Abstract: Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.
Type:
Application
Filed:
September 10, 2009
Publication date:
December 31, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Hans-Jurgen Wester, Margret Schottelius, Markus Schwaiger
Abstract: The invention provides processes for the conversion of a 6-keto morphinan to a 6-hydroxy morphinan. In particular, the invention provides a stereoselective process for the conversion of a 6-keto morphinan to a 6-beta-hydroxy morphinan.
Abstract: A pharmaceutical pig is used to transport a syringe containing a liquid radiopharmaceutical from a radiopharmacy to a medical facility for administration to a patient. The pharmaceutical pig includes an elongate polymer cap that is removably attached to an elongate polymer base. The elongate polymer cap includes a cap shell that completely encloses a cap shielding element and the elongate polymer base includes a base shell that completely encloses a base shielding element. Preferably the polymer utilized for the cap shell and the base shell is polycarbonate resin, e.g., LEXAN®. An inner liner is not utilized and the cap shielding element and the base shielding element, which are preferably, but not necessarily, made of lead, are completely sealed and unexposed.
Type:
Application
Filed:
August 20, 2009
Publication date:
December 10, 2009
Applicant:
Mallinckrodt, Inc.
Inventors:
Frank M. Fago, Matt Bantly, David W. Wilson
Abstract: The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans.
Type:
Application
Filed:
May 21, 2009
Publication date:
December 3, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Tao Jiang, Robert E. Halvachs, Christopher W. Grote
Abstract: The present invention is directed to novel radiopharmaceuticals, which can be used to image myocardium. In addition, the present invention is directed to methods for risk stratification of patients who have suffered at least one myocardial infarction.
Type:
Application
Filed:
June 2, 2009
Publication date:
December 3, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Raghoottama Pandurangi, Raghavan Rajagopalan, Mary Dyszlewski, Robert Carretta, Joseph Pierro
Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
Type:
Grant
Filed:
April 30, 2007
Date of Patent:
November 24, 2009
Assignee:
Mallinckrodt Inc.
Inventors:
Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell
Abstract: The filling of a syringe can be performed at a faster rate using a filling sequence which expels air from the fill tube before filling the syringe. A similar method is used when changing contrast containers during a filling sequence to ensure that all the air is expelled from the fill tube before filling resumes with the new contrast container. Additionally, by including a contrast container holder that is affixed to an injector head and holds the container near the syringe tip, the filling sequence can be accomplished without requiring the operator to hold the contrast container during the sequence.
Type:
Grant
Filed:
December 31, 2003
Date of Patent:
November 24, 2009
Assignee:
Mallinckrodt Inc.
Inventors:
Frank Fago, Robert Bergen, James F. Farmer
Abstract: A pharmaceutical pig is used to transport a syringe containing a liquid radiopharmaceutical from a radiopharmacy to a medical facility for administration to a patient. The pharmaceutical pig includes an elongate polymer cap that is removably attached to an elongate polymer base. The elongate polymer cap includes a cap shell that completely encloses a cap shielding element and the elongate polymer base includes a base shell that completely encloses a base shielding element. Preferably the polymer utilized for the cap shell and the base shell is polycarbonate resin, e.g., LEXAN®. An inner liner is not utilized and the cap shielding element and the base shielding element, which are preferably, but not necessarily, made of lead, are completely sealed and unexposed.
Type:
Application
Filed:
June 17, 2009
Publication date:
November 12, 2009
Applicant:
MALLINCKRODT, INC.
Inventors:
Frank M. Fago, Matt Bantly, David W. Wilson
Abstract: The invention relates to molecules for treatment and diagnosis of tumors and malignancies, comprising a tumor seeking biomolecule, which is coupled to an intercalating moiety, which is capable of complexing a metal, which metal is preferably a radioactive metal, to the use of these molecules and to therapeutic and diagnostic compositions containing them.
Type:
Application
Filed:
July 20, 2009
Publication date:
November 12, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Roger Ariel Alberto, Pascal Jean-Marie Hafliger
Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
Type:
Grant
Filed:
July 16, 2007
Date of Patent:
October 27, 2009
Assignee:
Mallinckrodt Inc.
Inventors:
Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
Type:
Application
Filed:
June 1, 2009
Publication date:
October 22, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
Abstract: The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof.
Type:
Application
Filed:
April 8, 2009
Publication date:
October 15, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Gary L. Cantrell, Robert E. Halvachs, Narayanasamy Gurusamy, Dawn M. Kyle, Frank W. Moser
Abstract: The present invention relates to a compound for use as a chelator in the radioactive labeling of biomolecules with metal tricarbonyl complexes, which compound has the general Formula (I) wherein M is a monovalent cation, such as Li, Na, K, Tl, Rb, Cs or an alkyl ammonium; R1 is H, alkyl, aryl or a biomolecule; R2 is H or a pendant arm, said pendant arm optionally comprises a biomolecule, with the proviso that when R1 is H, R2 is not H or COOH, and when R1 is alkyl or aryl, R2 is not H.
Type:
Application
Filed:
December 15, 2006
Publication date:
October 8, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Isabel Rego Santos, Antonio Manuel Rocha Paulo
Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
Type:
Application
Filed:
June 10, 2009
Publication date:
October 1, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Christopher W. GROTE, Peter X. WANG, Frank W. MOSER, Gary L. CANTRELL
Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl3 that is necessary to form the 3,4-dihydroisoquinoline.
Type:
Application
Filed:
June 10, 2009
Publication date:
October 1, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Christopher W. Grote, Peter X. Wang, Frank W. Moser, Gary L. Cantrell
Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.
Type:
Application
Filed:
June 10, 2009
Publication date:
October 1, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Gary L. Cantrell, Dan P. Magparangalan, Frank W. Moser, Jian Bao, Christopher W. Grote, Peter X. Wang
Abstract: The invention provides lubricant compositions comprising magnesium stearate dihydrate. The lubricant compositions may be used to lubricate a variety of bioactive formulations including pharmaceutical compositions.
Type:
Application
Filed:
February 11, 2009
Publication date:
September 17, 2009
Applicant:
Mallinckrodt Inc.
Inventors:
Stephen H. Wu, Brian K. Cheng, Gary A. Nichols, Jae H. Park
Abstract: Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.
Type:
Grant
Filed:
April 23, 2002
Date of Patent:
September 15, 2009
Assignee:
Mallinckrodt Inc.
Inventors:
Hans-Jurgen Wester, Margret Schottelius, Markus Schwaigen