Chalcogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/254.07)
  • Publication number: 20130202657
    Abstract: The present invention generally relates to foams and, in particular, to foams for applications such as drug delivery, and particles that are made from such foams. One aspect relates to foams or particles containing pharmaceutically active agents. The foam may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foam or particle has an unexpectedly high specific surface area. A high specific surface area may, in some cases, facilitate delivery or release of the pharmaceutically active agent when the foam or particles made from the foam (e.g., by milling) are administered to a subject. The foam may also exhibit a relatively high loading of the pharmaceutically active agent. In some cases, the foam may be a microcellular foam. In one set of embodiments, the foam is created using a supercritical fluid, such as supercritical C02.
    Type: Application
    Filed: May 20, 2011
    Publication date: August 8, 2013
    Applicants: BASF SE, President and Fellows of Harvard College
    Inventors: Kosta Ladavac, Rodrigo E. Guerra, David Kaz, Vinothan Manoharan, Jens B. Rieger, Roland S. Koltzenburg, David A. Weitz
  • Publication number: 20130203602
    Abstract: The present invention relates to biologically active compounds, particularly liquid compounds, which are immobilized on a solid carrier material, particularly on mesoporous silica. The compounds are non-covalently supported on the solid carrier material thereby forming stable, easily handled solids which have the further advantage that the adsorbed biologically active compounds have improved thermal stability compared with the non-adsorbed compounds, and that they are released rapidly and completely from the carrier material when placed in an aqueous environment.
    Type: Application
    Filed: March 11, 2011
    Publication date: August 8, 2013
    Applicants: Danmarks Tekniske Universitet, The Board of Trustees Of The Univ. Of Alabama For And On Behalf Of The Univ. Of Alabama, The Queens University of Belfast
    Inventors: Anders Riisager, Rasmus Fehrmann, Hector Rodriguez, Katharina Bica, Robin D. Rogers, Daniel T. Daly, Gabriela Gurau
  • Patent number: 8501743
    Abstract: A personal care composition comprising a eutectic mixture, the eutectic mixture comprising a tertiary system, in which menthol may form part of the eutectic mixture or in the eutectic mixture comprises an antidandruff agent such as ketoconazole.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: August 6, 2013
    Assignee: Conopco, Inc.
    Inventors: Jason Shaun Burry, Richard Livesey Evans, Caroline Alexandra Hall, Ezat Khoshdel, Colina MacKay
  • Publication number: 20130195769
    Abstract: 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: Application
    Filed: March 11, 2013
    Publication date: August 1, 2013
    Applicant: FOAMIX LTD.
    Inventor: Foamix Ltd.
  • Patent number: 8486456
    Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Htr represents the endotherm (J/g) accompanying a transition at about 240° C). The solid dispersion product shows an improved bioavailability.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: July 16, 2013
    Assignee: Abbott GmbH & Co., KG
    Inventors: Gunther Berndl, Matthias Degenhardt, Markus Mäegerlein, Gerrit Dispersyn
  • Publication number: 20130171268
    Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.
    Type: Application
    Filed: June 5, 2012
    Publication date: July 4, 2013
    Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
  • Publication number: 20130171223
    Abstract: A pharmaceutical or cosmetic composition, comprising a substantially poorly water-soluble pharmaceutical active ingredient; and a nanoporous folic acid material, wherein the active pharmaceutical ingredient is incorporated inside the nanoporous channels of the particles.
    Type: Application
    Filed: September 14, 2011
    Publication date: July 4, 2013
    Applicant: Nanologica AB
    Inventors: Chunfang Zhou, Xin Xia, Alfonso E. Garcia-Bennett
  • Publication number: 20130158042
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
  • Publication number: 20130144264
    Abstract: Bioactive, hydroforming luminal liner compositions are formed of high molecular weight crystalline, absorbable copolyesters 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: Application
    Filed: January 30, 2013
    Publication date: June 6, 2013
    Inventors: Shalaby W. Shalaby, Kenneth David Gray, Georgios T. Hilas
  • Publication number: 20130137635
    Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.
    Type: Application
    Filed: February 9, 2011
    Publication date: May 30, 2013
    Applicant: LEXICON PHARMACEUTICALS, INC.
    Inventor: Arthur Thomas Sands
  • Publication number: 20130136700
    Abstract: A hair regrowth system consisting of sensitization, growth, and maintenance kits for alopecia areata and related alopecia balding conditions. Graduated doses of specific engineered and or extracted haptens are included in a sensitization kit for initiating immune system response in hairless areas. A growth kit containing topical hormones to increase papilla size and vigor and a maintenance kit to sustain immune system response and papilla size and vigor for the long term are included in some embodiments.
    Type: Application
    Filed: November 28, 2011
    Publication date: May 30, 2013
    Inventor: George Davey
  • Publication number: 20130122058
    Abstract: The present invention provides organic nanoparticles that include a molecule having a Log P value of about 3 or above, an amphiphilic diblock copolymer or a surfactant, and a pharmaceutically-acceptable hydrophilic polymer. The present invention also provides methods of making these nanoparticles, e.g., by flash nanoprecipitation, with control over particle size and surface properties. The methods of the present invention provide a means for co-precipitating a water-insoluble compound with an amphiphilic stabilizer within a few milliseconds. The nanoparticles of the present invention exhibit high drug loading, e.g., 50% w/w, and can be produced with a mean particle size less than 200 nm and with a narrow particle size distribution.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: THE CHINESE UNIVERSITY OF HONG KONG
    Inventor: THE CHINESE UNIVERSITY OF HONG KONG
  • Patent number: 8435998
    Abstract: The present invention relates to crystalline form IV of posaconazole and pharmaceutical compositions comprising the same. The pharmaceutical composition can be used to treat or prevent fungal infections.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: May 7, 2013
    Assignee: Sandoz AG
    Inventors: Josef Wieser, Arthur Pichler, Andreas Hotter, Ulrich Griesser, Christoph Langes
  • Publication number: 20130109700
    Abstract: Methods of transdermally delivering a therapeutic amount of a triazole-triazolone compound are provided, e.g. for the prevention or treatment of basal cell carcinoma (BCC) in a subject. A therapeutic level of a triazole-triazolone compound such as itraconazole is delivered transdermally to a subject. Also provided are topical triazole-triazolone compositions that find use in practicing the subject methods.
    Type: Application
    Filed: September 7, 2012
    Publication date: May 2, 2013
    Inventors: Ervin H. Epstein, JR., Jean Tang, Philip A. Beachy, Jayakumar Rajadas, James Kim
  • Publication number: 20130102614
    Abstract: Described herein are methods of inhibiting angiogenesis, and treating and preventing disorders associated with angiogenesis by administering anti-angiogenesis compounds to a subject.
    Type: Application
    Filed: April 11, 2012
    Publication date: April 25, 2013
    Inventors: Jun O. Liu, Curtis R. Chong, Jing Xu, Juu Lu, Shridhar Bhat
  • Publication number: 20130102606
    Abstract: Cosmetic compositions comprising substituted carbamoyl heterocyclic analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted carbamoyl heterocyclic analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Application
    Filed: October 24, 2011
    Publication date: April 25, 2013
    Applicant: AVON PRODUCTS, INC.
    Inventors: Cheng Hwang, John Lyga, Hong Hu
  • Patent number: 8426420
    Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: April 23, 2013
    Assignee: Sanofi
    Inventors: Marc Nazaré, Gernot Zech, Melitta Just, Tilo Weiss, Gerhard Hessler, Markus Kohlmann
  • Publication number: 20130096069
    Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across 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 guanidino 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: Application
    Filed: September 10, 2012
    Publication date: April 18, 2013
    Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V.S. Sista, Thorsten A. Kirschberg
  • Publication number: 20130096095
    Abstract: 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: Application
    Filed: December 6, 2012
    Publication date: April 18, 2013
    Applicant: The Regents of the University of California
    Inventor: The Regents of the University of California
  • Publication number: 20130065897
    Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 14, 2013
    Applicant: PETER MACCALLUM CANCER INSTITUTE
    Inventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
  • Publication number: 20130059861
    Abstract: 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: Application
    Filed: September 27, 2012
    Publication date: March 7, 2013
    Applicant: Universitätsklinikum Freiburg
    Inventor: Universitätsklinikum Freiburg
  • Publication number: 20130052248
    Abstract: An item of clothing (10) for daily pharmacological treatment of a fungal infection, comprising: a textile material (20) to manage moisture when the item of clothing (10) is worn; microcapsules (30) grafted on the textile material (20); and antifungal agents encapsulated within the microcapsules (30) to pharmacologically treat the fungal infection when released from the microcapsules (30).
    Type: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Inventors: Marcus Chun Wah YUEN, Joanne Yiu Wan YIP, Kevin CHEUK, Chi Wai KAN, Shuk Yan CHENG
  • Patent number: 8383660
    Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: February 26, 2013
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
  • Publication number: 20130040948
    Abstract: 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: Application
    Filed: February 10, 2012
    Publication date: February 14, 2013
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Patent number: 8372440
    Abstract: The invention relates to a composition in the form of an emulsion that can be expanded by an aerosol dispenser, characterized in that it comprises from 15 to 20 volume % of alcohol, from 1 to 10 volume % of C3-C8 polyolen, a thickening agent, at least one non-ionic surfactant, a wetting agent, and one or more active ingredients dissolved or in suspension; the invention also relates to the medical and cosmetic applications thereof.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: February 12, 2013
    Assignee: Pierre Fabre Dermo-Cosmetique
    Inventors: Michel Jeanjean, Nadine Senegas
  • Patent number: 8372844
    Abstract: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: February 12, 2013
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
  • Publication number: 20130029978
    Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.
    Type: Application
    Filed: December 24, 2010
    Publication date: January 31, 2013
    Inventors: Tomoyuki Kamino, Yoshitaka Maeda
  • Publication number: 20130023522
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: July 17, 2012
    Publication date: January 24, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
  • Publication number: 20130004592
    Abstract: The invention comprises various aqueous PEG-carbohydrate-lipid based formulations of pharmaceutical active ingredients including compositions for intravenous injections. This invention relates to methods and compositions for improving solubility and the safety profile of pharmaceutical compounds. More particularly, the present invention relates to employing PEG-carbohydrate-lipid conjugates for formulating drug compositions having increased solubility or dispersivity and enhanced stability.
    Type: Application
    Filed: June 25, 2012
    Publication date: January 3, 2013
    Inventor: Nian Wu
  • Publication number: 20130005666
    Abstract: The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: CORNELL UNIVERSITY
    Inventors: Rajiv RATAN, Irina GAZARYAN, Natalya A. SMIRNOVA
  • Patent number: 8337871
    Abstract: The present invention provides a new insecticide formulation based on cyclodextrin characterized in that the active substance (insecticide and/or insect growth regulator), and a compound synergistic with the active substance, are complexed simultaneously with cyclodextrin. The formulation presents as a solid or as a solid/oil composition, and is soluble or completely emulsifiable in water or in aqueous mixtures of water miscible solvents. The activity of the present formulations was found to be greater than that of a mixture of the two active components each complexed separately with cyclodextrin, for the same dose. The preparation process of said formulation and its use as an insecticide in agriculture, for veterinary use or to eliminate household insects, are further aspects of the present invention.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: December 25, 2012
    Assignee: Endura S.p.A.
    Inventors: Oreste Piccolo, Giovanna Delogu, Valerio Borzatta
  • Publication number: 20120321574
    Abstract: The present invention provides anhydrous compositions for topical delivery of a medicament comprising (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol, or any combination of any of the foregoing; and (C) an anhydrous vehicle. In an alternate embodiment, the present invention provides anhydrous compositions for topical delivery of a medicament which comprise (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol or any combination of any of the foregoing; (C) an anhydrous vehicle; and (D) a medicament. Also provided are methods for topically delivering a medicament to an animal.
    Type: Application
    Filed: July 27, 2012
    Publication date: December 20, 2012
    Inventors: Katherine M. Burnett, Ellen S. Kurtz
  • Publication number: 20120309623
    Abstract: Provided in various embodiments are surface-modified hydrogels and hydrogel microparticles, methods for their preparation, and uses thereof for delivery of personal care and healthcare active ingredients, and agricultural active ingredients. In some embodiments, such hydrogels and hydrogel microparticles comprise surface coatings that are resistant to solvent washing and can act as barriers for the migration of water and/or water-compatible alcohols and actives soluble therein.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 6, 2012
    Inventors: Dongchan Ahn, James Thompson
  • Publication number: 20120301422
    Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.
    Type: Application
    Filed: January 16, 2003
    Publication date: November 29, 2012
    Inventor: Petrus Johannes Meyer
  • Publication number: 20120295845
    Abstract: Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is —C(O)—O—R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, —C(O)—NH2, or C1-C6 alkyl substituted with hydroxy or C1-C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, —CH2—(C1-C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or —CH2—(C1—C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: November 16, 2010
    Publication date: November 22, 2012
    Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Publication number: 20120283269
    Abstract: The present invention provides a method of suppression and/or deceleration of mammalian cellular aging. The method involves contacting mammalian cells with a composition that contains a non-genotoxic inducer of p53 (NGIP). In certain embodiments, the NCIP is a Mdm-binding agent or Mdm-2 antagonist. The NGIP can be nutlin, nutlin-3A, a nutlin analog, or a combination thereof. The invention also provides a method for reducing cellular hypertrophy in an organism by administering a composition that contains an anti-hypertrophic compound, such as nutlin, nutlin-3A, a nutlin analog, rapamycin or a rapamycin analog and combinations thereof, to the organism.
    Type: Application
    Filed: November 4, 2010
    Publication date: November 8, 2012
    Applicant: HEALTH RESEARCH INC.
    Inventors: Mikhail V. Blagosklonny, Andrei V. Gudkov, Zoya N. Demidenko
  • Publication number: 20120277249
    Abstract: There may be provided compositions of lipophilic pharmaceutical agents with improved solubility and stability. For example, there may be provided a non-aqueous composition that comprises a lipophilic pharmaceutical agent, and an amphiphilic polymeric solvent such as PEG400 but essentially free of organic solvents and non-solubilized particles. The composition may be further diluted with a desired aqueous diluent such as an infusion fluid for parenteral administration to a subject such as a human. The compositions may be useful for the treatment for diseases or conditions that are sensitive to lipophilic agents, such as infectious diseases, malignant or autoimmune diseases.
    Type: Application
    Filed: April 20, 2012
    Publication date: November 1, 2012
    Inventors: Borje S. Andersson, Benigno C. Valdez, Jeffrey Tarrand
  • Patent number: 8299072
    Abstract: The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: October 30, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Ghilsoo Nam, Kyung Il Choi, Hye Ran Kim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Hyunah Choo, Hyewhon Rhim, Yong Seo Cho, Eun Joo Roh, Gyo Chang Keum, Kee Hyun Choi, Kye Jung Shin, Hoh Gyu Hahn, Chan Seong Cheong, Jae Kyun Lee, Kee Dal Nam, Yong Koo Kang, Youngsoo Kim, Woong Seo Park, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Dong Yun Shin, Chi man Song
  • Patent number: 8299063
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: October 30, 2012
    Assignee: The University of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120258972
    Abstract: A method for treating hair loss caused by androgenic alopecia and/or male pattern baldness. The method, which not only slows hair loss but causes hair re-growth, includes approximately daily application to a subject's scalp of a novel composition comprising finasteride (Propecia® or Proscar®), dutasteride (Avodart®), and minoxidil (Rogaine®) as active ingredients in a hypoallergenic cream-based vehicle, preferably coupled with daily ingestion of 1 mg per day of finasteride (Propecia® or Proscar®), application to the scalp of 5% minoxidil (Rogaine®) foam approximately once per day, and use of a ketoconazole-containing shampoo (e.g., Nizoral®) approximately 2-3 times per week. The method described herein also resolves scalp dermatitis in atopic subjects suffering therefrom. A method for making the novel composition is also provided.
    Type: Application
    Filed: April 5, 2012
    Publication date: October 11, 2012
    Inventors: Asif Rafi, Roger M. Katz
  • Publication number: 20120251629
    Abstract: The present invention relates to a method of treating a patient for a condition where blood flow to a tissue or organ is interrupted. This method involves administering to a patient with a hypoxic condition where blood flow to a tissue or organ is interrupted, or at risk thereof, a compound that reduces the rate of HIF-1? inactivation in cells affected by the condition, thereby treating the patient for the condition. Also disclosed is a method of treating a tumor in a patient. In addition, the present invention relates to methods of identifying compounds as candidate drugs for treatment of hypoxic conditions and for treating tumors in a subject.
    Type: Application
    Filed: October 8, 2010
    Publication date: October 4, 2012
    Applicant: UNIVERSITY OF ROCHESTER
    Inventor: Marc Halterman
  • Publication number: 20120251595
    Abstract: The present invention relates to methods and compositions to prepare small size particles of poorly water soluble agents or drugs with surface enriched hydrophilicity.
    Type: Application
    Filed: November 9, 2010
    Publication date: October 4, 2012
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Robert O. Williams, III, Keat Theng Chow
  • Publication number: 20120225118
    Abstract: Compositions and methods of making the same for improving the bioavailability of a substantially water-insoluble pharmacologically active agent are described. The composition includes a substantially water-insoluble pharmacologically active agent, and a substantially water-insoluble matrix forming material comprising enzyme digestible or bile soluble nutrients, wherein the substantially water-insoluble pharmacologically active agent is dispersed in a solid matrix and wherein said pharmacologically active agent in said matrix is substantially free of the original crystalline form.
    Type: Application
    Filed: February 23, 2012
    Publication date: September 6, 2012
    Applicant: Latitude Pharmaceuticals Incorporated
    Inventors: Hailiang Chen, Andrew Xian Chen
  • Publication number: 20120225867
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: September 6, 2012
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Publication number: 20120207845
    Abstract: The invention relates to a method for treating disorders or diseases of a tight junction comprising delivering a pharmaceutical composition of nanoparticles to the tight junction, wherein the nanoparticles consist of positively charged chitosan, a negatively charged substrate, optionally a zero-charge compound, and at least one bioactive agent for treating said disorders or diseases of the tight junction of an animal subject.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 16, 2012
    Inventors: Hsing-Wen Sung, Kiran Sonaje, Ho-Ngoc Nguyen, Er-Yuan Chuang, Hosheng Tu
  • Publication number: 20120208795
    Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamopituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.
    Type: Application
    Filed: January 13, 2012
    Publication date: August 16, 2012
    Applicant: Board of Supervisors of Louisiana State University & Agricultural & Mechanical College
    Inventor: Nicholas E. Goeders
  • Publication number: 20120207751
    Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 16, 2012
    Applicant: NOVARTIS AG
    Inventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
  • Patent number: 8236791
    Abstract: Provided are methods of determining whether a compound is an inhibitor of an S100 protein. The methods utilize a biosensor that comprises the S100 protein that has a covalently bound fluorescent dye at an amino acid residue of the S100 protein that becomes less exposed to the aqueous solution upon activation of the S100 protein, where the fluorescent dye has decreased fluorescence when exposed to the aqueous solution than when protected from exposure to the aqueous solution. Also provided are methods of treating a subject having metastatic cancer.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: August 7, 2012
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Anne Reba Bresnick, Sarah Claire Garrett
  • Patent number: 8236806
    Abstract: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: August 7, 2012
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
  • Publication number: 20120196873
    Abstract: The present invention relates to drug formulations for the stabilization of amorphous forms of drugs. In particular the present invention relates to pharmaceutical compositions comprising sponge-like carrier matrices, particularly polyelectrolyte complexes or porous particles. The invention also relates to methods for the production of such pharmaceutical compositions.
    Type: Application
    Filed: June 19, 2009
    Publication date: August 2, 2012
    Inventors: Marc Nolte, Jörg Mayer, Maria Gonzalez Ferreiro, Annette Assogba-Zandt, Volker Fehring, Lutz Kröhne, Andreas Voigt, Christoph Dunmann