Abstract: An amorphous solid form of a compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and sodium cations is provided. This is compound is useful for the treatment of hypertension and/or heart failure.
Type:
Grant
Filed:
June 23, 2022
Date of Patent:
May 9, 2023
Assignee:
Novartis Pharmaceuticals Corporation
Inventors:
Lili Feng, Sven Erik Godtfredsen, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Bin Hu, Yugang Liu, Thomas J. Blacklock, Piotr Henryk Karpinski
Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.
Type:
Application
Filed:
May 18, 2021
Publication date:
March 10, 2022
Applicant:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
John BURNIER, Thomas GADEK, Frederic NAUD
Abstract: An amorphous solid form of a compound comprising the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and sodium cations is provided. This compound is useful for the treatment of hypertension and/or heart failure.
Type:
Grant
Filed:
September 23, 2019
Date of Patent:
August 24, 2021
Assignee:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
Lili Feng, Sven Erik Godtfredsen, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Bin Hu, Yugang Liu, Thomas J. Blacklock, Piotr Henryk Karpinski
Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.
Type:
Grant
Filed:
August 12, 2016
Date of Patent:
June 8, 2021
Assignee:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
John Burnier, Thomas Gadek, Frederic Naud
Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
Type:
Application
Filed:
July 27, 2020
Publication date:
May 20, 2021
Applicant:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
Wang SHEN, Kenneth BARR, Johan D. OSLOB, Min ZHONG
Abstract: Methods of preparation and purification of a compound of Formula I, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed.
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
February 2, 2021
Assignee:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
James Robert Zeller, Sripathy Venkatraman, Elisabeth C. A. Brot, Subashree Iyer, Michael Hall
Abstract: The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
Type:
Grant
Filed:
November 11, 2013
Date of Patent:
June 23, 2015
Assignee:
Novartis Pharmaceuticals Corporation
Inventors:
David Hook, Bernard Riss, Daniel Kaufmann, Matthias Napp, Erhard Bappert, Philippe Polleux, Jonathan Medlock, Antonio Zanotti-Gerosa
Abstract: A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.
Type:
Application
Filed:
June 23, 2014
Publication date:
February 26, 2015
Applicant:
NOVARTIS PHARMACEUTICALS CORPORATION
Inventors:
Li Feng, Sven Erik Godtfredsen, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Bin Hu, Yugang Liu, Thomas J. Blacklock, Piotr Henryk Karpinski
Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.
Abstract: A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and/or heart failure. ARB includes S—N-valeryl-N-{[2?-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3?-methyl-2?-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hemipentahydrate.
Type:
Grant
Filed:
November 8, 2006
Date of Patent:
November 4, 2014
Assignee:
Novartis Pharmaceuticals Corporation
Inventors:
Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
Abstract: A method of intravenously administering a bisphosphonate to a patient in need of bisphosphonate treatment comprising intravenously administering 4 mg of 2-(imidazol-1yl)-1-hydroxyethane-1,1-diphosphonic acid (zoledronic acid) or a pharmaceutically acceptable salt thereof over a period of 15 minutes to a patient in need of said treatment.
Type:
Grant
Filed:
November 8, 2006
Date of Patent:
December 4, 2012
Assignee:
Novartis Pharmaceuticals Corporation
Inventors:
Bruno Galli, Horst F Schran, John J Seaman
Abstract: The invention relates to a pharmaceutical composition comprising (i) a renin inhibitor, (ii) a calcium channel blocker (CCB), and a diuretic and to a method of using such composition for the treatment of cardiovascular disease.
Abstract: The invention relates to bisphosphonates, in particular more potent N-bisphosphonates such as zoledronic acid and derivatives, and to methods of treatment using bisphosphonates. These bisphosphonates are used with satisfactory results for prolonged inhibition of bone resorption in conditions of abnormally increased bone turnover, e.g. osteoporosis, by intermittent administration, the periods between bisphosphonate administrations are longer than was previously considered appropriate, e.g. a dosing interval of at least about 6 months or less frequently.
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
November 8, 2011
Assignee:
Novartis Pharmaceuticals Corporation
Inventors:
Zebulun D. Horowitz, Peter C. Richardson, Ulrich Trechsel
Abstract: Use of a compound which is (a) a benzodiazepine derivative of the formula (I) or an N-oxide thereof or (b) a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing an RSV infection wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6alkyl)amino, vitro, cyano, —CO2R?, —CONR?R?, —NH—CO—R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R?, wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; n is from O to 3; R4 represents hydrogen or C1-6 alkyl; X represents —CO—, —CO—NR?—, —S(O)— or —S(O)2—, wherein R? is hydrogen or a C1-C6 alkyl group; and R5 represents a heteroaryl or heterocyclyl group which is substituted by a C1C6 hydroxyalkyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl} group
Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic residue.