At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
  • Patent number: 10457685
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal, Adriaan Pieter Ijzerman
  • Patent number: 10457684
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal
  • Patent number: 10457686
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal
  • Patent number: 10450321
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: October 22, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal, Adriaan Pieter Ijzerman
  • Patent number: 10011605
    Abstract: The present invention relates to a process for preparation of triazolo[4,5-d] pyrimidine cyclopentane compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention also provides novel compounds that can be used as intermediates in the process for preparing triazolo[4,5-d] pyrimidine cyclopentane compounds. The process and the intermediates are particularly useful for the preparation of ticagrelor and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: July 3, 2018
    Assignee: FLAMMA SPA
    Inventors: Anna Rencurosi, Massimo Previtali, Federico Della Negra, Francesco Mormile, Renato Canevotti
  • Patent number: 9988380
    Abstract: The invention relates to compounds for use as quorum sensing inhibitors, and in particular, to quorum sensing inhibitors of Pseudomonas aeruginosa.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: June 5, 2018
    Assignees: Nanyang Technological University, National University of Singapore
    Inventors: Michael Givskov, Liang Yang, Yang Yi Sean Tan
  • Patent number: 9932317
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: April 3, 2018
    Assignees: Imperial Innovations Limited, Emory University
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Snyder, Thota Ganesh, Jin Liu, Aiming Sun
  • Patent number: 9512128
    Abstract: The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) in which the respective radicals have the meanings given in the description.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: December 6, 2016
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Silvia Cerezo-Galvez, Reiner Fischer, Adeline Koehler, Julia Johanna Hahn, Angela Becker, Kerstin Ilg, Arnd Voerste, Ulrich Goergens, Daniela Portz
  • Patent number: 9487518
    Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: November 8, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
  • Patent number: 9067943
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: June 30, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Patent number: 9056838
    Abstract: The present invention is related to new intermediates and processes for preparing Ticagrelor disclosed in this patent application.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: June 16, 2015
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: Vinod Kumar Kansal, Dhirenkumar Mistry, Sanjay Vasoya, Ghanshyam Pandey, Amit Taneja, Pramod Kadappa Shindey, Jiri Stohandl, Jaroslav Frantisek
  • Patent number: 8987279
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: March 24, 2015
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Patent number: 8980893
    Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: March 17, 2015
    Assignee: Merial, Inc.
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Publication number: 20150073146
    Abstract: Provided are processes for preparing Ticagrelor and its intermediates that are useful in the processes. Also provided are salts of Ticagrelor, their processes and solid dispersion of Ticagrelor having Ticagrelor in amorphous form.
    Type: Application
    Filed: April 5, 2013
    Publication date: March 12, 2015
    Inventors: Vilas Hareshwar Dahanukar, Goverdhan Gilla, Sreenivasulu Kurella, Shweta Mahajan Kulkarni, Raghupathi Reddy Anumula, Sampath Aalla, Yakambram Bojja, Ravi Ram Chandra Sekhar Elati, Veerender Murki, Venkata Annapurna Sasikala Cheemalapati
  • Patent number: 8937150
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: January 20, 2015
    Assignee: AbbVie Inc.
    Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
  • Publication number: 20150005498
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of Ticagrelor (TCG).
    Type: Application
    Filed: September 14, 2012
    Publication date: January 1, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nened Maras, Borut Zupancic
  • Publication number: 20140378431
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
  • Publication number: 20140371449
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 18, 2014
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
  • Patent number: 8883802
    Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: November 11, 2014
    Assignee: Astrazeneca AB
    Inventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
  • Publication number: 20140323727
    Abstract: Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 30, 2014
    Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Patent number: 8871785
    Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 21, 2013
    Date of Patent: October 28, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Carina E. Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten A. Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie O'Shea, Sundaramoorthi Swaninathan, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20140296258
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: October 31, 2013
    Publication date: October 2, 2014
    Applicant: AstraZeneca UK Limited
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20140256747
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Patent number: 8802850
    Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: August 12, 2014
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Publication number: 20140206867
    Abstract: Disclosed herein is an improved process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Particularly described is an improved, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, [3aR-(3a?,4?,6?,6a?]-2-[[6-amino-2,2-dimethyltetrahydro-4H-cyclopenta-1,3-dioxol-4-yl]oxy]-ethanol, alternatively named, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.
    Type: Application
    Filed: June 13, 2012
    Publication date: July 24, 2014
    Applicant: Actavis Group PTC EHF
    Inventors: Anil Shahaji Khile, Vignesh Nair, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Patent number: 8785653
    Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: July 22, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Ask Puschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morton Langgard
  • 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: 8759357
    Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
  • Publication number: 20140154772
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Application
    Filed: November 27, 2013
    Publication date: June 5, 2014
    Applicant: ICOS CORPORATION
    Inventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
  • Patent number: 8741909
    Abstract: The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the compounds.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: June 3, 2014
    Assignee: Respivert Ltd.
    Inventors: John King-Underwood, Kazuhiro Ito, Peter John Murray, George Hardy, Frederick Arthur Brookfield, Christopher John Brown
  • Patent number: 8741906
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20140148472
    Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 29, 2014
    Applicant: CENTRO CARDIOLOGICO MONZINO SpA
    Inventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
  • Publication number: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
  • Publication number: 20140094604
    Abstract: The present invention is related to new intermediates and processes for preparing Ticagrelor disclosed in this patent application.
    Type: Application
    Filed: April 6, 2012
    Publication date: April 3, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: Vinod Kumar Kansal, Dhirenkumar Mistry, Sanjay Vasoya, Ghanshyam Pandey, Amlt Taneja, Pramond Kadappa, Jiri Stohandl, Jaroslay Frantisek
  • Publication number: 20140073624
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: February 19, 2013
    Publication date: March 13, 2014
    Applicant: RIB-X PHARMACEUTICALS, INC.
    Inventor: Rib-X Pharmaceuticals, Inc.
  • Publication number: 20140038988
    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: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, SONJA ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG
  • Patent number: 8609668
    Abstract: A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: December 17, 2013
    Assignees: Philadelphia Health & Education Corporation, Institute For Hepatitis and Virus Research
    Inventors: Andrea Cuconati, Timothy M. Block, Xiaodong Xu
  • Publication number: 20130324525
    Abstract: The present invention relates to novel heterocyclic compounds 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 Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
  • Patent number: 8598184
    Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: February 28, 2009
    Date of Patent: December 3, 2013
    Assignee: Tiger Pharmatech
    Inventor: Junhu Zhang
  • Publication number: 20130317220
    Abstract: Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.
    Type: Application
    Filed: December 16, 2011
    Publication date: November 28, 2013
    Applicant: Actavis Group Ptc Ehf
    Inventors: Vignesh Nair, Nikhil Trivedi, Anil Shahaji Khile, Nitin Sharadchandra Pradhan
  • Patent number: 8501795
    Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: August 6, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
  • Publication number: 20130150577
    Abstract: Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Application
    Filed: April 19, 2011
    Publication date: June 13, 2013
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
  • Publication number: 20130137676
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 19, 2012
    Publication date: May 30, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8450328
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: May 28, 2013
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Publication number: 20130131087
    Abstract: The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1?, 2?, 3?(1S*,2R*),5?]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 23, 2013
    Applicant: AstraZeneca AB
    Inventor: Simon Banks
  • Publication number: 20130116236
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130109702
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: October 31, 2012
    Publication date: May 2, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • Publication number: 20130072503
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: March 19, 2012
    Publication date: March 21, 2013
    Applicant: AstraZeneca
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Publication number: 20130045962
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Application
    Filed: November 6, 2008
    Publication date: February 21, 2013
    Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart