Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
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Publication number: 20130184300Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: January 14, 2013Publication date: July 18, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents of the University of Texas System
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Patent number: 8486858Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: September 14, 2010Date of Patent: July 16, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8486989Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: GrantFiled: May 22, 2007Date of Patent: July 16, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie, Jr.
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Patent number: 8486943Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 14, 2009Date of Patent: July 16, 2013Assignee: Eli Lilly and CompanyInventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
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Patent number: 8486990Abstract: Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.Type: GrantFiled: April 14, 2009Date of Patent: July 16, 2013Assignee: Elixir Pharmaceuticals, Inc.Inventors: Andrew Napper, Peter DiStefano, Rory A. Curtis, Jeffrey Hixon, Thomas McDonagh, L. Julie Huber, Jonathan M. Solomon, Russell J. Thomas, Jean-Francois Pons
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Patent number: 8481456Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: November 17, 2010Date of Patent: July 9, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
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Publication number: 20130165453Abstract: The invention provides for the use of protein kinase activators or boosters of nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF) or other neurotrophic factors to treat stroke. Specifically, the present invention provides methods of treating stroke comprising the steps of identifying a subject having suffered a stroke and administering to said subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of stroke.Type: ApplicationFiled: July 19, 2012Publication date: June 27, 2013Inventors: Miao-Kun Sun, Daniel L. Alkon
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Publication number: 20130150398Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot
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Publication number: 20130143916Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.Type: ApplicationFiled: November 9, 2012Publication date: June 6, 2013Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: THE REGENTS OF THE UNIVERSITY OF CALIF, Gabriel Fenteany
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Patent number: 8450360Abstract: The present invention relates to a new process for preparing dithiine-tetracarboximides.Type: GrantFiled: April 14, 2011Date of Patent: May 28, 2013Assignee: Bayer CropScience AGInventors: Thomas Himmler, Winfried Etzel, Frank Volz
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Patent number: 8449914Abstract: A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, including a human, in such a manner that a prolonged residence of carvedilol is obtained in the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(?) carvedilol for obtaining the desired therapeutic effect.Type: GrantFiled: March 13, 2008Date of Patent: May 28, 2013Assignee: Egalet Ltd.Inventors: Christine Andersen, Gina Fischer, Daniel Bar-Shalom, Lillian Slot, Anne-Marie Lademann
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Patent number: 8445491Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: GrantFiled: May 27, 2009Date of Patent: May 21, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20130109674Abstract: The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and/or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.Type: ApplicationFiled: December 17, 2010Publication date: May 2, 2013Applicant: Achelios Therapeutics LLCInventors: Harry J. Leighton, Matthew J. Buderer, Crist J. Frangakis
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Publication number: 20130109686Abstract: The present invention is directed to isoindolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: June 27, 2011Publication date: May 2, 2013Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
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Patent number: 8426611Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.Type: GrantFiled: January 27, 2011Date of Patent: April 23, 2013Assignee: Theron Pharmaceuticals Inc.Inventors: Jürg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Publication number: 20130095176Abstract: A controlled release delivery composition comprising: a housing adapted for oral administration; and a plurality of discrete vehicles assembled within the housing, each of the vehicles are not compressed together, each of the vehicles being a bead, a pellet, a tablet, and/or granules compressed into a preselect shape, wherein each of the vehicles comprise a different combination and/or amount of an active agent, an amino acid, a buffer, and a polymer, such that each of the vehicles comprises a different active agent and/or release property from each other, wherein each of the vehicles releases the active agent independently of each other, and wherein each of the vehicles remains independent from each other and intact within the housing prior to oral administration of the delivery composition.Type: ApplicationFiled: September 25, 2012Publication date: April 18, 2013Applicant: Intellipharmaceutics Corp.Inventor: Intellipharmaceutics Corp.
