Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Publication number: 20130171158Abstract: A method of treating or preventing an abnormality of glucose metabolism in a subject, the method comprising administering an antagonist of Inhibitor of Differentiation 1 (Id1) to the subject.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Applicant: GARVAN INSTITUTE OF MEDICAL RESEARCHInventors: Mia Akerfeldt, Ross Laybutt
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Publication number: 20130164221Abstract: Provided herein are methods for detecting, quantifying, differentiating, diagnosing and imaging pathogenic bacteria or condition associated therewith using substrates for bacterial enzymes. Fluorescent, luminescent or colorimetric signals emitted by substrates or enzyme products in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring a signal emitted from the substrates or products in the presence and absence of the potential therapeutic agent and a diagnostic method for detecting a mycobacterial infection in a subject by contacting biological samples with a substrate and imaging for signals emitted from a mycobacterial beta-lactamase product. Also provided are fluorogenic substrates or substrates comprising a colored dye or a chemical reagent effective to induce a color or pH change.Type: ApplicationFiled: December 4, 2012Publication date: June 27, 2013Inventors: Jeffrey D. Cirillo, James C. Sacchettini, Jianghong Rao, Hexin Xie
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Publication number: 20130165368Abstract: A composition for use in the prevention and/or treatment of microbial infection comprising essentially of one or more pure alkanol alkoxylates, diol alkoxylates and/or triol alkoxylates.Type: ApplicationFiled: February 1, 2011Publication date: June 27, 2013Inventors: Ian Steel, Paul Armstrong
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Patent number: 8470827Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: GrantFiled: September 25, 2008Date of Patent: June 25, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Patent number: 8470365Abstract: This invention relates to a process for preparing a pharmaceutical composition comprising four antitubercular drugs: rifampin or a pharmaceutically acceptable salt thereof, isoniazid or a pharmaceutically acceptable salt thereof, pyrazinamide or a pharmaceutically acceptable salt thereof and ethambutol or a pharmaceutically acceptable salt thereof, wherein rifampin and isoniazid are in separate layers. The invention also provides a pharmaceutical composition prepared therefrom having advantageous stability and bioavailability.Type: GrantFiled: July 29, 2010Date of Patent: June 25, 2013Assignee: Taiwan Biotech Co., Ltd.Inventors: Li-Heng Pao, Nion-Heng Shiao, Kuo-Hua Yang, Jui-Ming Chou
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Publication number: 20130158048Abstract: In the method of administering rifampicin to a human subject, the improvement wherein a prolongation composition is also administered, said prolongation composition comprising: Pectin 0.94 g Potassium bitartrate 0.48 g Tannic acid 0.8 g L-Tyrosine 0.21 g Riboflavin 2 ml 10% solution of 15% Ethyl Alcohol Hexanoic Acid (Caproic acid) 0.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Aida Salatinjants, Robert Salantinjants
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Publication number: 20130157930Abstract: The present invention is directed to linear, biodegradable polyesteramide (PEA) polymers synthesized with repeating units derived from aminophenol esters and diacids. These PEAs have a monomer repeat represented by as well as a variety of uses to coat, form or comprise medical devices, combination medical devices and pharmaceutical compositions, including sustained release formulations.Type: ApplicationFiled: February 13, 2013Publication date: June 20, 2013Applicant: TYRX, INC.Inventor: TYRX, INC.
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20130131081Abstract: A pharmaceutical composition that includes a carbamoyloxy arylalkanoyl arylpiperazine compound SERUM CHOLESTEROL and effectively prevents or treats diabetic nephropathy, diabetic neuropathy, diabetic vascular complications, hyperlipidemia, coronary artery disease, or inflammation.Type: ApplicationFiled: July 8, 2011Publication date: May 23, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Hong Sik Moon, Han Ju Yi, Eun Hee Chae, Sang Mi Chae, Hye Won Shin
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Patent number: 8445497Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: June 23, 2011Date of Patent: May 21, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, Brett R. Beno, John F. Kadow
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Publication number: 20130123263Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 10, 2013Publication date: May 16, 2013Applicants: F. HOFFMANN - LA ROCHE AG, GENENTECH, INC.Inventors: GENENTECH, INC., F. HOFFMANN - LA ROCHE AG
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Publication number: 20130115286Abstract: Oral administration forms are described for the controlled release of an antibiotic selected from the group consisting of rifampicin, rifabutin, rifapentine, rifalazil and mixtures thereof, for treating bacterial infections of the gastrointestinal tract, in particular travellers' diarrhoea, hepatic encephalopathy, ulcerative colitis, irritable bowel syndrome (IBS), Crohn's disease, and IBD (inflammatory bowel disease) in general. Moreover, said oral administration forms allow reduction of the amounts of antibiotic to be taken, with respect to the known administration forms and without reaching blood concentrations such as to select resistant strains of tuberculosis mycobacteria.Type: ApplicationFiled: July 13, 2011Publication date: May 9, 2013Inventors: Mario Brufani, Bianca Maria Lagrasta, Rolando Marzella, Ilaria Medici, Silvio Silvestri
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Publication number: 20130116247Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.Type: ApplicationFiled: April 5, 2011Publication date: May 9, 2013Applicant: MANNKIND CORPORATIONInventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
