Patents Examined by Binta Robinson
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Patent number: 8242276Abstract: 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: GrantFiled: June 23, 2011Date of Patent: August 14, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jodie Brice, Miall Cedilote, Zhiming Dong, Pingsheng Zhang
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Patent number: 8168652Abstract: 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: GrantFiled: March 3, 2010Date of Patent: May 1, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Philip E. Sanderson, Mark E. Layton, Kevin J. Rodzinak
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Patent number: 8153653Abstract: 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: GrantFiled: June 15, 2011Date of Patent: April 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 8143273Abstract: 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: GrantFiled: June 16, 2011Date of Patent: March 27, 2012Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 7855297Abstract: 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: GrantFiled: September 14, 2001Date of Patent: December 21, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Mitsuharu Nakamura, Takao Kamahori, Seigo Ishibuchi, Yoichi Naka, Hiroshi Sumichika, Katsuhiko Itoh
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Patent number: 7855219Abstract: 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: GrantFiled: February 20, 2002Date of Patent: December 21, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
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Patent number: 7803821Abstract: 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: GrantFiled: September 28, 2007Date of Patent: September 28, 2010Assignee: Bayer Cropscience SAInventors: Philippe Desbordes, Ralf Dunkel, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
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Patent number: 7795439Abstract: 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: GrantFiled: June 25, 2004Date of Patent: September 14, 2010Assignee: BASF AktiengesellschaftInventor: Michael A. Levy
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Patent number: 7683170Abstract: 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: GrantFiled: December 11, 2006Date of Patent: March 23, 2010Assignee: W. C. Heraeus GmbHInventors: Friedrich Wissmann, Holger Rauter, Silvia Werner
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Patent number: 7622468Abstract: 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: GrantFiled: December 16, 2003Date of Patent: November 24, 2009Assignee: Merck & Co. Inc.Inventors: Mark E. Fraley, Robert M. Garbaccio
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Patent number: 7604815Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: October 20, 2009Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Patent number: 7582658Abstract: 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: GrantFiled: December 23, 2004Date of Patent: September 1, 2009Assignee: Asahi Kasei Pharma CorporationInventors: Shiro Miyoshi, Toshinori Ishizuya
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Patent number: 7579366Abstract: 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: GrantFiled: March 11, 2003Date of Patent: August 25, 2009Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Nigel Paul King, Maurice Raymond Verschoyle Finlay, Yun He, Frank Roschangar, Dionisios Vourloumis, Hans Vallberg, Antony Bigot
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Patent number: 7572819Abstract: 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 consistingType: GrantFiled: February 9, 2007Date of Patent: August 11, 2009Assignee: Glaxo Group LimitedInventors: Daniel Marcus Bradley, Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7572808Abstract: 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: GrantFiled: June 16, 2006Date of Patent: August 11, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Chongqing Sun, Philip M. Sher, Gang Wu, William R. Ewing, Yanting Huang, Taekyu Lee, Natesan Murugesan, Richard B. Sulsky
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Patent number: 7572818Abstract: 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: GrantFiled: August 8, 2003Date of Patent: August 11, 2009Assignee: 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
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Patent number: 7566683Abstract: 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: GrantFiled: August 15, 2005Date of Patent: July 28, 2009Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Patent number: 7557214Abstract: 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: GrantFiled: September 3, 2004Date of Patent: July 7, 2009Assignee: Morphochem Aktiengesellschaft für Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
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Patent number: 7550606Abstract: 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: GrantFiled: September 26, 2008Date of Patent: June 23, 2009Assignees: BASF Aktiengesellschaft, Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.Inventors: Arno Boehm, Peter Blaschka, Willi Helfer, Dirk Hammel, Peter Schlichting, Klaus Muellen
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Patent number: 7491736Abstract: 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: GrantFiled: July 19, 2007Date of Patent: February 17, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li