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Patent number: 8420690Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: February 7, 2008Date of Patent: April 16, 2013Assignee: GlaxoSmithKline LLCInventors: Mark Andrew Seefeld, Meagan B. Rouse
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Patent number: 8420638Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.Type: GrantFiled: June 29, 2011Date of Patent: April 16, 2013Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrance W. Deyle
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Patent number: 8415484Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: GrantFiled: August 26, 2009Date of Patent: April 9, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
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Patent number: 8410130Abstract: The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.Type: GrantFiled: November 7, 2008Date of Patent: April 2, 2013Assignee: Academia SinicaInventors: Tsann-Long Su, Ting-Chao Chou
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Publication number: 20130078284Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Patent number: 8399503Abstract: The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.Type: GrantFiled: January 15, 2009Date of Patent: March 19, 2013Assignee: Gruenenthal GmbHInventors: Saskia Zemolka, Stefan Schunk, Ellen Bergrath, Babette-Yvonne Kögel, Werner Englberger, Klaus Linz, Hans Schick
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Patent number: 8399507Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: October 27, 2008Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gui-Bai Liang, Xibin Liao, Weiguo Liu, Paul E. Finke, Dooseop Kim, Lihu Yang, Songnian Lin
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Patent number: 8394819Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: GrantFiled: February 19, 2010Date of Patent: March 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
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Publication number: 20130059879Abstract: Small molecule inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) having the following formula: Formula (1) are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting PFK.FB3 enzymatic activity, methods of inhibiting glycolytic flux, and methods of treating tumors by administering an effective amount of a Formula I compound.Type: ApplicationFiled: February 22, 2011Publication date: March 7, 2013Applicants: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC., ADVANCED CANCER THERAPEUTICS, LLCInventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Patent number: 8389560Abstract: This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.Type: GrantFiled: September 15, 2009Date of Patent: March 5, 2013Assignee: TaiGen Biotechnology Co., Ltd.Inventors: Chen-Fu Liu, Kuang-Yuan Lee, Pei-Chin Cheng, Yo-Chin Liu, Pin Lo, Kuo-Feng Tseng, Chih-Ming Chen, Chi-Hsin Richard King, Chu-Chung Lin
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Publication number: 20130053425Abstract: A pharmaceutical composition contains a gap junction blocker, and a pharmaceutically acceptable carrier. In addition, a pharmaceutical composition contains a gap junction blocker, a pharmaceutically acceptable carrier, a preservative and a buffer. Also, a method of lowering intraocular pressure includes the step of administrating to a subject a pharmaceutical composition containing a gap junction blocker, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 30, 2011Publication date: February 28, 2013Inventors: Chi-Ho To, Chi-Wal Do, Choung-Sing Law, Yan-Yin Tse
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Publication number: 20130046275Abstract: A hydrophilic biocompatible sustained-release material is disclosed. The material comprises amounts of Pluronic F-127, PEG-400, HPMC and water, effective to produce a composition of sufficiently low viscosity at room temperature to be injectable into an internal body cavity via a tube inserted within a urinary catheter. At body temperature, the material exhibits a much higher viscosity and will stably adhere to the internal surface of a body cavity. As the material dissolves, a therapeutic agent incorporated therein is slowly released to the body cavity, while the material itself is excreted from the body.Type: ApplicationFiled: July 19, 2012Publication date: February 21, 2013Applicant: THERACOAT LTD.Inventors: Asher HOLZER, Dorit DANIEL, Michael MULLERAD, Jaime DE LA ZERDA, Uri SHPOLANSKY, Nadav MALCHI, Yosh DOLLBERG, Dor TAL, Yossi YAVIN, Marina KONORTY
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Publication number: 20130046005Abstract: Allergies and immune system disorders (e.g. autoimmune diseases) are treated by administration of an agent that blocks activation of the kainic acid receptor (KAR) in B cells. The agents include antagonists and weakly activating agonists.Type: ApplicationFiled: January 25, 2011Publication date: February 21, 2013Inventors: Jamie Lynn Sturgill, Daniel Harper Conrad
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Publication number: 20130045952Abstract: The present invention relates to ABA agonist compounds which increase plant stress resistance. The invention also relates to methods of using these compounds. The invention further relates to compositions and formulations comprising the ABA agonist compounds, and uses thereof.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: Van Andel Research InstituteInventors: Yong Xu, Xiaoyin Edward Zhou, Karsten Melcher, Huaqiang Eric Xu
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Patent number: 8377981Abstract: A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole2), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.Type: GrantFiled: November 13, 2008Date of Patent: February 19, 2013Assignee: The Scripps Research InstituteInventor: Dale Boger
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Publication number: 20130041007Abstract: This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same.Type: ApplicationFiled: February 4, 2011Publication date: February 14, 2013Inventor: Chris P. Miller
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Publication number: 20130040977Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: August 24, 2012Publication date: February 14, 2013Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20130040938Abstract: Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula: The composition is effective for treating cognitive disorders, and methods of treating such disorders using the composition are also disclosed.Type: ApplicationFiled: October 11, 2012Publication date: February 14, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Patent number: 8372876Abstract: A method for improving memory in healthy subjects is disclosed. This method makes use of melatonin receptor antagonists such as luzindole and/or K-185 to reverse the inhibitory effect of melatonin. This invention is particularly relevant among subjects that do not show signs of central nervous system disorders and wish to improve their cognitive performance, especially in tasks.Type: GrantFiled: March 6, 2008Date of Patent: February 12, 2013Assignee: The University of Houston SystemInventors: Gregory M. Cahill, Oliver Rawashdeh
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Patent number: 8362065Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: GrantFiled: November 9, 2011Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Patent number: 8362277Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.Type: GrantFiled: July 7, 2010Date of Patent: January 29, 2013Assignee: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20130023504Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.Type: ApplicationFiled: August 3, 2012Publication date: January 24, 2013Applicant: HUNTER-FLEMING LIMITEDInventor: ERNST WULFERT
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Patent number: 8357704Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: GrantFiled: June 10, 2010Date of Patent: January 22, 2013Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd, Alexander Kover
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Publication number: 20130004550Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D50) of 40 ?m or smaller, (C) a cellulose derivative, and (D) a saccharide or a nonionic water-soluble polymer followed by molding.Type: ApplicationFiled: August 22, 2012Publication date: January 3, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Taro Kanamaru, Shinichiro Tajiri, Sachiko Fukui, Kazuhiro Yoshida
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Publication number: 20130005763Abstract: It is intended to avoid dose dumping of a drug and improve the dissolution properties of a drug in the lower gastrointestinal tract, and thereby provide a sustained-release solid preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release solid preparation containing (A) a pharmacologically active drug, (B) carboxyvinyl polymer, (C) povidone, and (D) carmellose sodium, xanthan gum, or sodium carboxymethyl starch.Type: ApplicationFiled: August 22, 2012Publication date: January 3, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Taro Kanamaru, Shinichiro Tajiri
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Patent number: 8344018Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: GrantFiled: July 14, 2009Date of Patent: January 1, 2013Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20120329848Abstract: The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Tawfik Gharbaoui, Benjamin R. Johnson, Michelle Kasem, Thomas O. Schrader, Scott Stirn
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Publication number: 20120321613Abstract: The invention relates to at least one molecular target for healing or treating wounds and, in particular chronic, human wounds. The molecular target is nWASP or a protein 50% homolgous therewith and which retains the same activity as nWASP protein, such as WASP. Further, the invention concerns a novel therapeutic for treating said wounds and a novel gene therapy approach, involving said molecular target, for treating said wounds.Type: ApplicationFiled: February 16, 2011Publication date: December 20, 2012Applicant: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITEDInventors: Keith Harding, Wen Guo Jiang
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Patent number: 8334300Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 24, 2011Date of Patent: December 18, 2012Assignee: Bayer AktiengesellshaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Patent number: 8324184Abstract: Described herein are composites that inhibit or reduce adhesion between two or more tissues. Also described herein are methods of using the composites.Type: GrantFiled: May 13, 2004Date of Patent: December 4, 2012Assignee: University of Utah Research FoundationInventors: Glenn D. Prestwich, Kelly R. Kirker, Steven D. Gray, Janice Gray, legal representative, Xiao Zheng Shu, Hao Li, Yanchun Liu
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Publication number: 20120295946Abstract: The present invention provides compounds and methods of administering compounds to a subject that can reduce ?APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce ?APP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease ?APP production.Type: ApplicationFiled: July 26, 2012Publication date: November 22, 2012Inventors: Nigel H. Greig, Karen T.Y. Shaw, Qiang-Sheng Yu, Harold W. Holloway, Tada Utsuki, Timothy T. Soncrant, Donald K. Ingram, Arnold Brossi, Anthony Giordano, Gordon Powers, Diane M. Davidson, Michael Sturgess
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Publication number: 20120295947Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).Type: ApplicationFiled: January 27, 2011Publication date: November 22, 2012Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Khulman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta