Chalcogen Bonded Directly At 4-position Patents (Class 544/287)
  • Patent number: 9987281
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: June 5, 2018
    Assignee: IGNYTA, INC.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Patent number: 9776975
    Abstract: A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed. Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: October 3, 2017
    Assignee: University of Notre Dame du Lac
    Inventors: Mayland Chang, Shahriar Mobashery, Renee Bouley
  • Patent number: 9745318
    Abstract: Compounds of formula I and a process for manufacturing the compounds. A method of using the compounds for the detection of calcium ions and a method of detecting intracellular calcium are also described.
    Type: Grant
    Filed: November 27, 2014
    Date of Patent: August 29, 2017
    Assignee: PARIS SCIENCES ET LETTRES—QUARTIER LATIN
    Inventors: Jean-Maurice Mallet, Mayeul Collot
  • Patent number: 9718810
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: August 1, 2017
    Assignee: IGNYTA, INC.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Patent number: 9353097
    Abstract: This application relates to various salts and solid state forms of Compound (I). This application also relates to pharmaceutical compositions and therapeutic uses of these materials and compositions.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: May 31, 2016
    Assignee: Ignyta, Inc.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Patent number: 9169218
    Abstract: This invention is related to the alkyl-piperazine-phenyl 4 (3H)-quinazolinones general formula (I) compounds, pharmacologicaly active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: October 27, 2015
    Assignees: ACHE LABORATORIOS FARMACEUTICOS S.A., ACHE INTERNATIONAL (BVI) LTD.
    Inventors: Valter Freire Torres Russo, Elisa Mannochio De Souza Russo
  • Publication number: 20150148535
    Abstract: The present invention relates to a method for preparing nitrogen compounds using carbon dioxide, and to the use of the method in the production of vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers. The invention also relates to a method for producing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers, which includes a step of preparing nitrogen compounds using the method of the invention. The invention further relates to a method for preparing labelled nitrogen compounds using carbon dioxide and to the uses thereof.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Applicant: Commissariat A L'Energie Atomique Et Aux Energies Alternatives
    Inventors: Thibault Cantat, Christophe Gomes, Olivier Jacquet
  • Patent number: 9034887
    Abstract: A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: May 19, 2015
    Assignee: F2G Limited
    Inventors: Jason David Oliver, John Leslie Thain, Michael John Bromley, Graham Edward Morris Sibley, Michael Birch
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Patent number: 9006257
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 14, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 9000162
    Abstract: The present disclosure relates to compounds of Formula 1,5,8-difluoro-4-(2-(4-(heteroaryloxy)phenyl)ethylamino)quinazolines, and their use as agrochemicals and animal health products.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: William K. Brewster, Carla J. R. Klittich, Chenglin Yao, Yuanming Zhu, Brent J. Rieder
  • Publication number: 20150086627
    Abstract: Oral and parenteral dosage forms comprising halofuginone, including enteric-coated solid oral dosage forms, subcutaneous dosage forms and intravenous dosage forms, for administration to subjects in need thereof, e.g., subjects having been identified with musculoskeletal disorders, fibrotic diseases, malaria, or cancer are described herein.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 26, 2015
    Applicant: HALO THERAPEUTICS, LLC.
    Inventors: Ernest D. Bush, Diane Mcguire, Marc B. Blaustein
  • Publication number: 20150065710
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 5, 2015
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Alfredo Paio
  • Publication number: 20150057297
    Abstract: The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
    Type: Application
    Filed: January 11, 2013
    Publication date: February 26, 2015
    Applicants: President and Fellows of Harvard College, The General Hospital Corporation d/b/a Massachusetts General Hospital
    Inventors: Malcolm Whitman, Tracy Keller, Ralph Mazitschek
  • Patent number: 8962639
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: February 24, 2015
    Assignee: AbbVie Inc.
    Inventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
  • Patent number: 8957087
    Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: February 17, 2015
    Assignees: Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.
    Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
  • Publication number: 20150025071
    Abstract: Compounds of the formula I in which U, V and W have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Hans-Peter Buchstaller, Christina Esdar, Birgitta Leuthner
  • Patent number: 8937078
    Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: January 20, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, Jr., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 8927559
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, Jr., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Purakkattle Johny Biju, Li Dong, Xianhai Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi, Ashwin U. Rao
  • Publication number: 20150005327
    Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventor: Thomas Helleday
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140336199
    Abstract: This invention is related to the alkyl-piperazine-phenyl 4(3H)-quinazolinones compounds of general formula (I) below: which are pharmacologicaly active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors.
    Type: Application
    Filed: May 5, 2014
    Publication date: November 13, 2014
    Applicants: ACHE LABORATORIOS FARMACEUTICOS S.A., ATC Trustees Abbot Building, 2nd FLoor, Road Town, ACHE INTERNATIONAL (BVI) LTD.
    Inventors: Valter FREIRE TORRES RUSSO, Elisa Mannochio De Souza Russo
  • Publication number: 20140330016
    Abstract: Provided herein are processes for the preparation of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2014
    Publication date: November 6, 2014
    Applicant: CELGENE CORPORATION
    Inventors: Alexander L. RUCHELMAN, Benjamin M. COHEN, Anusuya CHOUDHURY, Matthew M. KREILEIN, William W. LEONG, Hon-Wah MAN
  • Patent number: 8865898
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Japan Science and Technology Agency
    Inventor: Yoshihito Ueno
  • Publication number: 20140296247
    Abstract: Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 2, 2014
    Inventors: Vladimir Kogan, Leonid Lurya, Lev Tabachnik
  • Publication number: 20140288101
    Abstract: The invention provides 3-deuterium-enriched 3-(6-, 7-, or 8-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Patent number: 8841289
    Abstract: 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: Grant
    Filed: October 11, 2010
    Date of Patent: September 23, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
  • Patent number: 8815878
    Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: August 26, 2014
    Assignee: NovaDrug, LLC
    Inventor: Eliezer Huberman
  • Publication number: 20140235634
    Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Application
    Filed: February 14, 2014
    Publication date: August 21, 2014
    Applicant: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
  • Patent number: 8809528
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Publication number: 20140228382
    Abstract: The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.
    Type: Application
    Filed: January 14, 2014
    Publication date: August 14, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Patent number: 8802685
    Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: August 12, 2014
    Assignee: Celgene Corporation
    Inventors: George Muller, Hon-Wah Man, Benjamin M. Cohen, Ying Li, Jean Xu, William W. Leong
  • Patent number: 8779131
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed. An exemplary compound disclosed in this application is shown below.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: July 15, 2014
    Assignee: Icos Corporation
    Inventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer Treiberg
  • Publication number: 20140194422
    Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
    Type: Application
    Filed: June 12, 2012
    Publication date: July 10, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
  • Publication number: 20140171455
    Abstract: Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 19, 2014
    Applicant: The Regents of the University of California
    Inventors: Heike Wulff, Lee-Way Jin, Izumi Meezawa
  • Publication number: 20140155378
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: June 5, 2014
    Applicant: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • Publication number: 20140155396
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: June 27, 2013
    Publication date: June 5, 2014
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • Patent number: 8735578
    Abstract: This invention is related to the alkyl-piperazine-phenyl 4 (3H)-quinazolinones general formula (I) compounds, pharmacologically active and able to act on the 5-HT1A and 5-HT2A serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: May 27, 2014
    Assignees: Aché Laboratórios Farmacêuticos S.A., Aché International (BVI) Ltd.
    Inventors: Valter Freire Torres Russo, Elisa Mannochio De Souza Russo
  • Publication number: 20140080835
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.
    Type: Application
    Filed: November 12, 2013
    Publication date: March 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Jerome Emile Jorges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Patent number: 8664388
    Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Niklas Heine, Christian Eickmeier, Sandra Handschuh, Cornelia Dorner-Ciossek, Stefan Hoerer
  • Publication number: 20140046061
    Abstract: Chiral salts comprising anionic cyclodextrin derivatives with particular types of non-metal cations are provided. The anionic CD derivative salts can serve as ionic liquids and can possess substantial advantages over currently commercially available ionic liquids particularly for use as chiral phase transfer catalyst, chiral reaction medium, chiral extraction medium, and/or as chiral additive to a chemical process. Methods of preparing the same are provided.
    Type: Application
    Filed: June 28, 2013
    Publication date: February 13, 2014
    Inventor: Jose R. MATOS
  • Publication number: 20140011810
    Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
    Type: Application
    Filed: September 11, 2013
    Publication date: January 9, 2014
    Applicant: Gatekeeper Pharmaceuticals, Inc.
    Inventors: Nathanael S. Gray, Wenjun Zhou
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Patent number: 8614319
    Abstract: Novel heterocyclic compounds having the Formula I: wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: December 24, 2013
    Assignee: ATIR Holding S.A.
    Inventors: Dmitry Tworowski, Ron Matsievitch, Vladimir Kogan
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8609674
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein G1, R2, R1a, R1b, X, X1, X2, X3, Rx, J, k, n, q, and t are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: December 17, 2013
    Assignee: AbbVie Inc.
    Inventors: Arturo Perez-Medrano, Sridhar Peddi, David DeGoey
  • Patent number: 8609667
    Abstract: Disclosed is a kind of E-type phenyl acrylic ester compound containing substituted anilino pyrimidine group, which is shown by general structure formula I, wherein each substituent is defined as that in the description. The compounds of general formula I show high insecticidal and acaricidal activities to adults and nymphs of harmful insects and mites in agricultural, civil and zoic technical fields, especially to Tetranychus cinnabarinus, Tetranychidae, and the like. The said compounds show more excellent performance on inhibiting the incubation of eggs of harmful mites. The uses of the said compounds as insecticides and/or acaricides in agricultural and other fields also are disclosed.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: December 17, 2013
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Huichao Li, Hong Zhang, Baoshan Chai, Yanmei Luo, Xiaomin He, Guang Huang, Shaowu Liu, Baoxiang Sun
  • Patent number: RE44638
    Abstract: The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3K? activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancers, lymphomas, multiple myelomas and leukemia. The compounds are also useful in disrupting or inhibiting cellular processes such as leukocyte function or accumulation, neutrophils function, lymphocyte proliferation, and endogenous immune responses.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: December 10, 2013
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri