Nitrogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/407)
-
Patent number: 11691974Abstract: Disclosed in the present invention is a novel compound as FLT3 and AXL inhibitors. Specifically, disclosed are a compound represented by formula (I) and a pharmacologically acceptable salt thereof.Type: GrantFiled: September 27, 2019Date of Patent: July 4, 2023Assignee: MEDSHINE DISCOVERY INC.Inventors: Xiangyu Fu, Charles Z. Ding, Lihong Hu, Jianyu Lu, Wen Jiang, Jian Li, Shuhui Chen
-
Patent number: 11602570Abstract: The present disclosure relates to systems and methods for determining the renal glomerular filtration rate or assessing the renal function in a patient in need thereof. The system includes a computing device, a power supply, one or more sensors, and at least one tracer agent that fluoresces when exposed to electromagnetic radiation. The electromagnetic radiation is detected using the sensors, and the rate in which the fluorescence decreases in the patient is used to calculate the renal glomerular filtration rate in the patient.Type: GrantFiled: October 26, 2018Date of Patent: March 14, 2023Assignee: MediBeacon Inc.Inventors: Martin P. Debreczeny, Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann, Thomas E. Rogers
-
Patent number: 10898591Abstract: 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: GrantFiled: November 25, 2019Date of Patent: January 26, 2021Assignee: MediBeacon Inc.Inventors: Richard B. Dorshow, Thomas E. Rogers
-
Patent number: 9868719Abstract: 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: GrantFiled: August 25, 2014Date of Patent: January 16, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: 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: 9480687Abstract: 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: GrantFiled: July 21, 2015Date of Patent: November 1, 2016Assignee: MEDIBEACON, INC.Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
-
Patent number: 9382246Abstract: 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: GrantFiled: December 3, 2014Date of Patent: July 5, 2016Assignee: Pharmacyclics LLCInventors: Zhaozhong J. Jia, Wei Chen, William D. Thomas
-
Publication number: 20150147277Abstract: 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: ApplicationFiled: November 11, 2014Publication date: May 28, 2015Inventors: Richard B. Dorshow, Steven J. Hanley, Phillip I. Tarr
-
Patent number: 9029382Abstract: 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: GrantFiled: December 13, 2013Date of Patent: May 12, 2015Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
-
Publication number: 20150099764Abstract: 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: ApplicationFiled: December 9, 2014Publication date: April 9, 2015Applicant: PARION SCIENCES, INC.Inventors: Michael Ross JOHNSON, William Robert Thelin, Richard C. Boucher
-
Patent number: 8980898Abstract: 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: GrantFiled: May 29, 2013Date of Patent: March 17, 2015Assignee: Parion Sciences, Inc.Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
-
Patent number: 8969336Abstract: 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: GrantFiled: May 6, 2010Date of Patent: March 3, 2015Assignees: 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: 8962631Abstract: 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: GrantFiled: May 12, 2011Date of Patent: February 24, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper
-
Publication number: 20150051187Abstract: 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: ApplicationFiled: August 25, 2014Publication date: February 19, 2015Inventors: 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: 20150051199Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.Type: ApplicationFiled: October 31, 2012Publication date: February 19, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: 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: 20150045326Abstract: 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: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
-
Publication number: 20150031661Abstract: 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: ApplicationFiled: March 24, 2014Publication date: January 29, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: 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: 20150011535Abstract: 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: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Armin HECKEL, Joerg KLEY
-
Publication number: 20140378461Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.Type: ApplicationFiled: February 14, 2013Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
-
Patent number: 8895564Abstract: 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: GrantFiled: December 1, 2011Date of Patent: November 25, 2014Assignee: Nihon UniversityInventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
-
Patent number: 8877760Abstract: 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: GrantFiled: November 23, 2012Date of Patent: November 4, 2014Assignee: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Anjali Pandey
-
Publication number: 20140309209Abstract: 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: ApplicationFiled: November 23, 2012Publication date: October 16, 2014Inventors: Yonghong Song, Qing Xu, Zhaozhong J. Jia, Brian Kane, Shawn M. Bauer, Anjali Pandey
-
Publication number: 20140274692Abstract: 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: ApplicationFiled: October 31, 2012Publication date: September 18, 2014Applicant: Syngenta Participations AGInventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
-
Patent number: 8809340Abstract: 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: GrantFiled: March 12, 2013Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Catherine Howsham, Christian Lindenberg, Anett Perlberg, Nicola Tufilli
-
Publication number: 20140221286Abstract: 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: ApplicationFiled: September 20, 2012Publication date: August 7, 2014Inventors: Luiz Belardinelli, Arvinder Dhalla
-
Patent number: 8791260Abstract: 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: GrantFiled: October 7, 2013Date of Patent: July 29, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Joerg Kley, Daniel Haerle, Guenter Linz, Sandra Stehle
-
Patent number: 8778309Abstract: 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: GrantFiled: December 22, 2005Date of Patent: July 15, 2014Assignee: MediBeacon LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann, Dennis A. Moore
-
Patent number: 8759349Abstract: 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: GrantFiled: October 29, 2012Date of Patent: June 24, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Sara Frattini, Dieter Hamprecht, Joerg Kley
-
Publication number: 20140171447Abstract: 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: ApplicationFiled: December 13, 2013Publication date: June 19, 2014Applicant: Parion Sciences, Inc.Inventor: Michael R. Johnson
-
Publication number: 20140170244Abstract: 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: ApplicationFiled: December 13, 2013Publication date: June 19, 2014Applicant: Parion Sciences, Inc.Inventor: Michael R. Johnson
-
Publication number: 20140142118Abstract: 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: ApplicationFiled: June 27, 2012Publication date: May 22, 2014Applicant: PARION SCIENCES, INC.Inventor: Michael Ross Johnson
-
Publication number: 20140135329Abstract: 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: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
-
Publication number: 20140135328Abstract: 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: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
-
Patent number: 8722685Abstract: 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: GrantFiled: January 4, 2012Date of Patent: May 13, 2014Assignee: Medibeacon, LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
-
Patent number: 8703100Abstract: 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: GrantFiled: December 17, 2009Date of Patent: April 22, 2014Assignee: Medibeacon, LLCInventors: Amruta Poreddy, William L. Neumann
-
Patent number: 8697033Abstract: 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: GrantFiled: December 17, 2009Date of Patent: April 15, 2014Assignee: Medibeacon, LLCInventors: Amruta Poreddy, William L. Neumann
-
Patent number: 8697871Abstract: 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: GrantFiled: November 13, 2012Date of Patent: April 15, 2014Assignee: Medibeacon, LLCInventors: William L. Neumann, Richard B. Dorshow
-
Publication number: 20140088097Abstract: 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: ApplicationFiled: September 23, 2013Publication date: March 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
-
Patent number: 8664228Abstract: 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: GrantFiled: May 11, 2009Date of Patent: March 4, 2014Assignee: Novartis AGInventors: Stephen Paul Collingwood, Catherine Howsham, Thomas Anthony Hunt
-
Patent number: 8664392Abstract: 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: GrantFiled: January 6, 2012Date of Patent: March 4, 2014Assignee: MediBeacon, LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow
-
Publication number: 20140039191Abstract: 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: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: MediBeacon, LLCInventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann, Dennis A. Moore
-
Publication number: 20140039189Abstract: 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: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Daniel HAERLE, Guenter LINZ, Sandra STEHLE
-
Publication number: 20140031348Abstract: 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: ApplicationFiled: July 9, 2013Publication date: January 30, 2014Inventors: 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: 20130324559Abstract: 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: ApplicationFiled: May 29, 2013Publication date: December 5, 2013Applicant: PARION SCIENCES, INC.Inventors: Michael Ross JOHNSON, William Robert THELIN, Richard C. BOUCHER
-
Publication number: 20130316981Abstract: 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: ApplicationFiled: May 22, 2013Publication date: November 28, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
-
Publication number: 20130303547Abstract: 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: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: 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: 8575176Abstract: 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: GrantFiled: January 18, 2012Date of Patent: November 5, 2013Assignee: Parion Sciences, Inc.Inventor: Michael Ross Johnson
-
Publication number: 20130281464Abstract: 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: ApplicationFiled: December 1, 2011Publication date: October 24, 2013Applicant: NIHON UNIVERSITYInventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
-
Publication number: 20130231351Abstract: 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: ApplicationFiled: January 23, 2013Publication date: September 5, 2013Applicant: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Patent number: 8492546Abstract: 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: GrantFiled: August 29, 2008Date of Patent: July 23, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Yuegang Zhang, Patrick R. Connelly, Steve Johnston
-
Patent number: RE47255Abstract: 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: GrantFiled: August 3, 2017Date of Patent: February 26, 2019Assignee: MediBeacon, Inc.Inventors: Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann