1,4-diazine As One Of The Cyclos Patents (Class 514/249)
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Patent number: 8822470Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, and X, are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: May 8, 2013Date of Patent: September 2, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 8822469Abstract: 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: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Somhairle MacCormick, Pierre-Henri Storck, Michael Paul Mortimore, Jean-Damien Charrier, Ronald Knegtel, Stephen Clinton Young, Joanne Pinder, Steven John Durrant
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Patent number: 8822449Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: GrantFiled: August 25, 2009Date of Patent: September 2, 2014Assignee: SanofiInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 8822431Abstract: The present invention relates to methods for treating optic disorders or for reducing or alleviating the signs, symptoms, or pathological conditions related to such optic disorders. In particular, methods are provided for treating optic disorders, or reducing the symptoms thereof, the methods involving the administration of one or more downstream folate compounds and/or methyl-B12. In one particular embodiment, the method comprises administration of L-methylfolate. In other embodiments, the method involves administering both L-methylfolate and methyl-B12. In still further embodiments, the method further involves reducing dietary intake of folic acid. In certain embodiments, the method further involves identifying a subject organism with a malfunction in one or more of the folate or B4 cycles. In certain embodiments, such a malfunction is one or more of the C677T and A1298C mutations.Type: GrantFiled: June 22, 2011Date of Patent: September 2, 2014Inventor: Brian W. Buell
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Publication number: 20140243281Abstract: Provided herein are pediatric dosage forms for use in the treatment of a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of the pediatric dosage form comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are said pediatric dosage form for use in the treatment of a pediatric liver disease, for use in decreasing the levels of serum bile acids or hepatic bile acids, for use in the treatment of pruritis, for use in reducing liver enzymes or bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: August 28, 2014Applicant: Lumena Pharmaceuticals, Inc.Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
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Publication number: 20140243344Abstract: Provided is a method for treating ALS in a subject, comprising administering to the subject a therapeutically effective amount of riluzole and a therapeutically effective amount of CK-2017357. Also provided are methods of reducing the variability of riluzole exposure (e.g., Cmax and/or AUC24h) in a subject, methods of reducing the variability of riluzole exposure (e.g., Cmax and/or AUC24h) between two or more subjects, methods of decreasing the total daily dose of riluzole in a subject, methods of increasing the half-life of riluzole in a subject, methods for decreasing the frequency of riluzole dosing in the subject, and methods for reducing the incidence and/or severity of adverse events in a subject treated with riluzole.Type: ApplicationFiled: July 12, 2012Publication date: August 28, 2014Inventors: Jesse Cedarbaum, John Mao, Fady Malik, Andrew A. Wolff
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Publication number: 20140242135Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. 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: April 25, 2012Publication date: August 28, 2014Applicant: Vanderbilt UniversityInventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
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Publication number: 20140243345Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.Type: ApplicationFiled: January 31, 2014Publication date: August 28, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20140243346Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.Type: ApplicationFiled: April 30, 2014Publication date: August 28, 2014Applicant: NOVARTIS AGInventors: Steven John CHARLTON, Catherine LEBLANC, Stephen Carl McKEOWN
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Publication number: 20140243263Abstract: Disclosed are compositions and methods for increasing diabetes resolution in a diabetic patient having undergone gastric restrictive surgery, entailing use of active agent that produces an incretin-like effect in the patient.Type: ApplicationFiled: April 2, 2014Publication date: August 28, 2014Inventor: Michael Rothkopf
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Publication number: 20140242148Abstract: The invention provides methods and materials for decontamination of surfaces and fabrics, such as non-woven fabrics, that are contaminated with infestations of microorganisms such as bacteria. Biocidal oligomers having conjugated oligo-(aryl/heteroaryl ethynyl) structures and comprising at least one cationic group can be used to decontaminate infested surfaces in the presence of oxygen and, optionally, illumination. Fibers incorporating biocidal oligomers having conjugated oligo-(aryl/heteroaryl ethynyl) structures and comprising at least one cationic group, wherein the oligomer is physically associated with or covalently bonded to, or both, the fiber-forming polymer can be used to form non-woven mats. Biocidal non-woven mats prepared by methods of the invention, incorporating the biocidal oligomers, can be used to suppress bacterial growth in wound and surgical dressings and personal hygiene products.Type: ApplicationFiled: August 3, 2012Publication date: August 28, 2014Applicant: University of Florida Research Foundation, Inc.Inventors: David G. Whitten, Kirk S. Schanze, Eunkyung Ji, Dimitri Dascier, Anand Parthasarathy, Thomas S. Corbitt, Kirsten Cicotte, Elizabeth LeBleu Dirk, Xuzhi Zhu
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Publication number: 20140243347Abstract: The present invention relates to 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 compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: October 4, 2012Publication date: August 28, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Elena Casale, Marisa Montemartini, Claudia Piutti
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Publication number: 20140243302Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.Type: ApplicationFiled: June 26, 2012Publication date: August 28, 2014Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
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Publication number: 20140243273Abstract: The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I.Type: ApplicationFiled: May 7, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Irina Nikolaevna Kadiyala, Shahla Jamzad, Thomas Carl Hoock, Lori Kell Taylor, Kathryn Lea Sewell
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Patent number: 8815861Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: July 20, 2012Date of Patent: August 26, 2014Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Patent number: 8815859Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: GrantFiled: March 31, 2009Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
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Patent number: 8815860Abstract: The present disclosure is generally related to methods of preventing oxidative stress injury induced by renal ischemia-reperfusion by a Folate-TEMPOL conjugate.Type: GrantFiled: September 21, 2010Date of Patent: August 26, 2014Assignees: Emory University, Georgia Tech Research CorporationInventors: W. Robert Taylor, Sarah F. Knight, Niren Murthy, Kousik Kundu
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Patent number: 8815862Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.Type: GrantFiled: December 3, 2012Date of Patent: August 26, 2014Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
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Publication number: 20140235569Abstract: Described herein is a method for increasing levels of S-adenosylmethionine within the human body without administering S-adenosylmethionine directly. The method of the invention may be achieved by administering one or more of L-methionine, methylcobalamin, 5-Methyl tetrahydrofolate, betaine, and malic acid, together with at least one compound selected from the group consisting of folic acid, vitamin B12, magnesium, calcium, and other cofactors.Type: ApplicationFiled: February 4, 2014Publication date: August 21, 2014Applicant: Fast Balance, Inc.Inventor: Brian D. Halevie-Goldman
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Publication number: 20140235620Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
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Publication number: 20140235582Abstract: Compounds of Formula (I) wherein B is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; Y is a linker moiety selected from the group consisting of a direct bond. R, R1, R2, and R3 are each individually selected from the group consisting substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or heterocycle.Type: ApplicationFiled: August 27, 2012Publication date: August 21, 2014Applicants: Sanford-Burnham Medical Research Institute, Southern Research InstituteInventors: Marintha L. Heil, Nicholas D.P. Cosford, Nicholas Pagano, Peter Teriete
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Publication number: 20140234389Abstract: Biocompatible intraocular implants may include a brimonidine free base and a biodegradable polymer associated with the brimonidine free base to facilitate the release of the brimonidine free base into an eye with the polymer matrix lasts a period of time of not more than twice the drug release duration, but more than the drug release duration.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Allergan, Inc.Inventors: Jane-Guo Shiah, Chetan Pujara
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Publication number: 20140235615Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 24, 2014Publication date: August 21, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
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Publication number: 20140234428Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.Type: ApplicationFiled: February 15, 2013Publication date: August 21, 2014Applicant: Cymbiotics, Inc.Inventors: Raj R. Barathur, Jack Bain Bookout
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Publication number: 20140235638Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: March 31, 2014Publication date: August 21, 2014Applicant: AbbVie Inc.Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
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Publication number: 20140235643Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of cancer and inflammatory diseases. In particular, the method comprises administration of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: October 4, 2012Publication date: August 21, 2014Inventors: Jerry B. Evarts, Kamal D. Puri, Roger G. Ulrich, Edward A. Kesicki, Thomas Judge
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Publication number: 20140234420Abstract: The present invention describes methods and compositions for treating diverse dermatological conditions, including acne and psoriasis, using zein containing nanocarrier devices for topical delivery of methotrexate, retinoic acid and benzoyl peroxide to select targets in the skin.Type: ApplicationFiled: August 14, 2013Publication date: August 21, 2014Inventors: Omathanu P. Perumal, Ranjith Kumar Averineni
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Publication number: 20140235604Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.Type: ApplicationFiled: May 7, 2014Publication date: August 21, 2014Inventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
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Publication number: 20140234440Abstract: The invention relates to the use of encapsulates of cancer cells, in agarose coated, agarose containing beads, for isolating chemotherapeutic resistant cells which have at least one stem cell property, such as expression of OCT4.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicant: THE ROGOSIN INSTITUTE, INC.Inventors: Lawrence GAZDA, Barry SMITH
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Publication number: 20140234390Abstract: Biocompatible intraocular implants may include a brimonidine free base and a biodegradable polymer associated with the brimonidine free base to facilitate the release of the brimonidine free base into an eye with the polymer matrix lasts a period of time of not more than twice the drug release duration, but more than the drug release duration.Type: ApplicationFiled: March 18, 2014Publication date: August 21, 2014Applicant: ALLERGAN, INC.Inventors: Jane-Guo Shiah, Chetan Pujara
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Patent number: 8809332Abstract: Besylate salts 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.Type: GrantFiled: June 26, 2013Date of Patent: August 19, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8808742Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.Type: GrantFiled: April 14, 2009Date of Patent: August 19, 2014Assignee: Ardea Biosciences, Inc.Inventors: Barry D. Quart, Colin Edward Rowlings
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Patent number: 8809333Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: GrantFiled: March 27, 2012Date of Patent: August 19, 2014Assignee: Pfizer Inc.Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140228371Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.Type: ApplicationFiled: January 29, 2014Publication date: August 14, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
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Publication number: 20140228372Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, G1, G2, G3, Y1, Y2, n, and p are as defined in the claims. The invention also relates to methods of using the compounds of formula (I) to control or prevent infestation of plants, propagation material thereof, harvested crops or non-living materials by phytopathogenic spoilage microorganisms or organisms potentially harmful to man.Type: ApplicationFiled: September 14, 2012Publication date: August 14, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140228352Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 24, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
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Publication number: 20140228357Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.Type: ApplicationFiled: September 27, 2012Publication date: August 14, 2014Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
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Publication number: 20140228347Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: IRM LLCInventors: Valentina MOLTENI, Hank Michael James PETRASSI, Xiaolin LI, Xiaodong LIU, Jon LOREN, Juliet NABAKKA, Bao NGUYEN, Vince YEH
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Publication number: 20140227284Abstract: Described herein are compounds, compositions and methods for treatment of cancer. Also described are methods and uses for identifying subject with cancer that are suitable for treatment with the compounds, composition and methods are described herein. In one aspect of the present invention, there is provided a method of treating a subject having a cancer deficient in NMT2, comprising: administering to said subject an NMT inhibitor.Type: ApplicationFiled: July 23, 2012Publication date: August 14, 2014Applicant: PACYLEX PHARMACEUTICALS INC.Inventors: Luc G. Berthiaume, Erwan Beauchamp, Conganige Maneka Anne Perinpanayagam, Chuiyee Yap
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Publication number: 20140228361Abstract: The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: November 14, 2012Publication date: August 14, 2014Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Jiancun Zhang, Yingjun Zhang, Weihong Zhang, Bing Liu, Jiquan Zhang, Jinlei Liu, Lu Zhang
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Publication number: 20140227297Abstract: Provided herein is technology relating to theranostic agents and particularly, but not exclusively, to compositions comprising cell-specific theranostic agents and associated methods and systems for using the cell-specific theranostic agents to treat subjects.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Sascha N. Goonewardena, Bertram Pitt, Hong Zong
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Publication number: 20140227260Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Auspex Pharmaceuticals, Inc.Inventor: Chengzhi Zhang
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Patent number: 8802657Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: October 22, 2012Date of Patent: August 12, 2014Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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Patent number: 8802675Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.Type: GrantFiled: January 31, 2010Date of Patent: August 12, 2014Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
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Publication number: 20140221335Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: January 28, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS
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Publication number: 20140221310Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates 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: January 31, 2014Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
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Publication number: 20140221348Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: ApplicationFiled: March 17, 2014Publication date: August 7, 2014Applicant: Basilea Pharmaceutica AGInventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Publication number: 20140221336Abstract: 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 5, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Publication number: 20140221311Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales