Nitrogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/407)
  • Patent number: 10898591
    Abstract: Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: January 26, 2021
    Assignee: MediBeacon Inc.
    Inventors: Richard B. Dorshow, Thomas E. Rogers
  • Patent number: 9868719
    Abstract: Disclosed are compounds of formula (I) which possess pesticidal, especially nematicidal properties wherein the structural elements have the meaning as indicated in the description.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: January 16, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Martin Fuesslein, Anne Decor, Joerg Nico Greul, Hans-Georg Schwarz, Daniela Portz, Kerstin Ilg, Olga Malsam, Peter Luemmen, Ulrich Goergens, Claudia Welz, Adeline Koehler, Kirsten Boerngen
  • Patent number: 9480687
    Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: November 1, 2016
    Assignee: MEDIBEACON, INC.
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
  • Patent number: 9382246
    Abstract: Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: July 5, 2016
    Assignee: Pharmacyclics LLC
    Inventors: Zhaozhong J. Jia, Wei Chen, William D. Thomas
  • Publication number: 20150147277
    Abstract: Compositions and methods for assessing gut function are disclosed. They are designed to provide accurate, rapid, point-of-care or in-community assessment of enteric dysfunction.
    Type: Application
    Filed: November 11, 2014
    Publication date: May 28, 2015
    Inventors: Richard B. Dorshow, Steven J. Hanley, Phillip I. Tarr
  • Patent number: 9029382
    Abstract: The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 12, 2015
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Publication number: 20150099764
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael Ross JOHNSON, William Robert Thelin, Richard C. Boucher
  • Patent number: 8980898
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: March 17, 2015
    Assignee: Parion Sciences, Inc.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 8969336
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 3, 2015
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
  • Patent number: 8962631
    Abstract: The present invention relates to pyrazine 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 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 II: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: February 24, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
  • Publication number: 20150051187
    Abstract: The present invention relates to pyrazine 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: wherein the variables are as defined herein.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 19, 2015
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Publication number: 20150045326
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 7, 2014
    Publication date: February 12, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
  • Publication number: 20150031661
    Abstract: The present invention relates to pyrazine 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: wherein the variables are as defined herein.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 29, 2015
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Publication number: 20150011535
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Armin HECKEL, Joerg KLEY
  • Publication number: 20140378461
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
  • Patent number: 8895564
    Abstract: Provided is a novel compound which simultaneously inhibits both NMDA receptors and ASIC1a, which are associated with neurodegenerative disease and so on, and thus is useful for the prevention and treatment of various nervous system diseases. A biguanide derivative represented by the following general formula (1), a salt thereof, or a hydrate of the derivative or the salt: wherein, X1 represents a halogen atom, R1 represents an alkyl group, an optionally substituted aryl group, or an optionally substituted aralkyl group.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: November 25, 2014
    Assignee: Nihon University
    Inventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
  • Patent number: 8877760
    Abstract: Provided are substituted pyrazine-2-carboxamide compounds of Formula I: useful for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: November 23, 2012
    Date of Patent: November 4, 2014
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Yonghong Song, Anjali Pandey
  • Publication number: 20140309209
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 16, 2014
    Inventors: Yonghong Song, Qing Xu, Zhaozhong J. Jia, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Publication number: 20140274692
    Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, a substituted phenol; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 is, for example, A1 is N or C—X, A3 is C—X, and A2, A4 and A5 are C—H, where X, is, for example, halogen; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 18, 2014
    Applicant: Syngenta Participations AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
  • Patent number: 8809340
    Abstract: This invention relates to a new crystalline form of the succinate salt of the epithelial sodium channel (ENaC) blocker 3-(3-{2-[(E)-3,5-Diamino-6-chloro-pyrazine-2-carbonylimino]-1,3,8-triaza-spiro[4.5]decane-8-carbonyl}-benzenesulfonylamino)-propionic acid dipropylcarbamoylmethyl ester, pharmaceutical compositions comprising said crystalline form, uses of said crystalline form and pharmaceutical compositions, and methods for preparing said crystalline form.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: Catherine Howsham, Christian Lindenberg, Anett Perlberg, Nicola Tufilli
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Patent number: 8791260
    Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: July 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Daniel Haerle, Guenter Linz, Sandra Stehle
  • Patent number: 8778309
    Abstract: The present invention relates to pyrazine derivatives represented by Formula I. X1 and X2 of Formula I may be characterized as electron withdrawing groups, while Y1 and Y2 of Formula I may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may be capable of one or both absorbing and emanating spectral energy of at least about 400 nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: July 15, 2014
    Assignee: MediBeacon LLC
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann, Dennis A. Moore
  • Patent number: 8759349
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Sara Frattini, Dieter Hamprecht, Joerg Kley
  • Publication number: 20140171447
    Abstract: This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.
    Type: Application
    Filed: December 13, 2013
    Publication date: June 19, 2014
    Applicant: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Publication number: 20140170244
    Abstract: The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.
    Type: Application
    Filed: December 13, 2013
    Publication date: June 19, 2014
    Applicant: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Publication number: 20140142118
    Abstract: A very stable, selective and renally safe sodium channel blocker represented by the formula: The invention also includes a variety of compositions, combinations and methods of treatment using this inventive sodium channel blocker.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 22, 2014
    Applicant: PARION SCIENCES, INC.
    Inventor: Michael Ross Johnson
  • Publication number: 20140135329
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 15, 2014
    Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
  • Publication number: 20140135328
    Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
  • Patent number: 8722685
    Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: May 13, 2014
    Assignee: Medibeacon, LLC
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
  • Patent number: 8703100
    Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: April 22, 2014
    Assignee: Medibeacon, LLC
    Inventors: Amruta Poreddy, William L. Neumann
  • Patent number: 8697871
    Abstract: The present invention discloses a number of photoactive compounds designed to bind and inhibit serine proteases. Compounds disclosed herein may be utilized in a number of appropriate medical diagnostic and/or therapeutic procedures such as the monitoring of hemostasis, imaging and/or treatment of vulnerable plaques, and/or tumor imaging and/or treatment.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: April 15, 2014
    Assignee: Medibeacon, LLC
    Inventors: William L. Neumann, Richard B. Dorshow
  • Patent number: 8697033
    Abstract: In some embodiments, the invention provides modified pyrazine derivatives containing a central pyrazine ring with two secondary amine groups attached directly to the central pyrazine ring and two amino carbonyl groups attached directly to the central pyrazine ring. The secondary amine groups are terminated by alkyl groups containing from 1 to 6 carbons. The amino carbonyl groups can be terminated by a wide range of substituents including, but not limited to, alkyl and alkylene groups, polyether groups, including poly(ethylene glycol) groups, secondary and tertiary amine groups, polyhydroxylated alkyl groups, amino carbonyl groups, amino thioketone groups, and combinations thereof. In some embodiments, the invention provides modified pyrazine derivatives useful as optical agents in a wide variety of biomedical imaging procedures, including diagnostic and imaging procedures.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: April 15, 2014
    Assignee: Medibeacon, LLC
    Inventors: Amruta Poreddy, William L. Neumann
  • Publication number: 20140088097
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
  • Patent number: 8664228
    Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: March 4, 2014
    Assignee: Novartis AG
    Inventors: Stephen Paul Collingwood, Catherine Howsham, Thomas Anthony Hunt
  • Patent number: 8664392
    Abstract: Provided are compounds and compositions of general Formula IX: E1-L-Ar—X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 4, 2014
    Assignee: MediBeacon, LLC
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow
  • Publication number: 20140039189
    Abstract: The present invention relates to a novel process for the preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg KLEY, Daniel HAERLE, Guenter LINZ, Sandra STEHLE
  • Publication number: 20140039191
    Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II. X1 to X4 of Formulas I and II may be characterized as electron withdrawing groups, while Y1 to Y4 of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may capable of one or both absorbing and emanating spectral energy of at least about 400 nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
    Type: Application
    Filed: October 7, 2013
    Publication date: February 6, 2014
    Applicant: MediBeacon, LLC
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann, Dennis A. Moore
  • Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Publication number: 20130324559
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael Ross JOHNSON, William Robert THELIN, Richard C. BOUCHER
  • Publication number: 20130316981
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 28, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
  • Publication number: 20130303547
    Abstract: This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions.
    Type: Application
    Filed: July 17, 2013
    Publication date: November 14, 2013
    Inventors: Brian E. Green, David D. Anderson, Todd D. Bosse, Curt S. Cooper, Larry L. Klein, Allan C. Krueger, Daniel P. Larson, Dachun Liu, Keith F. McDaniel, Christopher E. Motter, John K. Pratt, Todd W. Rockway, Teresa A. Rosenberg, Ming C. Yeung, Hui-Ju Chen, Jason P. Shanley
  • Patent number: 8575176
    Abstract: Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: November 5, 2013
    Assignee: Parion Sciences, Inc.
    Inventor: Michael Ross Johnson
  • Publication number: 20130281464
    Abstract: Provided is a novel compound which simultaneously inhibits both NMDA receptors and ASIC1a, which are associated with neurodegenerative disease and so on, and thus is useful for the prevention and treatment of various nervous system diseases. A biguanide derivative represented by the following general formula (1), a salt thereof, or a hydrate of the derivative or the salt: wherein, X1 represents a halogen atom, R1 represents an alkyl group, an optionally substituted aryl group, or an optionally substituted aralkyl group.
    Type: Application
    Filed: December 1, 2011
    Publication date: October 24, 2013
    Applicant: NIHON UNIVERSITY
    Inventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
  • Publication number: 20130231351
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: January 23, 2013
    Publication date: September 5, 2013
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Patent number: 8492546
    Abstract: The invention relates to co-crystals and compositions each comprising VX-950 and a co-crystal former selected from the group consisting of 3-methoxy-4-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, and 2,5-dihydroxybenzoic acid. Also within the scope of this invention are methods of making and using the same.
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: July 23, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Yuegang Zhang, Patrick R. Connelly, Steve Johnston
  • Publication number: 20130178482
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Application
    Filed: June 26, 2012
    Publication date: July 11, 2013
    Applicant: Parion Sciences, Inc.
    Inventor: MICHAEL R. JOHNSON
  • Patent number: 8481734
    Abstract: Disclosed herein are pyrazine derivatives of Formula I: Formula I; wherein each of X1 and X2 is independently —CONR7R9; and each of Y1 and Y2 is independently —NR48R49; and methods of using the same. The disclosed pyrazine derivatives include those having urea, amide, sulfonamide, thiourea, and/or carbamate substituents. Among the various aspects of the present invention are pyrazine derivatives that may be detected in vivo and used in a number of medical procedures (e.g., renal function monitoring). Without being bound by a particular theory, the pyrazine derivatives described herein may be designed to be hydrophilic, thus allowing for rapid renal clearance for continuous monitoring of renal function.
    Type: Grant
    Filed: January 12, 2009
    Date of Patent: July 9, 2013
    Assignee: Medibeacon Development LLC
    Inventors: Richard B. Dorshow, John Freskos, William L. Neumann, Amruta Reddy Poreddy, Raghavan Rajagopalan
  • Patent number: RE47255
    Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
    Type: Grant
    Filed: August 3, 2017
    Date of Patent: February 26, 2019
    Assignee: MediBeacon, Inc.
    Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann