At Least Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/117)
  • Patent number: 10087182
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: October 2, 2018
    Assignees: INCOZEN THERAPEUTICS PVT. LTD., RHIZEN PHARMACEUTICALS SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
  • Patent number: 9815831
    Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: November 14, 2017
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
  • Patent number: 9040555
    Abstract: The present invention provides compounds having the general structural formula (I), and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.
    Type: Grant
    Filed: January 26, 2013
    Date of Patent: May 26, 2015
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
  • Publication number: 20150133658
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20150133449
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150057309
    Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 26, 2015
    Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
  • Patent number: 8952034
    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: Grant
    Filed: July 26, 2010
    Date of Patent: February 10, 2015
    Assignee: 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: 20150025094
    Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, hal
    Type: Application
    Filed: August 1, 2012
    Publication date: January 22, 2015
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan University
    Inventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Patent number: 8933094
    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: October 16, 2013
    Date of Patent: January 13, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Patent number: 8927720
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: January 6, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 8921319
    Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 30, 2014
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Sebastian Martin Saupe
  • Patent number: 8912331
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: December 16, 2014
    Assignees: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
  • Publication number: 20140364603
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20140349990
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • Publication number: 20140315928
    Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 23, 2014
    Applicant: Pfizer Inc.
    Inventors: Etzer Darout, Robert Dullea, Julie Jia Li Hawkins, Allyn T. Londregan, Paula M. Loria, Bruce Maguire, Kim F. McClure, Donna N. Petersen, David W. Piotrowski
  • Publication number: 20140309424
    Abstract: The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([18F]Fluoromethyl)tyrosines.
    Type: Application
    Filed: June 29, 2012
    Publication date: October 16, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Thomas Brumby, Keith Graham, Martin Kruger
  • 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
  • Patent number: 8846913
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3—R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: September 30, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20140275015
    Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De Angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
  • Patent number: 8822689
    Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Grant
    Filed: September 19, 2012
    Date of Patent: September 2, 2014
    Assignees: Merial Limited, Aventis Agriculture
    Inventors: Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Robert Toms Jacobs
  • Patent number: 8779142
    Abstract: It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: July 15, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura, Satoshi Yamashita, Hiromi Oshiumi, Takao Uno, Yuichi Kawai
  • Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Patent number: 8754103
    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: Grant
    Filed: July 26, 2010
    Date of Patent: June 17, 2014
    Assignee: 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
  • Patent number: 8741919
    Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: June 3, 2014
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20140128426
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 8, 2014
    Applicant: Siga Technologies Inc.
    Inventor: Siga Technologies Inc.
  • Patent number: 8691838
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds of Formula I, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: April 8, 2014
    Assignee: Amgen Inc.
    Inventors: Brian K. Albrecht, Steven Bellon, Christiane M. Bode, Alessandro Boezio, Deborah Choquette, Jean-Christophe Harmange
  • Publication number: 20140080862
    Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Application
    Filed: September 19, 2012
    Publication date: March 20, 2014
    Applicants: AVENTIS AGRICULTURE, MERIAL LIMITED
    Inventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20130324531
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
  • Publication number: 20130261116
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: May 10, 2013
    Publication date: October 3, 2013
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Publication number: 20130245260
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: April 24, 2013
    Publication date: September 19, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • 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
  • Patent number: 8481739
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: July 9, 2013
    Assignees: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
  • Patent number: 8461177
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: June 11, 2013
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Patent number: 8461176
    Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives substantially enriched in an enantiomer of formula (I): and compounds of formula (IH) wherein R3, R4, R5, R6, R7, R13a, R13b, R14a, R14b, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: June 11, 2013
    Assignee: Merial Limited
    Inventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs, Brent Christopher Beck
  • Publication number: 20130144541
    Abstract: Novel cross-linking compounds that can be used in mass spectrometry, tandem mass spectrometry, and multi-stage tandem mass spectrometry to facilitate structural analysis of proteins and protein complexes are provided and have the formula: where X is an N-hydroxy-succinimidyl or similar heterocyclic group. Also provided is a method of mapping protein-protein interactions of protein complexes using various mass spectrometry techniques.
    Type: Application
    Filed: May 14, 2012
    Publication date: June 6, 2013
    Inventors: Scott Rychnovsky, Lan Huang
  • Publication number: 20130065883
    Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: February 18, 2011
    Publication date: March 14, 2013
    Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)
    Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
  • Patent number: 8372860
    Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: February 12, 2013
    Assignee: PTC Therapeutics, Inc.
    Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang, Thomas Davis
  • Patent number: 8334291
    Abstract: The present application relates to novel aliphatically substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: December 18, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hartmut Schirok, Nils Griebenow, Chantal Fürstner, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Stefan Heitmeier
  • Publication number: 20120283239
    Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 8, 2012
    Applicant: MSD OSS B.V.
    Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
  • Publication number: 20120264739
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Application
    Filed: December 30, 2010
    Publication date: October 18, 2012
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Publication number: 20120245138
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: May 2, 2012
    Publication date: September 27, 2012
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20120213807
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20120213806
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20120201816
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: April 12, 2012
    Publication date: August 9, 2012
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
  • Patent number: 8227485
    Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having general formula (I), which have a good affinity with certain sub-types of melanocortin receptors, particularly MC4 receptors. Said derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said products.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: July 24, 2012
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
  • Patent number: 8173811
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: May 8, 2012
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt