Morpholines (i.e., Fully Hydrogenated 1,4-oxazines Patents (Class 544/106)
  • Patent number: 8217037
    Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: July 10, 2012
    Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD)
    Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Vasudevan Sudarsanam
  • Patent number: 8207167
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”).
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: June 26, 2012
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Patent number: 8202866
    Abstract: The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: June 19, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu
  • Patent number: 8197646
    Abstract: Process for the continuous fractional distillation of mixtures including morpholine (MO), monoaminodiglycol (ADG), ammonia and water obtained by reaction of diethylene glycol (DEG) with ammonia, which includes separating off ammonia at the top of a first distillation column K10, feeding the bottoms from K10 to a second distillation column K20 in which water and organic products are separated off at the top at a temperature at the top in the range from 45 to 198° C. and a pressure in the range from 0.1 to 15 bar, feeding the bottoms from K20 to a third distillation column K30 in which MO and organic products having a boiling point of <140° C. (1.013 bar) are separated off at the top or at a side offtake and ADG and organic products having a boiling point of >190° C. (1.013 bar) are separated off at the bottom, feeding the MO including stream which is separated off at the top or at a side offtake of the column K30 to a fourth column K40 in which organic products having a boiling point of ?128° C. (1.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: June 12, 2012
    Assignee: BASF SE
    Inventors: Helmut Schmidtke, Oliver Buβmann, Ralph Versch, Udo Rheude, Uwe Leyk, Manfred Julius, Martin Rudloff, Erhard Henkes
  • Patent number: 8173647
    Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: May 8, 2012
    Inventors: Gordana Atallah, Sarah Bartulis, Matthew Burger, Hanne Merritt, Simon Ng, Zhi-Jie Ni, Sabina Pecchi, Keith B. Pfister, Aaron Smith, Charles Voliva, Allan Wagman, Yanchen Zhang
  • Patent number: 8153631
    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 has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: April 10, 2012
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Mario G. Cardozo, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Patent number: 8143201
    Abstract: Morpholine derivatives useful as ashless TBN sources for lubricating oil compositions that are compatible with fluoroelastomeric engine seal materials, and lubricating oil compositions containing such compounds.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: March 27, 2012
    Assignee: Infineum International Limited
    Inventors: Jacob Emert, Jie Cheng, Jun Hua, Tushar K. Bera, Mark L. Bushey, Jesse D. Dambacher
  • Publication number: 20120071651
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Patent number: 8119796
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: February 21, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • Patent number: 8114873
    Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 14, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Yanbin Liu, Syed M. Ali, Jason Hill, Woj Wrona
  • Patent number: 8106190
    Abstract: To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
    Type: Grant
    Filed: November 29, 2006
    Date of Patent: January 31, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Takahiro Kuramochi, Ryoji Hirabayashi, Yohei Koganemaru, Ryosuke Munakata, Koichi Yonezawa, Tetsuo Kiso
  • Publication number: 20120022252
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 8101749
    Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: January 24, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Publication number: 20120000118
    Abstract: A fuel additive composition comprising (A) polyisobutyl-based nitrogen-containing dispersants with MN of the polyisobutyl group of from 650 to 1800 Dalton, (B) carrier oils substantially free of nitrogen and (C) polyisobutyl-based dispersant boosters with MN of the polyisobutyl group of from 200 to 650 Dalton, with the proviso that the difference between the MN of the polyisobutyl group of component (A) and the MN of the polyisobutyl group of component (C) is more than 100 Dalton. Said component (C) is especially useful as an intake valve clean-up booster in gasoline-operated port fuel injection internal combustion engines.
    Type: Application
    Filed: June 1, 2011
    Publication date: January 5, 2012
    Applicant: BASF SE
    Inventors: Arno LANGE, Peter Schreyer, Robert Stuart Grace
  • Patent number: 8076072
    Abstract: Nucleic acid labeling compounds including the following are disclosed: These compounds are useful for attaching a detectable label to a nucleic acid.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: December 13, 2011
    Assignee: Affymetrix, Inc.
