Abstract: Tenascin-W, an extracellular matrix molecule that is specifically expressed in metastatic tumours is provided. A system comprising a sample expressing tenascin-W is used as an in vitro method for screening possible anti-tumour agents or for agents that promote osteogenesis.
Type:
Grant
Filed:
March 26, 2003
Date of Patent:
March 23, 2010
Assignee:
Novartis Forschungsstiftung Zweignlederlassung Friedrich Miescher Institute for Biomedical Research
Abstract: The invention relates to isothiourea derivatives of formula I: wherein R1 is a residue of one of the following structures: where the variables are as defined in the claims of the invention, as well as processes for production of these compounds.
Type:
Grant
Filed:
February 25, 2005
Date of Patent:
March 2, 2010
Assignee:
Novartis AG
Inventors:
Fraser Glickman, Markus Streiff, Gebhard Thoma, Hans-Günter Zerwes
Abstract: The invention relates to a process for the purification of riboflavin comprising the steps of (a) precipitating a first crystalline form of riboflavin, (b) isolating the first crystalline form of riboflavin, (c) transforming the first crystalline form of riboflavin into a second crystalline form of riboflavin under conditions that decompose diluted DNA, and (d) isolating the second crystalline form of riboflavin, provided that at ambient temperature the first crystalline form of riboflavin is thermodynamically less stable than the second crystalline form of riboflavin.
Abstract: Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders
Type:
Grant
Filed:
May 29, 2006
Date of Patent:
February 23, 2010
Assignee:
Novartis AG
Inventors:
Rolf Baenteli, Fraser Glickman, Jiri Kovarik, Ian Lewis, Markus Streiff, Gebhard Thoma, Hans-Günter Zerwes
Abstract: This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation.
Type:
Grant
Filed:
January 19, 2005
Date of Patent:
January 19, 2010
Assignee:
Novartis AG
Inventors:
Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou, Walter Schuler
Abstract: The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.
Abstract: A process for the manufacture of an acetylenically unsaturated alcohol comprising reacting formaldehyde, an aldehyde or a ketone (a carbonyl compound) with acetylene in the presence of ammonia and an alkali metal hydroxide, the molar ratio of the alkali metal hydroxide to the carbonyl compound being less than 1:200. The reaction products, which depending on the starting carbonyl compound are propargyl alcohol or 1-monosubstituted or 1,1-disubstituted derivatives thereof, are of use as intermediates in the synthesis of many useful end products, inter alia in the field of vitamins and carotenoids.
Type:
Grant
Filed:
August 9, 2003
Date of Patent:
December 29, 2009
Assignee:
DSM IP Assets B.V.
Inventors:
Werner Bonrath, Peter Scheer, Johannes Tschumi, Reto Zenhaeusern
Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.
Type:
Grant
Filed:
February 5, 2008
Date of Patent:
December 1, 2009
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler
Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and n are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
Type:
Grant
Filed:
April 29, 2004
Date of Patent:
December 1, 2009
Assignee:
Novartis AG
Inventors:
Klaus Hinterding, Carsten Spanka, Frédéric Zecri
Abstract: A compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof wherein the variables have the meanings as defined in the specification. Further disclosed are a method of inhibiting IKK activity using a compound of formula I, a method of inhibiting production of TNF using a compound of formula I, a compound of formula I for use as a pharmaceutical, a pharmaceutical composition comprising a compound of formula I, and use of a compound of formula I in the manufacture of a medicament for use as an immunosuppressant or anti-inflammatory agent.
Type:
Grant
Filed:
April 8, 2004
Date of Patent:
November 10, 2009
Assignee:
Novartis AG
Inventors:
Birgit Bollbuck, Alastair DenholmMritain, Jörg Eder, René Hersperger, Philipp Janser, Lászlo Révész, Achim Schlapbach, Rudolf Wálchi
Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
Type:
Grant
Filed:
September 12, 2003
Date of Patent:
November 3, 2009
Assignee:
Novartis AG
Inventors:
Peter Buehlmayer, Klaus Hinterding, Carsten Spanka, Frédéric Zecri
Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
Type:
Grant
Filed:
March 20, 2006
Date of Patent:
October 20, 2009
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jörg Velker, Thomas Weller
Abstract: Novel hydroxamic acid derivatives, e.g., of formula (I), wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided.
Type:
Grant
Filed:
April 8, 2003
Date of Patent:
September 15, 2009
Assignee:
Novartis AG
Inventors:
Philipp Janser, Wolfgang Miltz, Ulf Neumann
Abstract: The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
Abstract: The present invention provides a method for identifying an agent to be tested for an ability to treat a psychotic disorder in a patient in need of such treatment. The invention provides a method for screening candidate drugs for anti-psychotic drug activity, preferably atypical anti-psychotic activity, comprising contacting cells or tissues with a candidate drug, determining levels of phosphorylation of the intracellular signaling proteins, DARPP-32, ERK1, ERK2 and CREB, in said cells or tissues and determining the pattern of the levels of phosphorylation of the proteins. The pattern of the levels of phosphorylation of DARPP-32, ERK1, ERK2 and CREB is, in certain embodiments, compared with the pattern of the levels of phosphorylation of DARPP-32, ERK1, ERK2 and CREB in the presence of an atypical anti-psychotic drug.
Abstract: A human protein (designated Carboxy-terminal Modulating protein, CTMP) is described and is identified as having tumour suppressor properties. CTMP has been shown to interact with protein kinase B and inhibit protein kinase B activity, establishing its importance in the protein kinase B signalling pathway.
Type:
Grant
Filed:
June 7, 2001
Date of Patent:
July 8, 2008
Assignee:
Novartis Forschungsstiftung Zweigniederlassung Friedrich Miescher Institute for Biomedical Research
Abstract: The invention concerns a method for obtaining extracts based on polyphenol compounds contained in cocoa, characterised in that it includes: using fresh beans, which have not been pre-treated or defatted, said fresh beans whereof their pulp and shell have been eliminated, so as to obtain clean almonds; grinding said almonds, in the presence of solvent(s); macerating the ground almonds in conditions enabling extraction of the desired compounds; filtering the macerated mixture; recuperating an extract containing said compounds from the filtrate. The invention also concerns the extracts and their uses for cosmetic, food and therapeutic purposes.
Type:
Grant
Filed:
August 10, 2001
Date of Patent:
May 6, 2008
Assignee:
Barry Callebaut France
Inventors:
Jean-Paul Lecoupeau, Joseph Vercauteren
Abstract: The invention provides 1-phenethyl-3 (R)-(9[H]-xanthene-9-carbonyloxy)-1 -azoniabicyclo[2.2.2]octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders.
Type:
Grant
Filed:
December 8, 2006
Date of Patent:
April 15, 2008
Assignee:
Laboratories Almirall, S.A.
Inventors:
María Dolors Fernandez Forner, María Prat Quiñones, María Antonia Buil Albero
Abstract: Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.
Abstract: The invention relates to novel alkansulfonamides of structure (I), wherein R1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions.
Type:
Grant
Filed:
December 10, 2002
Date of Patent:
January 29, 2008
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller