Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
  • Crystalline rosuvastatin calcium and compositions thereof for treatment of hyperlipidaemia
    Patent number: 7994178
    Abstract: The present invention provides a crystalline form of rosuvastatin calcium characterized by an X-ray powder diffraction pattern having peaks at about 4.7, 19.4 and 22.3° 2?±0.2° 2?. The crystalline form of the invention may be further characterized by a DSC thermogram with an endotherm at about 132° C. and another broad endotherm at about 220° C. to about 240° C., and a TGA thermogram showing a weight loss of about of 3 to about 5 percent up to about 100° C. The invention also provides a pharmaceutical composition comprising the crystalline rosuvastatin calcium, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: August 9, 2011
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Shlomit Wizel, Valerie Niddam-Hildesheim, Shalom Shabat
  • Carbamoyl compounds as DGAT1 inhibitors 190
    Patent number: 7994179
    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, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?O; 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: Grant
    Filed: December 19, 2008
    Date of Patent: August 9, 2011
    Assignee: AstraZeneca AB
    Inventors: Petra Johannesson, Jan Magnus Johansson, Annika Ulrika Petersson, Alan Martin Birch, Roger John Butlin
  • Pyrazine kinase inhibitors
    Patent number: 7989456
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: August 2, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Julian M. C. Golec
  • HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION, MEDICAMENTS COMPRISING THESE COMPOUNDS, AND THE USE THEREOF
    Publication number: 20110183998
    Abstract: Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes.
    Type: Application
    Filed: July 7, 2009
    Publication date: July 28, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard Zoller, Dieter Schmoll, Marco Mueller, Guido Haschke, Ingo Focken
  • 2-Aminocarbonyl Substituted Piperazine or Diaza-Cyclic Compounds as Apoptosis Protein Inhibitors (Iap) Modulators
    Publication number: 20110183955
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.
    Type: Application
    Filed: March 21, 2011
    Publication date: July 28, 2011
    Applicant: NOVARTIS AG
    Inventors: Robert ECKL, Roswitha TAUBE, Michael ALMSTETTER, Michael THORMANN, Andreas TREML, Christopher STRAUB, Zhuoliang CHEN
  • SIR2 REGULATION
    Publication number: 20110178102
    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: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • THERAPEUTIC AGENT FOR CHRONIC RENAL FAILURE
    Publication number: 20110178103
    Abstract: The present invention aims to provide a therapeutic agent for chronic renal failure, comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof. That is, the present invention provides provision of a drug comprising as an effective ingredient a compound represented by General Formula (1) or a pharmaceutically acceptable salt thereof, which drug is useful not only for amelioration of renal function, but also for amelioration of anemia, activation of SOD and excretion of uremic substances.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 21, 2011
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Fuko Matsuda, Katsuhiko Iseki, Hajimu Kurumatani, Mitsuko Miyamoto
  • Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
    Patent number: 7981898
    Abstract: The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a subject in need of increased mucociliary clearance and mucosal hydration.
    Type: Grant
    Filed: September 7, 2007
    Date of Patent: July 19, 2011
    Assignee: Parion Sciences, Inc.
    Inventors: Michael Ross Johnson, Richard C. Boucher, Andrew J. Hirsh
  • CATHEPSIN S INHIBITORS
    Publication number: 20110166141
    Abstract: Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.
    Type: Application
    Filed: December 6, 2010
    Publication date: July 7, 2011
    Applicants: DCB-USA, LLC, National Tsing Hua University, National Health Research Institutes
    Inventors: Chun-Cheng Lin, Wun-Shaing Wayne Chang, Biing-Jiun Uang, Jang-Yang Chang, Jo-Chun Chen, Hsing-Pang Hsieh
  • HETEROCYCLIC CARBOXAMIDE COMPOUNDS
    Publication number: 20110166161
    Abstract: This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 7, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Takeshi Terasawa, Shinji Shigenaga, Shinji Itoh, Jun Maeda, Hideyuki Watanabe, Satoshi Kubo, Noe Iahii
  • Modulators of glucocorticoid receptor, AP-1, and/or NF-?B activity and use thereof
    Patent number: 7968577
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
  • Organic compounds
    Publication number: 20110152261
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.
    Type: Application
    Filed: August 5, 2009
    Publication date: June 23, 2011
    Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Rooney, Emily Stanley, Lilya Sviridenko
  • Promoting Cycling of ApoE4 Isoform
    Publication number: 20110136832
    Abstract: Cycling of ApoE4 isoform is promoted in a person in need thereof by contacting the person with an effective amount of a pharmaceutically-acceptable modulator of intracellular ApoE4 transport vesicle pH.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: Joachim Herz, Xunde Xian, Yuan Yang
  • COMPOSITIONS AND METHODS FOR PROTECTING SENSORY HAIR CELLS
    Publication number: 20110135756
    Abstract: The invention provides compounds, compositions and methods that can be used for the attenuation of damage to sensory hair cells and symptoms thereof. More particularly, the invention identifies drugs that can be used to protect sensory hair cells from ototoxic medications, noise-induced damage and age-related loss.
    Type: Application
    Filed: December 8, 2010
    Publication date: June 9, 2011
    Applicants: University of Washington, Fred Hutchinson Cancer Research Center
    Inventors: Kelly N. Owens, Anna L. Corke, Henry C. Ou, Edwin W. Rubel, David W. Raible, Julian A. Simon
  • N-2-(Hetero)Arylethylcarboxamide Derivative, and Pest-Controlling Agent Comprising the Same
    Publication number: 20110136831
    Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.
    Type: Application
    Filed: March 20, 2007
    Publication date: June 9, 2011
    Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Haseba, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
  • SUBSTITUTED N-OXIDE PYRAZINE DERIVATIVES
    Publication number: 20110136828
    Abstract: N-oxide pyrazine derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: R1. R2, R3, R4, and R5 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 9, 2011
    Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
  • Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
    Patent number: 7956059
    Abstract: The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where the structural variables are defined herein. The compounds are useful as, for example, sodium channel blockers.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: June 7, 2011
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • INHIBITORS OF SERINE PROTEASES, PARTICULARLY HEPATITIS C VIRUS NS3 PROTEASE
    Publication number: 20110112114
    Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.
    Type: Application
    Filed: June 9, 2010
    Publication date: May 12, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
  • Methods of Treating Pulmonary Hypertension
    Publication number: 20110112094
    Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.
    Type: Application
    Filed: January 14, 2011
    Publication date: May 12, 2011
    Inventor: Arthur T. Sands
  • Haloalkyl-substituted amides as insecticides and acaricides
    Publication number: 20110105532
    Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
    Type: Application
    Filed: October 27, 2010
    Publication date: May 5, 2011
    Applicant: Bayer CropScience AG
    Inventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
  • COMPOSITIONS AND METHODS FOR IDENTIFICATION OF SUBSPECIES CHARACTERISTICS OF MYCOBACTERIUM TUBERCULOSIS
    Publication number: 20110105531
    Abstract: The present invention provides compositions, kits and methods for rapid genotyping of strains of Mycobacterium tuberculosis by molecular mass and base composition analysis. Drug-resistant strains of Mycobacterium tuberculosis may be identified in human clinical samples and as such, provide for methods of treatment of humans infected with drug resistant strains of Mycobacterium tuberculosis.
    Type: Application
    Filed: June 23, 2008
    Publication date: May 5, 2011
    Applicant: IBIS BIOSCIENCES, INC.
    Inventors: Christian Massire, Rangarajan Sampath, Lawrence B. Blyn, David J. Ecker
  • NOVEL COMPOUNDS, USE AND PREPARATION THEREOF
    Publication number: 20110098310
    Abstract: The present invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as defined herein, which can act as inhibitors of protein kinases, specially the Fms-like tyrosine kinase 3 (FLT3). The invention also relates to the use of the compounds in therapy, pharmaceutical compositions comprising the compounds and the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of hematological malignancies, such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative disorders, other proliferative disorders like cancer, autoimmune disorders and skin disorders like psoriasis and atopic dermatitis.