    Inventors: Glenn Hugh McGall, Anthony D. Barone
  • Publication number: 20110300044
    Abstract: Corrosion inhibitors and processes, uses, methods, compositions, devices, and apparatus involving corrosion inhibitors are disclosed. In certain embodiments the use of specific corrosion inhibitors, specific concentrations of inhibitors, blends of inhibitors, processes utilizing such inhibitors, and compositions comprising such inhibitors, for example in acid gas separation systems such as aqueous amine- or ammonia-based CO2 separation systems (e.g., the post combustion capture of CO2 from flue gases using amines). According to some embodiments, corrosion inhibitors are used in a process for separating at least a portion of an acid gas from a gaseous mixture wherein the inhibitor is at least one selected from dodecylamine, sodium molybdate, morpholine, or a combination thereof.
    Type: Application
    Filed: May 5, 2011
    Publication date: December 8, 2011
    Applicant: University of Regina
    Inventors: Paitoon Tontiwachwuthikul, Raphael Idem, Nattawan Kladkaew, Chintana Saiwan
  • Patent number: 8063098
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
  • Patent number: 8058441
    Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkyny
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: November 15, 2011
    Assignee: N.V. Organon
    Inventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
  • Publication number: 20110268671
    Abstract: Use of a compound having the formula (I) in the manufacture of a medicament for the prevention or treatment of a diseased caused by oral bacterial in an animal Formula (I); wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxyl group except in the alpha-position, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 12, 2011
    Publication date: November 3, 2011
    Inventors: HUGO DE BRUYN, Rolf Valter ATTSTRÖM, Daniel ATTSTRÖM
  • Patent number: 8049007
    Abstract: Amorolfine base, which is a compound of formula (I): is improvedly prepared by: (i) contacting a compound of formula (II): with a Friedel-Crafts catalyst; and (ii) adding one equivalent of 2-halogeno-2-methylbutane, wherein the reaction mixture obtained in step (i) is cooled to a temperature from ?40° to ?60° C. prior to step (ii) and the Friedel-Craft catalyst is selected from the group consisting of gallium chloride, antimony pentafluoride, molybdenum pentachloride, indium chloride, antimony pentachloride.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 1, 2011
    Assignee: Galderma S.A.
    Inventors: Beat Weber, Stefan Rosenberger
  • Patent number: 8034978
    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: Grant
    Filed: May 24, 2007
    Date of Patent: October 11, 2011
    Assignee: BASF SE
    Inventors: Jan Eberhardt, Harald Meiβner, Bram Willem Hoffer, Johann-Peter Melder, Ekkehard Schwab
  • Patent number: 8017772
    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: September 11, 2009
    Date of Patent: September 13, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Thomas Christoph, Stefan Oberboersch, Klaus Schiene, Gregor Bahrenberg, Robert Frank, Sven Kuehnert, Wolfgang Schroeder
  • Patent number: 8013152
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: September 6, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • Patent number: 7994270
    Abstract: The present invention provides a method for producing a thermosetting resin having a benzoxazine ring, comprising the step of: reacting a bifunctional phenol compound, a diamine compound, and an aldehyde compound in a mixed solvent of an aromatic nonpolar solvent and an alcohol.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: August 9, 2011
    Assignee: Sekisui Chemical Co., Ltd
    Inventors: Tomoaki Katagiri, Yuji Eguchi
  • Patent number: 7994315
    Abstract: Production method of an optically active morpholine compound represented by the formula 10, or a compound represented by the formula 55, which includes the following steps: or wherein each symbol is as defined in the specification. An optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: August 9, 2011
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Masahiro Okuyama, Fumiaki Uehara, Hiroshi Iwamura, Kazutoshi Watanabe
  • Publication number: 20110178200
    Abstract: The invention relates to new reactive mesogenic compounds (RM), polymerisable liquid crystal (LC) mixtures and polymers comprising them, and the use of the compounds, mixtures and polymers in optical, electrooptical, electronic, semiconducting or luminescent components or devices, in decorative, security or cosmetic applications, especially for use in polymer films having high optical dispersion.
    Type: Application
    Filed: December 22, 2008
    Publication date: July 21, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Owain Llyr Parri, Donald Gordon Graham, Alison Linda May
  • Publication number: 20110172417
    Abstract: This invention relates to a heterogeneous copper nanocatalyst composed of copper nanoparticles immobilized on a boehmite support, a method of preparing the same, and the use thereof. The copper nanocatalyst composed of the copper nanoparticles supported on boehmite exhibits excellent performance in a Huisgen cycloaddition reaction and an A3 coupling reaction of aldehyde, amine and alkyne. The copper nanocatalyst is able to be prepared in a large scale and shows superior reactivity even when used in a small amount under mild conditions without an additive in an organic reaction. This heterogeneous catalyst is easy to separate and reuse after the reaction.
    Type: Application
    Filed: July 9, 2008
    Publication date: July 14, 2011
    Applicant: Postech Academy-Industry Foundation
    Inventors: Jai Wook Park, In Soo Park
  • Publication number: 20110172208
    Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: July 14, 2011
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
  • Patent number: 7977508
    Abstract: Methods of synthesizing ammonia borane are provided. The methods comprise reacting at least one amine borane with ammonia such that ammonia borane is produced. Ammonia borane has a chemical formula Of NH3—BH3 and provides a good source of storage hydrogen making it useful in a variety of applications including a potential hydrogen source for fuel cells. The methods can further comprise separating the ammonia borane from the other products of the reaction. Exemplary methods can produce ammonia borane having purity greater than about 90 percent. In further examples, the methods can produce ammonia borane having purity greater than about 95 percent or greater than about 99 percent.
    Type: Grant
    Filed: April 2, 2007
    Date of Patent: July 12, 2011
    Assignee: The Ohio State University
    Inventors: Sheldon Gerald Shore, Xuenian Chen
  • Publication number: 20110144067
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 16, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20110137030
    Abstract: A process for preparing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia and primary and secondary amines, in the presence of a supported copper-, nickel- and cobalt-containing catalyst, wherein the catalytically active material of the catalyst, before the reduction thereof with hydrogen, comprises oxygen compounds of aluminum, of copper, of nickel and of cobalt, and in the range from 0.2 to 5.0% by weight of oxygen compounds of tin, calculated as SnO, and catalysts as defined above.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 9, 2011
    Applicant: BASF SE
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Johann-Peter Melder, Thomas Heidemann
  • Publication number: 20110137029
    Abstract: A process for preparing an amine by reacting a primary or secondary alcohol, aldehyde and/or ketone with hydrogen and a nitrogen compound selected from the group of ammonia and primary and secondary amines, in the presence of a supported copper-, nickel- and cobalt-containing catalyst, wherein the catalytically active material of the catalyst, before the reduction thereof with hydrogen, comprises oxygen compounds of aluminum, of copper, of nickel, of cobalt and of tin, and in the range from 0.2 to 5.0% by weight of oxygen compounds of yttrium, of lanthanum, of cerium and/or of hafnium, each calculated as Y2O3, La2O3, Ce2O3 and Hf2O3 respectively, and catalysts as defined above.
    Type: Application
    Filed: December 2, 2010
    Publication date: June 9, 2011
    Applicant: BASF SE
    Inventors: PETR KUBANEK, Wolfgang Mägerlein, Johann-Peter Melder, Thomas Heidemann
  • Patent number: 7947513
    Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: February 12, 2007
    Date of Patent: May 24, 2011
    Assignee: DH Technologies Ptd. Ltd.
    Inventors: Darryl J. C. Pappin, Michael Bartlett-Jones
  • Publication number: 20110118254
    Abstract: The main object of the present invention is to provide an agent for the treatment of inflammatory bowel diseases. The present invention relates to an agent for the treatment of inflammatory bowel diseases 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: June 22, 2009
    Publication date: May 19, 2011
    Inventor: Takashi Kyoi
  • Patent number: 7943649
    Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: May 17, 2011
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
  • Patent number: 7935696
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: May 3, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 7915249
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: March 29, 2011
    Assignee: Janssen Pharmaceutical NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20110054167
    Abstract: Processes for preparing an amine, which processes comprise: 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 and tin, and 0.5 to 8.0% by weight of an oxygen compound of cobalt, calculated as CoO, and wherein the catalytically active composition does not comprise any ruthenium.
    Type: Application
    Filed: December 10, 2008
    Publication date: March 3, 2011
    Inventors: Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
  • Patent number: 7897599
    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: December 14, 2009
    Date of Patent: March 1, 2011
    Assignee: iTherX Pharmaceuticals Inc.
    Inventors: Erik Boman, Susana Conde Ceide, Russell Dahl, Nancy G. J. Delaet, Justin Ernst, Antonio Garrido Montalban, Jeffrey Kahl, Christopher Larson, Stephen Miller, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhinjun Wang
  • Patent number: 7893257
    Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: February 22, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Anusuya Choudhury, Jeffrey S. Grimm, Kirk L. Sorgi, David Palmer, Jing Liu
  • Patent number: 7893099
    Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: February 22, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Ruben Alvarez Sanchez
  • Patent number: 7888379
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 15, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 7888355
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 15, 2011
    Assignee: Burnham Institute for Medical Research
    Inventors: Ze′ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
  • Patent number: 7879888
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 1, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Publication number: 20110009627
    Abstract: The invention relates to a reactor for performing high-pressure reactions, comprising at least one tube (31) whose ends are each conducted through a tube plate (33) and which is bonded to the tube plate (33). The tube plates (33) and the at least one tube (31) are surrounded by an outer jacket, such that an outer space (39) is formed between the tube (31) and the outer jacket. The tube plates (33) each have at least one surface composed of a nickel-base alloy and the at least one tube (31) is in each case welded on to the surface composed of the nickel-base alloy. The surface composed of the nickel-base alloy points in each case in the direction of the particular reactor end. The outer jacket has a thickness which is sufficient to absorb tensile forces which occur between tube (31) and outer jacket owing to a temperature difference in the event of different expansion. The invention further relates to a process for starting up the reactor and for performing an exothermic reaction in the reactor.
    Type: Application
    Filed: January 21, 2009
    Publication date: January 13, 2011
    Applicant: BASF SE
    Inventors: Helmut Schmidtke, Wilhelm Ruppel, Helmut Berrsche, Johann-Peter Melder, Udo Rheude, Petr Kubanek, Gerhard Ruf, Wolfgang Gunkel, Wolfgang Mägerlein, Karl-Heinz Ross
  • Patent number: 7858618
    Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Grant
    Filed: August 17, 2007
    Date of Patent: December 28, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Rainer Walter, Heiner Ebel, Henri Doods, Angelo Ceci, Annette Schuler-Metz, Ingo Konetzki
  • Patent number: 7842803
    Abstract: Nicotinic acetylcholine receptor ligands of Formula I wherein X, n, R1 and R2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: November 30, 2010
    Assignee: AstraZeneca AB
    Inventors: Hui-Fang Chang, Christopher Holmquist, Eifion Phillips, Timothy Piser, Thomas Simpson, Rebecca Urbanek, James Woods, Hui Xiong
  • Patent number: 7842804
    Abstract: The present invention relates to salts comprising pyrrolidinium, triazolinium, piperidinium or morpholinium cations that can have substituents thereon and alkyltrifluorophosphate anions, to processes for preparation thereof and to the use thereof, in particular for the preparation of ionic liquids.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: November 30, 2010
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Nikolai (Mykola) Ignatyev, German Bissky, Helge Willner
  • Patent number: 7838671
    Abstract: A new nitrogen-containing organosilicon compound contains tertiary amine groups and carbonyl groups wherein the tertiary amine groups are selected from R1R2N— (where R1 and R2 are the same or different univalent hydrocarbon groups of 1-15 carbon atoms), alicyclic amino groups, or heterocyclic amino groups containing in their rings one or more tertiary amine groups.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: November 23, 2010
    Assignee: Dow Corning Toray Company, Ltd.
    Inventors: Makoto Iwai, Mitsuyoshi Hamada
  • Patent number: 7829702
    Abstract: A process for preparing optically active trans-2,6-dimethylmorpholine by (i) reacting racemic trans-2,6-dimethylmorpholine with D-mandelic acid, (ii) removing the salt formed from D-mandelic acid and one enantiomer of trans-2,6-dimethylmorpholine from the other enantiomer of trans-2,6-dimethylmorpholine and (iii) isolating the desired optically active trans-2,6-dimethylmorpholine.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: November 9, 2010
    Assignee: BASF SE
    Inventors: Klaus Ditrich, Frank Haese