Abstract: A compound of Formula I or a hydrate or solvate thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
June 8, 2009
Date of Patent:
August 7, 2012
Assignee:
Novartis AG
Inventors:
Stephen Paul Collingwood, Nicholas James Devereux, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt
Abstract: The provision of animal feed pellets is described, which pellets comprise, as antibiotic, a pleuromutilin derivative is stabilized form, namely in the form of microspherules. The pleuromutilin derivatives in question have the general formula (I) wherein R1 is ethyl or vinyl, there is either a double bond or a single bond between carbon atoms 1 and 2, Ra and Rb are each independently of the other hydrogen or halogen, and T is a short or long-chain organic radical.
Type:
Grant
Filed:
November 27, 2002
Date of Patent:
August 7, 2012
Assignee:
Novartis AG
Inventors:
Susanne Christine Wieland-Berghausen, Ferenc Jozsef Rakoczi, Brigitte Monika Cron-Eckhardt
Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
Type:
Grant
Filed:
October 31, 2008
Date of Patent:
August 7, 2012
Assignee:
Novartis AG
Inventors:
Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
Abstract: The invention pertains to dispersible tablets comprising as active ingredient 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or pharmaceutically acceptable salt thereof in an amount of from 5 to 40% in weight by weight of the total tablet.
Abstract: The present application relates to cyclic depsipeptides, or derivatives thereof, having the structure of formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7 and human neutrophil elastase.
Type:
Application
Filed:
February 14, 2012
Publication date:
August 2, 2012
Applicant:
NOVARTIS AG
Inventors:
Philipp KRASTEL, Brigitta-Maria LIECHTY, Josef Gottfried MEINGASSNER, Esther SCHMITT, Erwin Paul SCHREINER
Abstract: This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.
Type:
Application
Filed:
October 20, 2010
Publication date:
August 2, 2012
Applicant:
NOVARTIS AG
Inventors:
Gregory Raymond Bebernitz, Mark Gary Bock, Debnath Bhuniya, Laxmikant Datrange, Suresh Eknath Kurhade, P. Venkata Palle, Dumbala Srinivas Reddy
Abstract: Benzotriazole UV/Visible light-absorbing monomers are disclosed. The UV/Vis absorbers are particularly suitable for use in intraocular lens materials.
Abstract: An improved multifocal design for an ocular implant is provided. This ocular implant includes an intraocular lens (IOL) and a number of haptics. The IOL passes optical energy. A microstructure within the IOL places the IOL under tension. The microstructure is operable to be broken in a controlled manner to release tension in the IOL and reshape the IOL. This may be done at any time post operatively and in conjunction with wavefront aberrometry to provide improved results. The haptics mechanically couple to the IOL in order to position and secure the IOL within the eye.
Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.
Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-9, and/or MMP-12 and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
Type:
Grant
Filed:
March 27, 2007
Date of Patent:
July 31, 2012
Assignee:
Novartis AG
Inventors:
Thomas Leutert, Jonathan E Grob, Ruben Alberto Tommasi, Erin E. Pusateri, Ayako Honda
Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
Type:
Grant
Filed:
February 21, 2012
Date of Patent:
July 24, 2012
Assignee:
Novartis AG
Inventors:
Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
Abstract: NMB1870 is a protein in Neisseria meningitidis. Three families of NMB1870 are known. To increase the ability of a NMB1870 protein to elicit antibodies that are cross-reactive between the families, NMB1870 is engineered. Sequences can be substituted from one NMB1870 family into the corresponding position in another family. Proteins of NMB1870 sequences from different families can be joined to each other.
Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
Type:
Grant
Filed:
September 10, 2009
Date of Patent:
July 24, 2012
Assignee:
Novartis AG
Inventors:
Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach, Giorgio Caravatti, Pascal Furet
Abstract: The present invention provides novel methods of inhibiting fibrosis, as well as methods of treating or inhibiting fibrotic disorders, using BMP9 and/or BMP10 antagonists. The present invention also provides methods of assessing whether a subject has or is at risk of developing a fibrotic disorder by detecting levels of BMP9 and/or BMP10. Further provided are methods of assessing the efficacy of a treatment regimen for treating a fibrotic disorder by detecting and comparing pre-treatment levels of BMP9 and BMP10 with post-treatment levels of BMP9 and BMP10.
Type:
Application
Filed:
May 7, 2010
Publication date:
July 19, 2012
Applicant:
NOVARTIS AG
Inventors:
Alan Buckler, Chao-Min Chen, Chantale T. Guy, Jeffrey Hewett
Abstract: The present invention relates to polypeptides directed against or specifically binding to chemokine receptor CXCR2 and in particular to polypeptides capable of modulating signal transduction from CXCR2. The invention also relates to nucleic acids, vectors and host cells capable of expressing the polypeptides of the invention, pharmaceutical compositions comprising the polypeptides and uses of said polypeptides and compositions for treatment of diseases involving aberrant functioning of CXCR2.
Type:
Application
Filed:
November 7, 2011
Publication date:
July 19, 2012
Applicant:
NOVARTIS AG
Inventors:
Michelle BRADLEY, Zarin BROWN, Steven John CHARLTON, Karen CROMIE, Bruno DOMBRECHT, Soren STEFFENSEN, Gino VAN HEEKE
Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
November 16, 2010
Date of Patent:
July 17, 2012
Assignee:
Novartis AG
Inventors:
Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi
Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
Type:
Grant
Filed:
March 23, 2009
Date of Patent:
July 17, 2012
Assignee:
Novartis AG
Inventors:
Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
Abstract: A filter and method for filtering an optical beam are disclosed. One embodiment of the filter is an optical filter for filtering an incident light beam, comprising an optically effective material characterized by: a light transmittance of less than 1% for wavelengths below 420 nm; and a light transmittance for wavelengths complementary and near complementary to wavelengths below 420 nm that, combined with the transmittance for wavelengths below 420 nm, will yield a filtered light beam having a luminosity of about 90% and an excitation purity of 5% or less. The complementary wavelengths can be wavelengths above about 640 nm, wavelengths above about 660 nm, and/or wavelengths from about 540 nm to about 560 nm. Further, in one embodiment the difference between the light transmittance just below 420 nm and the light transmittance just above 420 nm can be greater than 90%. Above 420 nm, in some embodiments, the light transmittance can be arbitrarily determined.
Abstract: A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.
Type:
Grant
Filed:
May 17, 2006
Date of Patent:
July 17, 2012
Assignee:
Novartis AG
Inventors:
Gabriel Galvin, Eric Harwood, David Ryckman, Shuguang Zhu