Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
Type:
Grant
Filed:
December 16, 2008
Date of Patent:
October 16, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
Type:
Grant
Filed:
June 2, 2010
Date of Patent:
September 25, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
Abstract: Certain substituted pyrrolidine amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
Type:
Grant
Filed:
May 19, 2009
Date of Patent:
August 7, 2012
Assignee:
Janssen Pharmaceutica NV
Inventors:
Nicholas I Carruthers, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, Daniel J. Pippel, Chandravadan R. Shah, Akinola Soyode-Johnson, Emily M. Stocking, Lana Young
Abstract: This invention relates to an electrotransport device, which incorporates a flexible conductive element within the reservoir housing of the device, which permits electrical communication from within the housing to outside of the housing without the use of opening, which require various methods of sealing the opening against leaks and moisture.
Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.
Abstract: The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
Type:
Grant
Filed:
July 20, 2010
Date of Patent:
November 22, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Neelakandha S. Mani, David C. Palmer, Chennagiri R. Pandit, Mayra B. Reyes, Tong Xiao, Sergio Cesco-Cancian
Abstract: Syntheses of unsaturated piperidines from piperidones through a silyl piperidine reagent via the Shapiro reaction and palladium-catalyzed cross-coupling reactions with organo halides.
Abstract: The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity.
Type:
Grant
Filed:
May 4, 2007
Date of Patent:
March 29, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani
Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
Type:
Grant
Filed:
July 2, 2009
Date of Patent:
March 1, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Dvorak, Annette K. Kwok, Jimmy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
Type:
Grant
Filed:
December 10, 2007
Date of Patent:
February 22, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Anusuya Choudhury, Jeffrey S. Grimm, Kirk L. Sorgi, David Palmer, Jing Liu
Abstract: Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
Abstract: This invention relates to an electrotransport device, which incorporates a conductive element within the reservoir housing of the device, which permits electrical communication from within the housing to outside of the housing without the use of opening, which require various methods of sealing the openings against leaks and moisture.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
November 30, 2010
Assignee:
Alza Corporation
Inventors:
Wanda Faye Dent, J. Richard Gyory, Michael Joseph Grace
Abstract: Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.
Abstract: A transdermal electrotransport drug delivery device having an anode, a cathode and a source of electrical power electrically connected to the anode and the cathode. At least one of the anode and the cathode includes an electrode and a reservoir comprised of a housing composed of a polymeric material and an aqueous medium in contact with the housing. The aqueous medium includes (i) a drug or an electrolyte salt or a mixture thereof, (ii) propylene glycol, and (iii) an antimicrobial agent in an amount sufficient to inhibit microbial growth in the aqueous medium. The propylene glycol prevents the antimicrobial agent from being adsorbed by other materials used in the construction of the delivery device. A process for preparing a transdermal electrotransport drug delivery device is also provided.
Abstract: The present invention relates to processes for the preparation of cyclopropyl-amine derivatives of formula (II), as defined in the specification, useful for the treatment of disorders and conditions mediated by the histamine receptor.
Type:
Grant
Filed:
October 26, 2006
Date of Patent:
September 14, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Neelakandha S. Mani, David C. Palmer, Chennagiri R. Pandit, Mayra B. Reyes, Tong Xiao, Sergio Cesco-Cancian
Abstract: Processes are disclosed for making certain compounds of Formula (II): or their pharmaceutically active salts, that are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases. In one embodiment, the process comprises reacting a compound of formula (7-1): with a compound of formula (B3): in the presence of at least one equivalent of a first base, in a first organic solvent, to give a compound of Formula (II).
Type:
Grant
Filed:
May 25, 2007
Date of Patent:
August 17, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
Type:
Grant
Filed:
June 21, 2007
Date of Patent:
August 3, 2010
Assignee:
Janssen Pharmaceutica NV
Inventors:
John M. Keith, Michael A. Letavic, Emily M. Stocking