    Type: Application
    Filed: January 28, 2009
    Publication date: April 28, 2011
    Inventors: Annika Jenmalm Jensen, Fredrik Lehmann, Bjorn M. Nilsson, Erik Nordling, Vendela Parrow
  • COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
    Publication number: 20110098311
    Abstract: The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
    Type: Application
    Filed: October 22, 2010
    Publication date: April 28, 2011
    Applicant: Vertex Pharmaceuticals Incorported
    Inventors: Fredrick F. Van Goor, William Lawrence Burton
  • ()-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile: a pyrazinone modulator of corticotropin-releasing factor receptor activity
    Patent number: 7932256
    Abstract: The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: April 26, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, Vivekananda M. Vrudhula, Joanne J. Bronson
  • Marine actinomycete taxon for drug and fermentation product discovery
    Patent number: 7928138
    Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: April 19, 2011
    Assignee: Regents of the University of California
    Inventors: Robert H. R. Feling, William Fenical, Paul R. Jensen, Tracy J. Mincer
  • Purine receptor inhibition as a therapeutic strategy in spinal cord and brain
    Patent number: 7923448
    Abstract: The present invention is directed to a method of treating a subject with acute spinal cord injury by administering a purine receptor antagonist to the subject under conditions effective to treat spinal cord injury. The purine receptor antagonist inhibits P2X purine receptor activation. The inhibition of P2X purine receptor activation can also be used in conjunction with methods of treating a subject with spinal cord ischemia resulting from stroke or vascular insult, interruption, or mechanical injury, treating a subject with ischemic or traumatic insults of brain tissue in regions expressing P2X receptors, and for inhibiting ATP-triggered brain or spinal cord cell death.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: April 12, 2011
    Assignees: Cornell Research Foundation, Inc., New York Medical College
    Inventors: Maiken Nedergaard, Steven A. Goldman
  • FATTY ACID ACIPIMOX DERIVATIVES AND THEIR USES
    Publication number: 20110082156
    Abstract: The invention relates to fatty acid acipimox derivatives; compositions comprising an effective amount of a fatty acid acipimox derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid acipimox derivative.
    Type: Application
    Filed: October 5, 2010
    Publication date: April 7, 2011
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Analogs of dehydrophenylahistins and their therapeutic use
    Patent number: 7919497
    Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
    Type: Grant
    Filed: September 20, 2006
    Date of Patent: April 5, 2011
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi
  • COMPOUNDS FOR MODULATING RNA BINDING PROTEINS AND USES THEREFOR
    Publication number: 20110077250
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Application
    Filed: June 25, 2010
    Publication date: March 31, 2011
    Inventor: Sean RYDER
  • CICLETANINE IN COMBINATION WITH ORAL ANTIDIABETIC AND/OR BLOOD LIPID-LOWERING AGENTS AS A COMBINATION THERAPY FOR DIABETES AND METABOLIC SYNDROME
    Publication number: 20110071111
    Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and an oral antidiabetic agent for treating and/or preventing complications (including microalbuminuria, nephropathies, retinopathies and other complications) in patients with diabetes or metabolic syndrome.
    Type: Application
    Filed: July 15, 2010
    Publication date: March 24, 2011
    Inventors: Benson M. Fong, Glenn V. Cornett
  • ERG CHANNEL OPENERS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS
    Publication number: 20110071164
    Abstract: This invention relates to the use of ERG channel openers for the treatment of cardiac arrhythmias, and to the use of specific compounds for such treatment. In a separate aspect the invention provides novel compounds useful as ERG channel openers.
    Type: Application
    Filed: November 9, 2010
    Publication date: March 24, 2011
    Inventors: Søren Peter OLESEN, Morten Grunnet, Palle Christophersen, Dorte STRØBÆK, Joachim Demnitz, Rie S. Hansen
  • BENZENE OR THIOPHENE DERIVATIVE AND USE THEREOF AS VAP-1 INHIBITOR
    Publication number: 20110059957
    Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 29, 2009
    Publication date: March 10, 2011
    Applicant: R-TECH UENO, LTD.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
  • MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20110053958
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: March 17, 2009
    Publication date: March 3, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • CAPPED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS
    Publication number: 20110046158
    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: November 4, 2010
    Publication date: February 24, 2011
    Applicant: PARION SCIENCES, Inc.
    Inventors: Michael R. JOHNSON, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
  • SOLUBLE EPOXIDE HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
    Publication number: 20110039860
    Abstract: Compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof is disclosed. The compounds are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: April 27, 2009
    Publication date: February 17, 2011
    Inventors: Cangming Yang, Zhicai Wu, Rui Liang, Steven L Colletti
  • NANOPARTICLE CARRIERS FOR DRUG ADMINISTRATION AND PROCESS FOR PRODUCING SAME
    Publication number: 20110033550
    Abstract: The invention provides a process for the production of nanoparticle carriers for drug delivery, said nanoparticles being produced by preparing a double emulsion of water-oil-water including one or more polymer which forms the basis of the nanoparticle carrier, blending the drug to be delivered into one of the emulsion phases, doping either the oil-phase or the outer-water phase with a carbohydrate, and spray drying the emulsion to form nanoparticles of a narrow particle size distribution of 100 nm to 1000 nm, which nanoparticles are substantially spherical.
    Type: Application
    Filed: August 17, 2010
    Publication date: February 10, 2011
    Applicant: CSIR
    Inventor: Lonji Kalombo
  • Certain substituted pyrazinones
    Patent number: 7884108
    Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/ or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: February 8, 2011
    Assignee: CGI Pharmaceuticals, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
  • Pyrazolospiroketone Acetyl-CoA Carboxylase Inhibitors
    Publication number: 20110028390
    Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: May 18, 2009
    Publication date: February 3, 2011
    Applicant: PFIZER, INC.
    Inventors: Jeffrey W. Corbett, Richard Elliott, Kevin Freeman-Cook, David A. Griffith, Dennis P. Phillion
  • ARYL SULFONAMIDES
    Publication number: 20110021523
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: October 1, 2010
    Publication date: January 27, 2011
    Applicant: CHEMOCENTRYX, INC.
    Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
  • GPR 119 MODULATORS
    Publication number: 20110020460
    Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: June 4, 2010
    Publication date: January 27, 2011
    Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Hetero substituted sodium channel blockers
    Patent number: 7875619
    Abstract: The present invention relates to group of butylphenyl-pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces.
    Type: Grant
    Filed: February 18, 2004
    Date of Patent: January 25, 2011
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • FIBROSIS INHIBITOR
    Publication number: 20110015211
    Abstract: [Object] The main object of the present invention is to provide a fibrosis inhibitor. [Solving Means] The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
    Type: Application
    Filed: February 26, 2009
    Publication date: January 20, 2011
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventors: Koji Murakami, Takuya Toramoto
  • TARGETING CDK4 AND CDK6 IN CANCER THERAPY
    Publication number: 20110009353
    Abstract: The invention involves methods of inhibiting the cancer cell cycle to make cancer cells more susceptible to chemotherapeutic agents. In particular, inhibition of CDK4 and/or CDK6 inhibits cell cycle progression in cancer cells. When combined with chemotherapy such cell cycle inhibition can effectively treat even aggressive cancer types that are drug-resistant and intractable to most chemotherapies.
    Type: Application
    Filed: October 1, 2008
    Publication date: January 13, 2011
    Inventors: Selina Chen-Kiang, Maurizio Di Liberto, Xiangao Huang
  • Therapeutic Treatment Of Wounds
    Publication number: 20110009332
    Abstract: The present disclosure relates to compositions and methods for treating wounded skin and/or increasing the mechanical strength of wounded skin through the administration of an effective amount of a proteasome inhibitor to such wounded skin.
    Type: Application
    Filed: June 10, 2010
    Publication date: January 13, 2011
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventor: Jorge Gianny ROSSINI
  • PHENYL SUBSTITUTED PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS POSSESSING BETA AGONIST ACTIVITY
    Publication number: 20110008268
    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: June 11, 2007
    Publication date: January 13, 2011
    Applicant: PARION SCIENCES, Inc.
    Inventors: Michael Ross Johnson, Andrew J. Hirsh, Richard C. Boucher, Jianzhong Zhang
  • 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS
    Publication number: 20110009426
    Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
    Type: Application
    Filed: August 6, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
  • Capped pyrazinoylguanidine sodium channel blockers
    Patent number: 7868010
    Abstract: The invention relates to substituted pyrazinoylguanidine compounds. These compounds are useful as sodium channel blockers, and may be effective in treating a variety of conditions including chronic bronchitis and cystic fibrosis.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: January 11, 2011
    Assignee: Parion Sciences, Inc.
    Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
  • NEW CAPPED Pyrazinoylguanidine SODIUM CHANNEL BLOCKERS
    Publication number: 20110003832
    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: September 7, 2010
    Publication date: January 6, 2011
    Applicant: PARION SCIENCES, Inc.
    Inventors: Michael R. JOHNSON, Bruce F. Molino, Bruce Sargent, Jianzhong Zhang
  • BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE
    Publication number: 20100331328
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Application
    Filed: February 19, 2009
    Publication date: December 30, 2010
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Ian Collins, John Charles Reader, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Michael Cherry
  • AMINOALCOHOL LIPIDOIDS AND USES THEREOF
    Publication number: 20100331234
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 30, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson