Patents Represented by Attorney, Agent or Law Firm Mary A. Appollina
  • Patent number: 8324186
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: December 4, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Zhihua Sui
  • Patent number: 8299073
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: October 30, 2012
    Assignee: Respivert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
  • Patent number: 8299074
    Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: October 30, 2012
    Assignee: RespiVert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
  • Patent number: 8293748
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: October 23, 2012
    Assignee: Respivert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
  • Patent number: 8293771
    Abstract: There is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, including all tautomers thereof, compositions comprising the same, use of said compound and compositions for treatment, in particular for the treatment of asthma and COPD, and processes for the preparation of said compound.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: October 23, 2012
    Assignee: Respivert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Peter John Murray, Catherine Elisabeth Charron
  • Patent number: 8278455
    Abstract: The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)namino-carbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: October 2, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-François Bonfanti, Koenraad Jozef Lodewijk Andries, Jérôme Michel Claude Fortin, Philippe Muller, Frédéric Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
  • Patent number: 8269015
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: September 18, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
  • Patent number: 8188287
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: May 29, 2012
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Chaozhong Cai, Zhihua Sui
  • Patent number: 8178694
    Abstract: Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothien
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: May 15, 2012
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
  • Patent number: 8058439
    Abstract: The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone.
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: November 15, 2011
    Assignee: Noramco, Inc.
    Inventors: D. Phillip Cox, Yong Zhang, Wen-Chun Zhang, Karen E. James
  • Patent number: 8044073
    Abstract: Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1C1-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(—CH2—CH2—O)n—, C1-6alkyloxy(—CH2—CH2—O)n— or Ar1C1-6alkyloxy(—CH2—CH2—O)n—; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(?Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: October 25, 2011
    Assignee: Tibotec Pharmaceuticals
    Inventors: Jean-François Bonfanti, Koenraad Jozef Lodewijk Andries, Jér{hacek over (o)}me Michel Claude Fortin, Philippe Muller, Frédéric Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
  • Patent number: 8034835
    Abstract: Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH— or —CH?CH—CH?N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: October 11, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
  • Patent number: 7906647
    Abstract: The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: March 15, 2011
    Assignee: Noramco, Inc.
    Inventors: D. Phillip Cox, Yong Zhang, Wen-Chun Zhang, Karen E. James
  • Patent number: 7884186
    Abstract: The present invention is directed to an isotopically labeled trapping agent, methods for detecting reactive metabolites and methods of identifying drug candidates. More specifically, the isotopically labeled trapping agent and methods for detecting reactive metabolites may be used to detect both “hard” and “soft” reactive metabolites, thereby eliminating false positives.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: February 8, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Norman D. Huebert, Zhengyin Yan
  • Patent number: 7875719
    Abstract: The present invention is directed to a process for using n-butanol to prepare an oxycodone base compositions having reduced levels of impurities such as 14-hydroxycodeinone and DHDHC.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: January 25, 2011
    Inventors: D. Phillip Cox, Yong Zhang
  • Patent number: 7868023
    Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are as defined in the specification, as are A Z, Q, R1 and R2.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: January 11, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nalin L. Subasinghe, Shelley Ballentine, Jeremy M. Travins, Ehab M. Khalil, Farah Ali, Kristi A. Leonard, Joan M. Gushue, Michael Peter Winters, Heather Hufnagel, Maxwell David Cummings
  • Patent number: 7795279
    Abstract: A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: September 14, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Shelley K. Ballentine, Christian Andrew Baumann, Jinsheng Chen, Carl R. Illig, Sanath K. Meegalla, M. Jonathan Rudolph, Robert W. Tuman, Mark J. Wall, Kenneth Wilson, Dana L. Johnson
  • Patent number: 7662837
    Abstract: The invention is directed to compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: February 16, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee L. Desjarlais, Carl L. Manthey, Christopher Flores, Christopher J. Molloy
  • Patent number: 7645755
    Abstract: The invention is directed to compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: January 12, 2010
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee L. Desjarlais, Carl L. Manthey, Christopher Flores, Christopher J. Molloy
  • Patent number: 7582753
    Abstract: The present invention is directed to a novel process for the preparation of benzo[e][1,2,4]triazepin-2-one derivatives, useful in the preparation of gastrin and cholecystokinin receptor ligands.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: September 1, 2009
    Assignee: JanssenPharmaceutica, NV
    Inventors: Ahmed F. Abdel-Magid, Luigi Anzalone, Judith Cohen, Steven Mehrman, Frank Villani