1,3-thiazines Patents (Class 544/53)
  • Publication number: 20140378444
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: November 22, 2013
    Publication date: December 25, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Patent number: 8852846
    Abstract: The present invention provides a salt represented by the formula (I): wherein Q1 and Q2 independently each represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a C1-C20 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, W represents a group represented by the formula (W1), (W2), (W3), (W4) or (W5): and Z+ represents an organic counter ion.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yukako Anryu, Koji Ichikawa
  • Publication number: 20140058097
    Abstract: A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.
    Type: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuuji Kooriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 8637504
    Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: January 28, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akihiro Hori, Terukazu Kato
  • Patent number: 8546380
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted heterocyclic group; E is lower alkylene; X is S; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; or its pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: October 1, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 8541408
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: September 24, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
  • Patent number: 8507479
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: August 13, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
  • Publication number: 20120258961
    Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 11, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Shinji Suzuki, Yuuji Kooriyama
  • Publication number: 20120245154
    Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 8, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kousuke Anan, Yukio Tada, Akihiro Hori, Moriyasu Masui
  • Publication number: 20120238557
    Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3, R4, R5, X, L1, L2, A, ring B and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 20, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Kousuke Anan
  • Patent number: 8173642
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: May 8, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 8168630
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: April 23, 2008
    Date of Patent: May 1, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuke Tamura, Shinji Suzuki, Yukio Tada, Shuji Yonezawa, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama, Tatsuhiko Ueno
  • Publication number: 20120022249
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 26, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
  • Publication number: 20120016116
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Naotake KOBAYASHI, Kazuo UEDA, Naohiro ITOH, Shinji SUZUKI, Gaku SAKAGUCHI, Akira KATO, Akira YUKIMASA, Akihiro HORI, Yuji KORIYAMA, Hidekazu HARAGUCHI, Ken YASUI, Yasuhiko KANDA
  • Patent number: 8080605
    Abstract: Polymer-filler coupling compounds with the formula B-A-Sx—N are claimed. In these compounds, B is an azaheterocyclic oxygen or sulfur containing moiety, or an allyltin moiety; Sx is a polysulfide, where x is between 2 and about 10; A is a linking atom or group that forms a bridge between B and Sx; and N is a blocking group. Sx can be a disulfide. N can be a conventional blocking group or other group such as -A-B. Methods for using the polymer-filler coupling compounds to modify polymers containing unsaturated carbon-carbon bonds and promote filler dispersion are also claimed. Additionally, vulcanizable rubber compositions containing the polymer-filler coupling compounds and methods for making vulcanized rubber compositions using the polymer-filler coupling compounds are also claimed.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 20, 2011
    Assignee: Bridgestone Corporation
    Inventors: Yasuo Fukushima, William L. Hergenrother, Russell W. Koch
  • Patent number: 8063205
    Abstract: The present invention is a method for producing a 2-oxazoline analogue or a 1,3-oxazine analogue represented by the following general formula (3) by reacting a 1,2-aminoalcohol compound or a 1,2-aminothiol compound with an ?,?-dihaloamine compound. (In the formula, n represents 0 or 1, and R represents an oxygen atom or a sulfur atom. R1, R2 and R3 each represents an atom or a group shown in Group 1 to Group 3, and R0 represents an atom or a group shown in Group 2 or Group 3. Two or more of R1, R2 and R3 may be bonded to each other to form a ring.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: November 22, 2011
    Assignees: National University Corporation Hokkaido University, Mitsubishi Gas Chemical Company, Inc.
    Inventors: Shoji Hara, Tsuyoshi Fukuhara, Toshio Hidaka
  • Patent number: 8022018
    Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine or dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C12 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group; R1 is selected from the group consisting of a C1-C24 straight chain or branched alkyl group or a C1-C24 arylalkyl; R2 is selected from the group consisting of X-R4-X, R4 being a C1-C6 alkyl group; and X is chlorine, bromine or iodine. The dithiazine may he isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. The dithiazines of formulae (II) and (III) are quaternized derivatives of the dithiazine of formula (I).
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: September 20, 2011
    Assignee: Baker Hughes Incorporated
    Inventor: Grahame Nigel Taylor
  • Patent number: 8022017
    Abstract: Corrosion of metallic tubulars in an oil, gas or geothermal well may be inhibited by introducing into the well a dithiazine of the formula: wherein R is selected from the group consisting of a C1 to C10 saturated or unsaturated hydrocarbyl group or a C1 to C10 ?-hydroxy saturated or unsaturated hydrocarbyl group. The dithiazine may be isolated from a whole spent fluid formed by reaction of hydrogen sulfide and a triazine. Alternately, the whole spent fluid containing the dithiazine may be introduced into the well. In addition, the dithiazine or whole spent fluid may be formulated with at least one component selected from alkyl, alkylaryl or arylamine quaternary salts; mono or polycyclic aromatic amine salts; imidazoline derivative or a quaternary salt thereof; a mono-, di- or trialkyl or alkylaryl phosphate ester; or a monomeric or oligomeric fatty acid.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: September 20, 2011
    Assignee: Baker Hughes Incorporated
    Inventor: Grahame Nigel Taylor
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Publication number: 20100120754
    Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.
    Type: Application
    Filed: May 6, 2009
    Publication date: May 13, 2010
    Inventors: Peter Oettgen, Alan Rigby, Towia Libermann
  • Publication number: 20090234116
    Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.
    Type: Application
    Filed: May 27, 2009
    Publication date: September 17, 2009
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
  • Patent number: 7524874
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: April 28, 2009
    Assignee: Amgen Inc.
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
  • Publication number: 20090082560
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: October 23, 2006
    Publication date: March 26, 2009
    Applicant: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 7459450
    Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: December 2, 2008
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
  • Patent number: 7420053
    Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.
    Type: Grant
    Filed: November 29, 2006
    Date of Patent: September 2, 2008
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
  • Patent number: 7335672
    Abstract: Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duoden
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: February 26, 2008
    Assignee: Amgen Inc.
    Inventors: Mark H. Norman, Liping H. Pettus, Xianghong Wang, Jiawang Zhu
  • Patent number: 7332511
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: February 19, 2008
    Assignee: Amgen Inc.
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
  • Patent number: 7259163
    Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.
    Type: Grant
    Filed: October 30, 2002
    Date of Patent: August 21, 2007
    Assignee: Glaxo Group Limited
    Inventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
  • Patent number: 7244725
    Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Grant
    Filed: September 10, 2003
    Date of Patent: July 17, 2007
    Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
    Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth TenBrink
  • Patent number: 7183275
    Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: February 27, 2007
    Assignee: Shionogi Co., Ltd.
    Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
  • Patent number: 7166609
    Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.
    Type: Grant
    Filed: November 3, 2003
    Date of Patent: January 23, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
  • Patent number: 7038039
    Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: May 2, 2006
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
  • Patent number: 6908937
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10, n represents 0, 1 or 2, Het represents the groups where R1 represents hydrogen; mercapto; optionally halogen-substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkenyl; optionally substituted aryl; or optionally substituted heterocyclyl, Y represents oxygen or sulphur, and R2 represents hydrogen, alkyl or optionally substituted aryl, and to processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: July 2, 2001
    Date of Patent: June 21, 2005
    Assignee: Bayer Cropscience AG
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6841668
    Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: April 4, 2003
    Date of Patent: January 11, 2005
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Deborah Judd, Sai P. Shum, Stephen D. Pastor
  • Patent number: 6818640
    Abstract: It is found out that compounds represented by general formula (I) bind selectively to cannabinoid 2 receptor (CB2R) and thus exhibit CB2R antagonism or CB2R agonis wherein R1 represents optionally substituted alkylene; R2 represents hydrogen, alkyl, a group represented by the formula —C(═R5)—R6 (wherein R5 represents O or S; and R6 represents alkyl, alkoxy, alkylthio, etc.) or a group represented by the formula SO2R7 (wherein R7 represents allyl, etc.); m is an integer of from 0 to 2; and A represents optionally substituted aryl, etc.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: November 16, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Hanasaki, Takami Murashi, Hiroyuki Kai
  • Publication number: 20040192910
    Abstract: Compounds of Formula I (I) wherein the substituents are as defined in claim 1, and the agrochemically tolerable salts and all stereoisomers and tautomers of the compounds of formula I, are suitable for use as herbicides.
    Type: Application
    Filed: February 26, 2004
    Publication date: September 30, 2004
    Inventors: Christoph Luthy, Andrew Edmunds
  • Publication number: 20040063934
    Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the &agr;v&bgr;3 integrin receptor, their use, and pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: September 8, 2003
    Publication date: April 1, 2004
    Inventors: Herve Geneste, Andreas Kling, Udo Lange, Werner Seitz, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger, Arnulf Lauterbach
  • Patent number: 6699898
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: March 2, 2004
    Assignee: Pharmacia COrporation Global Patent Department
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20030207869
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: May 6, 2003
    Publication date: November 6, 2003
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Publication number: 20030158184
    Abstract: The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.
    Type: Application
    Filed: December 21, 2001
    Publication date: August 21, 2003
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Publication number: 20030134848
    Abstract: There is provided heterocyclic compounds of the following formula (I): 1
    Type: Application
    Filed: November 21, 2001
    Publication date: July 17, 2003
    Inventors: Masahiro Imoto, Tatsuya Iwanami, Minako Akabane, Yoshihiro Tani
  • Publication number: 20030129081
    Abstract: The novel and known thiazines and thiazoles of the formula (I) 1
    Type: Application
    Filed: June 24, 2002
    Publication date: July 10, 2003
    Inventors: Rainer Bruns, Hermann Uhr, Martin Kugler, Peter Wachtler, Oliver Kretschik
  • Publication number: 20030130271
    Abstract: The invention provides compounds of formula 1
    Type: Application
    Filed: August 27, 2002
    Publication date: July 10, 2003
    Applicant: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
  • Patent number: 6579982
    Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc.
    Inventor: Julian Blagg
  • Publication number: 20030100755
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: October 25, 2002
    Publication date: May 29, 2003
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Patent number: 6534492
    Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: March 18, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
  • Publication number: 20020193314
    Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.
    Type: Application
    Filed: May 7, 2002
    Publication date: December 19, 2002
    Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
  • Patent number: 6469000
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: October 22, 2002
    Assignee: The Procter & Gamble Co.
    Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
  • Patent number: 6451830
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel