At 1-position Patents (Class 546/226)
  • Publication number: 20100286204
    Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0
    Type: Application
    Filed: November 19, 2008
    Publication date: November 11, 2010
    Applicant: Sterix Limited
    Inventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
  • Publication number: 20100256126
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: March 11, 2010
    Publication date: October 7, 2010
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 7807672
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: October 5, 2010
    Assignee: Schering Corporation
    Inventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
  • Publication number: 20100234307
    Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
    Type: Application
    Filed: May 6, 2010
    Publication date: September 16, 2010
    Applicant: Bayer HealthCare LLC
    Inventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
  • Patent number: 7772251
    Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: August 10, 2010
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
  • Publication number: 20100197691
    Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: July 11, 2008
    Publication date: August 5, 2010
    Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
  • Publication number: 20100197736
    Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.
    Type: Application
    Filed: July 13, 2009
    Publication date: August 5, 2010
    Applicant: Japan Tobacco Inc.
    Inventors: Hisashi SHINKAI, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 7767623
    Abstract: A fungicidal compound of formula (1): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R7, R8 and R9; R1 is hydrogen, optionally substituted (C1-4)alkylC(?O), optionally substituted (C1-4)alkylC(?O)O, optionally substituted (C1-4)alkoxy(C1-4)alkyl, optionally substituted allyl, optionally substituted propargyl or optionally substituted allenyl; R2, R3, R4and R5 are each, independently, hydrogen, halogen, optionally substituted (C1-4)alkoxy(C1-4)alkoxy or optionally substituted (C1-4)alkoxy(C1-4)alkyl; R6 is an organic group containing three to thirteen carbon atoms and at least one silicon atom and, optionally, one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, and is optionally substituted by one to four independently selected halogen atoms; R7, R8 and R9are each, independently, hydrogen, halogen, C1-3alkyl, C1-3haloalkyl, C1-3alkoxy(C
    Type: Grant
    Filed: March 21, 2003
    Date of Patent: August 3, 2010
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Josef Ehrenfreund, Pierre Joseph Marcel Jung, Hans Tobler, Harald Walter
  • Publication number: 20100179109
    Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: July 15, 2010
    Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao
  • Patent number: 7754737
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: July 13, 2010
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 7745441
    Abstract: New urokinase inhibitors having a triisopropylphenylsulfonyl residue as an N?-substituent for 3-amidinophenylalanine are provided. The introduction of the triisopropylphenylsulfonyl residue greatly increases the affinity of the compounds to urokinase and, thereby, increases their inhibitory activity against urokinase. These urokinase inhibitors are useful in determining the role of urokinase and urokinase receptor in various diseases, particularly in tumor propagation and metastasis. Methods of treating tumors and a pharmaceutical composition are also provided.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: June 29, 2010
    Assignee: Wilex AG
    Inventors: Peter Wikström, Helmut Vieweg, Jörg Stürzebecher
  • Publication number: 20100160320
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: December 21, 2009
    Publication date: June 24, 2010
    Applicant: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 7737127
    Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: June 15, 2010
    Assignee: University of Virginia Patent Foundation
    Inventors: Joel M. Linden, Jayson M. Rieger, Timothy L. Macdonald, Gail W. Sullivan, Lauren Jean Murphree, Robert Alan Figler
  • Publication number: 20100137600
    Abstract: This invention describes reagent precursors and methods for chemical and biochemical reactions. These reagent precursors that can be activated in solution upon irradiation to generate reagents required for the subsequent chemical reactions. Specifically, photogenerated reagents (PGR) are useful for controlling parallel combinatorial synthesis and various chemical and biochemical reactions.
    Type: Application
    Filed: May 18, 2009
    Publication date: June 3, 2010
    Inventors: Xiaolian Gao, Zhuo Xiaochruan, Wu Yao, Jean-Phillipe Pollols
  • Publication number: 20100130471
    Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: May 27, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiamo Ghirlanda, Xiaoping Hou, Alexey V. Ishebenko, Lara S. Kallander, Beth A. Knapp-Reed, Brian Lawhorn, Qing Lu, Gerard McGeehan, Simon Semus, Robert D. Simpson, Suresh B. Singh, Lamont R. Terrell, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Jing Zhang, Wei Zhao
  • Patent number: 7723307
    Abstract: Novel Amino Acid Derivatives and Pharmaceutical Uses Thereof Provided are novel compounds of Formula I: wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. Further provided are pharmaceutical formulations of the compounds and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally provided are methods, of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: May 25, 2010
    Assignee: Aston University
    Inventors: Martin Griffin, Ian G. Coutts, Robert E. Saint
  • Publication number: 20100125075
    Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.
    Type: Application
    Filed: December 14, 2006
    Publication date: May 20, 2010
    Applicant: British Biotech Pharmaceuticals Ltd.
    Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
  • Patent number: 7718673
    Abstract: The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: May 18, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael J. Costanzo, William J. Hoekstra, Bruce E. Maryanoff
  • Patent number: 7713979
    Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: May 11, 2010
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, John Gordon Allen, Zhaogen Chen, Thomas Edward Mabry, Jefferson Ray McCowan, Nancy June Snyder, Leonard Larry Winneroski, Jr.
  • Publication number: 20100113770
    Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group r
    Type: Application
    Filed: October 14, 2009
    Publication date: May 6, 2010
    Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.
    Inventors: Susumu MUTO, Akiko ITAI
  • Publication number: 20100104979
    Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).
    Type: Application
    Filed: March 25, 2008
    Publication date: April 29, 2010
    Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
  • Patent number: 7700778
    Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: April 20, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
  • Publication number: 20100093798
    Abstract: The present application describes modulators of MIP-1? or CCR-1 of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, ring A, T, V, X, R1, R2 and R8, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Application
    Filed: October 3, 2007
    Publication date: April 15, 2010
    Inventor: Percy H. Carter
  • Publication number: 20100075986
    Abstract: The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
    Type: Application
    Filed: November 30, 2009
    Publication date: March 25, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Philippe R. BOVY, Roberto CECCHI, Tiziano CROCI, Olivier VENIER
  • Publication number: 20100068150
    Abstract: Described here are novel, highly selective inhibitors and activity based probes (ABPs) for caspases 3, 7, 8, and 9 and legumain. The compounds selectively inhibit only certain caspases. A positional scanning combinatorial library (PSCL) approach was used to screen pools of peptide acyloxymethyl ketones (AOMKs) containing both natural and non-natural amino acids for activity against a number of purified recombinant caspases. These screens were used to identify structural elements at multiple positions on the peptide scaffold that could be modulated to control inhibitor specificity towards target caspases. Further disclosed are individual optimized covalent inhibitors that could also be equipped with various tags for use as activity based probes, as well as labeled substrates.
    Type: Application
    Filed: July 6, 2007
    Publication date: March 18, 2010
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew Bogyo, Alicia B. Berger
  • Patent number: 7678826
    Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: March 16, 2010
    Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine LeBlanc, David Andrew Sandham
  • Patent number: 7671055
    Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: March 2, 2010
    Assignee: FMC Corporation
    Inventors: Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
  • Patent number: 7645774
    Abstract: There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: August 5, 2005
    Date of Patent: January 12, 2010
    Assignee: Schering Corporation
    Inventors: Richard J. Friary, Joseph A. Kozlowski, Bandarpalle B. Shankar, Michael K. C. Wong, Guowei Zhou, Brian J. Lavey, Neng-Yang Shih, Ling Tong, Lei Chen, Youheng Shu
  • Publication number: 20090298833
    Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.
    Type: Application
    Filed: July 20, 2009
    Publication date: December 3, 2009
    Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
  • Patent number: 7625929
    Abstract: The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl Group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: December 1, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
  • Patent number: 7622489
    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, Christy M. Olson, Edward S. Tasber
  • Publication number: 20090281069
    Abstract: The present invention relates to compounds of the formula; and their use in therapy.
    Type: Application
    Filed: April 10, 2007
    Publication date: November 12, 2009
    Inventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
  • Publication number: 20090275581
    Abstract: Disclosed are compounds according to Formula I: wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula I.
    Type: Application
    Filed: April 5, 2007
    Publication date: November 5, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Lara S. Kallander, Colin A. Leach, Brian Lawhorn, Qing Lu, Lamont R. Terrell, Bahman Ghavini-Alagha, Jing Zhang, Damiano Ghirlanda, Xiaoping Hou, Simon Semus
  • Publication number: 20090264432
    Abstract: Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
    Type: Application
    Filed: April 5, 2007
    Publication date: October 22, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh
  • Publication number: 20090264428
    Abstract: Described are compounds of the formula (I) which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 5, 2007
    Publication date: October 22, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh
  • Patent number: 7595401
    Abstract: The invention relates to compounds of Formula I and their therapeutic uses, wherein substituent A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carboxylic group, B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group, R1 is chosen from hydro, alkyl, aryl, heteroaryl amino and halo, and L1 and L2 are as defined in the specification.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: September 29, 2009
    Assignee: Myriad Pharmaceuticals, Inc.
    Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
  • Publication number: 20090227798
    Abstract: The present invention provides various processes for the preparation of (R)-?-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.
    Type: Application
    Filed: March 13, 2009
    Publication date: September 10, 2009
    Applicants: SANOFI-AVENTIS DEUTSCHLAND GMBH, AVENTIS PHARMACEUTICALS INC.
    Inventors: Wolfgang Laux, Gerard Guillamot, Frederick M. Laskovics, Chi-Hsin R. King, James E. Hitt, Sandra K. Stolz-Dunn, Ian A. Tomlinson, Johannes Nicolaas Koek
  • Publication number: 20090209585
    Abstract: The present invention relates to a cycloalkene derivative represented by the formula (I): wherein each symbol is as defined in the specification, a pharmaceutical agent containing the derivative, and a production method thereof. The cycloalkene derivative of the present invention has high solubility in water and is suitable for use as an injection.
    Type: Application
    Filed: July 6, 2007
    Publication date: August 20, 2009
    Inventors: Takashi Ichikawa, Tomoyuki Kitazaki, Norikazu Tamura
  • Publication number: 20090186884
    Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
    Type: Application
    Filed: April 5, 2007
    Publication date: July 23, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
  • Publication number: 20090186920
    Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3 and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Application
    Filed: January 14, 2009
    Publication date: July 23, 2009
    Inventors: HENNER KNUST, MATTHIAS NETTEKOVEN, EMMANUEL PINARD, OLIVIER ROCHE, MARK ROGERS-EVANS
  • Publication number: 20090170895
    Abstract: The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P3 receptors and a medicine containing thereof as an active ingredient.
    Type: Application
    Filed: October 11, 2006
    Publication date: July 2, 2009
    Applicant: TOA EIYO LTD.
    Inventors: Shin-ya Ohnuma, Takeshi Hasegawa, Tomoyuki Sada
  • Publication number: 20090131441
    Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: January 24, 2006
    Publication date: May 21, 2009
    Applicant: DOMPE phar.r.ma S.p.A.
    Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
  • Publication number: 20090124610
    Abstract: Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof, wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R1a is an optionally substituted aryl or heteroaryl group; R1b is hydrogen or a group R1a; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BG1) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N?C(RZ), (RZ)C?N, (RZ)N—C(O), (RZ)2C—C(O), N?N and (RZ)C?C(R6); J4-J3 is a group N?C(RZ) or a group (RZ)N—CO; and RZ is hydrogen or a substituent.
    Type: Application
    Filed: April 25, 2007
    Publication date: May 14, 2009
    Inventors: Gordon Saxty, Marinus Leendert Verdonk, John Caldwell, Ian Collins, Kwai-Ming Cheung, Tatiana Faria Da Fonseca McHardy
  • Publication number: 20090118332
    Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity, diabetes mellitus, cancer and infection and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 20, 2007
    Publication date: May 7, 2009
    Applicant: AstraZeneca AB
    Inventors: Roger John Butlin, Peter William Rodney Caulkett, Andrew Leach, Nicholas John Newcombe, Charles John O'Donnell, James Matthew Wood
  • Publication number: 20090105305
    Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, cancer and infection and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 20, 2007
    Publication date: April 23, 2009
    Applicant: AstraZeneca AB
    Inventors: Roger John Butlin, Peter William Rodney Caulkett, Petra Johannesson, Laurent Daniel Knerr, Andrew Leach, Nicholas John Newcombe, Charles John O'Donnell, Helen Pointon, James Matthew Wood
  • Publication number: 20090042855
    Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 3, 2008
    Publication date: February 12, 2009
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Patent number: 7485728
    Abstract: A compound of the formula wherein R1, R2, R3, R4, R5, R6, R, Y, CA, A?, m and n each, independently of the others are as defined herein.
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: February 3, 2009
    Assignee: Xerox Corporation
    Inventor: Jeffrey H. Banning
  • Patent number: 7482365
    Abstract: The present invention relates to piperidine derivatives of formula (I): wherein R, R1, R2, R3, R4, R5, R6, X, Y, m and n are as defined herein; and pharmaceutically acceptable salts and solvates thereof; the process for their preparation and their use in the treatment of conditions mediated by tachykinins.
    Type: Grant
    Filed: February 5, 2003
    Date of Patent: January 27, 2009
    Assignee: Glaxo Group Limited
    Inventors: Giuseppe Alvaro, Alfredo Paio, Alessandro Pontiroli, Simone Spada, Maria Elvira Tranquillini
  • Publication number: 20090023711
    Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.
    Type: Application
    Filed: January 5, 2007
    Publication date: January 22, 2009
    Applicant: AstraZeneca AB
    Inventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
  • Publication number: 20090018143
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Application
    Filed: November 8, 2007
    Publication date: January 15, 2009
    Applicants: Cephalon, Inc., Cephalon France
    Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy