Patents Represented by Attorney, Agent or Law Firm Thomas R. Savitsky
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Patent number: 7355043Abstract: 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 ofType: GrantFiled: December 14, 2004Date of Patent: April 8, 2008Assignee: Novartis International Pharmaceutical Ltd.Inventor: John Robert Mansfield Dales
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Patent number: 7297703Abstract: 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: GrantFiled: December 23, 2004Date of Patent: November 20, 2007Assignee: Novartis AGInventors: Francois Navarro, Samuel Petit, Guy Stone
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Patent number: 7235555Abstract: 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: GrantFiled: October 12, 2006Date of Patent: June 26, 2007Assignee: Novartis AGInventors: Jean-Pierre Evenou, Peter Von Matt, Jürgen Wagner, Gerhard Zenke
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Patent number: 7235248Abstract: 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: GrantFiled: October 2, 2002Date of Patent: June 26, 2007Assignee: Novartis AGInventors: Birgit Hauer, Armin Meinzer, Ulrich Posanski, Friedrich Richter
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Patent number: 7220774Abstract: 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: GrantFiled: September 11, 2003Date of Patent: May 22, 2007Assignee: Novartis AGInventors: Rainer Albert, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
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Patent number: 7205279Abstract: 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: GrantFiled: December 15, 2000Date of Patent: April 17, 2007Assignee: Novartis AGInventors: Sylvain Cottens, Barbara Haeberlin, Richard Sedrani, Jacky Vonderscher
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Patent number: 7169389Abstract: 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: GrantFiled: March 14, 2001Date of Patent: January 30, 2007Assignee: Novartis AGInventors: Franco E Di Padova, Walter Schuler
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Patent number: 7148346Abstract: 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: GrantFiled: July 23, 2003Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Peter Fuenfschilling, Berthold Schenkel
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Patent number: 7081445Abstract: 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: GrantFiled: March 1, 2004Date of Patent: July 25, 2006Assignee: Novartis AGInventors: Thomas Cavanak, Ulrich Posanski
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Patent number: 7078054Abstract: 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: GrantFiled: May 13, 2003Date of Patent: July 18, 2006Assignee: Novartis AGInventors: Werner Brox, Armin Meinzer, Horst Zande
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Patent number: 7067084Abstract: 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: GrantFiled: October 16, 2000Date of Patent: June 27, 2006Assignee: Novartis AGInventors: Bernard Leroy, Christèle Gatel, Jean Christophe Hermange
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Patent number: 7025975Abstract: 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: GrantFiled: May 18, 2004Date of Patent: April 11, 2006Assignee: Novartis AGInventors: Gerd Fricker, Barbara Haeberlin, Armin Meinzer, Jacky Vonderscher
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Patent number: 6987104Abstract: 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: GrantFiled: June 14, 2002Date of Patent: January 17, 2006Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
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Patent number: 6977141Abstract: 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: GrantFiled: February 9, 1999Date of Patent: December 20, 2005Assignee: Vicuron Pharmaceuticals Inc.Inventors: Zhengyu Yuan, Zhong-Xiao Chen
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Patent number: 6897307Abstract: 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: GrantFiled: March 28, 2003Date of Patent: May 24, 2005Assignee: Novartis AGInventors: Lech Andrzej Ciszewski, Liladhar M. Waykole
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Patent number: 6852729Abstract: 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: GrantFiled: March 21, 2003Date of Patent: February 8, 2005Assignee: Novartis AGInventors: Francois Navarro, Samuel Petit, Guy Stone
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Patent number: 6846927Abstract: 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 oType: GrantFiled: March 11, 1999Date of Patent: January 25, 2005Assignee: Novartis International Pharmaceutical Ltd.Inventor: John Robert Mansfield Dales
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Patent number: 6818638Abstract: 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: GrantFiled: July 11, 2002Date of Patent: November 16, 2004Assignee: Novartis AGInventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jörg Kallen, Josef Gottfried Meingassner, François Nuninger, Gabriele Weitz Schmidt
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Patent number: 6806375Abstract: 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: GrantFiled: February 19, 2003Date of Patent: October 19, 2004Assignee: Novartis International Pharmaceutical Ltd.Inventors: Richard Freer, Graham Richard Geen, Thomas Weir Ramsay, Andrew Colin Share, Neil Michael Smith
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Patent number: 6767555Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.Type: GrantFiled: August 13, 2002Date of Patent: July 27, 2004Assignee: Novartis AGInventors: Michael Ambuhl, Barbara Lückel, Barbara Haberlin, Armin Meinzer