Abstract: Compounds of a certain formula (I) in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.
Type:
Grant
Filed:
May 24, 2006
Date of Patent:
July 27, 2010
Assignee:
4SC AG
Inventors:
Klaus Pekari, Mathias Schmidt, Thomas Bär, Thomas Beckers, Petra Gimmnich
Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
March 13, 2008
Date of Patent:
July 27, 2010
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
Abstract: Compounds of Formula (1) process for preparing them, pharmaceutical compositions comprising them. The use of compounds of formula (1) for hyperproliferative diseases, e.g. cancer as well as autoimmune diseases and heart disease.
Type:
Grant
Filed:
March 22, 2005
Date of Patent:
July 20, 2010
Assignee:
Aprea AB
Inventors:
Jacob Westman, Klas Wiman, Galina Selivanova, Vladimir Bykov
Abstract: This invention discloses novel quinolonecarboxylic acid derivatives, pharmaceutically acceptable salts or hydrates thereof, and their preparation methods and medical uses. The compounds in this invention show potent antibacterial activity against broad-spectrum pathogenic bacteria, with favorable pharmacokinetics and very low toxicity. The quinolinecarboxylic acid derivatives, which possess a hydrogen atom or an amino group at C-5 position, cis-substituted optical or racemic 2,8-diazo-dicyclo[4,3,0]nonanyl at C-7 position, and difluoromethoxyl at C-8 position of quinolone core, have superior activity against gram-positive bacteria and broad spectrum antibacterial activity compared with the known quinolones.
Type:
Grant
Filed:
April 13, 2005
Date of Patent:
July 20, 2010
Assignees:
Institut of Medicinal Biotechnology Chinese Academy of Medical Sciences, Xinchang Pharmaceutical Factory, Zhejiang Medicine Co. Ltd.
Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.
Type:
Grant
Filed:
December 5, 2007
Date of Patent:
July 13, 2010
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Andrei W. Konradi, Matthew N. Mattson, Martin L. Neitzel, Christopher M. Semko, Anh P. Truong, Jing Wu, Ying-zi Xu
Abstract: A method of preparing an aromatic phosphine monosulfonate in zwitterionic form, such as dicyclohexylphenylphosphine monosulfonate zwitterion, involving contacting an aromatic phosphine with a sulfonating agent to provide a reaction mixture containing aromatic phosphine monosulfonate in acid form and unconverted sulfonating agent; quenching or removing substantially all of the unconverted sulfonating agent; partially neutralizing the aromatic phosphine monosulfonate in acid form to phase separate aromatic phosphine monosulfonate in zwitterionic form as a solid or neat liquid layer; and collecting the zwitterion as a solid or neat liquid. The zwitterion may be neutralized to form the corresponding aromatic phosphine monosulfonate metal salt, which is useful in preparing catalysts for hydroformylation processes.
Type:
Grant
Filed:
September 14, 2006
Date of Patent:
July 13, 2010
Assignee:
Dow Global Technologies Inc.
Inventors:
Donald L. Morrison, Kurt D. Olson, Walter C. Reed, Anthony G. Abatjoglou
Abstract: Disclosed are cyanine dyes that are useful for labeling and detecting biological and other materials. The dyes are of formula (I) in which groups R3 and R4 are attached to the Z1 ring structure and groups R5 and R6 are attached to the Z2 ring structure, and n=1, 2 or 3; Z1 and Z2 independently represent the carbon atoms necessary to complete a one ring, or two-fused ring aromatic system; at least one of groups R1, R2, R3, R4, R5, R6 and R7 is the group -E-F where E is a single bond or a spacer group and F is a target bonding group; one or more of groups R11, R12, R13 and R14 are independently selected from the group —(CH2)k—W, where W is sulphonic acid or phosphonic acid and k is an integer from 1 to 10.
Type:
Grant
Filed:
October 29, 2004
Date of Patent:
July 6, 2010
Assignees:
GE Healthcare U.K. Limited, Carnegie Mellon University
Inventors:
Richard M. West, Nigel Bosworth, Ratnakar B. Mujumdar
Abstract: This invention relates to novel quinuclidine derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Grant
Filed:
June 29, 2004
Date of Patent:
July 6, 2010
Assignees:
Neurosearch A/S, Abbott Laboratories
Inventors:
Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring Jørgensen, Michael R. Schrimpf, Kevin B. Sippy
Abstract: The present invention provides compounds of the formula (I), which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, Type 2 diabetes and obesity.
Type:
Grant
Filed:
April 1, 2005
Date of Patent:
July 6, 2010
Assignee:
Novartis AG
Inventors:
Gregory Raymond Bebernitz, Ramesh Chandra Gupta, Vikrant Vijaykumar Jagtap, Appaji Baburao Mandhare, Davinder Tuli
Abstract: Compounds of formula I in free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Type:
Grant
Filed:
April 2, 2004
Date of Patent:
June 29, 2010
Assignee:
Novartis AG
Inventors:
Robin Alec Fairhurst, David Andrew Sandham, David Beattie, Ian Bruce, Bernard Cuenoud, Reamonn Madden, Neil John Press, Roger John Taylor, Katharine Louise Turner, Simon James Watson
Abstract: The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
May 12, 2006
Date of Patent:
June 29, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Andreas Termin, Nicole Zimmermann, Tara Leanne Knoll, Gabriel Martinez-Botella, Esther Martinborough
Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
Type:
Grant
Filed:
June 26, 2006
Date of Patent:
June 29, 2010
Assignee:
Inke, S.A.
Inventors:
Juan Antonio Perez Andres, Pere Dalmases Barjoan
Abstract: Compounds of a certain formula (I), in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.
Type:
Grant
Filed:
February 10, 2006
Date of Patent:
June 22, 2010
Assignee:
4SC AG
Inventors:
Klaus Pekari, Mathias Schmidt, Thomas Bär, Thomas Beckers, Björn Bartels
Abstract: The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.
Abstract: The present invention provides novel purine-based fluorescent dyes that may be used for staining, localizing and otherwise labeling target molecules, such as nucleic acids, for detection, amplification and quantification.
Type:
Grant
Filed:
July 7, 2005
Date of Patent:
June 15, 2010
Assignee:
Enzo Life Sciences, Inc. c/o Enzo Biochem, Inc.
Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
Abstract: The present invention provides processes for preparing Palonosetron salts, especially, the hydrochloride salt and intermediates used to prepare Palonosetron salts.
Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
February 15, 2007
Date of Patent:
June 15, 2010
Assignee:
Abbott Laboratories Inc.
Inventors:
Patrick Betschmann, Andrew F. Burchat, David J. Calderwood, Michael L. Curtin, Steven K. Davidsen, Heather M. Davis, Robin R. Frey, Howard R. Heyman, Gavin C. Hirst, Peter Hrnciar, Michael R. Michaelides, Melanie A. Muckey, Kelly D. Mullen, Paul Rafferty, Carol K. Wada
Abstract: The present invention concerns 2,6-quinolinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.