Polycyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/257)
  • Patent number: 11498930
    Abstract: Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.
    Type: Grant
    Filed: February 3, 2019
    Date of Patent: November 15, 2022
    Assignee: BLUERAY THERAPEUTICS (SHANGHAI) CO., LTD
    Inventors: Bin Zou, Xianlei Fu, Rui Zhang, Shichao Ma, Shuaijie Xu, Wencheng Fu, Lanzhen Liu
  • Patent number: 11452692
    Abstract: Provided herein is an oral pharmaceutical composition, comprising a plurality of xanomeline beads having a core comprising xanomeline or a salt thereof; and a plurality of trospium beads having a core comprising a salt of trospium.
    Type: Grant
    Filed: February 3, 2022
    Date of Patent: September 27, 2022
    Assignee: Karuna Therapeutics, Inc.
    Inventors: Aimesther Betancourt, Bruce Rehlaender, Roch Thibert
  • Patent number: 11446303
    Abstract: Methods of treating a subject for a liver condition, e.g., NAFLD, NASH, and/or DILI, are provided. Aspects of the methods include administering to the subject an effective amount of a UPase inhibitor, optionally in combination with a uridine active agent (e.g., uridine (UR), a UR pro-drug or a UR mimetic), such as supplemental uridine, to treat the subject for the liver condition. Also provided are compositions for use in practicing the subject methods.
    Type: Grant
    Filed: June 17, 2020
    Date of Patent: September 20, 2022
    Assignee: Tosk, Inc.
    Inventors: William A. Garland, Heshan Peiris, Philip Liaw, Brian D. Frenzel
  • Patent number: 11155552
    Abstract: The present invention provides RUT analogs with various biological activities. In particular, the biological activities comprise anti-inflammatory activity, vasodilator effects, migration/invasion-suppressive activities, ability against damage due to remodeling between the epithelium and endothelium, collagen deposition and cardiac fibrosis suppress, Snail protein inhibitory effect, etc., which may improve cardiac, vasodilation, and lung functions. The RUT analogs disclosed herein also exhibit a lower cytotoxicity comparing to RUT.
    Type: Grant
    Filed: September 25, 2019
    Date of Patent: October 26, 2021
    Assignees: TAIPEI MEDICAL UNIVERSITY, NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGY
    Inventors: Chun-Mao Lin, Chi-Ming Lee, Chi Wang, Sheng-Tung Huang, Jiun-An Gu, Tin-An Rau
  • Patent number: 11124514
    Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: September 21, 2021
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Sharon Mates, Robert Davis, Kimberly Vanover, Lawrence Wennogle
  • Patent number: 11103511
    Abstract: The present invention provides an application of N-benzyl tryptanthrin derivative as tryptophan dioxygenase (TDO) inhibitor, and more specifically an application of N-benzyl tryptanthrin derivative or a pharmaceutically acceptable salt thereof. Said derivative has a structural general formula as represented by formula 1, wherein each group is defined as in the specification. The derivative of the present invention has a good TDO inhibiting activity and can be used to prepare a treatment for diseases associated with TDO activity and expression.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: August 31, 2021
    Assignee: FUDAN UNIVERSITY
    Inventor: Qing Yang
  • Patent number: 10544162
    Abstract: The present disclosure provides crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, pharmaceutical compositions comprising crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, and methods of treating cancer and other diseases in a patient with crystalline polymorphic forms of TG02 free base and TG02 acid addition salts.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: January 28, 2020
    Assignee: ADASTRA PHARMACEUTICALS, INC.
    Inventors: Robert K. Mansfield, Tracy Parrott
  • Patent number: 10266543
    Abstract: This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: April 23, 2019
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jean-François Bonfanti, Jérôme Michel Claude Fortin, Philippe Muller, Frédéric Marc Maurice Doublet, Pierre Jean-Marie Bernard Raboisson, Eric Pierre Alexandre Arnoult
  • Patent number: 10183023
    Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: January 22, 2019
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventor: Lawrence Wennogle
  • Patent number: 9963464
    Abstract: The present invention relates to novel macrocyclic compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: May 8, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Pierre Wasnaire, Arne Scholz, Philip Lienau, Gerhard Siemeister, Christian Stegmann, Ulf Bömer, Kunzeng Zheng, Ping Gao, Gang Chen, Jiajun Xi
  • Patent number: 9801882
    Abstract: The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Grant
    Filed: February 17, 2014
    Date of Patent: October 31, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Lawrence P. Wennogle, Robert Davis
  • Patent number: 9675015
    Abstract: A stevia cultivar, designated ‘807086’, is disclosed. The invention relates to the plant parts of stevia cultivar ‘807086’, to the plants of stevia ‘807086’ and to methods for producing a stevia plant produced by crossing the cultivar ‘807086’ with itself or another stevia variety, including methods using marker assisted breeding. The invention further relates to hybrid stevia seeds and plants produced by crossing the cultivar ‘807086’ with another stevia cultivar.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: June 13, 2017
    Assignee: PureCircle USA Inc.
    Inventors: Shan Wang Li, Yu Cheng Bu, Avetik Markosyan
  • Patent number: 9668450
    Abstract: A stevia cultivar, designated ‘817096’, is disclosed. The invention relates to the plant parts of stevia cultivar ‘817096’, to the plants of stevia ‘817096’ and to methods for producing a stevia plant produced by crossing the cultivar ‘817096’ with itself or another stevia variety, including methods using marker assisted breeding. The invention further relates to hybrid stevia seeds and plants produced by crossing the cultivar ‘817096’ with another stevia cultivar.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: June 6, 2017
    Assignee: PureCircle USA Inc.
    Inventors: Shan Wang Li, Yu Cheng Bu, Avetik Markosyan
  • Patent number: 9668451
    Abstract: A stevia cultivar, designated ‘814011’, is disclosed. The invention relates to the plant parts of stevia cultivar ‘814011’, to the plants of stevia ‘814011’ and to methods for producing a stevia plant produced by crossing the cultivar ‘814011’ with itself or another stevia variety, including methods using marker assisted breeding. The invention further relates to hybrid stevia seeds and plants produced by crossing the cultivar ‘814011’ with another stevia cultivar.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: June 6, 2017
    Assignee: PureCircle USA Inc.
    Inventors: Shan Wang Li, Yu Cheng Bu, Avetik Markosyan
  • Patent number: 9630971
    Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: April 25, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Takashi Abe, Graham Buckton, Robert Davis, Mark Hooper, Peng Li, Hideaki Maruyama, Masahiro Takasuga, Lawrence P. Wennogle, Yuhei Yamamoto, Hironori Yamashita
  • Patent number: 9598426
    Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production and their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: March 21, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence Wennogle
  • Patent number: 9468637
    Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: October 18, 2016
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Allen A. Fienberg, Lawrence P. Wennogle, Sharon Mates
  • Patent number: 9439906
    Abstract: The present invention provides a method of treating patients in need of treatment with long acting injectable paliperidone palmitate formulations.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: September 13, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: An Vermeulen, Alfons Wouters
  • Patent number: 9173869
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: November 3, 2015
    Assignee: CURIS, INC.
    Inventors: Oivin M. Guicherit, Lee Rubin
  • Patent number: 9133214
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumors and cancers as well as other conditions or disorders associated with kinases.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: September 15, 2015
    Assignee: S*BIO Pte Ltd
    Inventors: Stéphanie Blanchard, Kantharaj Ethirajulu, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Ee Ling Teo, Anthony Deodaunia William
  • Patent number: 9120815
    Abstract: Provided herein are salt forms of macrocyclic protein kinase inhibitors, pharmaceutical compositions containing the same, methods of making and using these compounds and compositions to treat proliferative disease mediated by kinase activity.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: September 1, 2015
    Assignee: Tragara Pharmaceuticals, Inc.
    Inventors: Robert K. Mansfield, Tracy Lawhon, Brian Dymock
  • Patent number: 9115143
    Abstract: The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R1, R2, R3, A1, A2, A3, Y and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: August 25, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Garrett Berlond Minne, François Paul Bischoff, Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot
  • Patent number: 9096609
    Abstract: The present invention relates to novel macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: August 4, 2015
    Assignees: Ipsen Pharma S.A.S., Oncodesign S.A.
    Inventors: Jan Hoflack, Petra Blom
  • Patent number: 9061032
    Abstract: Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: June 23, 2015
    Assignee: The Penn State Research Foundation
    Inventors: Wafik S. El-Deiry, Joshua E. Allen, Gen Sheng Wu
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Patent number: 8999984
    Abstract: Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: April 7, 2015
    Assignee: University of Louisville Research Foundation, Inc.
    Inventors: Robert A. Mitchell, John O. Trent, Jason B. Meier
  • Publication number: 20150080357
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 4, 2014
    Publication date: March 19, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
  • Patent number: 8980899
    Abstract: Disclosed herein are, inter alia, methods for inhibiting Ire1 activity.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: March 17, 2015
    Assignee: The Regents of the University of California
    Inventors: Alexei Korennykh, Peter Walter, Han Li, Arvin Dar, Kevan Shokat
  • Publication number: 20150072965
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
  • Publication number: 20150051183
    Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 19, 2015
    Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Arnaud Piettre, Jean-François Gosalbes, Marc Thommen
  • Publication number: 20150038474
    Abstract: Optionally substituted 3-(thio, sulfinyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 3, 2014
    Publication date: February 5, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence P. WENNOGLE
  • Patent number: 8946219
    Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 3, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Pamela B. Conley, Patrick Andre, Uma Sinha
  • Patent number: 8940740
    Abstract: Certain compounds are provided that can selectively inhibit motile bacteria such as V. cholerae motility. These compounds can indirectly diminish production of cholera toxin and other major virulence required by the cholera bacterium to cause disease.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: January 27, 2015
    Assignee: Southern Research Institute
    Inventors: Ashish K. Pathak, Jorge A. Benitez, Anisia J. Silva-Benitez
  • Patent number: 8927530
    Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: January 6, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Juergen Moll, Mara Emanuela Casnaghi, Alessandro Luciano Croci
  • Patent number: 8906928
    Abstract: The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: December 9, 2014
    Assignee: ArQule, Inc.
    Inventors: Jason Hill, Manish Tandon, Nivedita Namdev, Rocio Palma, Neil Westlund, Anton Filikov
  • Patent number: 8906929
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
  • Publication number: 20140357606
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: August 15, 2014
    Publication date: December 4, 2014
    Inventor: Peng LI
  • Patent number: 8901133
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • 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
  • Patent number: 8889681
    Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: November 18, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventor: Nestor Antonio Lagos Wilson
  • Patent number: 8883799
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 11, 2014
    Assignee: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
  • Publication number: 20140329805
    Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
    Type: Application
    Filed: January 28, 2014
    Publication date: November 6, 2014
    Applicant: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20140329674
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140324016
    Abstract: A method and apparatus for treatment of cardiac and renal diseases associated with the elevated sympathetic renal nerve activity by implanting a device to block the renal nerve signals to and from the kidney. The device can be a drug pump or a drug eluding implant for targeted delivery of a nerve-blocking agent to the periarterial space of the renal artery.
    Type: Application
    Filed: March 21, 2014
    Publication date: October 30, 2014
    Applicant: Medtronic Ardian Luxembourg S.a.r.l.
    Inventors: Mark Gelfand, Howard R. Levin
  • Patent number: 8871763
    Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: October 28, 2014
    Assignee: Phytotox, Ltd.
    Inventor: Nestor Antonio Lagos Wilson
  • Patent number: 8865731
    Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: October 21, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
  • Patent number: 8858911
    Abstract: Tracers targeting phosphodiesterase 1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: October 14, 2014
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Peng Li, Lawrence P. Wennogle, Jun Zhao, Hailin Zheng
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty