Besterman, Pierre Tessier, David Smil, Silvana Leit, Robert Déziel
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Patent number: 8598162Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: October 11, 2011Date of Patent: December 3, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Jun Matsubara, Yohji Sakurai
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Publication number: 20130316006Abstract: Particles, compositions, and methods that aid particle transport in mucus are provided. The particles, compositions, and methods may be used, in some instances, for ophthalmic and/or other applications. In some embodiments, the compositions and methods may involve modifying the surface coatings of particles, such as particles of pharmaceutical agents that have a low aqueous solubility. Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for ophthalmic applications, and may be used for delivering pharmaceutical agents to the front of the eye and/or the back of the eye.Type: ApplicationFiled: May 3, 2013Publication date: November 28, 2013Applicant: Kala Pharmaceuticals, Inc.Inventor: Kala Pharmaceuticals, Inc.
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Patent number: 8591948Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: GrantFiled: June 1, 2006Date of Patent: November 26, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Elvire Colette Baert, Geert Verreck, Dany Thoné
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Publication number: 20130310397Abstract: The invention relates to a novel free-flowing powder pharmaceutical formulation for the delivery of a poorly-water-soluble drug substance that increases the solubility and bioavailability of the poorly- water soluble drug substance, as well as to a method of making the free-flowing powder pharmaceutical formulation. The invention also relates to dispersed particles that disperse instantaneously from the free-flowing powder formulation when the formulation is added to water, aqueous solvent, or organic solvent, wherein the bulk distribution of the poorly-water soluble drug substance of the free-flowing powder formulation in the dispersed particles is uniform. Such dispersed particles increase the bioavailable surface area of the poorly water-soluble drug substance and facilitate the drug substance's dissolution.Type: ApplicationFiled: October 31, 2011Publication date: November 21, 2013Applicant: WESTERN UNIVERSITY OF HEALTH SCIENCESInventors: Guru V. Betageri, Sunil A. Agnihotri, Kumaresh Soppimath
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Publication number: 20130303523Abstract: The present invention features, inter alia, pharmaceutically acceptable compositions that include metyrapol as the sole pharmaceutically active agent; compositions that include metyrapol and at least one additional pharmaceutically active agent; compositions in which the agent targeting the HPA axis is, itself, new or modified (e.g., a bi-specific antibody designed to traverse the blood-brain barrier or a known compound redesigned by, for example, conjugation to a substance that traverses the blood-brain barrier); and compositions in which the agent targeting the HPA axis is newly formulated in such a way that it fails to significantly inhibit cortisol production in the adrenal gland. For example, the composition can be formulated to include a dosage that is too low to reduce plasma cortisol levels or formulated to preferentially affect the skin.Type: ApplicationFiled: June 16, 2011Publication date: November 14, 2013Applicant: EMBERA NEUROTHERAPEUTICS, INC.Inventors: Nicholas E. Goeders, Barbara S. Fox, Glenn Guerin
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Patent number: 8580773Abstract: The present invention provides tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. The present invention provides a method of using tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof.Type: GrantFiled: December 6, 2012Date of Patent: November 12, 2013Assignee: The Regents of the University of CaliforniaInventors: Marc I. Diamond, Jeremy O. Jones, Adam R. Renslo
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Patent number: 8575161Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: GrantFiled: March 30, 2009Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Didier Roche, Gisèle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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Patent number: 8551985Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.Type: GrantFiled: April 28, 2010Date of Patent: October 8, 2013Assignee: Kowa Company, Ltd.Inventors: Minoru Koura, Hisashi Sumida, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
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Publication number: 20130261131Abstract: Pharmaceutical compositions and methods for treating skin or mucus fungal infections of feet, nails, groin, hands, tongue and other locations are disclosed herein. The pharmaceutical composition disclosed herein comprises at least one triazole agent. Methods of treating tinea pedis, tinea manuum, tinea unguium, tinea cruris, tinea corpora, tinea versicolor, candidiasis, aspergillosis, onychomycosis, coccidiodomycosis, cryptococcal meningitis, histoplasmosis, hoof thrush, hoof rot, tongue and mouth lesions, seborrheic dermatitis, and combinations thereof, are also presently disclosed.Type: ApplicationFiled: March 29, 2013Publication date: October 3, 2013Inventor: Nian Wu
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Patent number: 8541400Abstract: The present invention relates to compositions containing a) at least one monoacyl lipid; b) at least one diacyl glycerol and/or tochopherol; and c) at least one fragmentation agent; and optionally an active agent. The compositions are capable of self-dispersing to provide colloidal non-lamellar particles upon contact with an aqueous fluid. The invention additionally provides a method for forming non-lamellar particles from such compositions, and pharmaceutical formulations containing the compositions, plus non-lamellar particles formable from the compositions.Type: GrantFiled: August 4, 2005Date of Patent: September 24, 2013Assignee: Camurus ABInventors: Markus Johnsson, Fredrik Joabsson, Fredrik Tiberg
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Publication number: 20130245040Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.Type: ApplicationFiled: November 17, 2011Publication date: September 19, 2013Inventors: David Spiegel, Christopher Parker
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Publication number: 20130244962Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: April 11, 2013Publication date: September 19, 2013Applicant: Merck Frosst Canada Ltd.Inventors: Elise ISABEL, Christopher MELLON, Christian BEAULIEU