Morpholines (i.e., Fully Hydrogenated 1,4-oxazines Patents (Class 544/106)
  • Publication number: 20100274009
    Abstract: Processes for preparing an amine, the processes comprising: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, nickel, no oxygen compounds of cobalt, and 0.2 to 5.0% by weight of at least one oxygen compound of phosphorus or gallium, calculated as H3PO4 and Ga2O3 respectively.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 28, 2010
    Applicant: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Publication number: 20100274011
    Abstract: Processes for preparing an amine, the processes comprising: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, and nickel, 1.5 to 4.5% by weight of an oxygen compound of cobalt, calculated as CoO, and 0.2 to 5.0% by weight of at least one oxygen compound of niobium, sulfur, phosphorus, gallium, boron, lead or antimony, calculated in each case as Nb2O5, H2SO4, H3PO4, Ga2O3, B2O3, PbO and Sb2O3 respectively, and wherein the catalytically active composition does not comprise any molybdenum.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 28, 2010
    Applicant: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Publication number: 20100274008
    Abstract: Processes for preparing an amine, the processes comprising: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, and nickel, and 1.0 to 5.0% by weight of an oxygen compound of cobalt, calculated as CoO, and 0.2 to 5.0% by weight of a polyoxometalate.
    Type: Application
    Filed: December 10, 2008
    Publication date: October 28, 2010
    Applicant: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Publication number: 20100267948
    Abstract: Process for preparing an amine by reacting an aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group consisting of primary and secondary amines in the presence of a heterogeneous catalyst, wherein the reaction is carried out using a suspended catalyst as heterogeneous catalyst and is carried out in the semibatch mode in which the nitrogen compound as one reactant is placed in the reaction vessel and the aldehyde and/or the ketone as the other reactant is added during the course of the reaction and the aldehyde and/or the ketone is added in portions or continuously to the reaction mixture during the course of the reaction as a function of the achieved conversion of the nitrogen compound until a conversion of the nitrogen compound of at least 95% results, and all or part of the catalyst remains in the reaction vessel after the reaction batch and is reused for the next reaction batch.
    Type: Application
    Filed: May 24, 2007
    Publication date: October 21, 2010
    Applicant: BASF SE
    Inventors: Jan Eberhardt, Harald Meissner, Bram Willem Hoffer, Johann-Peter Melder, Ekkehard Schwab
  • Publication number: 20100267669
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: June 10, 2010
    Publication date: October 21, 2010
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 7816389
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: October 19, 2010
    Assignee: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Patent number: 7812017
    Abstract: The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: October 12, 2010
    Assignee: Biovitrum AB (publ.)
    Inventors: Johan Angbrant, Rune Ringom, Kristin Hammer, Erik Ringberg, Bengt Lindqvist, Gary Johansson, Peter Brandt, Katarina Beierlein, Björn M Nilsson
  • Publication number: 20100249404
    Abstract: The invention relates to a method for carrying out a chemical reaction for producing a target compound by heating in a reactor a reaction medium containing at least one first reactant, such that a chemical bond inside the first reactant or between the first and a second reactant is formed or modified. The reaction medium is brought into contact with a solid heating medium that can be warmed by electromagnetic induction and that is inside the reactor and is surrounded by the reaction medium. Said heating medium is heated by electromagnetic induction with the aid of an inductor and the target bond is formed from the first reactant or from the first and a second reactant and said target bond is separated from the heating medium.
    Type: Application
    Filed: June 11, 2010
    Publication date: September 30, 2010
    Inventors: Carsten Friese, Andreas Kirschning, Jurgen Wichelhaus, Sascha Volhan Ceylan
  • Patent number: 7795425
    Abstract: A process for the preparation of a compound of formula (Ia): includes: (i) contacting a compound of formula (III): with a compound of formula (IV): in the presence of a palladium catalyst, methanol and hydrogen gas, the step (i) preferably being conducted under basic conditions with acetic acid being added to the medium of reaction once the consumption of the hydrogen gas has ceased.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: September 14, 2010
    Assignee: Galderma S.A.
    Inventors: Beat Weber, Stefan Rosenberger
  • Patent number: 7790770
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: September 7, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20100222580
    Abstract: The invention relates to a process for the preparation of onium alkylsulfates by reaction of an onium halide with a symmetrically substituted dialkyl sulfate, in which the alkyl group can have 1 to 14 C atoms, with an asymmetrically substituted dialkyl sulfate, in which one alkyl group can have 4 to 20 C atoms and the second alkyl group denotes methyl or ethyl, with an alkyl trialkylsilyl sulfate, with an alkyl acyl sulfate or with an alkyl sulfonyl sulfate, where the reaction with a dialkyl sulfate is carried out at room temperature.
    Type: Application
    Filed: November 18, 2005
    Publication date: September 2, 2010
    Applicant: MERCK PATENT GMBH
    Inventors: Nikolai Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Publication number: 20100197564
    Abstract: The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
    Type: Application
    Filed: April 17, 2008
    Publication date: August 5, 2010
    Inventors: Jack D. Scott, Andrew Stamford
  • Patent number: 7767673
    Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: August 3, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Andrew P. Crew, Han-Qing Dong, Radoslaw Laufer, An-Hu Li, Li Qiu, Colin Peter Sambrook Smith, Tao Zhang
  • Patent number: 7754882
    Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: July 13, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
  • Patent number: 7749999
    Abstract: The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: July 6, 2010
    Assignee: Itherx Pharmaceuticals, Inc.
    Inventors: Erik Boman, Susana Conde Ceide, Russell Dahl, Nancy G. J. Delaet, Justin Ernst, Antonio Garrido Montalban, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhinjun Wang, Jeffrey Kahl, Christopher Larson
  • Publication number: 20100160247
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: June 17, 2009
    Publication date: June 24, 2010
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 7741357
    Abstract: Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1?-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (P4N, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxyphenyl])butane tetrakishydrochloride salt) has an IC50 of 0.88 ?M.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: June 22, 2010
    Assignee: Johns Hopkins University
    Inventors: Ru Chih C. Huang, Apostolos Gittis, Evangelos Moudrianakis, Julie A. Dohm, Jih Ru Hwu, Ming-Hua Hsu
  • Patent number: 7741343
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: June 22, 2010
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7737139
    Abstract: Selected sulfonic acids, their derivatives and pharmaceutical compositions containing such compounds are useful in inhibiting the chernotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, the selected sulfonic acids and their derivativas are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: June 15, 2010
    Assignee: Dompe PHA.R.MA S.p.A.
    Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
  • Patent number: 7732443
    Abstract: Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: June 8, 2010
    Inventors: Yariv Donde, Robert M. Burk, Jeremiah H. Nguyen
  • Patent number: 7728027
    Abstract: The present disclosure generally relates to a process for synthesizing methyl ((1S)-1-(((2S)-2-(5-(4?-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to intermediates useful in this process.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: June 1, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shawn K. Pack, Peng Geng, Michael J. Smith, Jason Hamm
  • Patent number: 7718675
    Abstract: The application relates to novel amino alcohols of the general formula (I) where R, R1, R2, R3, R4, R5 and R6 each have the definitions illustrated in detail in the description, to a process for their preparation, and to the use of these compounds as medicines, in particular as renin inhibitors.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: May 18, 2010
    Assignee: Speedel Experimenta AG
    Inventors: Peter Herold, Stefan Stutz, Aleksandar Stojanovic, Vincenzo Tschinke, Christiane Marti, Michael Quirmbach
  • Patent number: 7713968
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: May 11, 2010
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 7713967
    Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: May 11, 2010
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 7714012
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: May 11, 2010
    Assignee: Trustees of Dartmouth University
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Publication number: 20100113438
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Application
    Filed: March 30, 2007
    Publication date: May 6, 2010
    Applicant: DAC S.R.L.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi
  • Publication number: 20100104979
    Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).
    Type: Application
    Filed: March 25, 2008
    Publication date: April 29, 2010
    Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
  • Patent number: 7705042
    Abstract: The invention relates to arylamide and hetereoarylamide compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: April 27, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath Meegalla, Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee DesJarlais, Carl L. Manthey, Christopher M. Flores, Christopher J. Molloy
  • Patent number: 7700584
    Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: April 20, 2010
    Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.
    Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
  • Publication number: 20100094001
    Abstract: The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine, (wherein R1 and R2 are identical or different from each other, and represent a C1-C6 alkyl group, a C2-C6 alkenyl group or a C6-C14 aryl C1-C6 alkyl group which may have a substituent, and R1 and R2 may together form a ring), the process comprising the step of adding the tertiary amine having a boiling point at 1 atmosphere of 150° C. or higher to the compound represented by formula (I).
    Type: Application
    Filed: March 5, 2008
    Publication date: April 15, 2010
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Keizo Sato, Shinya Abe, Kazuhiro Yoshizawa, Kazunori Wakasugi, Shigeto Negi, Mamoru Miyazawa
  • Patent number: 7691863
    Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB2 receptors.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: April 6, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michel Dietz, Sabine Gruener, Paul Hebeisen, Sylvie C. Meyer Reigner, Matthias Nettekoven, Bernd Puellmann, Stephan Roever, Christoph Ullmer
  • Publication number: 20100081804
    Abstract: A process is described for continuously hydrogenating unsaturated compounds, in which particles of a first hydrogenation catalyst are suspended in a liquid phase in which an unsaturated compound is dissolved, the liquid phase, in the presence of a hydrogenous gas at a first partial hydrogen pressure and at a first temperature, is conducted through a packed bubble column reactor in cocurrent counter to the direction of gravity, the effluent from the bubble column reactor is sent to a gas-liquid separation, the liquid phase is sent to a crossfiltration to obtain a retentate and a filtrate, the retentate is recycled into the bubble column reactor and the filtrate, in the presence of a hydrogenous gas at a second partial hydrogen pressure and at a second temperature, is passed over a bed of a second hydrogenation catalyst, wherein the second partial hydrogen pressure is at least 10 bar higher than the first partial hydrogen pressure.
    Type: Application
    Filed: October 16, 2006
    Publication date: April 1, 2010
    Inventors: Bram Willem Hoffer, Hartwig Voss, Ekkehard Schwab, Udo Rheude, Gerd Kaibel, Mathias Haake, Jan Eberhardt, Michael Karcher
  • Publication number: 20100076186
    Abstract: Provided is a process for preparing a heterocycle by catalytic reaction of an aromatic dinitrile with an amino alcohol, wherein the process includes: initially charging into a reaction vessel the amino alcohol and a catalyst to produce a reaction mixture; adding the aromatic dinitrile into the reaction mixture, which is maintained at a reaction temperature, wherein no solvent other than the amino alcohol of formula (III) is added to the reaction mixture prior to and/or during the catalytic reaction; and after completion of the catalytic reaction, completely replacing, or substantially completely replacing, unreacted amino alcohol with a nonpolar solvent to obtain the heterocycle, wherein the unreacted amino alcohol is present in an amount of not more than 20 wt. %, preferably 3-10 wt. % or less, based on a total weight of the heterocycle.
    Type: Application
    Filed: September 22, 2009
    Publication date: March 25, 2010
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Thomas KUEBELBAECK, Manfred Neumann, Marianne Omeis
  • Patent number: 7683059
    Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.
    Type: Grant
    Filed: September 5, 2006
    Date of Patent: March 23, 2010
    Assignee: Amgen Inc.
    Inventors: Mario G. Cardozo, Jay P. Powers, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Patent number: 7678826
    Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: March 16, 2010
    Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine LeBlanc, David Andrew Sandham
  • Publication number: 20100063044
    Abstract: The present invention relates to aniline derivatives of formula I: wherein R1, R2, R3, R4, Z and q are as defined herein; or salts thereof and their use.
    Type: Application
    Filed: August 17, 2009
    Publication date: March 11, 2010
    Applicant: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornoe, Mario Rottlãnder, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
  • Patent number: 7666865
    Abstract: Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each l1 and l2 is independently 0-5; l3 is 0 or 1; each of R1, R2 and R3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R1 and R2 may independently be halo, COOR, CONR2, CF3, CN or NO2, wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l3 is 0, and either l1 and l2 is 0 or 1 and if R1 and/or R2 represent F in the para position, Z cannot be C or N; and are useful to treat pain.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: February 23, 2010
    Assignee: Neuromed Pharmaceuticals Ltd.
    Inventors: Terrance P. Snutch, Gerald W. Zamponi
  • Publication number: 20100035873
    Abstract: The invention relates to derivatives of a compound of formula I: wherein R1 to R7 and X1 to X6 are as defined herein. The invention relates to the uses thereof for treating diseases, conditions and/or disorders mediated by kappa opioid receptors (KORs). Specifically, the compounds are selective antagonists of KORs and are highly selective to KORs relative to mu and delta opioid receptors.
    Type: Application
    Filed: June 23, 2009
    Publication date: February 11, 2010
    Inventors: Patrick Verhoest, Matthew Merrill Hayward, Vinod Parikh, Stanton Furst McHardy, Stafford McLean
  • Patent number: 7659280
    Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: February 9, 2010
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
  • Patent number: 7655680
    Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.
    Type: Grant
    Filed: May 16, 2005
    Date of Patent: February 2, 2010
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
  • Patent number: 7655653
    Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: February 2, 2010
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozens
  • Publication number: 20100019657
    Abstract: The present invention relates to novel organic electroluminescent compounds, and organic electroluminescent devices employing the same as electroluminescent material. Specifically, the organic electroluminescent compounds according to the invention are characterized in that they are represented by Chemical Formula (1): Since the organic electroluminescent compounds according to the invention have good luminous efficiency and life property of material, OLED's having very good operation lifetime can be manufactured.
    Type: Application
    Filed: December 31, 2008
    Publication date: January 28, 2010
    Applicant: Gracel Display Inc.
    Inventors: Sung Jin Eum, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
  • Publication number: 20100016295
    Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
    Type: Application
    Filed: July 31, 2006
    Publication date: January 21, 2010
    Applicant: Bayer Healthcare LLC
    Inventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
  • Patent number: 7649004
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
    Type: Grant
    Filed: July 12, 2005
    Date of Patent: January 19, 2010
    Assignee: Pfizer, Inc.
    Inventors: Charlotte Alice Louise Lane, Graham Nigel Maw, David James Rawson, Lisa Rosemary Thompson
  • Publication number: 20090312315
    Abstract: The compound represented by the following formula (I) and the like have PAI-1 inhibition activity; wherein: R1 represents a C6-10 aryl group which may be substituted or the like; T represents a single bond or the like; m represents 0 or 1; when m is 0, G represents —N—C(?O)—CO2H or the like; when m is 1, G represents an oxygen atom or the like; R2 represents a C6-10 aryl group which may be substituted or the like; E represents the following formula (II) wherein one of R31, R32, R33 and R34 represents the formula R1-T-, each of the other three independently represents a hydrogen atom or the like, and R35 represents the formula —X—Y?, a hydrogen atom or the like; X represents —CH2— or the like; Y? represents a carboxy group or the like; M represents a single bond or the like.
    Type: Application
    Filed: April 10, 2009
    Publication date: December 17, 2009
    Inventors: Youichi Yamaguchi, Takeshi Yanase, Susumu Muto, Akiko Itai
  • Patent number: 7625900
    Abstract: Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I: processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these compounds for the treatment and/or inhibition of pain and other disorders or disease states at least partly mediated by KCNQ2/3 K+ channels.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: December 1, 2009
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Thomas Christoph, Stefan Oberboersch, Klaus Schiene, Gregor Bahrenberg, Robert Frank, Sven Kuehnert, Wolfgang Schroeder
  • Publication number: 20090286776
    Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
    Type: Application
    Filed: July 23, 2009
    Publication date: November 19, 2009
    Inventors: Jean Jacques ZEILLER, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Publication number: 20090286977
    Abstract: Processes comprising: (i) providing a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones and mixtures thereof; and (ii) reacting the reactant with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a catalyst comprising a zirconium dioxide- and nickel-containing catalytically active composition, to form an amine; wherein the catalytically active composition, prior to reduction with hydrogen, comprises oxygen compounds of zirconium, copper, nickel and cobalt, and one or more oxygen compounds of one or more metals selected from the group consisting of Pb, Bi, Sn, Sb and In.
    Type: Application
    Filed: July 4, 2007
    Publication date: November 19, 2009
    Applicant: BASF SE
    Inventors: Petr Kubanek, Bram Willem Hoffer, Ekkehard Schwab, Johann-Peter Melder, Holger Evers, Till Gerlach
  • Patent number: 7608658
    Abstract: This invention discloses a process for manufacturing an elastomeric article by liquid injection molding, said process comprising the steps of: (I) heating a curable composition comprised of (1) a liquid polymer comprised of repeat units that are derived from a conjugated diolefin monomer, wherein said liquid polymer has a weight average molecular weight which is within the range of 5,000 to 100,000, and wherein the liquid polymer is functionalized with an amine moiety, (2) a carbonyl inhibited platinum catalyst, and (3) a tetrakis(dialkyl siloxy) silane crosslinking agent, to a temperature which is within the range of 30° C. to 100° C.; (II) injecting the heated curable composition into a mold at a temperature which is within the range of 100° C. to 210° C. to produce the elastomeric article; and (III) removing the elastomeric article from the mold.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: October 27, 2009
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Michael Joseph Rachita, Vanessa Marika Guscoff, Lawson Gibson Wideman
  • Patent number: 7605261
    Abstract: The invention relates to new products of formula (I): in which: Y represents oxygen or sulphur, Z represents C?CH2, CH—CH3 or CH2, R1 represents hydrogen, morpholinyl or the radical. In which the two nitrogen atoms are linear or form a cyclic radical, X represents carbonyl, alkylene or alkenylene, linear or branched, containing at most 6 carbon atoms optionally interrupted by oxygen or sulphur, R4, R5 and R6 represent hydrogen, a protective group of the nitrogen, alkyl, cycloalkyl, aryl and arylalkyl optionally substituted, R2 represents alkyl optionally substituted by aryl, heteroaryl or —NR4R5, R3 represents alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally substituted, these products being in all isomer forms and the salts, as medicaments.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: October 20, 2009
    Assignee: Amgen Inc.
    Inventors: Pierre Deprez, Marcel Patek