Patents Examined by Alicia L Fierro
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Patent number: 7728018Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: GrantFiled: September 21, 2007Date of Patent: June 1, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Patent number: 7728022Abstract: Compounds of formula I: are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of A? in the brain.Type: GrantFiled: May 6, 2005Date of Patent: June 1, 2010Assignee: Merck Sharp & Dohme Ltd.Inventors: Michela Bettati, Ian Churcher, Victoria Alexandra Doughty, Timothy Harrison, Emmanuela Nizi, Adam Smith
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Patent number: 7723325Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 29, 2009Date of Patent: May 25, 2010Assignee: Hoffman-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7718653Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic ring which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: GrantFiled: July 16, 2008Date of Patent: May 18, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Patent number: 7714009Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A?): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A?): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.Type: GrantFiled: October 27, 2004Date of Patent: May 11, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Timothy Mark Turner, Scott Alan Pratt, Kazuyoshi Aso, Masakuni Kori, Michiyo Gyoten
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Patent number: 7714147Abstract: A novel process for the production of Fmoc (9H-fluoren-9-ylmethoxycarbonyl)-based compounds is provided, wherein a protecting group for the 9-hydroxymethyl group of the fluorene ring system is utilized. These compounds are useful for the modification of protein and peptide drugs.Type: GrantFiled: June 25, 2008Date of Patent: May 11, 2010Assignees: Baxter International Inc., Baxter Healthcare S.A.Inventors: Peter Turecek, Juergen Siekmann, Christian Noe, Gerhard Stoiber
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Patent number: 7709472Abstract: Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.Type: GrantFiled: January 24, 2006Date of Patent: May 4, 2010Assignee: Glaxo Group LimitedInventors: William Henry Miller, Meagan B. Rouse, Mark Andrew Seefeld
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Patent number: 7700618Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asType: GrantFiled: February 23, 2007Date of Patent: April 20, 2010Assignee: Pfizer IncInventors: Tomoki Kato, Kana Kon-I, Yohei Yuki, Kazuo Ando
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Patent number: 7683064Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.Type: GrantFiled: February 5, 2009Date of Patent: March 23, 2010Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loc, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Patent number: 7667049Abstract: An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidine or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields.Type: GrantFiled: March 8, 2007Date of Patent: February 23, 2010Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Takayuki Gotoh, Ichirou Araya
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Patent number: 7662827Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 24, 2006Date of Patent: February 16, 2010Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
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Patent number: 7662402Abstract: The present invention provides a nitrile compound represented by the formula (I): wherein R represents C1-C4 fluoroalkyl, Q represents halogen, C1-C11 alkyl optionally substituted with halogen, C2-C6 alkenyl group optionally substituted with halogen, C2-C6 alkynyl optionally substituted with halogen, C3-C7 cycloalkyl optionally substituted with halogen or (C3-C7 cycloalkyl optionally substituted with halogen) C1-C4 alkyl, which has excellent control effect against pests.Type: GrantFiled: December 22, 2004Date of Patent: February 16, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Daisuke Oohira, Ken Otaka
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Patent number: 7659304Abstract: A compound represented by the following formula (I) or a salt thereof is provided: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group.Type: GrantFiled: January 17, 2008Date of Patent: February 9, 2010Inventors: Masanori Somei, Atsuhiko Hattori, Nobuo Suzuki
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Patent number: 7612104Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: November 3, 2009Assignee: Sanofi-AventisInventors: Karl Schoenafinger, Stefanie Keil, Matthias Urmann, Hans Matter, Maike Glien, Wolfgang Wendler
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Patent number: 7601711Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: April 5, 2007Date of Patent: October 13, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7598280Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.Type: GrantFiled: February 28, 2008Date of Patent: October 6, 2009Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
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Patent number: 7589101Abstract: The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.Type: GrantFiled: August 15, 2006Date of Patent: September 15, 2009Assignees: IRM LLC, The Scripps Research InstituteInventors: Barun Okram, Pingda Ren, Nathanael S. Gray
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Patent number: 7572822Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: GrantFiled: January 30, 2008Date of Patent: August 11, 2009Assignee: Merck & Co. Inc.Inventors: Prasun K. Chakravarty, Louis L. Zuegner, III, legal representative, William H. Parsons, Brenda Palucki, Bishan Zhou, Min K. Park, Michael H. Fisher