Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/263)
  • Patent number: 11084826
    Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: March 30, 2020
    Date of Patent: August 10, 2021
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: David Francis Alain Lançois, Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Dirk André Emmy Roymans, Boris Rogovoy, Vadim Bichko, Delphine Yvonne Raymonde Lardeau, Antoine Benjamin Michaut, Anil Koul
  • Patent number: 11053248
    Abstract: The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: July 6, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Yves Emiel Maria Van Roosbroeck, Petrus Jacobus Johannes Antonius Buijnsters, Gary John Tresadern, Edgar Jacoby, Daniel Oehlrich, Henricus Jacobus Maria Gijsen
  • Patent number: 10858365
    Abstract: The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: December 8, 2020
    Inventors: Qingbei Zeng, Changhe Qi, Honchung Tsui, Zhenfan Yang, Xiaolin Zhang
  • Patent number: 10611769
    Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: April 7, 2020
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: David Francis Alain Lançois, Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Dirk André Emmy Roymans, Boris Rogovoy, Vadim Bichko, Delphine Yvonne Raymonde Lardeau, Antoine Benjamin Michaut, Anil Koul
  • Patent number: 10208048
    Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: February 19, 2019
    Assignee: Janssen Sciences Ireland UC
    Inventors: David Francis Alain Lançois, Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Dirk André Emmy Roymans, Boris Rogovoy, Vadim Bichko, Delphine Yvonne Raymonde Lardeau, Antoine Benjamin Michaut, Anil Koul
  • Patent number: 9890169
    Abstract: Triazolinone compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for the therapy of diseases and conditions in which HNE is implicated.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: February 13, 2018
    Assignee: CHIESI FARMACEUTICI S.P.A.
    Inventors: Elisabetta Armani, Carmelida Capaldi
  • Patent number: 9840509
    Abstract: The present invention relates to heterocyclic compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as selective Bruton's Tyrosine Kinase (BTK) inhibitors.
    Type: Grant
    Filed: February 2, 2015
    Date of Patent: December 12, 2017
    Assignee: Cadila Healthcare Limited
    Inventors: Ranjit C. Desai, Rajesh Bahekar, Dipam Patel, Kiran Shah
  • Patent number: 9115135
    Abstract: 5-Substituted-8-alkoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-amines are manufactured from 4-amino-2,5-dialkoxypyrimidines in an improved process in which the generation of gaseous by-products is controlled by the continuous addition of hydroxylamine as a free base.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: August 25, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas C. Bland, Christopher T. Hamilton
  • Publication number: 20150148332
    Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
  • Patent number: 9034882
    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: March 1, 2013
    Date of Patent: May 19, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • Publication number: 20150126532
    Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and thereby decreasing aggregate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.
    Type: Application
    Filed: November 3, 2014
    Publication date: May 7, 2015
    Inventors: Isabella A. Graef, Mamoun M. Alhamadsheh
  • Patent number: 9023855
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: May 5, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Patent number: 9012633
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: April 21, 2015
    Assignee: Cancer Research Technology Limited
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Patent number: 9000160
    Abstract: 2-Amino-5,8-dialkoxy[1,2,4]-triazolo[1,5-c]pyrimidines are manufactured from 4-chloro-2,5-dialkoxypyrimidines in a process that avoids hydrazine and cyanogen halide.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas C. Bland, Gary Roth, Craig Bott, Christopher T. Hamilton, Joseph Neuman
  • Publication number: 20140364415
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140350002
    Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: June 14, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
  • Publication number: 20140303158
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Publication number: 20140288062
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
  • Publication number: 20140255386
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: July 24, 2012
    Publication date: September 11, 2014
    Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTE
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Patent number: 8791090
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 29, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20140194418
    Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 10, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
  • Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Patent number: 8765770
    Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: July 1, 2014
    Assignee: Ataxion, Inc.
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dotre Strøbæk, Palle Christophersen
  • Publication number: 20140179714
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Application
    Filed: February 11, 2014
    Publication date: June 26, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Publication number: 20140171414
    Abstract: Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Lilian ALCARAZ, Robert Andrew Heald, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi
  • Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Publication number: 20140155594
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Application
    Filed: April 24, 2013
    Publication date: June 5, 2014
    Applicant: Cancer Research Technology Limited
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Publication number: 20140142122
    Abstract: Disclosed herein are erythropoietin-mimetic compounds of Formula I, which modulate the survival, function, or differentiation of, for example, kidney cells, neurons, erythroid cells, or other erythropoietin-responsive cells. The present invention also relates to compounds and methods that preferentially modulate cells expressing the tissue-protective erythropoietin receptor. The compounds of the invention are useful in preventing and treating diseases, such as anemia, organ injury, and diseases of the central nervous system, and as an adjunct to cellular treatments, such as stem cell therapies.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: STATegics, Inc.
    Inventors: Juha PUNNONEN, Jeffrey R. SPENCER, Timothy J. CHURCH, Connie S. TETTENBORN, Karen LARIOSA-WILLINGHAM, Dimitri LEONOUDAKIS, James L. MILLER
  • Publication number: 20140135219
    Abstract: The present invention relates to the use of the ALS inhibitor herbicides for controlling unwanted vegetation in ALS inhibitor herbicide tolerant Brassica plants, more especially, the present invention relates to the use of ALS inhibitor herbicides for control of unwanted vegetation in Brassica growing areas which Brassica plants comprise non-transgenic mutations of their endogenous acetolactate synthase (ALS) genes I and III.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 15, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ruediger Hain, MIchael Schindler, Katharina Wölfel, Ulrich Ebbinghaus-Kintscher, Arnd Voerste, Olga Malsam, Peter Lösel, Ulrich Görgens
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8691826
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: April 8, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Patent number: 8691827
    Abstract: The present invention is directed to amino tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • Patent number: 8685987
    Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: April 1, 2014
    Assignee: Ataxion, Inc.
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbæk, Palle Christophersen
  • Publication number: 20140081023
    Abstract: 2-Amino-5,8-dialkoxy[1,2,4]-triazolo[1,5-c]pyrimidines are manufactured from 4-chloro-2,5-dialkoxypyrimidines in a process that avoids hydrazine and cyanogen halide.
    Type: Application
    Filed: September 10, 2013
    Publication date: March 20, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Douglas C. Bland, Gary Roth, Craig Bott, Christopher T. Hamilton, Joseph Neuman
  • Publication number: 20140081024
    Abstract: 5-Substituted-8-alkoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-amines are manufactured from 4-amino-2,5-dialkoxypyrimidines in an improved process in which the generation of gaseous by-products is controlled by the continuous addition of hydroxylamine as a free base.
    Type: Application
    Filed: September 11, 2013
    Publication date: March 20, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Douglas C. Bland, Christopher T. Hamilton
  • Publication number: 20140073638
    Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 13, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Publication number: 20140046056
    Abstract: Provided is a novel compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
  • Patent number: 8614218
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: December 24, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
  • Patent number: 8609690
    Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: December 17, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
  • Publication number: 20130317002
    Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: February 2, 2010
    Publication date: November 28, 2013
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventor: Barbara Beckers
  • Publication number: 20130317021
    Abstract: The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: May 23, 2013
    Publication date: November 28, 2013
    Inventors: Andrea WOLKERSTORFER, Oliver Szolar, Norbert Handler, Stephen Cusack, Thibault Sauvaitre, Céline Simon, Christophe Morice, Bruno Giethlen, Thierry Langer, Mark Smith, Sung-Sau So, Dirk Classen-Houben, Helmut Buschmann
  • Patent number: 8592431
    Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
  • Patent number: 8592423
    Abstract: PDE10 inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit PDE10 are also disclosed.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: November 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Prasad V. Chaturvedula, S. Roy Kimura
  • Publication number: 20130310342
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.
    Type: Application
    Filed: October 24, 2012
    Publication date: November 21, 2013
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Patent number: 8586581
    Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: November 19, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Publication number: 20130296343
    Abstract: The invention relates to substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.
    Type: Application
    Filed: April 8, 2013
    Publication date: November 7, 2013
    Inventors: Stephan SIEGEL, Andreas WILMEN, Niels SVENSTRUP, Mark Jean GNOTH, Adrian TERSTEEGEN, Ulrich RESTER
  • Patent number: 8569314
    Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: October 29, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Patent number: 8563561
    Abstract: The 3-(3-pyrimidin-2ylbenzyl)-1,2,4-triazolo[4,3-b]pyrimidine compounds of formula in which R1, R2, R3, R3, R4 have the meanings indicated herein, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: October 22, 2013
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Publication number: 20130196985
    Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 1, 2013
    Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of Sciences
    Inventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng