Additional Hetero Ring, Which Is Attached Directly Or Indirectly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/517)
  • Patent number: 7638550
    Abstract: The invention describes new compounds derived from formula I pyrroles, methods for obtaining them and their application as drugs in pharmaceutical compositions for the treatment of cancer due to their inhibitory activity on certain histone deacetylases.
    Type: Grant
    Filed: December 27, 2005
    Date of Patent: December 29, 2009
    Assignee: Universidad del Pais Vasco-Euskal Herriko Unibertsitatea (UPV-EHU) Fundacion Centro Nacional de Investigaciones Oncologicas Carlos III (CNIO)
    Inventors: Fernando Pedro Cossio Mora, Manel Esteller Badosa, Aizpea Zubia Olascoaga, Dorleta Otaegui Ansa
  • Publication number: 20090306396
    Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.
    Type: Application
    Filed: October 3, 2006
    Publication date: December 10, 2009
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
  • Publication number: 20090306156
    Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Application
    Filed: August 4, 2009
    Publication date: December 10, 2009
    Inventors: Allen HOPPER, Robert Francis Dunn, Erik Mikal Kuester, Richard Dennis Conticello, Ruiping Liu, Ashok Tehim
  • Patent number: 7625932
    Abstract: The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: December 1, 2009
    Assignee: Eli Lilly and Company
    Inventors: Pamela Ann Albaugh, Esteban Dominguez-Manzanares, Jian Eric Hong, William Joseph Hornback, Delu Jiang, Paul Leslie Ornstein, Michelle Lee Thompson, Eric George Tromiczak, Zhipei Wu, Hamideh Zarrinmayeh, Dennis Michael Zimmerman, Ana Maria Castano Mansanet, Larry Gene Huffman, William David Miller
  • Publication number: 20090286980
    Abstract: The present invention provides a compound of the formula (III): wherein R is a C1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3?-pyrrolidine derivatives such as Ranirestat being a promising therapeutic agent for diabetic complications in a short process, in an economically advantageous manner and in high yields, and the process for preparing the same.
    Type: Application
    Filed: June 13, 2007
    Publication date: November 19, 2009
    Inventors: Daisuke Tanaka, Toshiyuki Negoro
  • Publication number: 20090281161
    Abstract: Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described.
    Type: Application
    Filed: June 11, 2007
    Publication date: November 12, 2009
    Inventors: Juergen Klaus Maibaum, Edwige Liliane Jeanne Lorthiois
  • Publication number: 20090270417
    Abstract: Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described.
    Type: Application
    Filed: June 11, 2007
    Publication date: October 29, 2009
    Applicant: NOVARTIS AG
    Inventors: Juergen Klaus Maibaum, Edwige Liliane Jeanne Lorthiois, Peter Buehimayer
  • Patent number: 7608592
    Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: October 27, 2009
    Assignee: ViroBay, Inc.
    Inventors: Michael Graupe, John O. Link, Chandrasekar Venkataramani
  • Patent number: 7601752
    Abstract: The invention is concerned with novel pyrrolidine derivatives of formula (I) wherein X, Y, R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
    Type: Grant
    Filed: November 6, 2006
    Date of Patent: October 13, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lilli Anselm, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Jacques Himber, Bernd Kuhn, Narendra Panday, Fabienne Ricklin, Stefan Thomi
  • Publication number: 20090247503
    Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.
    Type: Application
    Filed: March 25, 2009
    Publication date: October 1, 2009
    Applicants: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Chengyong Li, Shiwu Chen
  • Publication number: 20090239866
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: July 28, 2006
    Publication date: September 24, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Publication number: 20090239867
    Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: March 17, 2009
    Publication date: September 24, 2009
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Patent number: 7589119
    Abstract: This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound. The Benzopyranone Compounds have the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is halogen, trifluoromethyl or C1-6 alkyl.
