Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
  • Pyrazinoylguanidine compounds for use as taste modulators
    Patent number: 8288391
    Abstract: The present invention relates to blocking salt taste using compounds of Formula I as defined herein.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: October 16, 2012
    Assignee: Parion Sciences, Inc.
    Inventors: Michael R. Johnson, Richard C. Boucher, Andrew J. Hirsh
  • PHARMACEUTICAL CO-CRYSTALS OF QUERCETIN
    Publication number: 20120258170
    Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 11, 2012
    Applicant: Nutracryst Therapeutics Private Limited
    Inventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
  • SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20120252809
    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 24, 2012
    Publication date: October 4, 2012
    Applicant: SANOFI
    Inventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
  • METHODS OF REDUCING THE PROLIFERATION AND VIABLILITY OF MICROBIAL AGENTS
    Publication number: 20120245107
    Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Inventors: William Henry, Henk-Andre Kroon, Linda Summerton
  • Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
    Patent number: 8268834
    Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: September 18, 2012
    Assignee: Novartis AG
    Inventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
  • Stable bortezomib formulations
    Patent number: 8263578
    Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: September 11, 2012
    Assignee: InnoPharma, Inc.
    Inventors: Kumaresh Soppimath, Satish Pejaver, Kanaiyalal R. Patel, Lakkaraju Dasaradhi, Rama Sodum, Hari Desu, Navneet Puri
  • AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE
    Publication number: 20120225891
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: March 22, 2012
    Publication date: September 6, 2012
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • HETEROARYL BENZAMIDES, COMPOSITIONS AND METHODS OF USE
    Publication number: 20120225862
    Abstract: Provided are certain heteroaryl benzamides, compositions, and methods of their manufacture and use.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 6, 2012
    Applicants: AUCKLAND UNIVSERVICES LIMITED, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Patrick D. Sutphin, Denise A. Chan, Sandra Turcotte, William Alexander Denny, Michael Patrick Hay, Anna Claire Giddens, Muriel Marie Bonnet, Amato J. Giaccia
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • NEW CAPPED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS
    Publication number: 20120220606
    Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: May 9, 2012
    Publication date: August 30, 2012
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael R. JOHNSON, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
  • N-CYCLOPROPYL-3-FLUORO-5-[3-[[1-[2-[2- [(2-HYDROXETHYL)AMINO] ETHOXY]PHENYL] CYCLOPROPYL] AMINO]-2-OXO- 1 (2H)-PYRAZINYL]-4-METHYL-BENZAMIDE, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AND THEIR USES
    Publication number: 20120214822
    Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: March 6, 2012
    Publication date: August 23, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
  • Lipidomic Biomarkers of Diabetes
    Publication number: 20120214821
    Abstract: The invention, in some aspects, relates to methods for predicting a subject's risk of developing a glucose-related metabolic disorder, e.g., diabetes. In some aspects, the invention relates to methods for selecting and monitoring a treatment for a glucose-related metabolic disorder, e.g., diabetes.
    Type: Application
    Filed: January 20, 2012
    Publication date: August 23, 2012
    Applicants: THE BROAD INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION
    Inventors: Robert Gerszten, Thomas Wang, Eugene Rhee, Clary Clish
  • Organic Compounds
    Publication number: 20120214800
    Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and Y are defined in the description, to compositions and use of the compounds in the treatment of inflammatory and allergic conditions.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Inventors: Ian Bruce, Emma Budd, Lee Edwards, Catherine Howsham
  • ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND MEDICINAL APPLICATIONS
    Publication number: 20120214735
    Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
  • Pyrazine derivatives as ENAC blockers
    Patent number: 8236808
    Abstract: A compound of Formula I or a hydrate or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 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: June 8, 2009
    Date of Patent: August 7, 2012
    Assignee: Novartis AG
    Inventors: Stephen Paul Collingwood, Nicholas James Devereux, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt
  • BICYCLO[3.2.1]OCTYL AMIDE DERIVATIVES AND USES OF SAME
    Publication number: 20120190686
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: December 22, 2011
    Publication date: July 26, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Reverse Amide Compounds As Protein Deacetylase Inhibitors And Methods Of Use Thereof
    Publication number: 20120190693
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 26, 2012
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20120178756
    Abstract: The present invention relates to pyrazine and pyridine 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 I: wherein the variables are as defined herein.
    Type: Application
    Filed: May 12, 2011
    Publication date: July 12, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Joanne Pinder, Stephen Young, Philip Michael Reaper
  • NOVEL GLUCOKINASE ACTIVATORS AND PROCESSES FOR THE PREPARATION THEREOF
    Publication number: 20120178765
    Abstract: The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes.
    Type: Application
    Filed: September 17, 2010
    Publication date: July 12, 2012
    Applicant: YUHAN CORPORATION
    Inventors: Won-Hui Yi, Tae-Dong Han, Koo-Yeon Lee, Young-Hwan Kim, Eun-Hye Jung, Dong-Hoon Lee, Yoo-Hoi Park, Kyung-Nan Min, Jae-Gyu Kim, Byung-Kyu Lee
  • Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
    Patent number: 8217048
    Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: July 10, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
  • Capped pyrazinoylguanidine sodium channel blockers
    Patent number: 8211895
    Abstract: The present application relates to pyrazinoyl guanidine sodium channel blockers having the structure: or a pharmaceutically acceptable salt thereof, where the structural variables are as defined herein. The present invention also relates pharmaceutical compositions comprising the sodium channel blockers and their use in methods of treatment, including the treatment of cardiovascular disease, cystic fibrosis, and chronic bronchitis and in the rehydration of mucosal surfaces and promotion of mucus clearance in a patient.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: July 3, 2012
    Assignee: Parion Sciences, Inc.
    Inventors: Michael R. Johnson, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
  • Glucagon Receptor Modulators
    Publication number: 20120165343
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Applicant: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • OXIME COMPOUNDS
    Publication number: 20120157476
    Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Application
    Filed: December 8, 2011
    Publication date: June 21, 2012
    Inventors: Paul Hebeisen, Stephan Roever
  • PYRAZINAMIDE FOR IMMUNOSTIMULATION AND THE TREATMENT OF LEISHMANIASES
    Publication number: 20120157396
    Abstract: Applicants claim the use of a pyrazine compound of formula I: or a salt thereof, for treating or preventing leishmaniases, and diseases and disorders caused by Trypanosoma cruzi or Trypanosoma brucei, and for inducing immunostimulation.
    Type: Application
    Filed: November 21, 2011
    Publication date: June 21, 2012
    Applicants: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK, UNITED STATES GOVERMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIR, CORNELL UNIVERSITY
    Inventors: John T. WELCH, Susana MENDEZ, Michael H. CYNAMON
  • Amido Compounds
    Publication number: 20120149718
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Application
    Filed: December 13, 2011
    Publication date: June 14, 2012
    Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
  • Sodium channel blockers
    Patent number: 8198286
    Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: June 12, 2012
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCERS AND PATHOGENIC INFECTIONS
    Publication number: 20120141491
    Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.
    Type: Application
    Filed: August 9, 2010
    Publication date: June 7, 2012
    Applicant: University of Florida Research Foundation Inc.
    Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
  • Substituted Esters as Cannabinoid-1 Receptor Modulators
    Publication number: 20120135975
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.
    Type: Application
    Filed: May 14, 2007
    Publication date: May 31, 2012
    Applicant: MERCK & CO., INC.
    Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
  • Substituted pyrazines as DGAT-1 inhibitors
    Patent number: 8188092
    Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: May 29, 2012
    Assignee: AstraZeneca AB
    Inventors: Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
  • Pyrazinecarboxamide derivatives as HDL-cholesterol raising agents
    Patent number: 8188093
    Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: May 29, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
  • COMBINATION TREATMENT FOR DIABETES MELLITUS
    Publication number: 20120129817
    Abstract: The subject matter of this application is directed to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1.
    Type: Application
    Filed: February 1, 2012
    Publication date: May 24, 2012
    Applicant: NYCOMED GMBH
    Inventors: Thomas KLEIN, Anja BLASER, Bettina RUDOLPH, Ulrich KAUTZ, Jens SELIGE, Wolfgang KROMER
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20120122884
    Abstract: The present invention relates to pyrazine and pyridine 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 IV: wherein the variables are as defined herein.
    Type: Application
    Filed: May 12, 2011
    Publication date: May 17, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Anisa Nizarali Virani, Philip Michael Reaper
  • RAPIDLY DISINTEGRATING SOLID ORAL DOSAGE FORM
    Publication number: 20120114754
    Abstract: Disclosed is a rapidly disintegrating solid oral dosage form of a poorly soluble active ingredient and at least one pharmaceutically acceptable water-soluble or water-dispersible excipient, wherein the poorly soluble active ingredient particles have an average diameter, prior to inclusion in the dosage form, of less than about 2000 nm. The dosage form of the invention has the advantage of combining rapid presentation and rapid dissolution of the active ingredient in the oral cavity.
    Type: Application
    Filed: November 8, 2011
    Publication date: May 10, 2012
    Inventors: Rajeev A. Jain, Stephen B. RUDDY, Kenneth Iain CUMMING, Maurice Joseph Anthony CLANCY, Janet Elizabeth CODD
  • PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
    Publication number: 20120108592
    Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 3, 2012
    Inventors: J. Edward Semple, Jean-Francois Rossignol
  • INHIBITORS OF INTRACELLULAR UROKINASE PLASMINOGEN ACTIVATOR AND METHODS OF USE THEREOF
    Publication number: 20120108494
    Abstract: The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the compositions for treating cancer and for delivering an amiloride conjugate into cancer cells in a subject in need thereof.
    Type: Application
    Filed: August 1, 2008
    Publication date: May 3, 2012
    Applicant: The Regents of the University of California
    Inventors: Fredric A. Gorin, Michael H. Nantz
  • 5, 6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS
    Publication number: 20120108611
    Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
    Type: Application
    Filed: December 29, 2011
    Publication date: May 3, 2012
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Gilbert Lassalie, Frédéric Petit, Jean Claude Vernieres, Philip Janiak
  • Carbamoyl Compounds as DGAT1 Inhibitors 190
    Publication number: 20120108602
    Abstract: DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?0; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 3, 2012
    Applicant: AstraZeneca AB
    Inventors: Udo Andreas BAUER, Jonas Gunnar BARLIND, Petra JOHANNESSON, Jan Magnus JOHANSSON, Alexander Tobias NOESKE, Annika Ulrika PETERSSON, Alan Martin BIRCH, Roger John BUTLIN, Clive GREEN, Andrew LEACH, Ragnar HOVLAND
  • Phenyl substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity
    Patent number: 8163758
    Abstract: Provided is class of sodium channel blockers. One example of such a compound is shown by the following formula: The compounds are useful for promoting hydration of mucosal surfaces and treating a variety of disease conditions.
    Type: Grant
    Filed: June 11, 2007
    Date of Patent: April 24, 2012
    Assignee: Parion Sciences, Inc.
    Inventors: Michael Ross Johnson, Andrew J. Hirsh, Richard C. Boucher, Jianzhong Zhang
  • Compositions Including 6-Aminohexanoic Acid Derivatives As HDAC Inhibitors
    Publication number: 20120094971
    Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
    Type: Application
    Filed: September 3, 2009
    Publication date: April 19, 2012
    Applicant: REPLIGEN CORPORATION
    Inventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
  • Cyclic amide and ester pyrazinoylguanidine sodium channel blockers
    Patent number: 8143256
    Abstract: The present invention provides compounds represented by formula (I): where the structural variables are defined herein. The compound of the present invention are useful as sodium channel blockers.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: March 27, 2012
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS
    Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • COMPOUNDS AND THEIR USES 708
    Publication number: 20120065214
    Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 26, 2008
    Publication date: March 15, 2012
    Applicant: AstraZeneca AB
    Inventors: Stephen BROUGH, Richard Evans, Timothy Jon Luker, Piotr Raubo
  • Poly aromatic pyrazinoylguanidine sodium channel blockers
    Patent number: 8124607
    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: February 26, 2009
    Date of Patent: February 28, 2012
    Assignee: Parion Sciences, Inc.
    Inventor: Michael Ross Johnson
  • Compositions and Methods for Treating Disorders Associated with Salt or Fluid Retention
    Publication number: 20120040025
    Abstract: Methods for reducing the risk of or treating a disorder associated with fluid and/or salt retention in a patient are described. The methods include administering to the patient an agent selected from: a) an agent that reduces sodium absorption in the intestine; b) an agent that increases anion secretion in the intestine; or c) an agent that both reduces sodium absorption in the intestine and increases anion secretion in the intestine.
    Type: Application
    Filed: April 23, 2008
    Publication date: February 16, 2012
    Inventors: Mark G. Currie, Daniel P. Zimmer
  • PHARMACEUTICAL COMPOSITIONS
    Publication number: 20120040898
    Abstract: A pharmaceutical composition comprising a combination of (A) a 1-thio-D-glucitol compound represented by the general formula (I) and (B) at least one member of the group consisting of biguanides, insulin secretagogues, insulin sensitizers, insulins, dipeptidyl peptidase IV inhibitors, ?-glucosidase inhibitors, and GLP-1 mimetics, has superior efficacy in preventing or treating diabetes mellitus, diseases associated with diabetes mellitus, or complications of diabetes mellitus and yet it causes no appreciable side effects.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 16, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Teisuke Takahashi, Saeko Uchida
  • 3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
    Patent number: 8114871
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: February 14, 2012
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • 2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial
    Patent number: 8114881
    Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: February 14, 2012
    Assignee: AstraZeneca AB
    Inventors: Peter Hansen, Marianne Ivarsson, Karolina Lawitz, Hans Lönn, Antonios Nikitidis, Asim Ray
  • Pharmaceutical dosage form comprising nifedipine or nisoldipine and an angiotensin II antagonist and/or a diuretic
    Publication number: 20120034272
    Abstract: The present invention relates to a pharmaceutical dosage form comprising an active ingredient combination of nifedipine or nisoldipine and at least one angiotensin II antagonist and/or at least one diuretic, characterized in that nifedipine or nisoldipine is released in the body in a controlled (modified) manner and the angiotensin II antagonist and/or the diuretic is released rapidly (immediate release (IR)), and also to processes for their preparation, to their use as medicaments and to their use for the prophylaxis, secondary prophylaxis or treatment of disorders.
    Type: Application
    Filed: November 19, 2009
    Publication date: February 9, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexander Kuhl, Erich Brendel, Frank Bröcker, Adrian Funke, Andreas Ohm, Dennis Kvesic, Thomas Volkmer
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20120035408
    Abstract: The present invention relates to pyrazine and pyridine 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 V: wherein the variables are as defined herein.
    Type: Application
    Filed: May 12, 2011
    Publication date: February 9, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Stephen Clinton Young, Pierre-Henri Storck, Anisa Nizarali Virani, Phillip Michael Reaper, Joanne Pinder
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20120035407
    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: Application
    Filed: May 12, 2011
    Publication date: February 9, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, Ronald Marcellus Alphonsus Knegtel, Michael O'Donnell, Philip Michael Reaper