Z Radical Contains Two Or More Nitrogen Atoms At Least One Of Which Forms A C(=x)n Group (x Is Chalcogen) Patents (Class 514/542)
  • Publication number: 20150148395
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 9012500
    Abstract: The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-? activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient. A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-? activator containing same as an active ingredient, and is the like.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: April 21, 2015
    Assignee: Nishizaki Bioinformation Research Institute
    Inventors: Tomoyuki Nishizaki, Akito Tanaka
  • Patent number: 8853274
    Abstract: A composition including a farnesyl transferase inhibitor (FTI) and a gamma-secretase inhibitor (GSI) is useful for producing an effect against a glioblastoma cell and/or for treating glioblastoma multiforme (GBM).
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventor: Jialiang Wang
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Publication number: 20140155439
    Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C?O)—, —S(?O)2—, —C(C?O)O—, —C(C?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(C?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
  • Publication number: 20140093518
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: August 26, 2013
    Publication date: April 3, 2014
    Applicant: The Scripps Research Institute
    Inventor: Carlos F. Barbas, III
  • Patent number: 8637547
    Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: January 28, 2014
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, David Charles Festus Moffat, Francesca Ann Day, Alistair David Graham Donald
  • Publication number: 20130316985
    Abstract: A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein.
    Type: Application
    Filed: May 20, 2013
    Publication date: November 28, 2013
    Applicant: Corning Incorporated
    Inventors: Huayun Deng, Ye Fang
  • Patent number: 8592438
    Abstract: A plant disease control composition comprising, as an active ingredient, a compound of formula (I) or a salt thereof, and one or more anilinopyrimidine compounds selected from the group consisting of 4,6-dimethyl-N-phenyl-2-pyrimidinamine, 4-methyl-N-phenyl-6-(1-propynyl)-2-pyrimidinamine and 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine has an excellent plant disease control effect.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: November 26, 2013
    Assignee: Sumitomo Chemical Intellectual Property Service, Ltd
    Inventors: Masanao Takaishi, Norio Kimura
  • Patent number: 8552061
    Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient. These compounds have the general chemical structure (I, II, III or IV).
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: October 8, 2013
    Assignee: Yale University
    Inventor: Richard Hochberg
  • Publication number: 20130251787
    Abstract: Pulmonary arterial hypertension (PAH) can be prevented in persons susceptible to the diseases and PAH patients can be treated by administering an effective dose of a leukotriene inhibitor. Suitable inhibitors include leukotriene A4 hydrolase (LTA4H) inhibitors, leukotriene B4 receptor (BLT1/BLT2) antagonists, 5-lipoxygenase (5-LO) inhibitors, and 5-lipoxgygenase activating protein (FLAP) inhibitors.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 26, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Mark R. Nicolls, Wen Tian, Jayakumar Rajadas
  • Patent number: 8524701
    Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: September 3, 2013
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Brian Guth, Randolph Seidler, Juergen Daemmgen
  • Publication number: 20130102570
    Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 25, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC
  • Publication number: 20130018044
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: December 21, 2010
    Publication date: January 17, 2013
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20120277310
    Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.
    Type: Application
    Filed: June 25, 2012
    Publication date: November 1, 2012
    Applicants: Bar-Ilan University, Ramot at Tel-Aviv University Ltd.
    Inventors: Gideon STEIN, Abraham NUDELMAN, Ada REPHAELI, Irit GIL-AD, Abraham WEIZMAN
  • Publication number: 20120149736
    Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?5)—NR?, —C(?NH)NR? or —S(?O)2NR — wherein R? is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula —(Alk1)m,(Q)n(Alk2)p— wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—,— NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1
    Type: Application
    Filed: February 25, 2010
    Publication date: June 14, 2012
    Applicant: Chroma Therapeutics Ltd.
    Inventors: Alastair David Graham Donald, David Festus Charles Moffat, Andrew James Belfield, Carl Leslie North, Stewart Andrew Wayne Jones
  • Publication number: 20120088787
    Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Publication number: 20110230555
    Abstract: The present invention provides compounds and methods for the treatment of diseases or disorders such as heart failure, hyperlipidemia, hypercholesterolemia, gonadotropin deficiency, diabetes mellitus, metabolic syndrome, hyperglycemia, insulin resistance, glucose intolerance, obesity, psoriasis, atopic dermatitis, and cancer.
    Type: Application
    Filed: June 24, 2009
    Publication date: September 22, 2011
    Inventors: David Middlemiss, Kenneth J. Ingold
  • Patent number: 7973181
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi— or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: July 5, 2011
    Assignee: Chroma Therapeutics Ltd.
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
  • Publication number: 20110105485
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: July 21, 2010
    Publication date: May 5, 2011
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Publication number: 20110059114
    Abstract: Compositions and uses of gamma secretase inhibitors (GSIs) for the treatment and inhibition of gliomas in subjects in need thereof are provided. Methods for administering gamma secretase inhibitors in association with radiation for the treatment of radiation resistant gliomas are described. Compositions for the inhibition of Notch signaling and activity are provided.
    Type: Application
    Filed: August 5, 2010
    Publication date: March 10, 2011
    Applicant: DUKE UNIVERSITY
    Inventors: Bruce A. Sullenger, Jialiang Wang, Jeremy N. Rich
  • Publication number: 20100260674
    Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.
    Type: Application
    Filed: January 26, 2010
    Publication date: October 14, 2010
    Applicant: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Publication number: 20100184735
    Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 22, 2010
    Inventor: Richard Hochberg
  • Publication number: 20100144825
    Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
    Type: Application
    Filed: June 20, 2008
    Publication date: June 10, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Fiaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao, Linghang Zhuang
  • Publication number: 20100010010
    Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.
    Type: Application
    Filed: September 14, 2007
    Publication date: January 14, 2010
    Applicant: CHROMA THERAPEUTICS LTD.
    Inventors: Alan Hornsby Davidson, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
  • Publication number: 20090298924
    Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R
    Type: Application
    Filed: May 4, 2006
    Publication date: December 3, 2009
    Applicant: Chroma Therapeutics Ltd
    Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
  • Publication number: 20090170937
    Abstract: Compounds of formula (I) have activity in alleviating the effects of impaired dopaminergic signaling, for example in the treatment of Parkinsons Disease: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 and R3 are independently hydrogen, or a group —C(?O)R6 or —C(?O)OR6 wherein Re is C1-C6 alkyl, or a group —CH2Q wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclyl ring of 3 to 6 ring atoms; R4 and R5 are independently (a) the side chain of a natural amino acid, or (b) optionally substituted C1-C4 alkyl, C2-C4 alkenyl, or C2-C4 alkynyl, or (c) —CH2XCH3, —CH2CH2XCH3, or —CH2XCH2CH3, wherein X is —O—, S, or —NR7 wherein R7 is hydrogen, methyl or ethyl; or (d) —CH2Q or CH2OQ wherein Q is as defined in relation to R6; or R4 and R5 taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl or heterocyclic ring of 3 to 8 ring atoms, optionally fused to a second, optionally substituted, carbocyclic or heterocyclic ring
    Type: Application
    Filed: January 23, 2007
    Publication date: July 2, 2009
    Applicants: Proximagen Ltd., Hodgkin Building,King`s College London,Guy`s Compus
    Inventor: Christopher Hobbs
  • Publication number: 20090149535
    Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 11, 2009
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Publication number: 20090036525
    Abstract: Compounds of formula (I) have activity in alleviating the effects of impaired dopaminergic signaling, for example in the treatment of Parkinsons Disease: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 and R3 are independently hydrogen, or a group —C(?O)R6 or —C(?O)OR6 wherein R6 is C1-C6 alkyl, or a group —CH2Q wherein Q is an optionally substituted monocyclic cycloalkyl or heterocyclyl ring of 3 to 6 ring atoms; R7 is (i) optionally substituted phenyl or monocyclic heteroaryl, or (ii) a radical of formula —CHR4R5; R4 is (a) optionally substituted C1-C4 alkyl, C1-C4 alkoxy, C2-C4 alkenyl, C2-C4 alkenyloxy, or C2-C4 alkynyl, or (b) —CH2XCH3, —CH2CH2XCH3, or —CH2XCH2CH3, wherein X is —O—, S, or —NR7 wherein R7 is hydrogen, methyl or ethyl; or —CH2Q or CH2OQ wherein Q is as defined in relation to R6; and R5 is hydrogen, methyl, ethyl, or methyl substituted by 1, 2 or 3 fluoro atoms; or R4 and R5 taken together with the carbon atom to which they are attached form an optionally substituted
    Type: Application
    Filed: January 23, 2007
    Publication date: February 5, 2009
    Applicant: POXIMAGEN LTD.
    Inventor: Christopher Hobbs
  • Publication number: 20090036528
    Abstract: The present invention is an application, composition, and method of using a pharmaceutically effective amount of aspartame or its primary metabolite aspartyl-phenylalanine in systematic and periodic application or dose as an aspirin (NSAID) substitute, treatment for osteoporosis, and or topical treatment for Rosacea.
    Type: Application
    Filed: July 30, 2008
    Publication date: February 5, 2009
    Inventors: Tony E. Hugli, John E. Adams
  • Patent number: 7384979
    Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: June 10, 2008
    Assignee: Ortho McNeil Pharmaceutical, Inc.
    Inventors: Peter J. Connolly, William V. Murray, Steven K. Wetter, Sigmond Johnson, Victor T. Bandurco, Jacqueline Bussolari
  • Patent number: 7375120
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: May 20, 2008
    Assignee: Smithkline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Jinhwa Lee, Jia-ning Xiang
  • Patent number: 7199158
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: April 3, 2007
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7084178
    Abstract: A series of N-cycloalkylcarboxamide derivatives of N-benzyl benzenesulfonamides of Formula I are described. The compounds inhibit ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of ?-amyloid. Pharmaceutical compositions and methods of treatment using these compounds are also disclosed.
    Type: Grant
    Filed: November 18, 2004
    Date of Patent: August 1, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Mendi A. Higgins
  • Patent number: 6992105
    Abstract: Compounds of the formula wherein R, R1, COOR2, R3–R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: January 31, 2006
    Assignee: Novartis AG
    Inventor: Cynthia Anne Fink
  • Patent number: 6989384
    Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: January 24, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
  • Patent number: 6951886
    Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: October 4, 2005
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6946474
    Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.
    Type: Grant
    Filed: September 13, 2001
    Date of Patent: September 20, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Patent number: 6919343
    Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: July 19, 2005
    Assignee: Merck & Co., Inc.
    Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
  • Patent number: 6919374
    Abstract: It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) lowers whole blood viscosity in patient, including those suffering from sickle cell disease and plasma cell dyscrasias. Upon in vivo APM treatment patients experienced a significant lowering of whole blood viscosity. In vitro addition of APM to patients samples having elevated whole blood viscosity resulted in reduced viscosity over time. These in vivo and in vivo results identify APM as a therapeutic agent for molecular diseases which lead to elevated whole blood viscosity. A method by which APM treatment can be monitored is also disclosed.
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: July 19, 2005
    Assignee: Oklahoma Medical Research Foundation
    Inventor: Carl V. Manion
  • Patent number: 6888022
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 3, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu, Clark Norman Eid, William Leonard Scott
  • Patent number: 6803383
    Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: October 12, 2004
    Assignee: The Scripps Research Institute
    Inventors: Dale L. Boger, David A. Cheresh
  • Patent number: 6777443
    Abstract: Compounds of the formula wherein R, R1, COOR2, R3-R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: August 17, 2004
    Assignee: Novartis AG
    Inventor: Cynthia Anne Fink
  • Publication number: 20040157922
    Abstract: Carboxyalkoxy-substituted acyl-carboxyphenylurea derivatives and their use as medicaments
    Type: Application
    Filed: October 6, 2003
    Publication date: August 12, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Elisabeth Defossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger, Alfons Enhsen
  • Patent number: 6693137
    Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: February 17, 2004
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, David Michael Bender, Buddy Eugene Cantrell, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Edward C. R. Smith, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20030144311
    Abstract: Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.
    Type: Application
    Filed: November 1, 2002
    Publication date: July 31, 2003
    Inventors: Tiziano Bandiera, Paola Vianello, Paolo Cozzi, Arturo Galvani
  • Patent number: 6534501
    Abstract: Chemical structures have been identified which allosterically modify pyrvate kinase and inhibit enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate related to the delivery of oxygen by modifying hemoglobin's oxygen affinity, treatments of tumor and cancer and Alzheimer's disease (AD).
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: March 18, 2003
    Assignees: Allos Therapeutics, Inc., Virginia Commonwealth University
    Inventors: Donald J. Abraham, Changging Wang, Richmond Danso-Danquah, James C. Burnett, Gajanan S. Joshi, Stephen J. Hoffman
  • Patent number: 6528543
    Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: March 4, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Antonio Focella, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
  • Patent number: RE39088
    Abstract: An amide compound of the formula (I): ? wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-?, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: May 2, 2006
    Assignee: Japan Tobacco, Inc.
    Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe