Patents Examined by Binta Robinson
  • Patent number: 8242276
    Abstract: The present invention provides novel methods for preparing N—(S)-1 -azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic ?-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: August 14, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jodie Brice, Miall Cedilote, Zhiming Dong, Pingsheng Zhang
  • Patent number: 8168652
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: May 1, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philip E. Sanderson, Mark E. Layton, Kevin J. Rodzinak
  • Patent number: 8153653
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8143273
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: March 27, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 7855219
    Abstract: This invention relates to compounds of formula (I) in which the variable groups are as defined in the text and claims. A pharmaceutical composition and methods of using these materials in treatment of various conditions are also disclosed and claimed.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: December 21, 2010
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
  • Patent number: 7855297
    Abstract: The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like].
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: December 21, 2010
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Mitsuharu Nakamura, Takao Kamahori, Seigo Ishibuchi, Yoichi Naka, Hiroshi Sumichika, Katsuhiko Itoh
  • Patent number: 7803821
    Abstract: The present invention relates to N-cycloalkyl-carboxamide, N-cycloalkyl-thiocarboxamide and N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A represents carbo-linked, 5-membered heterocyclyl groups, T represents O, S, NRc, N—ORd, N—NRcRd or N—CN, Z1 represents cycloalkyl groups and Z2 and Z3, W1 to W5 represent various substituents; their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: September 28, 2010
    Assignee: Bayer Cropscience SA
    Inventors: Philippe Desbordes, Ralf Dunkel, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
  • Patent number: 7795439
    Abstract: A method for the in-situ treatment of a pyridine-2,3-dicarboxylic acid ester with an oxidizing agent, such as hydrogen peroxide, to improve product quality is provided. The method for the in-situ removal of impurities from a saponified solution of pyridine-2,3-dicarboxylic acid ester comprises the steps of providing a solution of pyridine-2,3-dicarboxylic acid ester, saponifying the solution with a base to form the corresponding pyridine-2,3-dicarboxylic acid salt, reacting the solution with an oxidizing agent in an amount effective to remove impurities, acidifying the solution with an acid to convert the pyridine-2,3-dicarboxylic acid into the corresponding pyridine-2,3-dicarboxylic acid, and collecting a purified solution comprising pyridine-2,3-dicarboxylic acid. Further provided is a method for the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinic acids, esters, and salts by using a pyridine-2,3-dicarboxylic acid salt prepared by the above method as an intermediate.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: September 14, 2010
    Assignee: BASF Aktiengesellschaft
    Inventor: Michael A. Levy
  • Patent number: 7683170
    Abstract: Methods for manufacturing 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxy-camptothecin are described comprising I. reacting a mixture of 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and 7-ethyl-10-hydroxycamptothecin in a polar aprotic solvent with a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms and optionally in the presence of a water binding agent in an amount which effectively binds any water present in the above reactants and solvents; or II. reacting: (a) 7-Ethyl-10-hydroxycamptothecin in a polar aprotic solvent with phosgene, trichlormethyl-chloroformate, bis(trichloromethyl)carbonate or a alternative to phosgene and a base in the presence of catalytic amounts of a N-containing cyclic organic compound having 3 to 20 carbon atoms; and (b) subsequently with piperidinopiperidine and an amine base.
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: March 23, 2010
    Assignee: W. C. Heraeus GmbH
    Inventors: Friedrich Wissmann, Holger Rauter, Silvia Werner
  • Patent number: 7622468
    Abstract: The present invention relates to tetrahydropyridine compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: November 24, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Mark E. Fraley, Robert M. Garbaccio
  • Patent number: 7604815
    Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: October 20, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
  • Patent number: 7582658
    Abstract: A novel compound represented by the following formula (1) or a salt thereof: wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R2, R3, and R4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R11 represents hydrogen atom, hydroxyl group, etc.), etc., R1 represents an alkyl group, and symbol “n” represents an integer of 2 to 6, which has a parathyroid hormone depressing action and showing low toxicity, and a medicament containing the compound or salt thereof as an active ingredient.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: September 1, 2009
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shiro Miyoshi, Toshinori Ishizuya
  • Patent number: 7579366
    Abstract: The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH?CH2; —C?CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: August 25, 2009
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Nigel Paul King, Maurice Raymond Verschoyle Finlay, Yun He, Frank Roschangar, Dionisios Vourloumis, Hans Vallberg, Antony Bigot
  • Patent number: 7572819
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: August 11, 2009
    Assignee: Glaxo Group Limited
    Inventors: Daniel Marcus Bradley, Kevin Michael Thewlis, Simon Edward Ward
  • Patent number: 7572818
    Abstract: Compound of general formula (I) in which p is an integer equal to 1, 2, 3 or 4; q is an integer equal to 1, 2, 3, 4 or 5; each substituent X is chosen, independently of the others, as being halogen, alkyl or haloalkyl, at least one of the substituents being a haloalkyl; each substituent Y is chosen, independently of the others, as being halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, amino, phenoxy, alkylthio, dialkylamino, acyl, cyano, ester, hydroxy, aminoalkyl, benzyl, haloalkoxy, halosulphonyl, halothioalkyl, alkoxyalkenyl, alkylsulphonamide, nitro, alkylsulphonyl, phenylsulphonyl or benzylsulphonyl; as to the N-oxides of 2-pyridine thereof; with the exception of N-{2-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-ethyl}-2,6-dichlorobenzamide. Method for preparing the compound of general formula (I). Fungicidal composition comprising the compound of general formula (I). Method for treating phytopathogenic diseases.
    Type: Grant
    Filed: August 8, 2003
    Date of Patent: August 11, 2009
    Assignee: Bayer Cropscience S.A.
    Inventors: Darren James Mansfield, Tracey Cooke, Peter Stanley Thomas, Pierre-Yves Coqueron, Jean-Pierre Vors, Geoffrey Gower Briggs, Hélène Lachaise, Heiko Rieck, Philippe Desbordes, Marie-Claire Grosjean-Cournoyer
  • Patent number: 7572808
    Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: August 11, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chongqing Sun, Philip M. Sher, Gang Wu, William R. Ewing, Yanting Huang, Taekyu Lee, Natesan Murugesan, Richard B. Sulsky
  • Patent number: 7566683
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: July 28, 2009
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 7557214
    Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: July 7, 2009
    Assignee: Morphochem Aktiengesellschaft für Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
  • Patent number: 7550606
    Abstract: The current invention relates to a perylene-3,4-dicarboxylic anhydride, substituted in the 9-position, of the general formula III wherein Z is bromine or cyano, and processes for preparing 9-bromoperylene-3,4-dicarboxylic anhydride and 9-cyanoperylene-3,4-dicarboxylic anhydride.
    Type: Grant
    Filed: September 26, 2008
    Date of Patent: June 23, 2009
    Assignees: BASF Aktiengesellschaft, Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Arno Boehm, Peter Blaschka, Willi Helfer, Dirk Hammel, Peter Schlichting, Klaus Muellen
  • Patent number: 7491736
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 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 19, 2007
    Date of Patent: February 17, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li