The Other Cyclo In The Bicyclo Ring System Is A Pyrrole Ring (including Hydrogenated) (e.g., Pyrrolo[3,2-d]pyrimidine, Etc.) Patents (Class 514/265.1)
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Publication number: 20130071495Abstract: The present invention relates to an inhibitor of glycogen synthase kinase 3 (GSK-3) for use in a method of treating or preventing emphysema, a method of activating an emphysema cell, an activated emphysema cell obtained by this method for use in a method of treating or preventing emphysema, and a method of screening for a substance for treating or preventing emphysema.Type: ApplicationFiled: March 16, 2011Publication date: March 21, 2013Applicant: Helmholtz Zentrum Muenchen Deutsches Forschungszentrum fuer Gesundheit und Umwelt (GmbHInventors: Melanie Koenigshoff, Oliver Eickelberg
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Publication number: 20130072492Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2011Publication date: March 21, 2013Inventors: Subharekha Raghavan, John E. Stelmach, Cameron J. Smith, Hong Li, Alan Whitehead, Sherman T. Waddell, Yi-Heng Chen, Shouwu Miao, Olga A. Ornoski, Joie Garfunkle, Xibin Liao, Jiang Chang, Xiaoqing Han, Jian Guo, Jonathan A. Groeper, Linda L. Brockunier, Keith Rosauer, Emma R. Parmee
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20130059870Abstract: The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.Type: ApplicationFiled: November 1, 2012Publication date: March 7, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Patent number: 8389516Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: GrantFiled: June 7, 2011Date of Patent: March 5, 2013Assignee: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20130053407Abstract: Pyrrolopyrimidones compounds of the formula (I), salts thereof, and pharmaceutical compositions containing them are disclosed herein, as well as methods for their use in medicine, for instance as activators of AMPK.Type: ApplicationFiled: May 3, 2011Publication date: February 28, 2013Applicant: GlaxoSmithKline LLCInventors: Olivier Mirguet, Anne Marie Jeanne Bouillot
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Patent number: 8383636Abstract: The present invention relates to compounds of the general formula (I) which are inhibitors of 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5?-methylthioadenosine phosphorylase or 5?-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.Type: GrantFiled: September 7, 2007Date of Patent: February 26, 2013Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Keith Clinch, Gary Brian Evans, Richard Frohlich, Richard Hubert Furneaux, Peter Michael Kelly, Jennifer Mary Mason, Vern L. Schramm, Peter Charles Tyler, Shivall Ashwah Ashwin Gulab
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Patent number: 8377946Abstract: Disclosed herein are compounds of Formula (II) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: GrantFiled: June 21, 2012Date of Patent: February 19, 2013Assignee: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury
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Publication number: 20130040974Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 26, 2012Publication date: February 14, 2013Applicant: Auspex Pharmaceuticals, Inc.Inventor: Auspex Pharmaceuticals, Inc.
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Publication number: 20130040973Abstract: Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicants: INCYTE CORPORATION, NOVARTIS PHARMA AGInventors: Alessandro M. Vannucchi, Costanza Bogani, Niccolo Bartalucci
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Publication number: 20130040972Abstract: The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide.Type: ApplicationFiled: September 24, 2012Publication date: February 14, 2013Inventor: Paul W. Manley
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Patent number: 8372852Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: May 11, 2012Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Patent number: 8372854Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.Type: GrantFiled: December 10, 2010Date of Patent: February 12, 2013Assignee: Pfizer Inc.Inventors: Jin Xie, Michele Ann Promo, Eric Jon Jacobsen, Horng-Chih Huang, Todd M. Maddux
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Publication number: 20130035336Abstract: A combination of a CDK4/8 inhibitor and an mTOR inhibitor for the treatment of cancer.Type: ApplicationFiled: April 12, 2011Publication date: February 7, 2013Applicant: Novartis AGInventors: Maria Borland, Christopher Thomas Brain, Shivang Doshi, Sunkyu Kim, Jianguo Ma, Josh Murtie, Hong Zhang
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Publication number: 20130035325Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.Type: ApplicationFiled: November 16, 2010Publication date: February 7, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
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Publication number: 20130029993Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: January 27, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Heinz Stadtmueller
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Publication number: 20130029944Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: June 20, 2012Publication date: January 31, 2013Applicant: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130030237Abstract: Provided herein are pharmaceutical compositions and methods of treating cancer wherein the cytotoxic activity of an anticancer agent is potentiated by the combination of base excision repair (BER) pathway inhibitors.Type: ApplicationFiled: April 15, 2011Publication date: January 31, 2013Inventor: Charles Theuer
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Patent number: 8362245Abstract: Provided are processes for preparing intermediates of pemetrexed.Type: GrantFiled: June 30, 2011Date of Patent: January 29, 2013Assignee: Sicor Inc.Inventors: Nicola Diulgheroff, Moran Pirkes, Alessandro Pontiroli, Marco Zrinski Villa
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Publication number: 20130023494Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 5, 2011Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130012527Abstract: The preQ1 riboswitch is a target for antibiotics and other small molecule therapies. The preQ1 riboswitch and portions thereof can be used to regulate the expression or function of RNA molecules and other elements and molecules. The preQ1 riboswitch and portions thereof can be used in a variety of other methods to, for example, identify or detect compounds. Compounds can be used to stimulate, active, inhibit and/or inactivate the preQ1 riboswitch. The preQ1 riboswitch and portions thereof, both alone and in combination with other nucleic acids, can be used in a variety of constructs and RNA molecules and can be encoded by nucleic acids.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: YALE UNIVERSITYInventors: Ronald R. Breaker, Jeffrey E. Barrick, Adam Roth, Wade Winkler
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Patent number: 8349848Abstract: The present invention provides compounds of the following formula and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: November 6, 2008Date of Patent: January 8, 2013Assignee: Dogwoof Pharmaceuticals, Inc.Inventors: Guoquan Wang, Robert D. Thompson
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Patent number: 8349843Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 6, 2011Date of Patent: January 8, 2013Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Andrea Hager-Wernet, legal representative, Liliane Unger, Manfred Raschack
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Publication number: 20130004481Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.Type: ApplicationFiled: January 5, 2012Publication date: January 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
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Publication number: 20130005748Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20120329819Abstract: The present invention relates to a new polymorphic or crystalline form of Pemetrexed Disodium, processes for its preparation and its use, in particular for the preparation of medicaments.Type: ApplicationFiled: November 24, 2010Publication date: December 27, 2012Applicants: UNIVERSITY OF ZURICH, AZAD PHARMACEUTICAL INGREDIENTS AGInventors: Uwe Jens Albrecht, Hannes Helmboldt, Vsevold Valerievich Nikolaev
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Publication number: 20120329818Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.Type: ApplicationFiled: June 1, 2012Publication date: December 27, 2012Inventors: Hugh Alfred BURGOON, Nicole Cathleen GOODWIN, Bryce Alden HARRISON, Jason Patrick HEALY, Ying LIU, Ross MABON, Brett MARINELLI, David Brent RAWLINS, Dennis Stewart RICE, Norris Andrew WHITLOCK
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Publication number: 20120322782Abstract: The present invention relates to veterinary compositions in a form of an orally deliverable tablet, and more particularly to a controlled-release composition that provides sufficiently long duration to permit once daily administration.Type: ApplicationFiled: February 15, 2011Publication date: December 20, 2012Inventors: Sunil Thomas Kumar Narishetty, Jeffrey Ellis Price, Sreenath Repakula
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Publication number: 20120316186Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 23, 2012Publication date: December 13, 2012Inventors: Mark Ledeboer, David Messersmith, Francois Maltais, Huai Gao, Tiansheng Wang, Jingrong Cao, John Duffy, Gabriel Martinez-Botella, Cornelia Forster, Marion Wannamaker, Francesco Salituro, Albert Pierce, Luc Farmer, Valerie Marone
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Publication number: 20120316185Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: ApplicationFiled: January 31, 2011Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Publication number: 20120316136Abstract: The present patent application relates to treatment of a respiratory disorder using TRPA1 antagonists. Particularly, the present patent application relates to treatment of a respiratory disorder using a TRPA1 antagonist, wherein the TRPA1 antagonist is administered by inhalation route to a subject in need thereof.Type: ApplicationFiled: June 13, 2012Publication date: December 13, 2012Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Neelima KHAIRATKAR-JOSHI, Abhay KULKARNI, Indranil MUKHOPADHYAY, Vidya Ganapati KATTIGE, Vikram Mansingh BHOSALE, Dinesh Pradeep WALE, Abraham THOMAS, Sukeerthi KUMAR, Sachin Sundarlal CHAUDHARI
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Publication number: 20120316166Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: January 10, 2011Publication date: December 13, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
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Publication number: 20120309776Abstract: The present invention provides pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: January 24, 2011Publication date: December 6, 2012Inventors: Ashley Fenwick, Timothy Allen Johnson, Graham M. Kyne
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Patent number: 8324225Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.Type: GrantFiled: May 24, 2007Date of Patent: December 4, 2012Assignees: Novartis AG, Astex Therapeutics LimitedInventors: Christopher Thomas Brain, Moo Je Sung, Gebhard Thoma
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Publication number: 20120302567Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.Type: ApplicationFiled: January 28, 2011Publication date: November 29, 2012Applicants: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, HANMI PHARM. CO. LTD.Inventors: Seung Hyun Jung, Young Hee Jung, Wha Il Choi, Jung Beom Son, Eun Ju Jeon, In Ho Yang, Tae Hun Song, Mi Kyoung Lee, Myoung Sil Ko, Young Gil Ahn, Maeng Sup Kim, Young Jin Ham, Tae Bo Sim, Hwan Geun Choi, Jung Mi Han, Dong-sik Park, Hwan Kim
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Publication number: 20120301464Abstract: Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor.Type: ApplicationFiled: August 1, 2012Publication date: November 29, 2012Applicant: INCYTE CORPORATIONInventors: Paul A. Friedman, Jordan S. Fridman, Monica E. Luchi, William V. Williams
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Publication number: 20120294930Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.Type: ApplicationFiled: February 23, 2012Publication date: November 22, 2012Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Publication number: 20120294957Abstract: Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.Type: ApplicationFiled: July 27, 2012Publication date: November 22, 2012Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Yoel Kloog, Adi Zundelevich, Roni Haklai
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Publication number: 20120295911Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.Type: ApplicationFiled: May 29, 2012Publication date: November 22, 2012Inventors: James C. Mannion, Scott L. Dax, Duncan Euan MacIntyre, Francis John Golder, James Francis McLeod
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Publication number: 20120295925Abstract: This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier.Type: ApplicationFiled: September 1, 2010Publication date: November 22, 2012Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Roger D. Tung, Craig E. Masse
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Publication number: 20120295927Abstract: A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor.Type: ApplicationFiled: July 30, 2012Publication date: November 22, 2012Applicants: Wayne State University, Duquesne University Of The Holy GhostInventors: Aleem Gangjee, Larry Matherly
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Publication number: 20120295926Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: ApplicationFiled: July 26, 2012Publication date: November 22, 2012Inventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 8314112Abstract: Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: January 9, 2009Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
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Patent number: 8314234Abstract: The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions.Type: GrantFiled: September 20, 2007Date of Patent: November 20, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Peter J. Connolly, Stuart Emanuel, Ronghui Lin, Yanhua Lu, Steven A. Middleton
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Publication number: 20120289501Abstract: The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease.Type: ApplicationFiled: November 23, 2010Publication date: November 15, 2012Applicant: NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Andreas Floersheimer, Pascal Furet, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Andrea Vaupel
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Publication number: 20120277225Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Applicant: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
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Publication number: 20120276093Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.Type: ApplicationFiled: November 17, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Dario Ballinari, Antonella Ciavolella, Enrico Pesenti, Alessia Montagnoli
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Publication number: 20120277240Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei