Patents Assigned to Novartis International Pharmaceutical Ltd.
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Patent number: 9399764Abstract: The present disclosure relates to recombinant proteins having N-acetylglucosaminyltransferase activity. The present disclosure further relates to methods for producing complex N-glycans including the steps of providing host cells containing such recombinant proteins and culturing the host cells such that the recombinant proteins are expressed.Type: GrantFiled: November 24, 2011Date of Patent: July 26, 2016Assignees: Novartis International Pharmaceutical, Ltd., Glykos Finland OyInventors: Jari Natunen, Anne Kanerva, Jukka Hiltunen, Markku Saloheimo, Heli Viskari, Anne Huuskonen
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Patent number: 8338591Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.Type: GrantFiled: May 6, 2005Date of Patent: December 25, 2012Assignee: Novartis International Pharmaceutical Ltd.Inventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
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Patent number: 8129395Abstract: 4,5-disubstituted-2-arypyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: January 26, 2009Date of Patent: March 6, 2012Assignee: Novartis International Pharmaceutical Ltd.Inventors: George D. Maynard, Manuka Ghosh, Jun Yuan, Kevin S. Currie, Scott Mitchell, Qin Guo, He Zhao
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Patent number: 8119665Abstract: The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.Type: GrantFiled: March 1, 2007Date of Patent: February 21, 2012Assignee: Novartis International Pharmaceutical Ltd.Inventors: George P. Luke, George D. Maynard, Scott Mitchell, Andrew Thurkauf, Linghong Xie, LuYan Zhang, Suoming Zhang, He Zhao, Bertrand L. Chenard, Yang Gao, Bingsong Han, Xiao Shu He
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Patent number: 8062858Abstract: A fibronectin type III (Fn3) polypeptide monobody, a nucleic acid molecule encoding said monobody, and a variegated nucleic acid library encoding said monobody, are provided by the invention. Also provided are methods of preparing a Fn3 polypeptide monobody, and kits to perform said methods. Further provided is a method of identifying the amino acid sequence of a polypeptide molecule capable of binding to a specific binding partner (SBP) so as to form a polypeptide:SSP complex, and a method of identifying the amino acid sequence of a polypeptide molecule capable of catalyzing a chemical reaction with a catalyzed rate constant, kcat, and an uncatalyzed rate constant, kuncat, such that the ratio of kcat/kuncat is greater than 10.Type: GrantFiled: April 24, 2006Date of Patent: November 22, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventor: Shohei Koide
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Patent number: 8007767Abstract: Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: December 22, 2006Date of Patent: August 30, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
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Patent number: 7981620Abstract: A fibronectin type III (Fn3) polypeptide monobody, a nucleic acid molecule encoding said monobody, and a variegated nucleic acid library encoding said monobody, are provided by the invention. Also provided are methods of preparing a Fn3 polypeptide monobody, and kits to perform said methods. Further provided is a method of identifying the amino acid sequence of a polypeptide molecule capable of binding to a specific binding partner (SBP) so as to form a polypeptide:SSP complex, and a method of identifying the amino acid sequence of a polypeptide molecule capable of catalyzing a chemical reaction with a catalyzed rate constant, kcat, and an uncatalyzed rate constant, kuncat, such that the ratio of kcat/kuncat is greater than 10.Type: GrantFiled: October 31, 2007Date of Patent: July 19, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventor: Shohei Koide
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Publication number: 20110118273Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: January 26, 2011Publication date: May 19, 2011Applicant: NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.Inventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
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Patent number: 7915288Abstract: 1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: May 6, 2005Date of Patent: March 29, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventors: Kyungae Lee, Jun Yuan, George D. Maynard, Alan Hutchison, Scott Mitchell
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Patent number: 7906528Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: October 5, 2005Date of Patent: March 15, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
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Patent number: 7863454Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: March 3, 2008Date of Patent: January 4, 2011Assignee: Novartis International Pharmaceutical Ltd.Inventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7858090Abstract: A fibronectin type III (Fn3) polypeptide monobody, a nucleic acid molecule encoding said monobody, and a variegated nucleic acid library encoding said monobody, are provided by the invention. Also provided are methods of preparing a Fn3 polypeptide monobody, and kits to perform said methods. Further provided is a method of identifying the amino acid sequence of a polypeptide molecule capable of binding to a specific binding partner (SBP) so as to form a polypeptide:SSP complex, and a method of identifying the amino acid sequence of a polypeptide molecule capable of catalyzing a chemical reaction with a catalyzed rate constant, kcat, and an uncatalyzed rate constant, kuncat, such that the ratio of kcat/kuncat is greater than 10.Type: GrantFiled: April 24, 2006Date of Patent: December 28, 2010Assignee: Novartis International Pharmaceutical Ltd.Inventor: Shohei Koide
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Patent number: 7696357Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.Type: GrantFiled: March 17, 2008Date of Patent: April 13, 2010Assignee: Novartis International Pharmaceutical Ltd.Inventors: Peter J Dunn, John G Matthews, Trevor J Newbury, Garry O'Connor
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Patent number: 7553482Abstract: The invention relates to the use of an adsorption material which has been modified with polynuclear metal oxide hydroxides for influencing the calcium level and, in particular, for treating or/and preventing atherosclerotic vascular diseases or/and disturbances of bone metabolism.Type: GrantFiled: June 12, 2002Date of Patent: June 30, 2009Assignee: Novartis International Pharmaceutical LtdInventors: Dietrich Seidel, Karl-Siegfried Boos
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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: 7138405Abstract: Pharmaceutical combinations suitable for treating the lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) in men are described herein. The combinations contain an alpha-adrenoceptor antagonist and a muscarinic antagonist that may be administered simultaneously, separately or sequentially. The methods of treatment using the combinations are particularly suitable for treating moderate or severe LUTS.Type: GrantFiled: May 31, 2005Date of Patent: November 21, 2006Assignee: Novartis International Pharmaceutical LtdInventor: Michael G Wyllie
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Patent number: 6930188Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.Type: GrantFiled: March 25, 2003Date of Patent: August 16, 2005Assignee: Novartis International Pharmaceutical, Ltd.Inventors: Peter James Dunn, John George Matthews, Trevor Jack Newbury, Garry O'Connor
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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: 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: 6765007Abstract: A pharmaceutical tablet wherein famciclovir is the active ingredient and wherein the percentage of famciclovir by weight in the tablet is 85% or greater.Type: GrantFiled: September 24, 1998Date of Patent: July 20, 2004Assignee: Novartis International Pharmaceutical Ltd.Inventors: Michael John Greenway, Jennifer Mary Slater