Abstract: Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
Type:
Grant
Filed:
March 17, 2004
Date of Patent:
May 20, 2008
Assignee:
Takeda San Diego, Inc.
Inventors:
Jerome C. Bressi, Jason W. Brown, Sheldon X. Cao, Anthony R. Gangloff, Andrew J. Jennings, Jeffrey A. Stafford, Phong H. Vu, Xiao-Yi Xiao
Abstract: Provided are crystals relating to human mitogen-activated protein kinase kinase2 (MAPKK2), also known as MAPK/ERK Kinase2 (MEK2) and its various uses.
Type:
Grant
Filed:
March 7, 2005
Date of Patent:
May 6, 2008
Assignee:
Takeda San Diego, Inc.
Inventors:
Ciaran N. Cronin, Douglas R. Dougan, Mark W. Knuth, Michelle L. Kraus, Kheng Lim, Clifford D. Mol, Gyorgy Snell, Hua Zou
Abstract: Provided are crystals relating to DPPIV and its various uses.
Type:
Grant
Filed:
September 9, 2003
Date of Patent:
March 18, 2008
Assignee:
Takeda San Diego, Inc.
Inventors:
Kathleen Aertgeerts, Ciaran N. Cronin, David J. Hosfield, Mark W. Knuth, Duncan E. McRee, Sridhar Prasad, Bi Ching Sang, Robert J. Skene, Robert A. Wijnands, Sheng Ye
Abstract: Provided are crystals relating to Cathepsin S and its various uses.
Type:
Grant
Filed:
August 22, 2003
Date of Patent:
January 15, 2008
Assignee:
Takeda San Diego, Inc.
Inventors:
Ellen Chien, Douglas R. Dougan, Mark W. Knuth, Duncan E. McRee, Bi Ching Sang, Robert J. Skene, Ronald V. Swanson, Leslie W. Tari, Robert A. Wijnands
Abstract: A fluid dispensing system comprising: a fluid container; a dispensing head in fluid communication with the fluid container; a displacement mechanism which delivers fluid from the fluid container to the dispensing head such that an aliquot of liquid is delivered to a distal end of the dispensing head where the aliquot of liquid is retained; and a pressurized gas displacement mechanism which delivers an aliquot of gas to the distal end of the dispensing head which causes the aliquot of liquid retained at the distal end of the dispensing head to separate from the distal end of the dispensing head.
Type:
Grant
Filed:
May 15, 2003
Date of Patent:
November 13, 2007
Assignee:
Takeda San Diego, Inc.
Inventors:
Jeffrey B. Goldberg, William Spencer, Bruce K. Bridges
Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, M and L have the definitions as described herein.
Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
Type:
Application
Filed:
November 7, 2006
Publication date:
June 28, 2007
Applicant:
Takeda San Diego, Inc.
Inventors:
Jerome Bressi, Sheldon Cao, Jeffrey Stafford, Phong Vu
Abstract: A probe, kit comprising the probe, and methods for using the probe are provided where the probe comprises: wherein DM is a detectable marker; and L is a straight or branched chain moiety providing between 1 and 20 atom separation between DM and the ring atom to which DM is attached.
Type:
Grant
Filed:
March 11, 2004
Date of Patent:
June 26, 2007
Assignee:
Takeda San Diego, Inc.
Inventors:
Christopher L. Caster, Andrew J. Jennings, Marc E. Navre, Michael B. Wallace, Yiqin Wu
Abstract: Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0–10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
Type:
Grant
Filed:
March 17, 2004
Date of Patent:
January 30, 2007
Assignee:
Takeda San Diego, Inc.
Inventors:
Jerome C. Bressi, Jason W. Brown, Sheldon X. Cao, Anthony R. Gangloff, Andrew J. Jennings, Jeffrey A. Stafford, Phong H. Vu, Xiao-Yi Xiao
Abstract: A method is provided for identifying a search model to use in molecular replacement for determining a structure of a target biomolecule, such as a protein, from X-ray diffraction data, the method comprising: employing computer executable logic to perform multiple molecular replacement searches on X-ray diffraction data of the target biomolecule where a group of different biomolecule structures are used as search models for the multiple molecular replacement searches; and employing computer executable logic to compare solutions from the multiple molecular replacement searches, the comparison producing data from which biomolecule structures can be identified as having superior structural identity with the target biomolecule as compared to the other biomolecule structures in the group.
Type:
Grant
Filed:
May 4, 2001
Date of Patent:
January 2, 2007
Assignee:
Takeda San Diego, Inc.
Inventors:
Duncan McRee, Peter R. David, Frank von Delft, John Rammelkamp, Enrique Abola
Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3–12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
Type:
Grant
Filed:
October 7, 2003
Date of Patent:
December 26, 2006
Assignee:
Takeda San Diego, Inc.
Inventors:
Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu