Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
September 15, 2009
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Mary Pat Beavers, J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Kevin L. Tays, Jianmei Wei
Abstract: It is now discovered that human chymase cleaves human SLPI at a specific site and that this cleavage can be used as an indicator of chymase activity. The present invention provides methods of diagnosing a chymase-associated disease or evaluating the efficiency of a treatment of a chymase-associated disease in a human subject by measuring SLPI processing, as well as other related methods and compositions.
Abstract: The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.
Type:
Grant
Filed:
April 20, 2007
Date of Patent:
July 7, 2009
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Francis Wilson, Alison Reid, Valerie Reader, Richard John Harrison, Mihiro Sunose, Remedios Hernadez-Perni, Jeremy Major, Cyrille Boussard, Kathryn Smelt, Jess Taylor, Adeline LeFormal, Andrew Cansfield, Svenja Burckhardt, Chih Yung Ho, Yan Zhang
Abstract: Quinazolines of the formula (I) in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein 1bIX antagonists.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
June 16, 2009
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Werner Mederski, Maria Devant, legal representative, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaegar, Richard Soll, Ralf Devant
Abstract: The present invention provides nucleic acid and polypeptide sequences describing an isoform of the ?2?-4 subunit of a voltage gated calcium channel. The nucleic acids described herein can be used to produce functional ?2?-4 protein. The calcium channel ?2?-4 protein may be isolated for the purposes of binding experiments or may be used in cells to form a functional calcium channel complex.
Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.
Type:
Grant
Filed:
August 2, 2007
Date of Patent:
March 17, 2009
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher, Liming Huang, Alice Lee, Kelly J. McClure
Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
Type:
Grant
Filed:
October 18, 2007
Date of Patent:
January 27, 2009
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
Abstract: This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant compounds and pharmaceutical compositions.
Type:
Grant
Filed:
June 29, 2005
Date of Patent:
December 23, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Geoffrey R. Heintzelman, James Lawrence Bullington, Kenneth C. Rupert
Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
Type:
Grant
Filed:
April 16, 2003
Date of Patent:
December 2, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Michael N. Greco, Harold R. Almond, Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
November 18, 2008
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Mary Pat Beavers, J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Kevin L. Tays, Jianmei Wei
Abstract: A novel human cDNA, termed PRSS11-L, was isolated which encodes a polypeptide that belongs to the S2/HtrA serine protease family. The PRSS11-L mRNA is widely expressed in several tissues throughout the body by multi-tissue Northern blotting. The full-length PRSS11-L cDNA, was cloned, expressed and purified. Proteolytic activity was demonstrated using the protein substrate casein. The isolated nucleic acid or polypeptide molecule of the invention can be used in detection assays, gene therapy, and screening assays.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
November 18, 2008
Assignee:
Ortho-Mcneil Pharmaceutical, Inc.
Inventors:
Andrew Lawrence Darrow, Jian-Shen Qi, Cailin Chen, Patricia Andrade-Gordon
Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
Type:
Grant
Filed:
October 18, 2007
Date of Patent:
November 4, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
September 30, 2008
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Mary Pat Beavers, J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Kevin L. Tays, Jianmei Wei
Abstract: The invention is directed to compounds of Formulae I: wherein A, R1, R2, R3, R4, X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
Type:
Grant
Filed:
October 22, 2004
Date of Patent:
September 23, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Mark R. Player, Nand Baindur, Benjamin Brandt, Naresh Chadha, Raymond J. Patch, Davoud Asgari, Taxiarchis Georgiadis
Abstract: The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
Type:
Grant
Filed:
March 30, 2006
Date of Patent:
August 26, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Han-Cheng Zhang, Bruce E. Maryanoff, Anjali Pandey, Robert M. Scarborough
Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
August 26, 2008
Assignee:
Ortho McNeil Pharmaceutical, Inc.
Inventors:
Mary Pat Beavers, J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Kevin L. Tays, Jianmei Wei
Abstract: DNAs encoding human voltage gated sodium channel ?1A subunit have been cloned and characterized. The recombinant protein is capable of forming biologically active protein. The cDNA's have been expressed in recombinant host cells that produce active recombinant protein. The recombinant protein is also purified from the recombinant host cells. In addition, the recombinant host cells are utilized to establish a method for identifying modulators of the receptor activity, and receptor modulators are identified.
Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12—R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
October 19, 2005
Date of Patent:
July 22, 2008
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Tianbao Lu, Bruce Tomczuk, Thomas P. Markotan, Colleen Siedem
Abstract: The present invention is directed to novel heterocyclic benzo[c]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.