Patents Represented by Attorney, Agent or Law Firm Carol Loeschorn
  • Patent number: 6258843
    Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: July 10, 2001
    Assignee: Novartis AG
    Inventor: Paul W. Manley
  • Patent number: 6214360
    Abstract: The invention concerns topical formulations such as nail varnishes comprising as the active agent the compound of formula I in free base form or in acid addition salt form, together with a polymeric film former and further excipients as appropriate. It also concerns a process of preparation of such preparations by mixing with an appropriate polymeric film former and conventional further excipients as appropriate, and a method of treatment of onychomycosis.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: April 10, 2001
    Assignee: Novartis AG
    Inventors: Friedrich Richter, Marianne Roser
  • Patent number: 6143793
    Abstract: The hydrophilic penetration agents customarily used for the transcutaneous penetration of active ingredients are, surprisingly, found to improve the penetration of antifungal agents through the nails. A corresponding dermatological composition contains at least one antifungal agent chosen, in particular, from among those of the allylamine family, such as terbinafine-HCl and naftifine-HCl; at least one hydrophilic penetration agent chosen, in particular, from among the glycols, glycol monoethers, glycol diethers, dimethylsulphoxide, caprolactam, dimethylisosorbide, isopropylidene glycerol, dimethylimidazolidinone, ethyl lactate, the polyoxyethylenated C.sub.8 -C.sub.10 glycerides, polyethylene glycol 20 glyceryl laurate and dimethylacetamide; and a water-alcohol solvent medium which dissolves the said antifungal agent(s) and in which the said penetration agent(s) is (or are) at least partially miscible.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: November 7, 2000
    Assignee: Novartis AG
    Inventors: Jean-Pierre Laugier, Marie-France Rude, Philippe Touzan, Francois Rigenbach
  • Patent number: 6136821
    Abstract: Novel 8-aryl-1,7-naphthyridines, in free or salt form, are PDE IV inhibitors and are thus useful as pharmaceuticals, e.g. for asthma therapy. Preferred compounds include compounds of formulae (I and II) wherein the R groups are as defined. Pharmaceutical compositions comprising the compounds, processes for preparation of the compounds and novel intermediates for use in the processes are disclosed.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: October 24, 2000
    Assignee: Novartis AG
    Inventor: Rene Hersperger
  • Patent number: 6124453
    Abstract: A novel class of macrolides in whichi) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/orii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic .alpha.-amino acid residue; and/oriii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic .alpha.-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula IX ##STR1## is provided having immunosuppressant and antinflammatory properties and protected and ring-open forms thereof.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: September 26, 2000
    Assignee: Novartis AG
    Inventors: Theodor Fehr, Lukas Oberer, Valerie Quesniaux Ryffel, Jean-Jacques Sanglier, Walter Schuler
  • Patent number: 6107293
    Abstract: Compounds of formula (I) wherein X is --CH.sub.2 --, --CO-- or direct linkage, Y is --O--, --S-- or --NH--, R.sub.1 is phenyl, R.sub.2 .dbd.H or phenyl and R.sub.3 is H or --CH.sup.3 -- and their pharmaceutically acceptable salts have tachykinin antagonist activity and are useful as pharmaceuticals e.g. for the treatment of pain and migraine.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: August 22, 2000
    Assignee: Novaris AG
    Inventors: Christopher Simon John Walpole, Mahavir Prashad, Denis Har
  • Patent number: 6090817
    Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-.alpha. release.
    Type: Grant
    Filed: September 1, 1998
    Date of Patent: July 18, 2000
    Assignee: Novartis AG
    Inventor: Paul W. Manley
  • Patent number: 6051577
    Abstract: There are described pyrrolo[2,3]pyrimidines of formula I ##STR1## wherein R.sub.1 -R.sub.5, m and n are as defined in the description. The compounds have valuable pharmaceutical properties and are effective especially as tyrosine protein kinase inhibitors. They can be used in the treatment of bone diseases and other diseases in warm-blooded animals that can be favorably influenced by the inhibition of tyrosine protein kinase.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: April 18, 2000
    Assignee: Novartis AG
    Inventor: Eva Altmann
  • Patent number: 6013627
    Abstract: Cyclopeptolides of formula I ##STR1## wherein A, B, R, Leu, Leu, C, X and Y are as defined, are inhibitors of adhesion molecule expression and are thus useful for treatment of inflammatory and other diseases which involve increased levels of adhesion molecule expression.
    Type: Grant
    Filed: January 24, 1997
    Date of Patent: January 11, 2000
    Assignee: Novartis AG
    Inventors: Michael Morris Dreyfuss, Carolyn Ann Foster, Hans-Ulrich Naegeli, Berndt Oberhauser
  • Patent number: 5990116
    Abstract: The invention concerns compounds of formula I ##STR1## wherein the substituents have various meanings, and their use in the prevention or treatment of inflammatory and proliferative skin diseases and cancer.
    Type: Grant
    Filed: September 15, 1997
    Date of Patent: November 23, 1999
    Assignee: Novartis AG
    Inventor: Peter Nussbaumer
  • Patent number: 5985906
    Abstract: Use of a combination of the squalene epoxidase inhibitor terbinafine and an azole 14-alpha-methyldemethylase inhibitor (fluconazole or itraconazole) in mycotic infections caused by azole-resistant fungal strains, and corresponding pharmaceutical compositions, process and method.
    Type: Grant
    Filed: November 12, 1997
    Date of Patent: November 16, 1999
    Assignee: Novartis AG
    Inventors: Josef Gottfried Meingassner, Neil Stewart Ryder
  • Patent number: 5935998
    Abstract: Use of compounds of formula (I), wherein R has various significances, in free base form or in pharmaceutically acceptable salt form, as agents against H. pylori infection and associated diseases.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: August 10, 1999
    Assignee: Novartis AG
    Inventors: Ivan James Dalton Lindley, Neil Stewart Ryder
  • Patent number: 5929067
    Abstract: 1-Aryl-2-acylaminoethane compounds of formula I ##STR1## wherein R.sub.1 -R.sub.4, X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1 antagonists.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: July 27, 1999
    Assignee: Novartis AG
    Inventors: Marc Gerspacher, Andreas Von Sprecher, Silvio Roggo, Robert Mah, Silvio Ofner, Siem Jacob Veenstra, Claudia Betschart, Yves Auberson, Walter Schilling
  • Patent number: 5925649
    Abstract: The invention provides novel ascomycins bearing one or more physiologically hydrolyzable and acceptable oxycarbonyl moieties or carboxy moieties, such compounds being found useful as pharmaceuticals, especially in the treatment of asthma an dermatitis. Methods of producing the compounds and pharmaceutical compositions comprising the compounds are also provided.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: July 20, 1999
    Assignee: Novartis AG
    Inventors: Rene Hersperger, Reto Naef
  • Patent number: 5912238
    Abstract: The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: June 15, 1999
    Assignee: Novartis AG
    Inventors: Karl Baumann, Gerhard Emmer
  • Patent number: 5905156
    Abstract: The invention provides novel 2,2-di(C.sub.1-5 alkyl)- or trans-2,2-di(C.sub.1-5 alkyl)-3,4-dihydro-3-hydroxy- -4-carboxamido-6-(N-arylsulfonamido)-2H-1-benzopyrans; and N-oxides, esters and salts thereof; processes for their production; and their uses as pharmaceuticals, e.g. as K.sup.+ -channel openers, bronchodilators and agents for the suppression of airways hyperreactivity, e.g., for use in the treatment of asthma.
    Type: Grant
    Filed: November 20, 1997
    Date of Patent: May 18, 1999
    Assignee: Novartis AG
    Inventor: Paul W. Manley
  • Patent number: 5866105
    Abstract: The invention concerns topical formulations such as nail varnishes comprising as the active agent the compound of formula I ##STR1## in free base form or in acid addition salt form, together with a polymeric film former and further excipients as appropriate. It also concerns a process of preparation of such preparations by mixing with an appropriate polymeric film former and conventional further excipients as appropriate, and a method of treatment of onychomycosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 2, 1999
    Assignee: Novartis AG
    Inventors: Friedrich Richter, Marianne Roser
  • Patent number: 5852005
    Abstract: The present invention relates to 17 .alpha.-dammara compounds having immunosuppressant and antiinflammatory activity and which are useful as pharmaceuticals, particularly for use as immunosuppressant and antiinflammatory agents. Specific 17 .alpha.-dammara compounds are included per se, for example the compound of formula IC, i.e. 17 .alpha.-23-(E)-dammara-20, 23-dien-3.beta., 25-diol, which may be obtained from the flour of the shoots of the Palmyrah palm, Borassus flabellifer L. In addition, processes for the synthesis of this and other dammara compounds and intermediates thereof are described.
    Type: Grant
    Filed: January 24, 1997
    Date of Patent: December 22, 1998
    Assignee: Novartis AG
    Inventors: Peter Hiestand, Reto Naef, Hans-Ulrich Naegeli, Lukas Oberer, Laszlo Revesz, Hans-Jorg Roth
  • Patent number: 5814305
    Abstract: The hydrophilic penetration agents customarily used for the transcutaneous penetration of active ingredients are, surprisingly, found to improve the penetration of antifungal agents through the nails. A corresponding dermatological composition contains at least one antifungal agent chosen, in particular, from among those of the allylamine family, such as terbinafine-HCl and naftifine-HCl; at least one hydrophilic penetration agent chosen, in particular, from among the glycols, glycol monoethers, glycol diethers, dimethylsulphoxide, caprolactam, dimethylisosorbide, isopropylidene glycerol, dimethylimidazolidinone, ethyl lactate, the polyoxyethylenated C.sub.8 -C.sub.10 glycerides, polyethylene glycol 20 glyceryl laurate and dimethylacetamide; and a water-alcohol solvent medium which dissolves the said antifungal agent(s) and in which the said penetration agent(s) is (or are) at least partially miscible.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: September 29, 1998
    Assignee: Novartis AG
    Inventors: Jean-Pierre Laugier, Marie-France Rude, Philippe Touzan, Fran.cedilla.ois Rigenbach
  • Patent number: 5759565
    Abstract: Pharmaceutical compositions for nasal administration comprising i) a calcitonin, and ii) benzalkonium chloride, and/or iv) a surfactant, suitable for application to the nasal mucosa, in iii) a liquid diluent or carrier, suitable for application to the nasal mucosa. The compositions are suitably adapted for administration in the form of a nasal spray.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: June 2, 1998
    Assignee: Novartis Corporation
    Inventors: Moise Azria, Thomas Cavanak