Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
Abstract: The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses.
Abstract: Disclosed herein are substituted pyrazine compounds and tautomers, stereoisomers, solvates, or pharmaceutically acceptable salts thereof for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition, including compounds of formula I:
Type:
Grant
Filed:
December 20, 2006
Date of Patent:
September 28, 2010
Assignee:
Novartis AG
Inventors:
Stephen Paul Collingwood, Nichola Smith
Abstract: The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri- Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
Abstract: A process for the preparation of polymer magnetic particles, which comprises: providing polymer particles having a porous interior, and contacting the polymer particles with a magnetic fluid comprising a homogeneous dispersion of magnetic particles, whereby the magnetic particles are incorporated into the porous interior to produce polymer magnetic particles.
Abstract: A method of preparing an antibody- or antibody fragment-targeted cationic immunoliposome or polymer complex comprises the steps of (a) preparing an antibody or antibody fragment; (b) mixing said antibody or antibody fragment with a cationic liposome to form a cationic immunoliposome or with a cationic polymer to form a polyplex; and (c) mixing said cationic immunoliposome or said polyplex with a therapeutic or diagnostic agent to form said antibody- or antibody fragment-targeted cationic immunoliposome or polymer complex.
Abstract: The present invention relates to a copolymer, which is the reaction product of (a) a first prepolymer, comprising a bioactive moiety and at least one radically polymerizable group, and (b) a second prepolymer which is a polyvinyl alcohol having a weight average molecular weight of at least about 2000 that, based on the number of hydroxy groups of the polyvinyl alcohol, comprises from 0.5 to 80% structural units of formula (I) wherein: R is alkylene having up to 8 carbon atoms, R1 is hydrogen or alkyl having up to seven carbon atoms, and R2 is an olefinically unsaturated, electron-attracting copolymerizable radical.
Type:
Grant
Filed:
February 27, 2004
Date of Patent:
August 10, 2010
Assignee:
Eyesense AG
Inventors:
Achim Müller, Roland Schmieder, Katharina Schmid
Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and X have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
December 13, 2006
Date of Patent:
July 13, 2010
Assignee:
Novartis AG
Inventors:
Emma Budd, Julia Doris Ida Hatto, Judy Fox Hayler, Darren Mark Legrand, Barbara Valade
Abstract: The present invention provides a method for the production of free-flowing additive compounds that comprises the steps of preparation of a particulate additive compound and storage of a mass of the particulate additive compound at a surface pressure of at least 30 g/cm2 until the mass of additive compound is baked together. Then follows the crushing of the baked-together mass of the additive compound into a crushed particulate additive compound and the sieving of the crushed particulate additive compound, whereby particles of a size in excess of 4.0 mm and particles of a size of less than 0.1 mm are separated from the crushed particulate additive compound such that a fraction containing a free-flowing additive compound with long-term stability of particle sizes is obtained.
Type:
Grant
Filed:
October 23, 2008
Date of Patent:
May 25, 2010
Assignee:
Raschig GmbH
Inventors:
Steffen Denzinger, Frank Harréus, Alexander Schmitt
Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5 R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: in free base or acid addition salt form, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
Type:
Grant
Filed:
December 14, 2006
Date of Patent:
May 11, 2010
Assignee:
Novartis AG
Inventors:
Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Manuel Koller
Abstract: The present invention relates to the use of a 2-cyanopyrimidine compound of the formula wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.
Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.
Type:
Grant
Filed:
April 24, 2006
Date of Patent:
April 13, 2010
Assignee:
Novartis AG
Inventors:
Ralf Glatthar, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
Abstract: The present invention relates to novel isoquinoline-3-carboxylic acid amides having ?7 nicotinic acetylcholine receptor agonistic activity, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
Type:
Grant
Filed:
April 10, 2006
Date of Patent:
February 2, 2010
Assignee:
Novartis AG
Inventors:
Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
Abstract: The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
June 26, 2007
Date of Patent:
February 2, 2010
Assignee:
Novartis AG
Inventors:
Yves Auberson, Ralf Glatthar, Rhys Salter, Oliver Simic, Marina Tintelnot-Blomley