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: 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: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.
Type:
Grant
Filed:
August 12, 2004
Date of Patent:
January 30, 2007
Assignees:
Takeda Pharmaceutical Company Limited, Array BioPharma Inc.
Inventors:
Laurence E. Burgess, Scott D. Cowen, Stephen L. Gwaltney, II, Jeongboeb Seo, Jeffrey A. Stafford
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
Abstract: Systems and methods are provided for evaluating a crystallization experiment, where a crystallization experiment of a molecule is to X-rays while housed within a container in which the crystallization experiment is performed; and one or more X-ray diffraction patterns from the X-ray exposure are used to evaluate whether crystalline material is present in the crystallization experiment.
Abstract: A microfluidic method is provided that comprises: delivering a first fluid to a first lumen of a microfluidic device and a second, different fluid to a second lumen of the microfluidic device, the first and second lumens sharing a common wall which allows for diffusion between the lumens over at least a portion of the length of the lumens; and having the first and second fluids diffuse between the first and second lumens.
Abstract: A microfluidic device is provided that comprises: a substrate; and a plurality of microvolumes at least partially defined by the substrate, each microvolume comprising a first submicrovolume and a second submicrovolume in fluid communication with the first submicrovolume when the device is rotated about a first rotational axis; wherein rotation of the device about the first rotational axis causes a fixed volume to be transported to each of the second submicrovolumes.
Abstract: A microfluidic device comprising: a substrate shaped so as to provide the device with an axis of rotation about which the device may be rotated; and a plurality of microvolumes at least partially defined by the substrate, each microvolume comprising a first submicrovolume and a second submicrovolume that is in fluid communication with the first submicrovolume when the device is rotated, the plurality of microvolumes being arranged in the device such that fluid in the first submicrovolumes of multiple of the microvolumes is transported to the second submicrovolumes of the associated microvolumes when the device is rotated about the rotational axis.
Abstract: A method for determining crystallization conditions for a material, the method comprising: taking a microfluidic device comprising one or more lumens having microvolume dimensions and a plurality of different crystallization samples within the one or more lumens, the plurality of crystallization samples comprising a material to be crystallized and crystallization conditions that vary among the plurality of crystallization samples; transporting the plurality of different crystallization samples within the lumens; and identifying a precipitate or crystal formed in the one or more lumens.
Abstract: A microfluidic device is provided that comprises: a card shaped substrate having first and second opposing faces; one or more microvolumes at least partially defined by a first face of the card shaped substrate; and one or more grooves at least partially defined by a second face of the card shaped substrate; wherein a lateral footprint of at least a portion of the one or more grooves overlaps with a lateral footprint of at least one of the one or more microvolumes.
Abstract: A microfluidic device is provided that comprises: a substrate; and a plurality of microvolumes at least partially defined by the substrate, each microvolume comprising a first submicrovolume and a second submicrovolume that is in fluid communication with the first submicrovolume when the device is rotated, the plurality of microvolumes being arranged in the device such that fluid in the first submicrovolumes of multiple of the microvolumes are transported to second submicrovolumes of the associated microvolumes when the device is rotated.
Abstract: A hybridization assay is provided which uses an oligonucleotide probe which includes a fluorescent reporter molecule and a quencher molecule capable of quenching the fluorescence of the reporter molecule. The oligonucleotide probe is constructed such that the probe exists in at least one single-stranded confirmation when unhybridized where the quencher molecule is near enough to the reporter molecule to quench the fluorescence of the reporter molecule. The oligonucleotide probe also exists in at least one conformation when hybridized to a target polynucleotide where the quencher molecule is not positioned close enough to the reporter molecule to quench the fluorescence of the reporter molecule. By adopting these hybridized and unhybridized conformations, the reporter molecule and quencher molecule on the probe exhibits different fluorescence signal intensities when the probe is hybridized and unhybridized.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
November 23, 2004
Assignee:
Applera Corporation
Inventors:
Kenneth J. Livak, Susan J. A. Flood, Jeffrey Mamoro, Khairuzzaman Bashar Mullah
Abstract: A microfluidic device is provided that comprises: a substrate; one or more microvolumes at least partially defined by the substrate, each microvolume comprising a first submicrovolume, a second submicrovolume where fluid in the first submicrovolume is transported to the second submicrovolume when the device is rotated about a first rotational axis, and a third submicrovolume where fluid in the first submicrovolume is transported to the third submicrovolume when the device is rotated about a second, different rotational axis.
Abstract: A microfluidic method is provided that comprises: delivering first and second fluids to a lumen of a microfluidic device such that the first and second fluids flow adjacent to each other within the lumen without mixing except for diffusion at an interface between the first and second fluids, wherein the first fluid is different than the second fluid.