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Publication number: 20130108573Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Patent number: 8426422Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: January 18, 2010Date of Patent: April 23, 2013Assignee: Abbvie Inc.Inventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
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Patent number: 8409619Abstract: An oral drug delivery system for treatment of tuberculosis is described. The oral drug delivery system includes (e.g., a mixture or combination of): poly DL-lactide-co-glycolide nano particles having encapsulated an azole therein; poly DL-lactide-co-glycolide nano particles having moxifloxacin encapsulated therein; and poly DL-lactide-co-glycolide nano particles having RIF encapsulated therein.Type: GrantFiled: October 15, 2008Date of Patent: April 2, 2013Assignee: Lifecare Innovations Pvt. Ltd.Inventors: Gopal Krishan Khuller, Jitendra Nath Verma
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Publication number: 20130072497Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
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Patent number: 8394794Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.Type: GrantFiled: March 21, 2008Date of Patent: March 12, 2013Assignee: Regents of The University of MinnesotaInventors: Chengguo Xing, Jignesh Doshi
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Publication number: 20130052265Abstract: This invention relates to the field of chemical-pharmaceutical industry, specifically a new tuberculosis treatment that contains, as an active ingredient, 4-thioureido-iminomethylpyridinium perchlorate at a therapeutically effective and safe level and pharmaceutically acceptable excipients. In addition, this treatment relates to a method of the preparation of the new drug, providing a high yield of the new treatment. The new treatment has a higher tuberculostatic activity (200 times as high) and lower toxicity (2.4 times as low), as compared to a prototype drug, and is stable during long-term storage. This medicament may be used for treating and preventing all forms of pulmonary and extrapulmonary TB by using the new treatment in combination with other TB drugs.Type: ApplicationFiled: October 22, 2012Publication date: February 28, 2013Applicant: JOINT STOCK COMPANY "PHARMASYNTEZ"Inventor: Joint Stock Company "Pharmasyntez"
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Publication number: 20130045941Abstract: Embodiments of the invention relate generally to formulations comprising dimethylsulfoxide (DMSO) alone or in combination with methylsulfonylmethane (MSM), and one or more therapeutic agents, and uses of such formulations to treat infectious diseases. In several embodiments, such formulations are effective in treating drug-resistant infectious diseases, for example, drug-resistant tuberculosis.Type: ApplicationFiled: October 29, 2010Publication date: February 21, 2013Applicant: Abela Pharmaceuticals, Inc.Inventors: Colette Cozean, Rodney Benjamin, Anthony Keller, Jeff Varelman
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Publication number: 20130039904Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.Type: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
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Publication number: 20130040948Abstract: 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: ApplicationFiled: February 10, 2012Publication date: February 14, 2013Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20130035329Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.Type: ApplicationFiled: June 8, 2012Publication date: February 7, 2013Inventors: Jeffrey O. Saunders, Francesco G. Salituro
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Publication number: 20130029978Abstract: 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: ApplicationFiled: December 24, 2010Publication date: January 31, 2013Inventors: Tomoyuki Kamino, Yoshitaka Maeda
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Publication number: 20130023522Abstract: 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: ApplicationFiled: July 17, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GMBHInventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
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Publication number: 20130022661Abstract: A bio-remodable augmentation device including an implantable member configured for maintaining space in a bone defect. The implantable member is formed from a bio-remodable composite having structural properties so as to aid in the generation of new bone tissue and eventually be reabsorbed in the newly formed bone tissue. This structural and bio-remodable implant reduces, if not eliminates, the need to remove the implantable member from the patient once new bone tissue is formed. A kit including the implantable devices and bone growth material is disclosed. Methods of use are also disclosed.Type: ApplicationFiled: July 21, 2011Publication date: January 24, 2013Applicant: Warsaw Orthopedic, Inc.Inventor: William F. McKay
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Publication number: 20130018047Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Publication number: 20130004586Abstract: Compositions, solid polymeric compositions, and/or articles of manufacture are provided that can include a polymer matrix having a plurality of ion-exchange particles distributed therein. Products by process are provided that can include prior to solidifying the polymeric precursors, blending the precursors with ion-exchange particles to form a mixture, and solidifying the mixture to form a solid polymeric composition product. Solid polymeric composition production methods are also provided that can include providing a plurality of ion-exchange particles, prior to solidifying the polymeric precursors, blending the precursors with the ion-exchange particles to form a mixture, and solidifying the mixture to form a solid polymeric composition. Article of manufacture production methods are provided that can include incorporating a solid polymeric composition into an article of manufacture, the solid polymeric composition including a polymer matrix and a plurality of ion-exchange particles distributed therein.Type: ApplicationFiled: June 25, 2012Publication date: January 3, 2013Inventors: David J. Vachon, Nathan Knapp
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Publication number: 20130004517Abstract: The invention relates to methods of treating neurological disorders in a subject, by activating a DISC1 pathway. Methods of promoting neurogenesis in adult neural progenitor cells, enhancing nerve generation and treating GSK3 disorders as well as related compositions are also provided.Type: ApplicationFiled: September 10, 2012Publication date: January 3, 2013Applicants: The General Hospital Corporation d/b/a, Massachusetts Institute of TechnologyInventors: Li-Huei Tsai, Yingwei Mao, Jon Madison, Stephen Haggarty
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Patent number: 8343959Abstract: The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: GrantFiled: October 28, 2011Date of Patent: January 1, 2013Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Andreas Haupt, Frauke Pohlki, Karla Drescher, Karsten Wicke, Liliane Unger, Ana-Lucia Relo, Anton Bespalov, Barbara Vogg, Gisela Backfisch, Juergen Delzer, Min Zhang, Yanbin Lao
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Patent number: 8337877Abstract: Anti-infective articles capable of preventing infection associated with implantation of medical devices include low levels of anti-infective agents, may cover only a fraction of the portion of the medical device and be effective, or may rapidly elute anti-infective agent, without sustained elution, and still be effective.Type: GrantFiled: April 11, 2011Date of Patent: December 25, 2012Assignee: Medtronic, Inc.Inventors: Thomas C. Bischoff, William V. Ferris, Jr.
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Publication number: 20120322797Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.Type: ApplicationFiled: December 9, 2010Publication date: December 20, 2012Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY, ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
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Publication number: 20120309768Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Applicant: BIONOMICS LIMITEDInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20120301422Abstract: 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: ApplicationFiled: January 16, 2003Publication date: November 29, 2012Inventor: Petrus Johannes Meyer
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Publication number: 20120294901Abstract: A process for producing a small-sized, lipid-based cochleates. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.Type: ApplicationFiled: April 6, 2012Publication date: November 22, 2012Applicants: University of Medicine and Dentistry of New Jersey, BioDelivery Sciences International, Inc.Inventors: Leila Zarif, Tuo Jin, Ignacio Segarra, Raphael J. Mannino
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Publication number: 20120283175Abstract: The present invention provides a methods and pharmaceutical compositions useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, a synergistic combination of an inhibitor of LpxC and second antibacterial agent.Type: ApplicationFiled: November 4, 2011Publication date: November 8, 2012Applicant: Achaogen, Inc.Inventors: Phillip A. Patten, Eliana Saxon Armstrong
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Patent number: 8304416Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumors, for neuroprotection and for protection of the stress proteins of the skin.Type: GrantFiled: February 15, 2011Date of Patent: November 6, 2012Assignee: Merck Patent GmbHInventors: Teresa Mujica-Fernaud, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR TREATING INFECTIOUS DISEASES
Publication number: 20120264678Abstract: Disclosed are methods of treating infectious diseases comprising administering to an animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicant: NEREUS PHARMACEUTICALS, INC.Inventor: Michael Palladino -
Publication number: 20120264764Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: June 11, 2012Publication date: October 18, 2012Inventors: John S. Kovach, Francis Johnson
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20120264736Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Applicant: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8288390Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.Type: GrantFiled: March 9, 2010Date of Patent: October 16, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
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Patent number: 8278290Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.Type: GrantFiled: February 14, 2006Date of Patent: October 2, 2012Assignee: Biononics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20120245141Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,Type: ApplicationFiled: March 29, 2012Publication date: September 27, 2012Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
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Publication number: 20120245165Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.Type: ApplicationFiled: June 5, 2012Publication date: September 27, 2012Applicants: DAEWOONG PHARMACEUTICAL CO., LTD, MEDIFRON DBT CO., LTD.Inventors: Dong Wook KANG, Jee Woo LEE, Young Ho KIM, Hee KIM, Hee Jin HA, Eun Joo NAM, Chan Mi JOUNG
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Publication number: 20120245107Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Inventors: William Henry, Henk-Andre Kroon, Linda Summerton
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120237591Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.Type: ApplicationFiled: May 8, 2012Publication date: September 20, 2012Applicant: The University of British ColumbiaInventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20120238563Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: ApplicationFiled: June 4, 2012Publication date: September 20, 2012Inventors: Jose Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20120232096Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.Type: ApplicationFiled: May 24, 2012Publication date: September 13, 2012Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
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Publication number: 20120232095Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.Type: ApplicationFiled: May 24, 2012Publication date: September 13, 2012Inventors: Tetsuya TSUKAMOTO, Takeshi WAKABAYASHI, Taiichi OHRA