Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/556)
  • Patent number: 10023573
    Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: July 17, 2018
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Seiichi Inamura, Akihiro Morinaka
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 9006230
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: April 14, 2015
    Assignee: Wockhardt Ltd.
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • Publication number: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • Patent number: 8986654
    Abstract: The present invention relates to certain labelled or un-labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives and their medical use. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: March 24, 2015
    Assignee: DanPET AB
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen
  • Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Patent number: 8946412
    Abstract: This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: February 3, 2015
    Assignee: Danpet AB
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Tino Dyhring, Philip K. Ahring
  • Patent number: 8895750
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: November 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
  • Patent number: 8846661
    Abstract: The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: September 30, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael R. Schrimpf, Kevin B. Sippy
  • Patent number: 8841289
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: September 23, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
  • Publication number: 20140275009
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: September 18, 2014
    Inventors: Guy Brenchley, Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
  • Publication number: 20140249141
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: August 20, 2012
    Publication date: September 4, 2014
    Applicant: Targacept, Inc.
    Inventors: Anatoly Mazurov, Lan Miao, Todd Showalter
  • Publication number: 20140221355
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
  • Publication number: 20140221356
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Patent number: 8778928
    Abstract: This invention relates to novel indolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: July 15, 2014
    Assignee: Danpet AB
    Inventors: Dan Peters, Daniel B. Timmermann, Tino Dyhring, Jeppe Kejser Christensen, Elsebet Østergaard Nielsen
  • Publication number: 20140163000
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
  • Patent number: 8747581
    Abstract: The invention relates to the field of explosives, and more particularly relates to particles of an explosive, wherein they are in crystalline form, have a rounded shape and a majority of them contain no internal defect. Particles of an explosive in crystalline form include a volume fraction of closed pores of less than or equal to 0.05%. A method for preparing explosive particles includes preparing crystalline particles, a majority of which are without an internal defect; and rounding the crystalline particles.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: June 10, 2014
    Assignee: Institut Franco-Allemand de Recherches de Saint-Louis
    Inventor: Lionel Borne
  • Publication number: 20140080813
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Publication number: 20140080814
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Publication number: 20140080816
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margot Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
  • Publication number: 20140030190
    Abstract: The present invention relates to certain labelled or un-labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives and their medical use. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
    Type: Application
    Filed: April 3, 2012
    Publication date: January 30, 2014
    Applicant: DANPET AB
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Patent number: 8623857
    Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
  • Publication number: 20130310364
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 8569289
    Abstract: Fumarate salt of 4-bromophenyl 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate, crystalline forms thereof, methods of preparation thereof, and therapeutic use thereof.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: October 29, 2013
    Assignee: Sanofi
    Inventors: Benoit Robert, Laurent Salle
  • Patent number: 8524706
    Abstract: The present invention discloses and claims compounds of general formula in which X, R1, P, Q, R and W are as described herein. The compounds of the invention are useful in a variety of therapeutic applications.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: September 3, 2013
    Assignee: Sanofi
    Inventors: Frederic Galli, Patrick Lardenois, Odile Leclerc, Alistair Lochead
  • Publication number: 20130211073
    Abstract: Synthetic voacangine, including in substantially enantiomerically enriched forms, and derivatives thereof are provided.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 15, 2013
    Applicant: DemeRx, Inc.
    Inventor: DemeRx, Inc.
  • Publication number: 20130210806
    Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Patent number: 8487093
    Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: July 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
  • Publication number: 20130150342
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: June 13, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
  • Publication number: 20130079326
    Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
    Type: Application
    Filed: May 24, 2011
    Publication date: March 28, 2013
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka
  • Patent number: 8399457
    Abstract: Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic ? and/or ? and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the isomeric forms and their mixtures included, wherein one or more atoms are in the corresponding isotopic forms: wherein: n is an integer equal to 1 or 2; one of the substituents R and R1 of the nitrogen atoms of the diazabicyclic ring is a —C(O)—RB group, wherein RB is a C1-C10 alkyl group, linear or branched when possible, the other remained substituent of R and R1 has the meanings reported in the description.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: March 19, 2013
    Assignee: Neuroscienze Pharmaness S.C. A.R.L.
    Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Luca Pani, Gerard Aime Pinna
  • Publication number: 20130053365
    Abstract: Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): where A, B, Y, Z, D, E, R1, R2, R3, and R4 are as defined herein. Also described are pharmaceutical compositions, methods of preparing, and methods of using a compound of Formula M to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 28, 2013
    Applicant: BioMarin Pharmaceutical, Inc.
    Inventors: Bing Wang, Daniel Chu
  • Patent number: 8377927
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: February 19, 2013
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Patent number: 8372832
    Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: February 12, 2013
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jens Damsgaard Mikkelsen, Henrik Björk Hansen, John Paul Redrobe, Jeppe Kejser Christensen, Tino Dyhring
  • Publication number: 20130012490
    Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8349824
    Abstract: The invention is concerned with triazolopyridine compounds of formula (I) 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 pharmaceuticals.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: January 8, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Luca Gobbi, Katrin Groebke Zbinden, Matthias Koerner, Jens-Uwe Peters
  • Publication number: 20130004428
    Abstract: This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.
    Type: Application
    Filed: December 16, 2010
    Publication date: January 3, 2013
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Tino Dyhring, Philip K. Ahring
  • Patent number: 8343954
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: January 1, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 8343960
    Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: January 1, 2013
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Ostergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, John Paul Redrobe, Jens Damsgaard Mikkelsen
  • Patent number: 8324200
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: December 4, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
  • Publication number: 20120288443
    Abstract: The present invention relates to certain labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
    Type: Application
    Filed: November 9, 2010
    Publication date: November 15, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Jens Damsgaard Mikkelsen, Anders Janusz Ettrup
  • Publication number: 20120270853
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: July 3, 2012
    Publication date: October 25, 2012
    Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
  • Publication number: 20120253036
    Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredient
    Type: Application
    Filed: December 10, 2010
    Publication date: October 4, 2012
    Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
  • Publication number: 20120238553
    Abstract: This invention relates to novel benzodioxolyl-oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances (I).
    Type: Application
    Filed: January 25, 2010
    Publication date: September 20, 2012
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Tino Dyhring, Jeppe Kejser Christensen
  • Patent number: 8268991
    Abstract: The present invention describes a novel heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexa(1-propenyl)hexaazaisowurtzitane (HPIW) and hence via reaction with singlet oxygen and subsequent nitrolysis to hexanitrohexaazaisowurtzitane (CL-20).
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: September 18, 2012
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Robert D. Chapman, Richard A. Hollins
  • Publication number: 20120208796
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by nicotinic acetylcholine receptors, such as schizophrenia and Alzheimer's disease.
    Type: Application
    Filed: October 11, 2010
    Publication date: August 16, 2012
    Inventors: Paul David Ratcliffe, Thomas Russell Clarkson, Fiona Jeremiah, John Kinnard Ferguson MacLean
  • Publication number: 20120172350
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20120172353
    Abstract: This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl oxadiazolyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: March 14, 2012
    Publication date: July 5, 2012
    Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Daniel B. Timmermann, Steven Charles Loechel, Jens Damsgaard Mikkelsen, Henrik Björk Hansen, John Paul Redrobe, Jeppe Kejser Christensen, Tino Dyhring