Abstract: The present invention relates to a process for isolating (?S,?R)-6-bromo-?-[2-(dimethylamino)ethyl]-2-methoxy-?-1-naphthalenyl-?-phenyl-3-quinolineethanol from a mixture of stereoisomeric forms of 6-bromo-?-[2-(dimethylamino)ethyl]-2-methoxy-?-1-naphthalenyl-?-phenyl-3-quinolineethanol by optical resolution with chiral 4-hydroxydinaphtho[2,1-d:1?,2?-f][1,3,2]dioxaphosphepin 4-oxide or a derivative thereof, in particular (11bR)-4-hydroxydinaphtho[2,1-d:1?,2?-f][1,3,2]dioxaphosphepin 4-oxide, as resolution agent.
Type:
Grant
Filed:
September 6, 2011
Date of Patent:
January 8, 2013
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frank Ralf Porstmann, Stefan Horns, Thomas Bader
Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
Type:
Grant
Filed:
December 4, 2007
Date of Patent:
October 23, 2012
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.
Type:
Grant
Filed:
July 9, 2010
Date of Patent:
August 14, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, Jr., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.
Type:
Grant
Filed:
July 9, 2010
Date of Patent:
July 31, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, Jr., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.
Type:
Grant
Filed:
October 9, 2009
Date of Patent:
July 31, 2012
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Mark R. Player, Daniel J. Parks, William Parsons, Sanath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.
Type:
Grant
Filed:
May 4, 2010
Date of Patent:
July 10, 2012
Assignee:
Janssen Pharmaceutica, NV
Inventors:
Raul R. Calvo, Sanath K. Meegalla, Mark R. Player
Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
July 15, 2010
Date of Patent:
February 21, 2012
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
May 24, 2010
Date of Patent:
January 24, 2012
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Mingde Xie, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
Abstract: The present invention relates to a process for isolating (?S,?R)-6-bromo-?-[2-(dimethylamino)ethyl]-2-methoxy-?-1-naphthalenyl-?-phenyl-3-quinolineethanol from a mixture of stereoisomeric forms of 6-bromo-?-[2-(dimethylamino)ethyl]-2-methoxy-?-1-naphthalenyl-?-phenyl-3-quinolineethanol by optical resolution with chiral 4-hydroxydinaphtho[2,1-d:1?,2?-f][1,3,2]dioxaphosphepin 4-oxide or a derivative thereof, in particular (11bR)-4-hydroxydinaphtho[2,1-d:1?,2?-f][1,3,2]dioxaphosphepin 4-oxide, as resolution agent.
Type:
Grant
Filed:
May 22, 2006
Date of Patent:
October 18, 2011
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frank Ralf Porstmann, Stefan Horns, Thomas Bader
Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2 or 3; R2 is hydrogen; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; X is a direct bond or CH2; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are
Type:
Grant
Filed:
July 31, 2006
Date of Patent:
September 13, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guillemont, Elisabeth Thérèse Jeanne, David Francis Alain Lançois
Abstract: This invention is directed to a tetrahydro-1H-1,2,6-triaza-azulene cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
March 27, 2007
Date of Patent:
September 6, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mingde Xia, Fina Liotta, Michael P. Wachter
Abstract: The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
Type:
Grant
Filed:
December 4, 2007
Date of Patent:
August 16, 2011
Assignee:
Janssen Pharmaceutical N.V.
Inventors:
Jérôme Emile Georges Guillemont, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
Type:
Grant
Filed:
April 13, 2007
Date of Patent:
May 31, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mark R. Player, Scott L. Dax, William H. Parsons, Michael Richard Brandt, Raul R. Calvo, Sharmila Patel, Jian Liu, Wing S. Cheung, Michele C. Jetter, Yu-Kai Lee, Mark A. Youngman, Wenxi Pan, Kenneth M. Wells, Derek A. Beauchamp
Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
September 22, 2006
Date of Patent:
December 14, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mingde Xia, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
Abstract: The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
Type:
Grant
Filed:
March 13, 2007
Date of Patent:
November 9, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mark R. Player, Tianbao Lu, Huaping Hu, Xizhen Zhu, Christopher Teleha, Kevin Kreutter
Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
March 20, 2007
Date of Patent:
November 2, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mingde Xia, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter, Mark J. Macielag
Abstract: This invention relates to novel salts of medicinal disulfides. The compounds include a terminal sulfonate or phosphonate moiety, and have many uses, such as toxicity reducing agents when administered with many antineoplastic agents.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
October 16, 2007
Assignee:
BioNumerik Pharmaceuticals, Inc.
Inventors:
Qiuli Huang, Harry Kochat, Xinghai Chen
Abstract: This invention relates to a method of treating patients who are receiving dialysis treatments. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
Abstract: The present invention relates to a process for preparing tetrasubstituted imidazole derivatives of the general formula (I) wherein R1, R2, R3 and R4 are as defined in the specification below. The present invention further relates to a process for preparing the compound of formula (II) and novel crystalline structures of the compound of formula (II).
Type:
Grant
Filed:
October 4, 2005
Date of Patent:
November 7, 2006
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Hua Zhong, Silke Dubberke, Stefan Müller, Armin Rossler, Thomas W. Schultz, Daniel J. Korey, Thomas Otten, Donald G. Walker, Ahmed Abdel-Magid
Abstract: A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with an aldehyde in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.
Type:
Grant
Filed:
July 25, 2003
Date of Patent:
April 20, 2004
Assignee:
BioNumerik Pharmaceuticals, Inc.
Inventors:
Kesavaram Narkunan, Harry Kochat, Xinghai Chen