Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
Abstract: A dosage form which is, in particular, sheet-like and rapidly disintegrating or soluble in an aqueous environment for rapid release of active ingredients in the oral cavity, in body orifices or in body cavities, where the dosage form comprises a matrix which comprises one or more water -soluble polymers as base substances, and comprises at least one active ingredient, is characterized in that the dosage form is provided with spaces or cavities which are present in the polymeric matrix and whose contents differ in terms of the state of aggregation from the matrix.
Type:
Grant
Filed:
July 29, 2011
Date of Patent:
November 20, 2012
Assignee:
LTS Lohmann Therapie-Systeme AG
Inventors:
Christian Von Falkenhausen, Markus Krumme, Wolfgang Laux
Abstract: What is described is a process for preparing compounds of the general formula (I) in which R1, R2 and R3 independently of one another represent hydrogen, an alkyl group or an aryl group, wherein compounds of the general formula (II) in which R1 and R2 have the meaning given for formula (I), are reacted with an alkylating agent of the general formula (III) R3X??(III), in which X represents a halogen atom and R3 has the meaning given for formula (I), if appropriate in a solvent.
Type:
Grant
Filed:
April 6, 2009
Date of Patent:
November 13, 2012
Assignee:
Saltigo GmbH
Inventors:
Andreas Job, Denys Baskakov, Ralf Krahwinkel, Antje Hieronymi
Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
February 13, 2012
Date of Patent:
November 13, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.
Type:
Grant
Filed:
May 14, 2009
Date of Patent:
November 13, 2012
Assignee:
Threshold Pharmaceuticals
Inventors:
Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
Abstract: A method for producing a compound represented by the following formula (2) (wherein, X, R1 and m represent respectively the same meaning as described below) which comprises reacting a compound represented by the following formula (1) (wherein, X represents an optionally substituted alkyl group or the like. R1 represents an optionally substituted alkyl group or the like. m represents an integer of 0 to 4. When m represents an integer of 2 to 4, R1s may be the same or different from each other) with hydrogen cyanide in an amount of 1.2 to 5 mol with respect to 1 mol of the compound, in the presence of an organic base, in an organic solvent.
Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
Type:
Grant
Filed:
October 4, 2007
Date of Patent:
November 13, 2012
Assignee:
Bionomics Limited
Inventors:
Bernard Luke Flynn, Jonathan B. Baell, Andrew J. Harvey, Jason Hugh Chaplin, Dharam Paul, Jorgen Alvar Mould
Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
Abstract: The present invention relates to N-cycloalkyl-benzyl-thiocarboxamide or N-cycloalkyl-benzyl-N-substituted-carboximidamide amide derivatives of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl; T represents S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl and Z2; Z3, X and n represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
Type:
Grant
Filed:
July 31, 2008
Date of Patent:
November 13, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Jean-Pierre Vors
Abstract: A method of preparing novel [11C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [11C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [11C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.
Abstract: Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban.
Abstract: This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
Type:
Grant
Filed:
June 20, 2012
Date of Patent:
November 13, 2012
Assignee:
Pfizer Inc.
Inventors:
Sally Gut Ruggeri, Joel M Hawkins, Teresa M Makowski, Jennifer L Rutherford, Frank J Urban
Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
Type:
Grant
Filed:
April 7, 2011
Date of Patent:
November 13, 2012
Assignee:
Serenex, Inc.
Inventors:
Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
Abstract: Provided herein are ruthenium complexes of Formula (I), and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.
Abstract: The present invention relates to multi-substituted m-diarylanilines or pharmaceutically acceptable salts thereof, wherein X, R1-R7 are as defined in the claims, their preparation process, pharmaceutical compositions comprising them and their use for the manufacture of a medicament for anti-HIV.
Type:
Grant
Filed:
October 7, 2008
Date of Patent:
November 13, 2012
Assignees:
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences P.L.A. China
Inventors:
Lan Xie, Bingjie Qin, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
Abstract: A method of providing a cooling sensation to the skin or the mucous membranes of the body, comprising the application thereto of at least one compound of the Formula I in which X is selected from S and O, R1 is selected from H and OMe, R2 is selected from OH, OMe and OEt, and R3 is selected from H and OH. Some of the compounds provide simultaneously cooling and sweetening effects.
Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted homopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R5 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, or a salt thereof.
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
July 18, 2006
Date of Patent:
October 2, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
Abstract: The invention relates to a process for preparing furanose derivatives, to furanose intermediates used in said process and to the use of said derivatives in the manufacture of atorvastatin.
Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
Type:
Grant
Filed:
September 27, 2011
Date of Patent:
September 25, 2012
Assignee:
Amira Pharmaceuticals, Inc.
Inventors:
John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr