Patents Represented by Attorney, Agent or Law Firm Thomas R. Savitsky
  • Patent number: 7355043
    Abstract: A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C1-6 alkoxy or pheny C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II) wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and as necessary or desired, interconverting variables R1, R2 and R3 to further values of
    Type: Grant
    Filed: December 14, 2004
    Date of Patent: April 8, 2008
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventor: John Robert Mansfield Dales
  • Patent number: 7297703
    Abstract: A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2, 6-di-tert.-butyl-4-methylphenol. The presence of the antioxidant improves the stability of the poly-ene macrolide to oxidation.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: November 20, 2007
    Assignee: Novartis AG
    Inventors: Francois Navarro, Samuel Petit, Guy Stone
  • Patent number: 7235248
    Abstract: Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva]2-Ciclosporin, in “microemulsion pre-concentrate” and microemulsion form. The compositions typically comprise (1.1) a C1-5alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: June 26, 2007
    Assignee: Novartis AG
    Inventors: Birgit Hauer, Armin Meinzer, Ulrich Posanski, Friedrich Richter
  • Patent number: 7235555
    Abstract: Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infarction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of formula I are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory disease or disorders or autoimmune diseases e.g.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: June 26, 2007
    Assignee: Novartis AG
    Inventors: Jean-Pierre Evenou, Peter Von Matt, Jürgen Wagner, Gerhard Zenke
  • Patent number: 7220774
    Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: May 22, 2007
    Assignee: Novartis AG
    Inventors: Rainer Albert, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
  • Patent number: 7205279
    Abstract: This invention provides a microemulsion pre-concentrate comprising a difficultly soluble active agent and a carrier medium comprising 1) a hydrophilic phase which comprises dimethylisosorbide and/or a lower alkyl alkanoic ester, 2) a lipophilic phase, and 3) a surfactant. The active agent may be a cyclosporin or a macrolide. In another aspect, this invention provides a pharmaceutical composition for enteral or parenteral administration comprising a macrolide and an acid.
    Type: Grant
    Filed: December 15, 2000
    Date of Patent: April 17, 2007
    Assignee: Novartis AG
    Inventors: Sylvain Cottens, Barbara Haeberlin, Richard Sedrani, Jacky Vonderscher
  • Patent number: 7169389
    Abstract: A CD154 binding molecule, in particular an antibody to human CD154, especially a human antibody to human CD154 is provided, wherein the CDRs of the heavy chain and light chain have amino acid sequences as defined, for use in the treatment and/or prevention of diseases or disorders wherein CD154 modulation and/or interference with or inhibition of the CD154:CD40 interactions is therapeutically beneficial.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: January 30, 2007
    Assignee: Novartis AG
    Inventors: Franco E Di Padova, Walter Schuler
  • Patent number: 7148346
    Abstract: This invention provides a process for purifying a cyclosporin, e.g. cyclosporin A, or a macrolide, to a high degree of purity on a large scale. In another aspect this invention provides a bulk quantity of cyclosporin A with an impurity level of less than about 0.7%, e.g. about 0.5%, and compositions thereof.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: December 12, 2006
    Assignee: Novartis AG
    Inventors: Peter Fuenfschilling, Berthold Schenkel
  • Patent number: 7081445
    Abstract: Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: July 25, 2006
    Assignee: Novartis AG
    Inventors: Thomas Cavanak, Ulrich Posanski
  • Patent number: 7078054
    Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: July 18, 2006
    Assignee: Novartis AG
    Inventors: Werner Brox, Armin Meinzer, Horst Zande
  • Patent number: 7067084
    Abstract: The invention relates to a plastic package for a pharmaceutical product, particularly a blister package to dispense liquids or strings, and a method of manufacturing and sterilizing said package. The blister package (1) consists of a lower base portion (2) and a cover member (3). The lower portion includes a cavity indicated generally as (4) which is advantageously formed by inclined sidewalls (5) and upstanding side walls (6) and a bottom (7) which has a circular, flat and smooth surface. The cavity (4) is surrounded by outward extending flange (8). Cover member (3) is welded completely to flange (8) around the opening of cavity (4). Cavity (4) is sized to receive a pharmaceutical product, preferably an ophthalmologic product. The inclined side walls (5) preferably have a rounded geometry to avoid sharp edges for safety reasons.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: June 27, 2006
    Assignee: Novartis AG
    Inventors: Bernard Leroy, Christèle Gatel, Jean Christophe Hermange
  • Patent number: 7025975
    Abstract: A pharmaceutical composition containing macrolide, e.g. a rapamycin compound in an emulsion preconcentrate or microemulsion preconcentrate for oral administration. The carrier medium for the rapamycin compound includes a hydrophilic phase, a lipophilic phase and a surfactant. The composition is stable and provides high absorption efficiency.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: April 11, 2006
    Assignee: Novartis AG
    Inventors: Gerd Fricker, Barbara Haeberlin, Armin Meinzer, Jacky Vonderscher
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6977141
    Abstract: Methods and materials for scintillation assays are disclosed. The scintillation assays rely on differences in general molecular property-based binding interactions, such as charge or hydrophobicity, to localize a radioactive substance near a scintillating material, stimulating scintillation. They are thus described as a direct adsorption scintillation assay (DASA) to distinguish them from the scintillation proximity assay (SPA). The assays are more convenient and inexpensive to implement than SPAs, which rely on specific binding of ligand-receptor pairs, antibody-antigen pairs, or other binding partners which rely on the precise and specific structural complementarity of the partners. The assays can be employed for studying enzymatic reactions, such as those involved in the synthesis of Mur-pentapeptide. The assays are readily adaptable to high throughput screening for use in conjunction with combinatorial libraries of compounds.
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: December 20, 2005
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Zhengyu Yuan, Zhong-Xiao Chen
  • Patent number: 6897307
    Abstract: A one-pot process for preparing 2,6-diaminopurine derivatives or an acid addition salt thereof comprising: (i) reacting a purine compound with an amine compound in the presence of a tertiary amine at a pH of 7 to 14 to form a 6-substituted aminopurine derivative, and (ii) reacting the 6-substituted aminopurine with an aromatic amine in the presence of an acid catalyst at a pH of 0.1 to less than 7.
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: May 24, 2005
    Assignee: Novartis AG
    Inventors: Lech Andrzej Ciszewski, Liladhar M. Waykole
  • Patent number: 6852729
    Abstract: A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2, 6-di-tert.-butyl-4-methylphenol. The presence of the antioxidant improves the stability of the poly-ene macrolide to oxidation.
    Type: Grant
    Filed: March 21, 2003
    Date of Patent: February 8, 2005
    Assignee: Novartis AG
    Inventors: Francois Navarro, Samuel Petit, Guy Stone
  • Patent number: 6846927
    Abstract: A process for the preparation of a compound of formula (A) wherein: X is hydrogen, hydroxy, chloro, C1-6 alkoxy or phenyl C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) whereiff R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II), wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and, as necessary or desired, interconverting variables R1, R2 and R3 to further values o
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: January 25, 2005
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventor: John Robert Mansfield Dales
  • Patent number: 6818638
    Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
    Type: Grant
    Filed: July 11, 2002
    Date of Patent: November 16, 2004
    Assignee: Novartis AG
    Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jörg Kallen, Josef Gottfried Meingassner, François Nuninger, Gabriele Weitz Schmidt
  • Patent number: 6806375
    Abstract: Intermediates such as methyl 2,2-dimethyl-5-ethenyl-1,3-dioxane-5-carbonate useful to prepare antiviral compounds such as penciclovir and famciclovir are disclosed.
    Type: Grant
    Filed: February 19, 2003
    Date of Patent: October 19, 2004
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Richard Freer, Graham Richard Geen, Thomas Weir Ramsay, Andrew Colin Share, Neil Michael Smith
  • Patent number: 6767555
    Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: July 27, 2004
    Assignee: Novartis AG
    Inventors: Michael Ambuhl, Barbara Lückel, Barbara Haberlin, Armin Meinzer