Nitrogen Attached Directly At 2-position By Nonionic Bonding And Sulfur Bonded Directly To The Nitrogen Patents (Class 544/297)
  • COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
    Publication number: 20110190263
    Abstract: The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
    Type: Application
    Filed: February 20, 2009
    Publication date: August 4, 2011
    Applicant: IRM LLC
    Inventors: Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Baogen Wu, Daniel Mutnick
  • AZETIDINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
    Publication number: 20110183958
    Abstract: Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis.
    Type: Application
    Filed: October 15, 2009
    Publication date: July 28, 2011
    Inventors: David Powell, Geoffrey K. Tranmer
  • PROCESS FOR THE PREPARATION OF METHYL ESTER OF ROSUVASTATIN
    Publication number: 20110184172
    Abstract: Process for the preparation of enantiomerically pure methyl ester of rosuvastatin has been developed, wherein the crude methyl ester ester is first purified by preparative chromatography, followed by crystallization.
    Type: Application
    Filed: August 1, 2008
    Publication date: July 28, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Andrej Bastarda, Rok Grahek, Martin Crnugelj
  • Process for preparing pyrimidine propenaldehyde
    Publication number: 20110178296
    Abstract: The present invention relates to an improved process for preparing (2E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-propenal of formula (I), which is an useful intermediate in the preparation of Rosuvastatin.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 21, 2011
    Inventors: Sambhu Prasad Sarma Mallela, Sakumar Nandi, Gangadhara Bhima Shankar Nangi, Rani Ananta, Sivakumaran Meenakshiunderam
  • SYNTHESIS OF STATINS
    Publication number: 20110178295
    Abstract: The process for the synthesis of statins featuring the use of an early intermediate (4R,6S)-6-(dialkoxymethyl)tetrahydro-2H-pyran-2,4-diol which already possesses the desired stereochemistry corresponding to the final statin.
    Type: Application
    Filed: April 2, 2008
    Publication date: July 21, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Zdenko Casar, Tomaz Mesar, Gregor Kopitar, Peter Mrak, Matej Oslaj
  • Benzene Sulfonamide Thiazole And Oxazole Compounds
    Publication number: 20110172215
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: May 4, 2009
    Publication date: July 14, 2011
    Inventors: George Adjabeng, Jeffrey Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
  • COMPOSITIONS AND METHODS OF USE FOR TREATING OR PREVENTING LIPID RELATED DISORDERS
    Publication number: 20110160225
    Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.
    Type: Application
    Filed: November 19, 2010
    Publication date: June 30, 2011
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Mark G. Currie, John Jeffrey Talley, Brian Cali
  • PYRROLIDINE COMPOUNDS
    Publication number: 20110152233
    Abstract: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: December 10, 2010
    Publication date: June 23, 2011
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA
    Publication number: 20110144107
    Abstract: The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
    Type: Application
    Filed: June 11, 2009
    Publication date: June 16, 2011
    Applicants: IRM LLC, DANA-FARBER CANCER INSTITUTE INC.
    Inventors: Arnab K. Chatterjee, Advait Nagle, Tao Wu, Nathanael S. Gray
  • SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME
    Publication number: 20110144066
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Application
    Filed: April 14, 2009
    Publication date: June 16, 2011
    Applicants: The Board of Regents of the University of Texas System, Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Vijay Gokhale, Garth Powis, Shuxing Zhang
  • PROCESS FOR PREPARING (4,6-DIMETHYLPYRIMIDIN-2-YL)PHENYLAMINE (PYRIMETHANIL)
    Publication number: 20110137033
    Abstract: A process for preparing (4,6-dimethylpyrimidin-2-yl)phenylamine (pyrimethanil) of the formula by reacting aniline with cyanamide in the presence of an aqueous acid to give the corresponding phenylguanidinium salt and reacting the phenylguanidinium salt with acetylacetone in the presence of an aqueous base, wherein the process is performed as a one-pot process, by not isolating the phenylguanidinium salt formed as an intermediate.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 9, 2011
    Applicant: BASF SE
    Inventors: HARALD WINSEL, Wolfgang Ladner, Ralph Busch
  • Cyclobut-3-ene-1,2,-dione inhibitors of polo-like kinases
    Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • PREPARATION METHOD OF ROSUVASTATIN CALCIUM AND ITS INTERMEDIATES
    Publication number: 20110124864
    Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.
    Type: Application
    Filed: May 27, 2009
    Publication date: May 26, 2011
    Applicant: CHANGZHOU PHARMACEUTICAL FACTORY
    Inventor: Benshun Chen
  • IMIDAZOPYRIDINES AS A NOVEL SCAFFOLD FOR MULTI-TARGETED KINASE INHIBITION
    Publication number: 20110124632
    Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Application
    Filed: October 18, 2010
    Publication date: May 26, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Nwe Y. Ba-maung, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Megumi Kawai, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang
  • QUINOXALINE AND QUINOLINE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20110105508
    Abstract: A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Application
    Filed: December 17, 2008
    Publication date: May 5, 2011
    Applicant: UCB PHARMA, S.A.
    Inventors: Daniel Rees Allen, George Martin Buckley, Roland Bürli, John Richard Davenport, Natasha Kinsella, Christopher James Lock, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Andrew James Ratcliffe, Marianna Dilani Richard, Verity Margaret Sabin, Andrew Sharpe, Laura Jane Tait, Graham John Warrelow, Sophie Caroline Williams
  • Crystalline forms of rosuvastatin calcium salt
    Patent number: 7932387
    Abstract: Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] (also known as rosuvastatin) calcium salt and hydrates can exist in new crystal forms B and C. These crystal forms provide a higher diversity on crystalline materials to optimize manufacture, formulation and biological efficiency.
    Type: Grant
    Filed: January 23, 2006
    Date of Patent: April 26, 2011
    Assignee: BASF SE
    Inventors: Fritz Blatter, Paul Adriaan Van Der Schaaf, Martin Szelagiewicz
  • PROCESS FOR PREPARING PENTANOIC DIACID DERIVATIVES
    Publication number: 20110065920
    Abstract: The present invention relates to a process for preparing pentanoic diacid derivatives useful for preparing pyrimidine derivatives, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 17, 2011
    Applicant: ratiopharm GmbH
    Inventors: Armin Boerner, Gerd Koenig, Natalia Andrushko, Vasyl Andrushko
  • ((2S,4R)-4,6-DIHYDROXYTETRAHYDRO-2H-PYRAN-2-YL)METHYL CARBOXYLATE AND PROCESS FOR THE PRODUCTION THEREOF
    Publication number: 20110046375
    Abstract: The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.
    Type: Application
    Filed: January 20, 2009
    Publication date: February 24, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Jerome Cluzeau, Zdenko Casar, Peter Mrak, Matej Oslaj, Gregor Kopitar
  • Compounds modulating c-fms and/or c-kit activity and uses therefor
    Patent number: 7893075
    Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: February 22, 2011
    Assignee: Plexxikon, Inc.
    Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Hongyao Zhu, Marika Nespi, Chao Zhang
  • Serotonin reuptake inhibitors
    Patent number: 7893261
    Abstract: A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.
    Type: Grant
    Filed: March 28, 2005
    Date of Patent: February 22, 2011
    Assignee: Baylor University
    Inventors: Kevin G. Pinney, Maria Graciela Miranda, James Michael Dorsey
  • Bisaryl-sulfonamides
    Patent number: 7893077
    Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR? or PPAR?. In particular, the compounds of the invention modulate the function of PPAR? or PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.
    Type: Grant
    Filed: November 12, 2008
    Date of Patent: February 22, 2011
    Assignee: Amgen Inc.
    Inventors: Philippe Bergeron, Christopher N. Farthing, Stuart D. Jones, John W. Liebeschuetz, Sarah E. Lively, Lawrence R. McGee, Sharon McKendry, David Sheppard, Stephen C. Young
  • COMPOUND HAVING 6-MEMBERED AROMATIC RING
    Publication number: 20110009421
    Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.
    Type: Application
    Filed: February 27, 2009
    Publication date: January 13, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masaki Setoh, Toshitake Kobayashi, Toshio Tanaka, Atsuo Baba
  • SUBSTITUTED BIARYL PIPERAZINYL-PYRIDINE ANALOGUES
    Publication number: 20110003813
    Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: February 15, 2010
    Publication date: January 6, 2011
    Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
  • Triol form of rosuvastatin and synthesis of rosuvastatin
    Patent number: 7851624
    Abstract: Provided is a rosuvastatin triol and its use as a reference standard for analysis of rosuvastatin. Also provided are methods for preparation of rosuvastatin.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: December 14, 2010
    Assignee: Teva Pharamaceutical Industries Ltd.
    Inventors: Valerie Niddam-Hildesheim, Anna Balanov, Irena Veinberg
  • Process for preparing the calcium salt of rosuvastatin
    Patent number: 7842807
    Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.
    Type: Grant
    Filed: February 13, 2009
    Date of Patent: November 30, 2010
    Assignee: AstraZeneca UK Limited
    Inventors: John Horbury, Nigel Philip Taylor
  • DIHYDROPYRIMIDINONES
    Publication number: 20100286158
    Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 11, 2010
    Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
  • (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING
    Publication number: 20100286170
    Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.
    Type: Application
    Filed: September 24, 2008
    Publication date: November 11, 2010
    Inventors: Arun K. Ghosh, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, John C. Lilly, Geoffrey M. Bilcer
  • FUNGICIDAL BICYCLIC PYRAZOLES
    Publication number: 20100273775
    Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 28, 2010
    Applicant: E.I. Du pont de Nemours and Company
    Inventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
  • PROCESS FOR MANUFACTURING ROSUVASTATIN POTASSIUM AND CRYSTALLINE AND AMORPHOUS FORMS THEREOF
    Publication number: 20100274014
    Abstract: A process of manufacturing of Rosuvastatin Potassium of formula (I) is disclosed. The process comprises the steps of (a) treating Rosuvastatin protected compound of formula (II) wherein R1 and R2 are same or different having C1-C4 carbon atom or hydrogen or R1 and R2 can combine together to afford a cyclic structure comprising a junction atom as carbon or metal atom such as Si (silicon); with an inorganic base of the kind such as herein described having potassium as cation in a suitable solvent to form Rosuvastatin potassium; (b) isolating Rosuvastatin potassium.
    Type: Application
    Filed: January 25, 2007
    Publication date: October 28, 2010
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Dhimant Jasubhai Patel, Rajiv Kumar, Virendra Kumar Agarwal
  • Arylsulfonyl naphthalene derivatives and uses thereof
    Patent number: 7799797
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, q, Ar, R1, R2 and R7 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: September 21, 2010
    Assignee: Roche Palo Alto LLC
    Inventor: Ralph New Harris, III
  • Certain pyrazoline derivatives with kinase inhibitory activity
    Patent number: 7795249
    Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: September 14, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Ruth S. Adams, Matthew Duffey, Alexandra E. Gould, Paul D. Greenspan, Bheemashankar A. Kulkarni, Tricia J. Vos
  • LINKED DIIMIDAZOLE ANTIVIRALS
    Publication number: 20100226882
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 9, 2010
    Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
  • PROCESSES FOR THE MANUFACTURE OF ROSUVASTATIN AND INTERMEDIATES
    Publication number: 20100228028
    Abstract: A process for the manufacture of a compound of formula (V), useful for making rosuvastatin, by a stereoselective aldol reaction is described. Novel intermediates and processes to make them are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: September 9, 2010
    Inventors: Michael Butters, David Kenneth Cox, Jeffrey Norman Crabb, Steven Robert Lenger, Paul Michael Murrray, Evan William Snape
  • Process for preparing phenoxypyridine derivatives
    Patent number: 7790885
    Abstract: A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.
    Type: Grant
    Filed: August 27, 2007
    Date of Patent: September 7, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mitsuo Nagai, Tomohiro Matsushima, Atsushi Kamada, Kazunori Wakasugi, Shuji Shirotori, Shinya Abe, Kazumasa Nara, Takahisa Sakaguchi
  • Crystalline Form of Bis [(E)-7-[4-(4-fluoro-phenyl)-6-isopropyl-2-[methyl(methyl-sulfonyl)amino] pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt
    Publication number: 20100222373
    Abstract: Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
    Type: Application
    Filed: November 10, 2009
    Publication date: September 2, 2010
    Applicant: AstarZeneca UK Limited
    Inventors: Rebecca Jane Booth, Peter Anthony Cittern, Jeffrey Norman Crabb, John Horbury, David Way Calvert Jones
  • Imidazopyridine Kinase Inhibitors
    Publication number: 20100216779
    Abstract: The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: May 28, 2008
    Publication date: August 26, 2010
    Inventors: Eric W. Baum, Kyle Allen Emmitte, Kevin Wayne Kuntz, Robert Anthony Mook, JR., Kristen Elizabeth Nailor, James Michael Salovich, John Brad Shotwell, Stephon Cornell Smith, Kirk Lawrence Stevens, David Edward Uehling, Alex Gregory Waterson, Mui Cheung, Ganesh S. Moorthy, Brian John Wilson
  • Tetrahydronaphthyridine derivatives and a process for preparing the same
    Patent number: 7781443
    Abstract: A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is optionally substituted heterocyclic group; R6, R7, and R8 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).
    Type: Grant
    Filed: September 27, 2006
    Date of Patent: August 24, 2010
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hitoshi Kubota, Yoshinori Nakamura, Takanori Higashijima, Yasuo Yamamoto, Kozo Oka, Shigeki Igarashi
  • PYRAZOLYLAMINOPYRIMIDINE DERIVATIVES USEFUL AS TYROSINE KINASE INHIBITORS
    Publication number: 20100210648
    Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
    Type: Application
    Filed: February 26, 2010
    Publication date: August 19, 2010
    Applicant: ASTRAZENECA R&D
    Inventors: Bin Wang, Tao Wang
  • Crystalline ammonium salts of rosuvastatin
    Patent number: 7777034
    Abstract: Provided are alkyl ammonium crystalline salts of rosuvastatin that provide for purification of rosuvastatin and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: November 24, 2004
    Date of Patent: August 17, 2010
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Valerie Niddam-Hildesheim, Judith Aronhime, Kobi Chen
  • DIASTEREOMERIC PURIFICATION OF ROSUVASTATIN
    Publication number: 20100197916
    Abstract: The invention relates to diastereomerically pure rosuvastatin and processes for preparing diastereomerically pure rosuvastatin and its intermediates.
    Type: Application
    Filed: February 2, 2010
    Publication date: August 5, 2010
    Inventors: Valerie NIDDAM-HILDESHEIM, Natalia SHENKAR, Kobi CHEN, Anna BALANOV
  • PYRIMIDINE DERIVATIVES AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS
    Publication number: 20100190811
    Abstract: The invention provides a novel class of pyrimidine derivatives, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR? and PDGFR? kinases.
    Type: Application
    Filed: May 1, 2008
    Publication date: July 29, 2010
    Applicant: IRM LLC
    Inventors: Xiaolin Li, Xiaodong Liu, Valentina Molteni
  • DENTINOGENESIS PROMOTER AND DENTINOGENIC PULP-CAPPING MATERIAL
    Publication number: 20100183563
    Abstract: The present invention provides a dentinogenesis inducer and dentinogenesis pulp-capping material, which are effectively used for formation (regeneration) of dentin. The present invention also provides a method of producing odontoblasts useful for dental regenerative therapy and the application of the obtained odontoblasts. The dentinogenesis inducer and the dentinogenesis pulp-capping material of the present invention are both characterized by the use of an HMG-CoA reductase inhibitor as an active ingredient. Additionally, odontoblasts can be produced by culturing cells capable of differentiating into odontoblasts in the presence of the HMG-CoA reductase inhibitor.
    Type: Application
    Filed: March 28, 2008
    Publication date: July 22, 2010
    Applicant: ORGAN TECHNOLOGIES, INC.
    Inventors: Takuo Kuboki, Mitsuaki Ono, Wataru Sonoyama, Takuo Fujisawa, Kengo Shimono, Masamitsu Oshima, Yosuke Okamoto
  • COMPOUNDS FOR ALZHEIMBER'S DISEASE
    Publication number: 20100184975
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?0)NH(C1-3alkyl), -L-C(?O)N(C1-3alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3alkyl)2, -L-S(?O)2NH(C1-3alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: March 8, 2010
    Publication date: July 22, 2010
    Applicant: Myriad Pharmaceuticals, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Substituted Heterocyclic Compounds
    Publication number: 20100173901
    Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
    Type: Application
    Filed: December 21, 2009
    Publication date: July 8, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Colin Zhang, Ding-quan Qian, Jincong Zhuo, Wenqing Yao
  • USE OF NITRIC OXIDE-RELEASING STATINS IN THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION
    Publication number: 20100174075
    Abstract: The present invention relates to the use of nitric oxide-releasing statins of formula (I) for the treatment of pulmonary arterial hypertension.
    Type: Application
    Filed: May 12, 2008
    Publication date: July 8, 2010
    Applicant: NICOX S.A.
    Inventors: John Wharton, Angela Monopoli
  • DIPHENYL SUBSTITUTED ALKANES
    Publication number: 20100168076
    Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: August 29, 2007
    Publication date: July 1, 2010
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellenk Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco
  • Pyrimidine derivatives and their use for controlling undesired plant growth
    Publication number: 20100167935
    Abstract: Pyrimidine derivatives and their use for controlling undesired plant growth Compounds of the formula (I) and their use in the field of crop protection are described.
    Type: Application
    Filed: December 28, 2009
    Publication date: July 1, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Klemens Minn, Hansjörg Dietrich, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger
  • Diacylglycerol Acyltransferase Inhibitors
    Publication number: 20100168419
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Application
    Filed: March 11, 2010
    Publication date: July 1, 2010
    Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Shiming Li, Lee Apostle McDermott, Yimin Qian, Weiya Yun
  • PYRROLIDINE DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS
    Publication number: 20100168088
    Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: October 2, 2009
    Publication date: July 1, 2010
    Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
  • Alpha amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
    Patent number: 7745454
    Abstract: Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: June 29, 2010
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Farouz, Christopher M. Semko, Ying-Zi Xu