    Type: Grant
    Filed: February 22, 2008
    Date of Patent: September 15, 2009
    Assignee: Signal Pharmaceutical, LLC
    Inventors: Glenn Friedman, Jeffrey McKie, Jonathan Wright, Sophie Perrin-Ninkovic, Bernd M. Stein
  • Publication number: 20090227635
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 10, 2009
    Applicant: ALLERGAN, INC.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7585882
    Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: September 8, 2009
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Allen Hopper, Robert Francis Dunn, Erik Mikal Kuester, Richard Dennis Conticello, Ruiping Liu, Ashok Tehim
  • Publication number: 20090221839
    Abstract: Atorvastatin lactone is prepared by hydrogenating tert-butyl isopropylidene nitrile to tert-butyl isopropylidene amine and condensing the amine with the diketone of atorvastatin to form acetonide ester. The diol protecting acetonide ester is deprotected to form a diol ester by dissolving the acetonide ester in methanol and treating with an acid. The diol ester is saponified to form a sodium salt. Methanol is removed from the reaction mixture by distillation. The sodium salt is reacidified to the free diol acid and atorvastatin lactone is formed from the diol acid. The atorvastatin lactone is directly dried without further purification.
    Type: Application
    Filed: September 9, 2005
    Publication date: September 3, 2009
    Inventors: Susan O'Sullivan, John O'Neill
  • Patent number: 7582749
    Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: September 1, 2009
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, Meng He, Terry A. Kellar, II, Forrest R. Blackburn
  • Patent number: 7576102
    Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: August 18, 2009
    Assignee: deCODE genetics ehf
    Inventors: Vincent Sandanayaka, Jasbir Singh, Mahnaz Keyvan, Michael David Krohn, Mark E. Gurney
  • Patent number: 7572824
    Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, and the products thereby are provided.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: August 11, 2009
    Assignee: Wyeth
    Inventor: Bogdan K. Wilk
  • Publication number: 20090186834
    Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.
    Type: Application
    Filed: March 24, 2006
    Publication date: July 23, 2009
    Applicant: MICROBIA, INC.
    Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
  • Patent number: 7563910
    Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
    Type: Grant
    Filed: May 9, 2005
    Date of Patent: July 21, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Mayweg, Robert Narquizian, Philippe Pflieger, Stephan Roever
  • Publication number: 20090176836
    Abstract: The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: July 28, 2006
    Publication date: July 9, 2009
    Inventors: Philippe G. Nantermet, Joseph P. Vacca
  • Patent number: 7553861
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Grant
    Filed: April 21, 2006
    Date of Patent: June 30, 2009
    Assignee: Alantos Pharmaceuticals Holding, Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Arthur Taveras
  • Patent number: 7550502
    Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.
    Type: Grant
    Filed: March 20, 2007
    Date of Patent: June 23, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7550487
    Abstract: The invention is concerned with novel pyrrolidine-3,4-dicarboxamide derivatives of formula (I) wherein R1 to R9 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: June 23, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lilli Anselm, Katrin Groebke Zbinden, Wolfgang Haap, Jacques Himber, Christoph Martin Stahl, Stefan Thomi
  • Patent number: 7547694
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: June 16, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Kirsten Arndt, Henri Doods, Gerhard Schaenzle
  • Patent number: 7538138
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: May 26, 2009
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
  • Patent number: 7534810
    Abstract: Novel salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: May 19, 2009
    Assignee: Pfizer Inc.
    Inventors: Anthony Michael Campeta, Joseph F. Krzyzaniak, Jason Albert Leonard
  • Publication number: 20090118298
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.
    Type: Application
    Filed: September 25, 2008
    Publication date: May 7, 2009
    Inventors: Dawn M. George, Lu Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
  • Patent number: 7528156
    Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: November 22, 2004
    Date of Patent: May 5, 2009
    Assignee: AstraZeneca AB
    Inventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
  • Patent number: 7521470
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: April 21, 2009
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • Patent number: 7504243
    Abstract: The present invention relates to compositions and methods for the production of biliverdin. In particular, the invention concerns methods for producing biliverdin in yeast, especially Candida albicans, and other microorganisms.
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: March 17, 2009
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Michael L. Pendrak, David D. Roberts
  • Patent number: 7504429
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a substituted pyrrole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: March 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Annette S. Kim, Xufang Zhang
  • Publication number: 20090062553
    Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protecting
    Type: Application
    Filed: August 14, 2008
    Publication date: March 5, 2009
    Applicant: NPIL PHARMACEUTICALS (UK) LIMITED
    Inventors: David John Moody, Jonathan William Wiffen
  • Patent number: 7498447
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: March 3, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090048429
    Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
    Type: Application
    Filed: March 7, 2008
    Publication date: February 19, 2009
    Inventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
  • Patent number: 7482475
    Abstract: Disclosed herein is a compound having a structure Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: January 27, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Robert M. Burk
  • Patent number: 7476747
    Abstract: A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090012148
    Abstract: Compounds disclosed herein may be used in disclosed methods for reducing the amount of cholesterol in a cell, for treating a patient suffering from a disorder characterized by cellular accumulation of cholesterol (such as Niemann-Pick Disease Type C or atherosclerosis), and/or for treating or preventing phospholipidosis. In some embodiments, the compounds may include a pyrrolone or triazine moiety.
    Type: Application
    Filed: October 31, 2006
    Publication date: January 8, 2009
    Inventors: Frederick R. Maxfield, Anthony Sauve
  • Publication number: 20080292587
    Abstract: The present invention discloses compounds of formulae I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 24, 2008
    Publication date: November 27, 2008
    Inventors: Ying Sun, Yat Sun Or, Zhe Wang
  • Patent number: 7456209
    Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: November 25, 2008
    Assignee: Tetralogic Pharmaceuticals Corporation
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Patent number: 7456164
    Abstract: The invention relates to 3- or 4-monosubstituted phenol and thiophenol derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol and thiophenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: May 9, 2005
    Date of Patent: November 25, 2008
    Assignee: Pfizer, Inc
    Inventors: Patrick Bernardelli, Andrew Michael Cronin, Alexis Denis, Stephen Martin Denton, Henry Jacobelli, Mark Ian Kemp, Edwige Lorthiois, Fiona Rousseau, Delphine Serradeil-Civit, Fabrice Vergne
  • Publication number: 20080262246
    Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, or a salt thereof, and a compound of formula VI or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.
    Type: Application
    Filed: October 16, 2006
    Publication date: October 23, 2008
    Inventors: Gottfried Sedelmeier, Dominique Grimler, Murat Acemoglu
  • Publication number: 20080255220
    Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: June 6, 2006
    Publication date: October 16, 2008
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Patent number: 7429603
    Abstract: The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
    Type: Grant
    Filed: April 26, 2004
    Date of Patent: September 30, 2008
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Mark R. Player, Nand Baindur, Benjamin Brandt, Naresh Chadha, Raymond J. Patch, Davoud Asgari, Taxiarchis M. Georgiadis
  • Publication number: 20080227806
    Abstract: The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.
    Type: Application
    Filed: September 28, 2006
    Publication date: September 18, 2008
    Applicant: AMERICAN LIFE SCIENCE PHARMACEUTICALS
    Inventor: Robert Ternansky
  • Patent number: 7425575
    Abstract: The present invention relates to novel phenyl-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y, Z and R3 are as defined above, to processes and intermediates for their preparation and to their use as pesticides, microbicides and herbicides.
    Type: Grant
    Filed: September 11, 2002
    Date of Patent: September 16, 2008
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Udo Reckmann, Christoph Erdelen
  • Publication number: 20080220286
    Abstract: The present invention relates to a dinaphthyl ethylene derivative of formula (I), a process for preparing it, a film prepared from it useful in the manufacure of an organic light emitting device (OLED), an OLED including the film, and the use of the dinaphthyl ethylene derivative in the manufacture of an OLED. Wherein R1 to R16 are defined as in the specification.
    Type: Application
    Filed: January 30, 2008
    Publication date: September 11, 2008
    Applicants: Tsinghua University, Beijing Visionox Technology Co., LTD
    Inventors: Yong Qiu, Han Chen, Yinkui Li
  • Patent number: RE40525
    Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: September 30, 2008
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic
  • Patent number: RE40667
    Abstract: [R-(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-((1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl)]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluoro-phenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 17, 2009
    Assignee: Warner-Lambert Company LLC
    Inventor: Bruce Roth