Cyano Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/344)
  • Patent number: 11161815
    Abstract: There is provided compounds of formula I (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3 and X have meanings provided in the description, which compounds are useful in the treatment of cancers.
    Type: Grant
    Filed: February 7, 2018
    Date of Patent: November 2, 2021
    Assignee: Oblique Therapeutics AB
    Inventors: Benjamin Pelcman, Edgars Suna, William Stafford, Martins Priede
  • Patent number: 11034751
    Abstract: The present invention provides methods for treating cancer using serotonin receptor inhibitors, such as serotonin receptor inhibitory antibodies, among others. The invention also features compositions containing serotonin receptor inhibitors, methods of diagnosing patients with serotonin receptor-associated cancer, and methods of predicting the response of cancer in a subject to treatment with serotonin receptor inhibitors.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: June 15, 2021
    Assignee: Flagship Pioneering Innovations V, Inc.
    Inventors: Avak Kahvejian, Jordi Mata-Fink, Jonathan Barry Hurov, Chengyi Jenny Shu, George Huck Neubauer, Manuel Andreas Fankhauser, Julian Alexander Stanley
  • Patent number: 11014889
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5, and R6 are as defined in the claims. The invention further provides compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: May 25, 2021
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas James Hoffman, Sarah Sulzer-Mosse, Kurt Nebel, Fredrik Emil Malcolm Cederbaum
  • Patent number: 10807948
    Abstract: Disclosed herein are substituted indane derivatives useful as HIF-2? inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2? activity are also disclosed.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: October 20, 2020
    Assignee: PELOTON THERAPEUTICS, INC.
    Inventors: Darryl David Dixon, Jonas Grina, John A. Josey, James P. Rizzi, Stephen T. Schlachter, Eli M. Wallace, Bin Wang, Paul Wehn, Rui Xu, Hanbiao Yang
  • Patent number: 10472332
    Abstract: The invention relates to compounds having antiviral and methods utilizing the compounds to treat viral infections.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: November 12, 2019
    Assignee: Biotron Limited
    Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
  • Patent number: 10221126
    Abstract: This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.
    Type: Grant
    Filed: June 26, 2018
    Date of Patent: March 5, 2019
    Assignee: VELICEPT THERAPEUTICS, INC.
    Inventors: Raymond E. Stevens, Dalian Zhao, Bingidimi Itute Mobele
  • Patent number: 10173983
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The invention further provides compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: January 8, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas James Hoffman, Sarah Sulzer-Mosse, Kurt Nebel, Fredrik Emil Malcolm Cederbaum
  • Patent number: 10098878
    Abstract: The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating iron overload disorders. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and reduced liver iron accumulation and serum iron parameters in both prophylactic and treatment mouse models.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: October 16, 2018
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Richard Keith Bruick, Yaomin Chen, Julio Cesar Francisco Ruiz
  • Patent number: 10059671
    Abstract: The present invention relates to novel substituted pyridine derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 3 (mGluR3) and/or altering glutamate level or glutamatergic signalling.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: August 28, 2018
    Assignee: PREXTON THERAPEUTICS SA
    Inventor: Justin Potnick
  • Patent number: 10016398
    Abstract: Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: July 10, 2018
    Assignee: Frost Biologic, Inc.
    Inventor: Adam Siddiqui-Jain
  • Patent number: 9987261
    Abstract: Described herein, inter alia, are compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: June 5, 2018
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
  • Patent number: 9382267
    Abstract: The present invention relates to novel compounds, their use as anti-cancer agents and their synthesis. In particular, the compounds contain cluster boron moieties such as carborane or a borohydride and act as inhibitors for the enzyme Nampt. The biological properties of the inventive cluster boron compounds, in terms of biological inhibition and antiproliferative effect, are greater than other small molecule inhibitors of Nampt.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: July 5, 2016
    Assignee: The Curators of the University of Missouri
    Inventors: Mark Wayne Lee, Jr., Yulia Sevryugina
  • Patent number: 9067891
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: June 30, 2015
    Assignees: JANSSEN PHARMACEUTICALS, INC., ADDEX PHARMA SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James Macdonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150038480
    Abstract: The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same.
    Type: Application
    Filed: May 29, 2012
    Publication date: February 5, 2015
    Applicants: UNIVERSITY OF FLORIDA RESERCH FOUNDATION INCORPORTED, THE REGENTS OF THE UNIVERSITY OF COLORADO, a body corporate
    Inventors: Aaron Michels, Maki Nakayama, David Ostrov
  • Publication number: 20150011496
    Abstract: The invention provides methods and compositions for stimulating or promoting bone regeneration or repairing bone fracture or for stimulating or increasing differentiation or activation of osteoblasts by administering to a subject a therapeutically effective amount of an adenosine receptor agonist, or an analog, derivative or combination thereof, an adenosine receptor antagonist, or an analog, derivative or combination thereof, or adenosine or a compound that upregulates, increases the amount of or increases the biological activity of adenosine. The invention also extends to pharmaceutical compositions such as those comprising an agent that modulates an adenosine receptor such as an adenosine A2A agonist or A1 antagonist.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Inventors: Bruce Cronstein, Aranzazu Mediero Munoz
  • Patent number: 8916553
    Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: December 23, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
  • Patent number: 8895749
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: November 25, 2014
    Assignee: AbbVie Inc.
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Publication number: 20140335019
    Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
  • Publication number: 20140315903
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: HASSAN JULIEN IMOGAI, JOSE MARIA CID-NUNEZ, JOSE IGNACIO ANDRES-GIL, ANDRES AVELINO TRABANCO-SUAREZ, JULEN OYARZABAL SANTAMARINA, FRANK MATTHIAS DAUTZENBERG, GREGOR JAMES MACDONALD, SHRILEY ELIZABETH PULLAN, ROBERT JOHANNES LUTJENS, GUILLAUME ALBERT JACQUES DUVEY, VANTHEA NHEM, TERRY PATRICK FINN, GAGIK MELIKYAN
  • Publication number: 20140296295
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Walter HÜBSCH, Daniel MEIBOM, Alexandros VAKALOPOULOS, Barbara ALBRECHT-KÜPPER, Peter NELL, Katja ZIMMERMANN, Frank SÜßMEIER, Joerg KELDENICH
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Patent number: 8822442
    Abstract: The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: September 2, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, Michael Dewitt Culler, Yeelena Shen
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140241990
    Abstract: Disclosed herein are methods for treating depression and depressive-like symptoms by administering a therapeutically effective amount of an adenosine 1 receptor agonist. Also disclosed herein are methods for identifying adenosine receptor agonists and the use of identified adenosine receptor agonists for treating diseases, disorders or conditions characterized by pathological sleep perturbations.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 28, 2014
    Applicant: TUFTS UNIVERSITY
    Inventors: Philip G. Haydon, Dustin J. Hines, L. Ian Schmitt
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140234245
    Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Patent number: 8802703
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: August 12, 2014
    Assignee: Merck Serono S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, Jr., Nhut Kiet Diep, Srinivasa R. Karra, Matthias Schwarz, Henry Yu
  • Publication number: 20140221411
    Abstract: The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.
    Type: Application
    Filed: April 18, 2014
    Publication date: August 7, 2014
    Applicant: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Semi KIM, Ill Young LEE, Hye-Jin MIN, Eun-Hee NAM, Pilho KIM, Chang Soo YUN, Dong Joon KO
  • Patent number: 8791091
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Patent number: 8754081
    Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: June 17, 2014
    Assignee: The United States of America as represented by the Secretary, Departmnet of Health and Human Services
    Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Terrence Burke, Jr., Gagani Athauda, Sarah Choyke, Alessio Giubellino, Nelly Tan, Zhen-Dan Shi
  • Publication number: 20140148453
    Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 29, 2014
    Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
  • Patent number: 8716318
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: May 6, 2014
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Patent number: 8697689
    Abstract: The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions as well as to the use of such compounds or compositions for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: April 15, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez
  • Publication number: 20140044806
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140024665
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: June 5, 2013
    Publication date: January 23, 2014
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Patent number: 8604062
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: December 10, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Pascal Dott, Steven Paul Hanlon, Stefan Hildbrand, Hans Iding, Andrew Thomas, Pius Waldmeier
  • Patent number: 8603945
    Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 10, 2013
    Assignee: The Regents of the University of California
    Inventors: Colleen Marie Knoth, Thomas Eulgem, Thomas Girke
  • Publication number: 20130210795
    Abstract: The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: June 27, 2011
    Publication date: August 15, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexandros Vakalopoulos, Daniel Meibom, Peter Nell, Frank Sussmeier, Barbara Albrecht-Kupper, Katja Zimmermann, Joerg Keldenich, Dirk Schneider, Ursula Krenz
  • Patent number: 8507536
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: August 13, 2013
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
  • Patent number: 8491923
    Abstract: The present invention, therefore, relates to a method for prophylaxis, control or reduction of fungi in a textile substrate, which comprises applying to a textile substrate that is susceptible to fungal infestation an amount effective for the prophylaxis, control or reduction of fungi of at least one fungicidal compound. The invention further provides a method for the prophylaxis, control or reduction of both fungi and dust mites in a textile substrate, which comprises co-application to a textile substrate that is susceptible to fungal and dust mite infestation of a prophylactic or acaricidally effective amount of a suitable acaricide and a prophylactic or fungicidally effective amount of at least one fungicidal compound.
    Type: Grant
    Filed: November 22, 2004
    Date of Patent: July 23, 2013
    Assignee: LANXESS Deutschland GmbH
    Inventors: William D. McClellan, Eric C. Tedford, Jeremy R. Godwin
  • Publication number: 20130143843
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8445686
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: May 21, 2013
    Assignee: AbbVie Inc.
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Mueller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steve Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Publication number: 20130109645
    Abstract: Disclosed are a method of treating or preventing a disorder in a mammal comprising administering to the mammal an adenosine receptor agonist or an adenosine receptor antagonist, either alone or in combination, in an amount effective to treat or prevent medial vascular or joint capsule calcification. Disclosed are methods of detecting or diagnosing a vascular or joint capsule calcification disorder, as well as a nucleic acid comprising a mutation in one or more exons of human NT5E selected from the group consisting of Exon 3, Exon 5, and Exon 9.
    Type: Application
    Filed: March 30, 2011
    Publication date: May 2, 2013
    Applicant: The united States of America,as represented by Secretary,Dept.,of Health and Human Services
    Inventors: William A. Gahl, Manfred Boehm, Cynthia St. Hilaire, Shira G. Ziegler, Thomas C. Markello
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Publication number: 20130102597
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 25, 2013
    Applicant: INTERMUNE, INC.
    Inventor: INTERMUNE, INC.
  • Patent number: 8389525
    Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: March 5, 2013
    Inventors: Renee Desai, Ketan Desai