1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Publication number: 20140294733Abstract: The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.Type: ApplicationFiled: November 20, 2012Publication date: October 2, 2014Inventors: James R. Baker, JR., Baohua M. Huang, Thommey P. Thomas
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Publication number: 20140296066Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: October 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
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Publication number: 20140296176Abstract: The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.Type: ApplicationFiled: August 17, 2012Publication date: October 2, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Julie Friedland
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Patent number: 8846672Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: September 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Patent number: 8846667Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.Type: GrantFiled: September 13, 2012Date of Patent: September 30, 2014Assignee: The General Hospital CorporationInventors: Vineet Gupta, M. Amin Arnaout
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140288053Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: September 25, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
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Publication number: 20140286902Abstract: A pharmaceutical combination comprising a platinum-containing anticancer agent, and an Hsp90 inhibitor according to the following formulae (I) & (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. Also provided is a method of treating a proliferative disorder such as cancer in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 1, 2012Publication date: September 25, 2014Inventor: David Proia
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Publication number: 20140288082Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20140288347Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: December 13, 2013Publication date: September 25, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Joanne Pinder, Ronald Marcellus Alphonsus Knegtel, Steven John Durrant, Damien Fraysse, Somhairle MacCormick, Anisa Nizarali Virani, Philip Michael Reaper
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Publication number: 20140286928Abstract: The present invention provides a method of protecting the heart from damage, by administering to a patient at risk of such damage, a pharmaceutically effective amount of a composition which inhibits the interaction of RSK3 and mAKAP?, or the expression or activity of one or both of those molecules. This composition may be in the form of a peptide that specifically inhibits mAKAP? binding to RSK3 or in the form of an siRNA construct which inhibits the expression of RSK3.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: ANCHORED RSK3 INHIBITORS, LLCInventors: Michael S. KAPILOFF, Jinliang LI, Michael KRITZER, Catherine PASSARIELLO, Kimberly DODGE-KAFKA
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Publication number: 20140288081Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
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Publication number: 20140288083Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Applicant: SANOFIInventors: Marc Nazare, Nis Halland, Friedemann Schmidt, Tilo Weiss, Uwe Dietz, Armin Hofmeister, Jean-Christophe Carry
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Publication number: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Publication number: 20140288059Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.Type: ApplicationFiled: April 25, 2014Publication date: September 25, 2014Applicant: THE PENN STATE RESEARCH FOUNDATIONInventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
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Patent number: 8841299Abstract: There are provided compounds of the formula wherein R1 and R2 are as described herein. The compounds are useful as anticancer agents.Type: GrantFiled: June 19, 2013Date of Patent: September 23, 2014Assignee: Genentech, Inc.Inventors: Johannes Hermann, Ann Catherine Petersen, Jutta Wanner, Lin Yi
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Patent number: 8841297Abstract: This invention provides the compound 5,8-Dimethyl-2-[2-(1-methyl-4-phenyl-1H-imidazol-2-yl)-ethyl]-[1,2,4]thazolo[1,5-a]pyrazine and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 17, 2010Date of Patent: September 23, 2014Assignee: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohammed M. Farah
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Patent number: 8841298Abstract: Substituted pyrazines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyrazines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyrazine compound of the formula I to act on plants, their seed and/or their habitat.Type: GrantFiled: May 31, 2010Date of Patent: September 23, 2014Assignee: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Anna Aleksandra Michrowska, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Bernd Sievernich, Anja Simon, Ricarda Niggeweg
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Patent number: 8841289Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: October 11, 2010Date of Patent: September 23, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
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Publication number: 20140275065Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
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Publication number: 20140275020Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
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Publication number: 20140275093Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: October 16, 2013Publication date: September 18, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Publication number: 20140275095Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Curt A. Dvorak, Brock T. Shireman
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Publication number: 20140275061Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Publication number: 20140271842Abstract: The present invention relates to oral sustained release formulations of tofacitinib and pharmaceutical acceptable salts thereof. The formulations described herein have desirable pharmacokinetic characteristics.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Pfizer Inc.Inventors: Scott Max Herbig, Sriram Krishnaswami, Joseph Kushner, IV, Manisha Lamba, Thomas C Stock
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Publication number: 20140275097Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.Type: ApplicationFiled: October 3, 2012Publication date: September 18, 2014Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
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Publication number: 20140275024Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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: March 12, 2014Publication date: September 18, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
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Publication number: 20140275017Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20140271844Abstract: Compositions, dietary supplement compositions, and topical compositions including activated fatty acids and methods for using activated fatty acids to treat a variety of diseases.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventor: Raymond A. Miller
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Publication number: 20140275059Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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: March 12, 2014Publication date: September 18, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
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Publication number: 20140275094Abstract: There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis.Type: ApplicationFiled: December 17, 2013Publication date: September 18, 2014Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
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Publication number: 20140271858Abstract: Coated tablets of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The tablets minimize the perceived bitterness of the medicament. A method for analyzing instantaneous dissolution of sub-microgram quantities of core material is also disclosed.Type: ApplicationFiled: April 2, 2014Publication date: September 18, 2014Applicant: Sunovion Pharmaceuticals Inc.Inventors: Richard HSIA, Cai Gu HUANG, Konstantinos E. SARANTEAS, Tushar K. MISRA, Philip J. BONASIA, JR.
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Publication number: 20140271734Abstract: Provided herein are methods of treating or ameliorating Barrett's esophagus 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. Provided herein are methods of treating or ameliorating gastroesophageal reflux disease (GERD) by administering to an individual in need thereof a therapeutically effective amount of an ASBTI or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating symptoms or complications associated with Barrett's esophagus or GERD comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
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Publication number: 20140275096Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
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Publication number: 20140275090Abstract: Provided herein are methods of treating or ameliorating primary sclerosing cholangitis and inflammatory bowel 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 primary sclerosing cholangitis comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Lumena Pharmaceuticals, Inc.Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
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Publication number: 20140275070Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
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Publication number: 20140275021Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
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Publication number: 20140271595Abstract: The present invention concerns the use of a combination consisting of D-aspartic and L-aspartic acids or L-aspartic acid used alone to stimulate the procreative activity in the man by increment of spermatozoon number and motility.Type: ApplicationFiled: May 28, 2014Publication date: September 18, 2014Applicant: MERCK SERONO S.p.A.Inventors: SALVATORE D'ANIELLO, ENRICO D'ANIELLO
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Publication number: 20140256722Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: Janssen Pharmaceutica NVInventors: Frances Meredith HOCUTT, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20140256735Abstract: The invention generally relates to method for assessing a liver of a patient having a chronic hepatitis B virus infection. In certain aspects, methods of the invention involve obtaining a sample from a patient having a chronic hepatitis B virus infection. An assay is conducted on the sample to determine a level of at least one biomarker regulated by Suz12/Znf198. The liver of the patient is then assessed based on the level of the at least one biomarker. Other aspects of the invention generally relate to reducing or eliminating replication of a hepatitis B virus, and preventing a chronic hepatitis B infection in a patient from progressing to a liver cancer.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: PURDUE RESEARCH FOUNDATIONInventor: Ourania Andrisani
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Publication number: 20140256734Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.Type: ApplicationFiled: March 10, 2014Publication date: September 11, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
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Publication number: 20140256736Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Applicant: XENON PHARMACEUTICALS INC.Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
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Publication number: 20140256706Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
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Publication number: 20140255348Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 1, 2012Publication date: September 11, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: David Proia
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Publication number: 20140249152Abstract: The present invention discloses that diabetic rats showed a reduction in nitrergic relaxation of the gastric, impaired nNOS dimerization, decreased BH4 and GTPCH1 levels and thus, are more susceptible to develop diabetic gastroparesis. The use of tetrahydrobiopterin and its derivatives and sex steroid hormones as disclosed herein provides a novel strategy for therapeutic intervention of diabetic gastroparesis and any other gut-related diseases. Additionally, the present invention also discloses methods to determine risk of developing gastroparesis in an individual that are drawn to detecting variations in the activity and levels of GCH gene and in gene encoding sex steroid hormone receptor.Type: ApplicationFiled: March 6, 2014Publication date: September 4, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Pankaj J. Pasricha, Pandu R.R. Gangula
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Publication number: 20140249154Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.Type: ApplicationFiled: October 4, 2012Publication date: September 4, 2014Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
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Publication number: 20140248345Abstract: This invention relates to a bilayer pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and atorvastatin, or a pharmaceutically acceptable salt thereof, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.Type: ApplicationFiled: October 20, 2012Publication date: September 4, 2014Inventors: Sutthilug Sotthivirat, Edward J. Fagan, Katherine H. Chin, Abraham B. Woldu, Charles DeLuca, Decheng Ma, Walter R. Wasylaschuk, Bhagwant Rege
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Publication number: 20140249146Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: October 4, 2012Publication date: September 4, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
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Publication number: 20140249153Abstract: The present invention is directed to compositions comprising combinations of brimonidine and bimatoprost useful for lowering intraocular pressure in a patient and for the treatment of glaucoma.Type: ApplicationFiled: July 20, 2012Publication date: September 4, 2014Applicant: Allergan, Inc.Inventors: Richard S. Graham, Chetan P. Pujara, Sesha Neervannan, Anuradha V. Gore, Kevin S. Warner
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai